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Pharmacodynamics, Safety and Pharmacokinetics of BMS-663068, an HIV Attachment Inhibitor, in HIV-1

Sponsor
ViiV Healthcare (Industry)
Overall Status
Completed
CT.gov ID
NCT01009814
Collaborator
GlaxoSmithKline (Industry)
50
Enrollment
1
Location
5
Arms
7
Actual Duration (Months)
7.1
Patients Per Site Per Month

Study Details

Study Description

Brief Summary

Research Hypothesis: Administration of BMS-663068, a prodrug for HIV attachment inhibitor BMS-626529, will result in a mean decrease of at least 1 log10 in HIV RNA at Day 9 following 8 days of therapy in at least one dosing regimen that is safe and well tolerated in Clade B HIV-1 infected subjects.

Condition or Disease Intervention/Treatment Phase
Phase 2

Study Design

Study Type:
Interventional
Actual Enrollment :
50 participants
Allocation:
Randomized
Intervention Model:
Parallel Assignment
Masking:
None (Open Label)
Primary Purpose:
Treatment
Official Title:
Randomized, Open Label, Multiple-Dose Study to Evaluate the Pharmacodynamics, Safety and Pharmacokinetics of BMS-663068 in HIV-1 Infected Subjects
Actual Study Start Date :
Nov 23, 2009
Actual Primary Completion Date :
Jun 25, 2010
Actual Study Completion Date :
Jun 25, 2010

Arms and Interventions

Arm Intervention/Treatment
Experimental: BMS-663068 600 mg Q12H + RTV 100 mg Q12H

All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8.

Drug: BMS-663068
BMS-663068 will be administered as a tablet formulation

Drug: Ritonavir
Ritonavir will be administered as a capsule.
Experimental: BMS-663068 1200 mg QHS + RTV 100 mg QHS

All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8.

Drug: BMS-663068
BMS-663068 will be administered as a tablet formulation

Drug: Ritonavir
Ritonavir will be administered as a capsule.
Experimental: BMS-663068 1200 mg Q12H + RTV 100 mg Q12H

All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8.

Drug: BMS-663068
BMS-663068 will be administered as a tablet formulation

Drug: Ritonavir
Ritonavir will be administered as a capsule.
Experimental: BMS-663068 1200 mg Q12H + RTV 100 mg QAM

All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8.

Drug: BMS-663068
BMS-663068 will be administered as a tablet formulation

Drug: Ritonavir
Ritonavir will be administered as a capsule.
Experimental: BMS-663068 1200 mg Q12H

All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.

Drug: BMS-663068
BMS-663068 will be administered as a tablet formulation

Outcome Measures

Primary Outcome Measures

  1. Mean Logarithm With Base 10 (Log10) Change From Baseline in Human Immunodeficiency Virus (HIV) Ribonucleic Acid (RNA) at Day 9 [Baseline and Day 9]

    The primary assessment of the antiviral activity of BMS-663068 was assessed on the log10 change from Baseline in HIV RNA to Day 9. Baseline was the last non-missing observation before first dose (Day 1 pre-dose) and change from Baseline was calculated by subtracting Baseline value from post-Baseline visit value. An analysis of covariance (ANCOVA) model correcting for Baseline HIV viral load and treatment group was used to test the differences in mean log10 decrease in HIV RNA at Day 9 between 2 regimen groups by antiretroviral treatment history (ARV [antiretroviral] naive, ARV experienced, and combined [ARV naive + ARV experienced]). For the combined group (ARV naive +ARV experienced) an additional ANCOVA was used correcting also for treatment history as an additional covariate. Only Clade B participants were included in the population.

Secondary Outcome Measures

  1. Change From Baseline in Cluster of Differentiation 4 Positive (CD4+) Cell Count and Cluster of Differentiation 8 Positive (CD8+) Cell Count [Baseline (Day 1 pre-dose), Day 8, Day 15 and Day 50]

    Blood samples were collected for evaluation of CD4+ and CD8+ cells at Baseline (Day 1, pre-dose), Day 8, Day 15 (Follow up) and Day 50 (study discharge). Baseline was the last non-missing observation before first dose (Day 1 pre-dose) and change from Baseline was calculated by subtracting Baseline value from post-Baseline visit value.

  2. Change From Baseline in Percent CD4+ Cell Count and Percent CD8+ Cell Count [Baseline (Day 1 pre-dose), Day 8, Day 15 and Day 50]

    Blood samples were collected for evaluation of percent CD4+ and percent CD8+ cells at Baseline (Day 1, pre-dose), Day 8, Day 15 (Follow up) and Day 50 (study discharge). Baseline was the last non-missing observation before first dose (Day 1 pre-dose) and change from Baseline was calculated by subtracting Baseline visit value from post-Baseline visit value.

  3. Number of Participants With Treatment Emergent Non-serious Adverse Event (Non-SAE) and Serious AE (SAE) [Up to 50 days]

    An AE is any new untoward medical occurrence or worsening of a pre-existing medical condition in a participant or clinical investigation participant administered an investigational (medicinal) product and that does not necessarily have a causal relationship with this treatment. Any untoward medical occurrence resulting in death, life threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, congenital anomaly/birth defect, any other situation according to medical or scientific judgment that may not be immediately life-threatening or result in death or hospitalization but may jeopardize the participant or may require medical or surgical intervention to prevent serious outcomes were categorized as SAE. Treatment emergent adverse events (occurred after start of treatment) have been presented.Safety Population comprised of all randomized participants who used the trial medication at least once.

  4. Number of Participants With Any Abnormality in Physical Examination [Up to 50 days]

    A complete physical examination included, at a minimum, assessment of the Cardiovascular, Respiratory, Gastrointestinal and Neurological systems. A brief physical examination included, at a minimum assessments of the skin, lungs, cardiovascular system, and abdomen (liver and spleen). Any abnormality found by investigator during physical examination were recorded. Number of participants with any abnormality in physical examination during study have been reported.

  5. Number of Participants With Worst-case Abnormalities in Diastolic Blood Pressure (DBP) and Systolic Blood Pressure (SBP) [Up to 50 days]

    Vital signs including DBP and SBP were recorded. Normal ranges were as following: For DBP, lower limit: value <55 millimeter of mercury (mmHg) and change <-20 mmHg; upper limit: value >90 mmHg and change >20 mmHg). For SBP, lower limit: value <90 mmHg and change <-10 mmHg; upper limit: value >140 mmHg and change >10 mmHg. Number of participants with worst-case abnormalities are presented. Worst-case abnormality was defined as: (1) Below Normal: at least one post-Baseline assessment was below normal range, and no post-Baseline assessment was above normal range. (2) Above Normal: at least one post-Baseline assessment was above normal range, and no post-Baseline assessment was below normal range. (3) Within Normal: all post-Baseline assessments were within normal range. It was to be considered as 'Missing' when there were no post-Baseline assessments.

  6. Number of Participants With Worst-case Abnormalities in Body Temperature, Respiratory Rate [RR], and Heart Rate [HR] [Up to 50 days]

    Vital signs (body temperature, RR, and HR) were recorded. Normal range were: For HR, lower limit: 55 beats per minute (bpm) and change <-15 bpm; upper limit: >100 bpm and change >30 bpm). For temperature, lower limit: 36.0 Celsius; upper limit: >37.5 Celsius or change >1.7 Celsius). For RR, lower limit: 8 breaths per minute; upper limit: >16 breaths per minute or change >10 breaths per minute. Number of participants with worst-case abnormalities are presented. Worst-case abnormality was defined as: (1) Below Normal: at least one post-Baseline assessment was below normal range, and no post-Baseline assessment was above normal range. (2) Above Normal: at least one post-Baseline assessment was above normal range, and no post-Baseline assessment was below normal range. (3) Within Normal: all post-Baseline assessments were within normal range. It was to be considered as 'Missing' when there were no post-Baseline assessments.

  7. Number of Participants With Worst-case Abnormalities in Electrocardiogram (ECG) Parameters [Up to 50 days]

    A 12-lead ECG was recorded during the study using an ECG machine that automatically measures ECG parameters. Normal range for ECG parameters were: PR interval (upper: 200 milliseconds [ms]); QRS (lower: 50 ms; upper: 120 ms); Corrected QT interval by Bazett formula (QTcB) (change from Baseline - increases by > 30 ms); Corrected QT interval by Fredericia formula (QTcF) (change from Baseline - increases by > 30 ms). Number of participants with worst-case abnormalities are presented which was defined as: (1) Below Normal: at least one post-Baseline assessment was below normal range, and no post-Baseline assessment was above normal range. (2) Above Normal: at least one post-Baseline assessment was above normal range, and no post-Baseline assessment was below normal range. Within Normal: all post-Baseline assessments were within normal range. It was to be considered as 'Missing' when there were no post-Baseline assessments.

  8. Number of Participants With Clinically Significant Abnormalities in Laboratory Parameters [Up to 50 days]

    Laboratory parameters included hematology, clinical chemistry and urine parameters. Clinically significant abnormal laboratory findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Any abnormal laboratory test results which were considered clinically significant by the investigator were recorded on the case report form. Number of participants with any clinically significant abnormalities in laboratory parameters have been presented.

  9. Maximum Observed Plasma Concentration (Cmax) of BMS-626529 Following Q12H Dosing [Days 1, 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours]

    Blood samples were collected at indicated time points to assess Cmax of BMS-626529 following Q12H dosing. Geometric mean and geometric coefficient of variation are presented for Day 1, Day 8 morning dose (Anti Meridiem [AM]), Day 8 evening dose (Post Meridiem [PM]) and Day 8 morning + evening dose (AM+PM). Pharmacokinetic parameter values were derived by non-compartmental methods. Pharmacokinetic (PK) Population was used which comprised of all participants who receive BMS-663068 and provided pharmacokinetic samples.

  10. Cmax of BMS-626529 Following QHS Dosing [Days 1, 8: pre-evening dose, 1,2,3,4,5,6,8 hours]

    Blood samples were collected at indicated time points to assess Cmax of BMS-626529 following QHS dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1, Day 8 evening dose (PM) and Day 8 morning (AM) + evening dose (PM).

  11. Trough Observed Plasma Concentration (Ctrough) of BMS-626529 Following Q12H Dosing [Days 1, 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours; Days 5,6,7: pre-morning dose]

    Blood samples were collected at indicated time points to access Ctrough of BMS-626529 following Q12H dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1, Days 5, 6, 7, 8, Day 8 morning dose (AM) and Day 8 evening dose (PM).

  12. Ctrough of BMS-626529 Following QHS Dosing [Days 1, 8: pre-evening dose, 1,2,3,4,5,6,8 hours; Days 5,6,7: pre-evening dose]

    Blood samples were collected at indicated time points to assess Ctrough of BMS-626529 following QHS dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1, Days 5, 6, 7, 8 and Day 8 evening dose (PM).

  13. Area Under the Concentration-time Curve in One Dosing Interval (AUC [Tau]) of BMS-626529 Following Q12H Dosing [Days 1, 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours]

    Blood samples were collected at indicated time points to assess AUC (tau) of BMS-626529 following Q12H dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1, Day 8 morning dose (AM) and Day 8 evening dose (PM).

  14. AUC (Tau) of BMS-626529 Following QHS Dosing [Days 1, 8: pre-evening dose, 1,2,3,4,5,6,8 hours]

    Blood samples were collected at indicated time points to assess AUC (tau) of BMS-626529 following QHS dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1 and Day 8 evening dose (PM).

  15. Area Under the Concentration-time Curve Over a 24-hour Period (AUC [0-24]) of BMS-626529 Following Q12H Dosing [Day 8: pre-morning dose, 1,2,3,4,5,6,8,12, 13,14,15,16,17,18,20 hours]

    Blood samples were collected at indicated time points to assess AUC (0-24) of BMS-626529 following Q12H dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 8.

  16. AUC (0-24) of BMS-626529 Following QHS Dosing [Day 8: pre-evening dose, 1,2,3,4,5,6,8 hours]

    Blood samples were collected at indicated time points to assess AUC (0-24) of BMS-626529 following QHS dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 8.

  17. Accumulation Index (AI) of BMS-626529 Following Q12H Dosing [Day 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours]

    Blood samples were collected at indicated time points to assess Accumulation Index of BMS-626529 following Q12H dosing. AI was calculated as ratio of AUC(tau) at steady-state to AUC(tau) after the first dose. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 8 morning dose (AM).

  18. Accumulation Index of BMS-626529 Following QHS Dosing [Day 8: pre-evening dose, 1,2,3,4,5,6,8 hours]

    Blood samples were collected at indicated time points to assess Accumulation Index of BMS-626529 following QHS dosing. AI was calculated as ratio of AUC(tau) at steady-state to AUC(tau) after the first dose. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 8 evening dose (PM).

  19. Inhibitory Quotient (IQ) of BMS-626529 by Css,Avg and by Lowest Concentration of a Drug During Dosing Interval (Cmin) Following Q12H Dosing [Days 1, 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours; Day 9: pre-dose, 4,12 hours; Day 10: pre-dose, 12 hours; Day 11: pre-dose; Days 5,6,7: pre-morning dose]

    Blood samples were collected at indicated time points to assess IQ of BMS-626529. Inhibitory quotient was calculated as the ratio of BMS-626529 in vivo exposure to in vitro measured protein binding adjusted EC90 (PBA-EC90). The following in vivo exposure measures were used in evaluating IQ: Cmin and Css,avg. Geometric mean and geometric coefficient of variation are presented.

  20. Inhibitory Quotient (IQ) of BMS-626529 by Css,Avg and by Lowest Concentration of a Drug During Dosing Interval (Cmin) Following QHS Dosing [Days 1, 8: pre-evening dose, 1,2,3,4,5,6,8 hours; Day 2: pre-evening dose, 12,16 hours; Day 9: pre-dose, 12,16 hours; Day 10: pre-dose, 12 hours; Day 11: pre-dose; Days 5,6,7: pre-evening dose]

    Blood samples were collected at indicated time points to assess IQ of BMS-626529. Inhibitory quotient was calculated as the ratio of BMS-626529 in vivo exposure to in vitro measured protein binding adjusted EC90 (PBA-EC90). The following in vivo exposure measures were used in evaluating IQ: Cmin and Css,avg. Geometric mean and geometric coefficient of variation are presented.

  21. Inhibitory Quotient of BMS-626529 by Ctrough Following Q12H Dosing [Days 1, 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours; Day 9: pre-dose, 4,12 hours; Day 10: pre-dose, 12 hours; Day 11: pre-dose; Days 5,6,7: pre-morning dose]

    Blood samples were collected at indicated time points to assess IQ of BMS-626529. Inhibitory quotient was calculated as the ratio of BMS-626529 in vivo exposure to in vitro measured protein binding adjusted EC90 (PBA-EC90). The following in vivo exposure measure was used in evaluating IQ: Ctrough. Geometric mean and geometric coefficient of variation are presented.

  22. Inhibitory Quotient of BMS-626529 by Ctrough Following QHS Dosing [Days 1, 8: pre-evening dose, 1,2,3,4,5,6,8 hours; Days 2: pre-evening dose, 12,16 hours; Day 9: pre-dose, 12,16 hours; Day 10: pre-dose, 12 hours; Day 11: pre-dose; Days 5,6,7: pre-evening dose]

    Blood samples were collected at indicated time points to assess IQ of BMS-626529. Inhibitory quotient was calculated as the ratio of BMS-626529 in vivo exposure to in vitro measured protein binding adjusted EC90 (PBA-EC90). The following in vivo exposure measure was used in evaluating IQ: Ctrough. Geometric mean and geometric coefficient of variation are presented.

  23. Cmax of Ritonavir Following Q12H Dosing [Days 1, 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours]

    Blood samples were collected at indicated time points to assess Cmax of ritonavir following Q12H dosing. Geometric mean and geometric coefficient of variation are presented for Day 1, Day 8 morning dose (AM), Day 8 evening dose (PM) and Day 8 morning + evening dose (AM+PM). Pharmacokinetic parameter values were derived by non-compartmental methods. PK Population was used which comprised of all participants who receive ritonavir and provided pharmacokinetic samples.

  24. Cmax of Ritonavir Following QHS Dosing [Days 1, 8: pre-evening dose, 1,2,3,4,5,6,8 hours]

    Blood samples were collected at indicated time points to assess Cmax of ritonavir following QHS dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1, Day 8 evening dose (PM) and Day 8 morning (AM) + evening dose (PM).

  25. Ctrough of Ritonavir Following Q12H Dosing [Days 1, 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours; Days 5,6,7: pre-morning dose]

    Blood samples were collected at indicated time points to access Ctrough of ritonavir following Q12H dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1, Days 5, 6, 7, 8, Day 8 morning dose (AM) and Day 8 evening dose (PM).

  26. Ctrough of Ritonavir Following QHS Dosing [Days 1, 8: pre-evening dose, 1,2,3,4,5,6,8 hours; Days 5,6,7: pre-evening dose]

    Blood samples were collected at indicated time points to assess Ctrough of ritonavir following QHS dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1, Days 5, 6, 7, 8 and Day 8 evening dose (PM).

  27. AUC (Tau) of Ritonavir Following Q12H Dosing [Days 1, 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours]

    Blood samples were collected at indicated time points to assess AUC (tau) of ritonavir following Q12H dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1, Day 8 morning dose (AM) and Day 8 evening dose (PM).

  28. AUC (Tau) of Ritonavir Following QHS Dosing [Days 1, 8: pre-evening dose, 1,2,3,4,5,6,8 hours]

    Blood samples were collected at indicated time points to assess AUC (tau) of ritonavir following QHS dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1 and Day 8 evening dose (PM).

  29. AUC (0-24) of Ritonavir Following Q12H Dosing [Day 8: pre-morning dose, 1,2,3,4,5,6,8,12, 13,14,15,16,17,18,20 hours]

    Blood samples were collected at indicated time points to assess AUC (0-24) of ritonavir following Q12H dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 8.

  30. AUC (0-24) of Ritonavir Following QHS Dosing [Day 8: pre-evening dose, 1,2,3,4,5,6,8 hours]

    Blood samples were collected at indicated time points to assess AUC (0-24) of ritonavir following QHS dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 8.

  31. Accumulation Index of Ritonavir Following Q12H Dosing [Day 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours]

    Blood samples were collected at indicated time points to assess Accumulation Index of ritonavir following Q12H dosing. AI was calculated as ratio of AUC(tau) at steady-state to AUC(tau) after the first dose. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 8 morning dose (AM).

  32. Accumulation Index of Ritonavir Following QHS Dosing [Day 8: pre-evening dose, 1,2,3,4,5,6,8 hours]

    Blood samples were collected at indicated time points to assess Accumulation Index of ritonavir following QHS dosing. AI was calculated as ratio of AUC(tau) at steady-state to AUC(tau) after the first dose. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 8 evening dose (PM).

Eligibility Criteria

Criteria

Ages Eligible for Study:
18 Years and Older
Sexes Eligible for Study:
All
Accepts Healthy Volunteers:
No
Inclusion Criteria:

  • Clade B HIV-1 infected subjects meeting following criteria at screening:

  • Plasma HIV RNA ≥ 5,000 copies/mL

  • CD4+ lymphocyte ≥ 200 cells/µL

  • Antiretroviral naive or experienced

  • Off all ARV therapy with HIV activity for > 8 weeks

  • BMI of 18 to 35 kg/m2, inclusive.

  • Not currently co-infected with HCV or HBV

  • Men and women, ≥ 18 years of age

Exclusion Criteria:

  • Woman of childbearing potential (WOCBP) unwilling or unable to use an acceptable method to avoid pregnancy for the entire study period up to 12 weeks after the last dose of study drug.

  • WOCBP using prohibited contraceptive method including oral, injectable, or implantable hormonal contraceptive agent within 12 weeks of enrollment.

  • Women who are pregnant or breastfeeding.

  • Women with positive pregnancy test on enrollment or prior to study drug intake.

  • Sexually active fertile men not using effective birth control during study and for at least 12 weeks after last dose of study drug if partners are WOCBP.

  • Significant acute or chronic medical illness not stable or not controlled with medication or not consistent with HIV infection.

  • Current or recent (within 3 months) gastrointestinal disease that, in the opinion of Investigator or Medical Monitor, may impact on drug absorption and/or put subject at risk for GI tract irritation and/or bleeding.

  • Acute diarrhea lasting ≥ 1 day, within 3 weeks prior to randomization.

  • Major surgery within 4 weeks of study drug intake.

  • Gastrointestinal surgery that could impact upon absorption of study drug.

  • Donation of blood or plasma to blood bank or in a clinical study (except a Screening visit or follow up visit of less than 50 mL) within 4 weeks of study drug intake.

  • Blood transfusion within 4 weeks of study drug intake.

  • Inability to tolerate oral medication.

  • Inability to be venipunctured and/or tolerate venous access.

  • Personal history of clinically relevant cardiac disease, symptomatic or asymptomatic arrhythmias, syncopal episodes, or additional risk factors for torsades de pointes.

  • Personal or family history of long QT syndrome.

  • Recent (within 6 months) drug/alcohol abuse

  • Any other medical, psychiatric and/or social reason which, in the opinion of the Investigator, would make the candidate inappropriate for participation.

  • Evidence of organ dysfunction or clinically significant deviation from normal in physical examination, vital signs, ECG or clinical lab determinations or not consistent with subject's degree of HIV infection.

  • Evidence of 2nd or 3rd degree heart block at screening or Day -1

  • Positive urine drug screen at Screening or Day -1 without valid prescription (subjects positive for cannabinoids and/or amphetamines will be included).

  • Positive blood screen for hepatitis B surface antigen.

  • Positive blood screen for hepatitis C antibody and hepatitis C RNA.

  • History of significant drug allergy

  • Exposure to any investigational drug or placebo within 4 weeks of study drug intake.

  • Prescription drugs within 4 weeks prior to study drug intake, unless approved by BMS medical monitor.

  • Other drugs, including over-the-counter medications, vitamins and/or herbal preparations, within 1 week prior to study drug intake, unless approved by BMS medical monitor.

  • Use of oral, injectable or implantable hormonal contraceptive agent within 12 weeks of study drug intake.

  • Use of prescription drugs or OTC drugs that may cause GI tract irritation or bleeding within 2 weeks of study drug intake, unless approved by BMS medical monitor.

  • Use of alcohol-containing beverages within 3 days prior to study drug intake.

  • Use of grapefruit, grapefruit-containing or Seville orange-containing products within 7 days prior to study drug intake.

  • Prisoners or subjects involuntarily incarcerated.

  • Subjects compulsorily detained for treatment of either a psychiatric or physical illness.

Contacts and Locations

Locations

Site City State Country Postal Code
1 GSK Investigational Site Berlin Germany 13353

Sponsors and Collaborators

  • ViiV Healthcare
  • GlaxoSmithKline

Investigators

  • Study Director: GSK Clinical Trials, ViiV Healthcare

Study Documents (Full-Text)

More Information

Publications

None provided.
Responsible Party:
ViiV Healthcare
ClinicalTrials.gov Identifier:
NCT01009814
Other Study ID Numbers:
  • 206267
  • AI438-006
First Posted:
Nov 9, 2009
Last Update Posted:
Jan 3, 2020
Last Verified:
Oct 1, 2019
Keywords provided by ViiV Healthcare
HIV, HIV attachment inhibitor, attachment inhibitor
Additional relevant MeSH terms:
HIV Infections
Ritonavir
Fostemsavir

Study Results

Participant Flow

Recruitment Details This was a randomized, open label, multiple-dose study to evaluate the pharmacodynamics, safety and pharmacokinetics of BMS-663068 in human immunodeficiency virus 1 (HIV-1) infected participants. The study was conducted at single center in Germany.
Pre-assignment Detail A total of 75 participants were screened, of which 25 were screen failure, and 50 eligible participants were enrolled into the study and were randomized.
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg QHS + RTV 100 mg QHS BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Period Title: Overall Study
STARTED 10 10 10 10 10
COMPLETED 9 9 10 10 10
NOT COMPLETED 1 1 0 0 0

Baseline Characteristics

Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg QHS + RTV 100 mg QHS BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H Total
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8. Total of all reporting groups
Overall Participants 10 10 10 10 10 50
Age (Years) [Mean (Standard Deviation) ]
Mean (Standard Deviation) [Years]
41.3
(8.29)
40.7
(13.70)
40.7
(6.53)
38.4
(7.83)
42.7
(8.42)
40.8
(9.01)
Sex: Female, Male (Count of Participants)
Female
1
10%
1
10%
1
10%
0
0%
0
0%
3
6%
Male
9
90%
9
90%
9
90%
10
100%
10
100%
47
94%
Race/Ethnicity, Customized (Count of Participants)
White
10
100%
10
100%
10
100%
10
100%
10
100%
50
100%

Outcome Measures

1. Primary Outcome
Title Mean Logarithm With Base 10 (Log10) Change From Baseline in Human Immunodeficiency Virus (HIV) Ribonucleic Acid (RNA) at Day 9
Description The primary assessment of the antiviral activity of BMS-663068 was assessed on the log10 change from Baseline in HIV RNA to Day 9. Baseline was the last non-missing observation before first dose (Day 1 pre-dose) and change from Baseline was calculated by subtracting Baseline value from post-Baseline visit value. An analysis of covariance (ANCOVA) model correcting for Baseline HIV viral load and treatment group was used to test the differences in mean log10 decrease in HIV RNA at Day 9 between 2 regimen groups by antiretroviral treatment history (ARV [antiretroviral] naive, ARV experienced, and combined [ARV naive + ARV experienced]). For the combined group (ARV naive +ARV experienced) an additional ANCOVA was used correcting also for treatment history as an additional covariate. Only Clade B participants were included in the population.
Time Frame Baseline and Day 9

Outcome Measure Data

Analysis Population Description
Pharmacodynamic Population. It comprised of all participants for whom pharmacodynamic measurements were available at Baseline and at least one other time.
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg QHS + RTV 100 mg QHS BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Measure Participants 9 9 10 10 10
Mean (Standard Error) [Log10 copies per milliliter (c/mL)]
-1.3445
(0.07925)
-1.2532
(0.10610)
-1.2381
(0.10455)
-1.1888
(0.12938)
-0.8760
(0.22621)
Statistical Analysis 1
Statistical Analysis Overview Comparison Group Selection BMS-663068 600 mg Q12H + RTV 100 mg Q12H, BMS-663068 1200 mg QHS + RTV 100 mg QHS
Comments Null hypothesis was that there was 0 difference in mean log10 decrease in HIV RNA at Day 9 between two groups.
Type of Statistical Test Other
Comments
Statistical Test of Hypothesis p-Value 0.6102
Comments
Method ANCOVA
Comments
Method of Estimation Estimation Parameter Mean Difference (Net)
Estimated Value -0.1089
Confidence Interval (2-Sided) 90%
-0.4656 to 0.2477
Parameter Dispersion Type: Standard Error of the Mean
Value: 0.2120
Estimation Comments
Statistical Analysis 2
Statistical Analysis Overview Comparison Group Selection BMS-663068 600 mg Q12H + RTV 100 mg Q12H, BMS-663068 1200 mg Q12H + RTV 100 mg Q12H
Comments Null hypothesis was that there was 0 difference in mean log10 decrease in HIV RNA at Day 9 between two groups.
Type of Statistical Test Other
Comments
Statistical Test of Hypothesis p-Value 0.5452
Comments
Method ANCOVA
Comments
Method of Estimation Estimation Parameter Mean Difference (Net)
Estimated Value -0.1266
Confidence Interval (2-Sided) 90%
-0.4758 to 0.2225
Parameter Dispersion Type: Standard Error of the Mean
Value: 0.2076
Estimation Comments
Statistical Analysis 3
Statistical Analysis Overview Comparison Group Selection BMS-663068 600 mg Q12H + RTV 100 mg Q12H, BMS-663068 1200 mg Q12H + RTV 100 mg QAM
Comments Null hypothesis was that there was 0 difference in mean log10 decrease in HIV RNA at Day 9 between two groups.
Type of Statistical Test Other
Comments
Statistical Test of Hypothesis p-Value 0.4178
Comments
Method ANCOVA
Comments
Method of Estimation Estimation Parameter Mean Difference (Net)
Estimated Value -0.1682
Confidence Interval (2-Sided) 90%
-0.5139 to 0.1775
Parameter Dispersion Type: Standard Error of the Mean
Value: 0.2055
Estimation Comments
Statistical Analysis 4
Statistical Analysis Overview Comparison Group Selection BMS-663068 600 mg Q12H + RTV 100 mg Q12H, BMS-663068 1200 mg Q12H
Comments Null hypothesis was that there was 0 difference in mean log10 decrease in HIV RNA at Day 9 between two groups.
Type of Statistical Test Other
Comments
Statistical Test of Hypothesis p-Value 0.0233
Comments
Method ANCOVA
Comments
Method of Estimation Estimation Parameter Mean Difference (Net)
Estimated Value -0.4885
Confidence Interval (2-Sided) 90%
-0.8375 to -0.1395
Parameter Dispersion Type: Standard Error of the Mean
Value: 0.2075
Estimation Comments
Statistical Analysis 5
Statistical Analysis Overview Comparison Group Selection BMS-663068 1200 mg QHS + RTV 100 mg QHS, BMS-663068 1200 mg Q12H + RTV 100 mg Q12H
Comments Null hypothesis was that there was 0 difference in mean log10 decrease in HIV RNA at Day 9 between two groups.
Type of Statistical Test Other
Comments
Statistical Test of Hypothesis p-Value 0.9314
Comments
Method ANCOVA
Comments
Method of Estimation Estimation Parameter Mean Difference (Net)
Estimated Value -0.0177
Confidence Interval (2-Sided) 90%
-0.3613 to 0.3259
Parameter Dispersion Type: Standard Error of the Mean
Value: 0.2043
Estimation Comments
Statistical Analysis 6
Statistical Analysis Overview Comparison Group Selection BMS-663068 1200 mg QHS + RTV 100 mg QHS, BMS-663068 1200 mg Q12H + RTV 100 mg QAM
Comments Null hypothesis was that there was 0 difference in mean log10 decrease in HIV RNA at Day 9 between two groups.
Type of Statistical Test Other
Comments
Statistical Test of Hypothesis p-Value 0.7734
Comments
Method ANCOVA
Comments
Method of Estimation Estimation Parameter Mean Difference (Net)
Estimated Value -0.0592
Confidence Interval (2-Sided) 90%
-0.4032 to 0.2847
Parameter Dispersion Type: Standard Error of the Mean
Value: 0.2045
Estimation Comments
Statistical Analysis 7
Statistical Analysis Overview Comparison Group Selection BMS-663068 1200 mg QHS + RTV 100 mg QHS, BMS-663068 1200 mg Q12H
Comments Null hypothesis was that there was 0 difference in mean log10 decrease in HIV RNA at Day 9 between two groups.
Type of Statistical Test Other
Comments
Statistical Test of Hypothesis p-Value 0.0702
Comments
Method ANCOVA
Comments
Method of Estimation Estimation Parameter Mean Difference (Net)
Estimated Value -0.3796
Confidence Interval (2-Sided) 90%
-0.7232 to -0.0360
Parameter Dispersion Type: Standard Error of the Mean
Value: 0.2043
Estimation Comments
Statistical Analysis 8
Statistical Analysis Overview Comparison Group Selection BMS-663068 1200 mg Q12H + RTV 100 mg Q12H, BMS-663068 1200 mg Q12H + RTV 100 mg QAM
Comments Null hypothesis was that there was 0 difference in mean log10 decrease in HIV RNA at Day 9 between two groups.
Type of Statistical Test Other
Comments
Statistical Test of Hypothesis p-Value 0.8359
Comments
Method ANCOVA
Comments
Method of Estimation Estimation Parameter Mean Difference (Net)
Estimated Value -0.0415
Confidence Interval (2-Sided) 90%
-0.3768 to 0.2937
Parameter Dispersion Type: Standard Error of the Mean
Value: 0.1993
Estimation Comments
Statistical Analysis 9
Statistical Analysis Overview Comparison Group Selection BMS-663068 1200 mg Q12H + RTV 100 mg Q12H, BMS-663068 1200 mg Q12H
Comments Null hypothesis was that there was 0 difference in mean log10 decrease in HIV RNA at Day 9 between two groups.
Type of Statistical Test Other
Comments
Statistical Test of Hypothesis p-Value 0.0759
Comments
Method ANCOVA
Comments
Method of Estimation Estimation Parameter Mean Difference (Net)
Estimated Value -0.3619
Confidence Interval (2-Sided) 90%
-0.6962 to -0.0275
Parameter Dispersion Type: Standard Error of the Mean
Value: 0.1988
Estimation Comments
Statistical Analysis 10
Statistical Analysis Overview Comparison Group Selection BMS-663068 1200 mg Q12H + RTV 100 mg QAM, BMS-663068 1200 mg Q12H
Comments Null hypothesis was that there was 0 difference in mean log10 decrease in HIV RNA at Day 9 between two groups.
Type of Statistical Test Other
Comments
Statistical Test of Hypothesis p-Value 0.1155
Comments
Method ANCOVA
Comments
Method of Estimation Estimation Parameter Mean Difference (Net)
Estimated Value -0.3203
Confidence Interval (2-Sided) 90%
-0.6555 to 0.0149
Parameter Dispersion Type: Standard Error of the Mean
Value: 0.1993
Estimation Comments
2. Secondary Outcome
Title Change From Baseline in Cluster of Differentiation 4 Positive (CD4+) Cell Count and Cluster of Differentiation 8 Positive (CD8+) Cell Count
Description Blood samples were collected for evaluation of CD4+ and CD8+ cells at Baseline (Day 1, pre-dose), Day 8, Day 15 (Follow up) and Day 50 (study discharge). Baseline was the last non-missing observation before first dose (Day 1 pre-dose) and change from Baseline was calculated by subtracting Baseline value from post-Baseline visit value.
Time Frame Baseline (Day 1 pre-dose), Day 8, Day 15 and Day 50

Outcome Measure Data

Analysis Population Description
Pharmacodynamic Population. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles).
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg QHS + RTV 100 mg QHS BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Measure Participants 9 9 10 10 10
CD4+, Day 8, n=9, 9, 10, 10, 10
114.2
(74.55)
93.4
(25.12)
109.8
(32.37)
38.5
(41.61)
32.0
(36.23)
CD4+, Day 15, n=9, 9, 10, 10, 10
58.4
(92.14)
-6.1
(28.15)
117.6
(27.67)
44.6
(69.94)
10.4
(23.38)
CD4+, Day 50, n=9, 9, 10, 10, 9
22.0
(91.55)
-50.3
(18.06)
71.1
(28.55)
-48.4
(61.21)
-19.2
(17.05)
CD8+, Day 8, n=9, 9, 10, 10, 10
384.2
(164.35)
189.0
(134.27)
218.4
(125.65)
114.9
(131.64)
94.6
(152.73)
CD8+, Day 15, n=9, 9, 10, 10, 10
64.8
(230.86)
-153.2
(137.18)
85.6
(112.65)
-99.6
(159.83)
-4.4
(126.77)
CD8+, Day 50, n=9, 9, 10, 10, 9
-37.6
(161.11)
-292.4
(121.73)
139.7
(95.00)
6.0
(170.29)
-48.2
(140.55)
3. Secondary Outcome
Title Change From Baseline in Percent CD4+ Cell Count and Percent CD8+ Cell Count
Description Blood samples were collected for evaluation of percent CD4+ and percent CD8+ cells at Baseline (Day 1, pre-dose), Day 8, Day 15 (Follow up) and Day 50 (study discharge). Baseline was the last non-missing observation before first dose (Day 1 pre-dose) and change from Baseline was calculated by subtracting Baseline visit value from post-Baseline visit value.
Time Frame Baseline (Day 1 pre-dose), Day 8, Day 15 and Day 50

Outcome Measure Data

Analysis Population Description
Pharmacodynamic Population. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles).
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg QHS + RTV 100 mg QHS BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Measure Participants 9 9 10 10 10
Percent CD4+, Day 8, n=9, 9, 10, 10, 10
-1.0
(1.12)
1.2
(0.97)
0.6
(0.78)
0.1
(0.72)
1.4
(1.11)
Percent CD4+, Day 15, n=9, 9, 10, 10, 10
1.6
(1.00)
1.2
(0.64)
1.4
(1.33)
2.4
(1.11)
0.9
(1.51)
Percent CD4+, Day 50, n=9, 9, 10, 10, 9
1.4
(0.84)
1.1
(1.15)
0.3
(0.90)
-1.7
(0.97)
0.6
(1.45)
Percent CD8+, Day 8, n=9, 9, 10, 10, 10
1.0
(0.76)
-0.4
(1.02)
0.1
(1.06)
-0.3
(1.11)
-0.2
(1.20)
Percent CD8+, Day 15, n=9, 9, 10, 10, 10
-3.4
(0.73)
-2.8
(1.00)
-2.9
(1.49)
-4.0
(1.73)
-2.9
(1.16)
Percent CD8+, Day 50, n=9, 9, 10, 10, 9
-2.2
(1.01)
-0.7
(1.22)
-0.9
(1.19)
1.6
(1.52)
-2.4
(1.57)
4. Secondary Outcome
Title Number of Participants With Treatment Emergent Non-serious Adverse Event (Non-SAE) and Serious AE (SAE)
Description An AE is any new untoward medical occurrence or worsening of a pre-existing medical condition in a participant or clinical investigation participant administered an investigational (medicinal) product and that does not necessarily have a causal relationship with this treatment. Any untoward medical occurrence resulting in death, life threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, congenital anomaly/birth defect, any other situation according to medical or scientific judgment that may not be immediately life-threatening or result in death or hospitalization but may jeopardize the participant or may require medical or surgical intervention to prevent serious outcomes were categorized as SAE. Treatment emergent adverse events (occurred after start of treatment) have been presented.Safety Population comprised of all randomized participants who used the trial medication at least once.
Time Frame Up to 50 days

Outcome Measure Data

Analysis Population Description
Safety Population
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg QHS + RTV 100 mg QHS BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Measure Participants 10 10 10 10 10
Non-SAE
8
80%
5
50%
9
90%
8
80%
9
90%
SAE
0
0%
0
0%
0
0%
0
0%
0
0%
5. Secondary Outcome
Title Number of Participants With Any Abnormality in Physical Examination
Description A complete physical examination included, at a minimum, assessment of the Cardiovascular, Respiratory, Gastrointestinal and Neurological systems. A brief physical examination included, at a minimum assessments of the skin, lungs, cardiovascular system, and abdomen (liver and spleen). Any abnormality found by investigator during physical examination were recorded. Number of participants with any abnormality in physical examination during study have been reported.
Time Frame Up to 50 days

Outcome Measure Data

Analysis Population Description
Safety Population
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg QHS + RTV 100 mg QHS BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Measure Participants 10 10 10 10 10
Count of Participants [Participants]
1
10%
0
0%
2
20%
1
10%
1
10%
6. Secondary Outcome
Title Number of Participants With Worst-case Abnormalities in Diastolic Blood Pressure (DBP) and Systolic Blood Pressure (SBP)
Description Vital signs including DBP and SBP were recorded. Normal ranges were as following: For DBP, lower limit: value <55 millimeter of mercury (mmHg) and change <-20 mmHg; upper limit: value >90 mmHg and change >20 mmHg). For SBP, lower limit: value <90 mmHg and change <-10 mmHg; upper limit: value >140 mmHg and change >10 mmHg. Number of participants with worst-case abnormalities are presented. Worst-case abnormality was defined as: (1) Below Normal: at least one post-Baseline assessment was below normal range, and no post-Baseline assessment was above normal range. (2) Above Normal: at least one post-Baseline assessment was above normal range, and no post-Baseline assessment was below normal range. (3) Within Normal: all post-Baseline assessments were within normal range. It was to be considered as 'Missing' when there were no post-Baseline assessments.
Time Frame Up to 50 days

Outcome Measure Data

Analysis Population Description
Safety Population
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg QHS + RTV 100 mg QHS BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Measure Participants 10 10 10 10 10
SBP, Above Normal
0
0%
3
30%
1
10%
0
0%
1
10%
SBP, Below Normal
0
0%
0
0%
0
0%
0
0%
0
0%
SBP, Within Normal
10
100%
7
70%
9
90%
10
100%
9
90%
DBP, Above Normal
0
0%
0
0%
0
0%
0
0%
0
0%
DBP, Below Normal
0
0%
0
0%
0
0%
0
0%
0
0%
DBP, Within Normal
10
100%
10
100%
10
100%
10
100%
10
100%
7. Secondary Outcome
Title Number of Participants With Worst-case Abnormalities in Body Temperature, Respiratory Rate [RR], and Heart Rate [HR]
Description Vital signs (body temperature, RR, and HR) were recorded. Normal range were: For HR, lower limit: 55 beats per minute (bpm) and change <-15 bpm; upper limit: >100 bpm and change >30 bpm). For temperature, lower limit: 36.0 Celsius; upper limit: >37.5 Celsius or change >1.7 Celsius). For RR, lower limit: 8 breaths per minute; upper limit: >16 breaths per minute or change >10 breaths per minute. Number of participants with worst-case abnormalities are presented. Worst-case abnormality was defined as: (1) Below Normal: at least one post-Baseline assessment was below normal range, and no post-Baseline assessment was above normal range. (2) Above Normal: at least one post-Baseline assessment was above normal range, and no post-Baseline assessment was below normal range. (3) Within Normal: all post-Baseline assessments were within normal range. It was to be considered as 'Missing' when there were no post-Baseline assessments.
Time Frame Up to 50 days

Outcome Measure Data

Analysis Population Description
Safety Population
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg QHS + RTV 100 mg QHS BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Measure Participants 10 10 10 10 10
HR, Above Normal
0
0%
0
0%
0
0%
0
0%
0
0%
HR, Below Normal
1
10%
2
20%
1
10%
0
0%
1
10%
HR, Within Normal
9
90%
8
80%
9
90%
10
100%
9
90%
RR, Above Normal
4
40%
3
30%
3
30%
3
30%
8
80%
RR, Below Normal
0
0%
0
0%
0
0%
0
0%
0
0%
RR, Within Normal
6
60%
7
70%
7
70%
7
70%
2
20%
Temperature, Above Normal
0
0%
0
0%
0
0%
0
0%
0
0%
Temperature, Below Normal
1
10%
2
20%
0
0%
1
10%
0
0%
Temperature, Within Normal
9
90%
8
80%
10
100%
9
90%
10
100%
8. Secondary Outcome
Title Number of Participants With Worst-case Abnormalities in Electrocardiogram (ECG) Parameters
Description A 12-lead ECG was recorded during the study using an ECG machine that automatically measures ECG parameters. Normal range for ECG parameters were: PR interval (upper: 200 milliseconds [ms]); QRS (lower: 50 ms; upper: 120 ms); Corrected QT interval by Bazett formula (QTcB) (change from Baseline - increases by > 30 ms); Corrected QT interval by Fredericia formula (QTcF) (change from Baseline - increases by > 30 ms). Number of participants with worst-case abnormalities are presented which was defined as: (1) Below Normal: at least one post-Baseline assessment was below normal range, and no post-Baseline assessment was above normal range. (2) Above Normal: at least one post-Baseline assessment was above normal range, and no post-Baseline assessment was below normal range. Within Normal: all post-Baseline assessments were within normal range. It was to be considered as 'Missing' when there were no post-Baseline assessments.
Time Frame Up to 50 days

Outcome Measure Data

Analysis Population Description
Safety Population
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg QHS + RTV 100 mg QHS BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Measure Participants 10 10 10 10 10
PR interval, Above Normal
0
0%
1
10%
0
0%
0
0%
1
10%
PR interval, Below Normal
0
0%
0
0%
0
0%
0
0%
0
0%
PR interval, Within Normal
10
100%
9
90%
10
100%
10
100%
9
90%
QTcB, Above Normal
0
0%
1
10%
2
20%
0
0%
1
10%
QTcB, Below Normal
0
0%
0
0%
0
0%
0
0%
0
0%
QTcB, Within Normal
10
100%
9
90%
8
80%
10
100%
9
90%
QTcF, Above Normal
1
10%
0
0%
1
10%
0
0%
2
20%
QTcF, Below Normal
0
0%
0
0%
0
0%
0
0%
0
0%
QTcF, Within Normal
9
90%
10
100%
9
90%
10
100%
8
80%
9. Secondary Outcome
Title Number of Participants With Clinically Significant Abnormalities in Laboratory Parameters
Description Laboratory parameters included hematology, clinical chemistry and urine parameters. Clinically significant abnormal laboratory findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Any abnormal laboratory test results which were considered clinically significant by the investigator were recorded on the case report form. Number of participants with any clinically significant abnormalities in laboratory parameters have been presented.
Time Frame Up to 50 days

Outcome Measure Data

Analysis Population Description
Safety Population
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg QHS + RTV 100 mg QHS BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Measure Participants 10 10 10 10 10
Count of Participants [Participants]
0
0%
0
0%
0
0%
0
0%
0
0%
10. Secondary Outcome
Title Maximum Observed Plasma Concentration (Cmax) of BMS-626529 Following Q12H Dosing
Description Blood samples were collected at indicated time points to assess Cmax of BMS-626529 following Q12H dosing. Geometric mean and geometric coefficient of variation are presented for Day 1, Day 8 morning dose (Anti Meridiem [AM]), Day 8 evening dose (Post Meridiem [PM]) and Day 8 morning + evening dose (AM+PM). Pharmacokinetic parameter values were derived by non-compartmental methods. Pharmacokinetic (PK) Population was used which comprised of all participants who receive BMS-663068 and provided pharmacokinetic samples.
Time Frame Days 1, 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles).
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Measure Participants 10 10 10 10
Day 1, n=10,10,10,10
1.74
(59.9)
3.52
(26.6)
4.05
(35.8)
2.55
(27.4)
Day 8, AM, n=9,10,10,10
2.22
(67.1)
5.55
(37.5)
5.10
(57.4)
3.18
(22.0)
Day 8, PM, n=9,10,10,10
2.25
(46.4)
4.60
(29.2)
4.77
(36.2)
3.61
(27.5)
Day 8, AM+PM, n=9,10,10,10
2.24
(43.3)
5.05
(31.7)
4.93
(40.1)
3.39
(15.9)
11. Secondary Outcome
Title Cmax of BMS-626529 Following QHS Dosing
Description Blood samples were collected at indicated time points to assess Cmax of BMS-626529 following QHS dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1, Day 8 evening dose (PM) and Day 8 morning (AM) + evening dose (PM).
Time Frame Days 1, 8: pre-evening dose, 1,2,3,4,5,6,8 hours

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles).
Arm/Group Title BMS-663068 1200 mg QHS + RTV 100 mg QHS
Arm/Group Description All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8.
Measure Participants 10
Day 1, n=10
3.85
(32.0)
Day 8, PM, n=9
3.47
(31.7)
Day 8, AM+PM, n=9
3.47
(31.7)
12. Secondary Outcome
Title Trough Observed Plasma Concentration (Ctrough) of BMS-626529 Following Q12H Dosing
Description Blood samples were collected at indicated time points to access Ctrough of BMS-626529 following Q12H dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1, Days 5, 6, 7, 8, Day 8 morning dose (AM) and Day 8 evening dose (PM).
Time Frame Days 1, 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours; Days 5,6,7: pre-morning dose

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles).
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Measure Participants 10 10 10 10
Day 1, n=10,10,10,10
0.349
(156)
0.499
(83.4)
0.640
(114)
0.244
(78.3)
Day 5, n=9,10,10,10
0.473
(119)
1.04
(72.2)
0.760
(67.1)
0.518
(48.2)
Day 6, n=9,10,10,10
0.436
(89.5)
0.839
(49.1)
0.737
(73.2)
0.451
(49.2)
Day 7, n=9,10,10,10
0.495
(96.5)
1.08
(72.9)
0.998
(91.8)
0.542
(73.5)
Day 8, n=9,10,10,10
0.460
(89.2)
0.743
(47.1)
0.720
(83.5)
0.628
(76.9)
Day 8, AM, n=9,10,10,10
0.422
(69.1)
0.951
(88.2)
0.579
(71.5)
0.469
(122)
Day 8, PM, n=9,10,10,10
0.358
(102)
0.653
(109)
0.553
(68.1)
0.487
(47.5)
13. Secondary Outcome
Title Ctrough of BMS-626529 Following QHS Dosing
Description Blood samples were collected at indicated time points to assess Ctrough of BMS-626529 following QHS dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1, Days 5, 6, 7, 8 and Day 8 evening dose (PM).
Time Frame Days 1, 8: pre-evening dose, 1,2,3,4,5,6,8 hours; Days 5,6,7: pre-evening dose

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles).
Arm/Group Title BMS-663068 1200 mg QHS + RTV 100 mg QHS
Arm/Group Description All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8.
Measure Participants 10
Day 1, n=10
0.699
(93.4)
Day 5, n=9
0.0705
(114)
Day 6, n=9
0.0743
(97.7)
Day 7, n=9
0.0719
(166)
Day 8, n=9
0.0546
(146)
Day 8, PM, n=9
0.0544
(156)
14. Secondary Outcome
Title Area Under the Concentration-time Curve in One Dosing Interval (AUC [Tau]) of BMS-626529 Following Q12H Dosing
Description Blood samples were collected at indicated time points to assess AUC (tau) of BMS-626529 following Q12H dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1, Day 8 morning dose (AM) and Day 8 evening dose (PM).
Time Frame Days 1, 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles).
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Measure Participants 10 10 10 10
Day 1, n=10,10,10,10
9.16
(68.7)
18.3
(28.8)
20.6
(45.0)
13.8
(28.3)
Day 8, AM, n=9,10,10,10
13.1
(62.7)
29.9
(37.0)
27.6
(48.4)
19.5
(20.5)
Day 8, PM, n=9,10,10,10
13.1
(63.8)
30.6
(26.3)
27.0
(45.2)
22.5
(34.0)
15. Secondary Outcome
Title AUC (Tau) of BMS-626529 Following QHS Dosing
Description Blood samples were collected at indicated time points to assess AUC (tau) of BMS-626529 following QHS dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1 and Day 8 evening dose (PM).
Time Frame Days 1, 8: pre-evening dose, 1,2,3,4,5,6,8 hours

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles).
Arm/Group Title BMS-663068 1200 mg QHS + RTV 100 mg QHS
Arm/Group Description All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8.
Measure Participants 10
Day 1, n=10
25.5
(38.0)
Day 8 PM, n=9
23.0
(48.2)
16. Secondary Outcome
Title Area Under the Concentration-time Curve Over a 24-hour Period (AUC [0-24]) of BMS-626529 Following Q12H Dosing
Description Blood samples were collected at indicated time points to assess AUC (0-24) of BMS-626529 following Q12H dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 8.
Time Frame Day 8: pre-morning dose, 1,2,3,4,5,6,8,12, 13,14,15,16,17,18,20 hours

Outcome Measure Data

Analysis Population Description
PK Population
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Measure Participants 10 10 10 10
Geometric Mean (Geometric Coefficient of Variation) [Hour*micrograms per milliliter]
26.8
(56.1)
60.6
(30.6)
55.1
(44.3)
42.6
(21.5)
17. Secondary Outcome
Title AUC (0-24) of BMS-626529 Following QHS Dosing
Description Blood samples were collected at indicated time points to assess AUC (0-24) of BMS-626529 following QHS dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 8.
Time Frame Day 8: pre-evening dose, 1,2,3,4,5,6,8 hours

Outcome Measure Data

Analysis Population Description
PK Population
Arm/Group Title BMS-663068 1200 mg QHS + RTV 100 mg QHS
Arm/Group Description All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8.
Measure Participants 10
Geometric Mean (Geometric Coefficient of Variation) [Hour*micrograms per milliliter]
23.0
(48.2)
18. Secondary Outcome
Title Accumulation Index (AI) of BMS-626529 Following Q12H Dosing
Description Blood samples were collected at indicated time points to assess Accumulation Index of BMS-626529 following Q12H dosing. AI was calculated as ratio of AUC(tau) at steady-state to AUC(tau) after the first dose. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 8 morning dose (AM).
Time Frame Day 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed.
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Measure Participants 9 10 10 10
Geometric Mean (Geometric Coefficient of Variation) [Ratio of AUC]
1.53
(49.4)
1.63
(26.7)
1.34
(25.4)
1.42
(37.0)
19. Secondary Outcome
Title Accumulation Index of BMS-626529 Following QHS Dosing
Description Blood samples were collected at indicated time points to assess Accumulation Index of BMS-626529 following QHS dosing. AI was calculated as ratio of AUC(tau) at steady-state to AUC(tau) after the first dose. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 8 evening dose (PM).
Time Frame Day 8: pre-evening dose, 1,2,3,4,5,6,8 hours

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed.
Arm/Group Title BMS-663068 1200 mg QHS + RTV 100 mg QHS
Arm/Group Description All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8.
Measure Participants 9
Geometric Mean (Geometric Coefficient of Variation) [Ratio of AUC]
0.912
(27.1)
20. Secondary Outcome
Title Inhibitory Quotient (IQ) of BMS-626529 by Css,Avg and by Lowest Concentration of a Drug During Dosing Interval (Cmin) Following Q12H Dosing
Description Blood samples were collected at indicated time points to assess IQ of BMS-626529. Inhibitory quotient was calculated as the ratio of BMS-626529 in vivo exposure to in vitro measured protein binding adjusted EC90 (PBA-EC90). The following in vivo exposure measures were used in evaluating IQ: Cmin and Css,avg. Geometric mean and geometric coefficient of variation are presented.
Time Frame Days 1, 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours; Day 9: pre-dose, 4,12 hours; Day 10: pre-dose, 12 hours; Day 11: pre-dose; Days 5,6,7: pre-morning dose

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed. No evidence of a correlation between changes in viral load from Baseline (on Day 9 or the nadir) and the BMS-626529 PK parameters was found. Log10 PBA EC90 and IQs of Cmin and Css,avg were found to correlate with antiviral activity.
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Measure Participants 8 9 10 10
IQ Cmin
11.0
(3510)
97.5
(382)
67.2
(543)
4.54
(21600)
IQ Css,avg
29.7
(4040)
327
(454)
252
(789)
15.4
(14900)
21. Secondary Outcome
Title Inhibitory Quotient (IQ) of BMS-626529 by Css,Avg and by Lowest Concentration of a Drug During Dosing Interval (Cmin) Following QHS Dosing
Description Blood samples were collected at indicated time points to assess IQ of BMS-626529. Inhibitory quotient was calculated as the ratio of BMS-626529 in vivo exposure to in vitro measured protein binding adjusted EC90 (PBA-EC90). The following in vivo exposure measures were used in evaluating IQ: Cmin and Css,avg. Geometric mean and geometric coefficient of variation are presented.
Time Frame Days 1, 8: pre-evening dose, 1,2,3,4,5,6,8 hours; Day 2: pre-evening dose, 12,16 hours; Day 9: pre-dose, 12,16 hours; Day 10: pre-dose, 12 hours; Day 11: pre-dose; Days 5,6,7: pre-evening dose

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed. No evidence of a correlation between changes in viral load from Baseline (on Day 9 or the nadir) and the BMS-626529 PK parameters was found. Log10 PBA EC90 and IQs of Cmin and Css,avg were found to correlate with antiviral activity.
Arm/Group Title BMS-663068 1200 mg QHS + RTV 100 mg QHS
Arm/Group Description All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8.
Measure Participants 9
IQ Cmin
3.86
(1070)
IQ Css,avg
67.8
(902)
22. Secondary Outcome
Title Inhibitory Quotient of BMS-626529 by Ctrough Following Q12H Dosing
Description Blood samples were collected at indicated time points to assess IQ of BMS-626529. Inhibitory quotient was calculated as the ratio of BMS-626529 in vivo exposure to in vitro measured protein binding adjusted EC90 (PBA-EC90). The following in vivo exposure measure was used in evaluating IQ: Ctrough. Geometric mean and geometric coefficient of variation are presented.
Time Frame Days 1, 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours; Day 9: pre-dose, 4,12 hours; Day 10: pre-dose, 12 hours; Day 11: pre-dose; Days 5,6,7: pre-morning dose

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed. No evidence of a correlation between changes in viral load from Baseline (on Day 9 or the nadir) and the BMS-626529 PK parameters was found. Log10 PBA EC90 and IQs of Cmin and Css,avg were found to correlate with antiviral activity.
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
Measure Participants 8 9 10 10
Geometric Mean (Geometric Coefficient of Variation) [Ratio]
12.2
(2750)
120
(568)
87.3
(763)
4.61
(19000)
23. Secondary Outcome
Title Inhibitory Quotient of BMS-626529 by Ctrough Following QHS Dosing
Description Blood samples were collected at indicated time points to assess IQ of BMS-626529. Inhibitory quotient was calculated as the ratio of BMS-626529 in vivo exposure to in vitro measured protein binding adjusted EC90 (PBA-EC90). The following in vivo exposure measure was used in evaluating IQ: Ctrough. Geometric mean and geometric coefficient of variation are presented.
Time Frame Days 1, 8: pre-evening dose, 1,2,3,4,5,6,8 hours; Days 2: pre-evening dose, 12,16 hours; Day 9: pre-dose, 12,16 hours; Day 10: pre-dose, 12 hours; Day 11: pre-dose; Days 5,6,7: pre-evening dose

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed. No evidence of a correlation between changes in viral load from Baseline (on Day 9 or the nadir) and the BMS-626529 PK parameters was found. Log10 PBA EC90 and IQs of Cmin and Css,avg were found to correlate with antiviral activity.
Arm/Group Title BMS-663068 1200 mg QHS + RTV 100 mg QHS
Arm/Group Description All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8.
Measure Participants 9
Geometric Mean (Geometric Coefficient of Variation) [Ratio]
4.77
(1010)
24. Secondary Outcome
Title Cmax of Ritonavir Following Q12H Dosing
Description Blood samples were collected at indicated time points to assess Cmax of ritonavir following Q12H dosing. Geometric mean and geometric coefficient of variation are presented for Day 1, Day 8 morning dose (AM), Day 8 evening dose (PM) and Day 8 morning + evening dose (AM+PM). Pharmacokinetic parameter values were derived by non-compartmental methods. PK Population was used which comprised of all participants who receive ritonavir and provided pharmacokinetic samples.
Time Frame Days 1, 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles).
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8.
Measure Participants 10 10 10
Day 1, n=10,10,10
0.330
(91.3)
0.314
(111)
0.294
(59.6)
Day 8, AM, n=9,10,10
1.31
(101)
1.30
(58.3)
0.841
(44.9)
Day 8, PM, n=9,10,0
1.24
(73.4)
1.48
(47.7)
Day 8, AM+PM, n=9,10,10
1.27
(80.0)
1.39
(50.7)
0.841
(44.9)
25. Secondary Outcome
Title Cmax of Ritonavir Following QHS Dosing
Description Blood samples were collected at indicated time points to assess Cmax of ritonavir following QHS dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1, Day 8 evening dose (PM) and Day 8 morning (AM) + evening dose (PM).
Time Frame Days 1, 8: pre-evening dose, 1,2,3,4,5,6,8 hours

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles).
Arm/Group Title BMS-663068 1200 mg QHS + RTV 100 mg QHS
Arm/Group Description All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8.
Measure Participants 10
Day 1, n=10
0.257
(53.8)
Day 8, PM, n=9
0.628
(56.4)
Day 8, AM+PM, n=9
0.628
(56.4)
26. Secondary Outcome
Title Ctrough of Ritonavir Following Q12H Dosing
Description Blood samples were collected at indicated time points to access Ctrough of ritonavir following Q12H dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1, Days 5, 6, 7, 8, Day 8 morning dose (AM) and Day 8 evening dose (PM).
Time Frame Days 1, 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours; Days 5,6,7: pre-morning dose

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles).
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8.
Measure Participants 10 10 10
Day 1, n=10,10,0
0.117
(90.1)
0.131
(98.2)
Day 5, n=9,10,10
0.502
(84.3)
0.554
(73.9)
0.0831
(77.8)
Day 6, n=9,10,10
0.526
(87.9)
0.594
(77.0)
0.0820
(77.9)
Day 7, n=9,10,10
0.477
(93.5)
0.587
(76.3)
0.0860
(79.9)
Day 8, n=9,10,10
0.470
(90.6)
0.503
(73.2)
0.0891
(81.7)
Day 8, AM, n=9,10,10
0.345
(105)
0.393
(66.3)
0.0912
(70.5)
Day 8, PM, n=9,10,0
0.453
(86.2)
0.476
(77.9)
27. Secondary Outcome
Title Ctrough of Ritonavir Following QHS Dosing
Description Blood samples were collected at indicated time points to assess Ctrough of ritonavir following QHS dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1, Days 5, 6, 7, 8 and Day 8 evening dose (PM).
Time Frame Days 1, 8: pre-evening dose, 1,2,3,4,5,6,8 hours; Days 5,6,7: pre-evening dose

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles).
Arm/Group Title BMS-663068 1200 mg QHS + RTV 100 mg QHS
Arm/Group Description All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8.
Measure Participants 10
Day 1, n=10
0.157
(87.0)
Day 5, n=9
0.107
(69.4)
Day 6, n=9
0.0845
(67.7)
Day 7, n=9
0.0844
(65.0)
Day 8, n=9
0.0808
(73.2)
Day 8, PM, n=9
0.0830
(71.7)
28. Secondary Outcome
Title AUC (Tau) of Ritonavir Following Q12H Dosing
Description Blood samples were collected at indicated time points to assess AUC (tau) of ritonavir following Q12H dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1, Day 8 morning dose (AM) and Day 8 evening dose (PM).
Time Frame Days 1, 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles).
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8.
Measure Participants 10 10 10
Day 1, n=10,10,0
2.37
(99.5)
2.05
(104)
Day 8, AM, n=9,10,10
9.43
(89.1)
9.05
(62.8)
6.76
(49.3)
Day 8, PM, n=9,10,0
9.23
(77.1)
10.4
(52.4)
29. Secondary Outcome
Title AUC (Tau) of Ritonavir Following QHS Dosing
Description Blood samples were collected at indicated time points to assess AUC (tau) of ritonavir following QHS dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 1 and Day 8 evening dose (PM).
Time Frame Days 1, 8: pre-evening dose, 1,2,3,4,5,6,8 hours

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed (represented by n=X in the category titles).
Arm/Group Title BMS-663068 1200 mg QHS + RTV 100 mg QHS
Arm/Group Description All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8.
Measure Participants 10
Day 1, n=10
2.91
(80.4)
Day 8 PM, n=9
6.13
(94.3)
30. Secondary Outcome
Title AUC (0-24) of Ritonavir Following Q12H Dosing
Description Blood samples were collected at indicated time points to assess AUC (0-24) of ritonavir following Q12H dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 8.
Time Frame Day 8: pre-morning dose, 1,2,3,4,5,6,8,12, 13,14,15,16,17,18,20 hours

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed.
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8.
Measure Participants 9 10 10
Geometric Mean (Geometric Coefficient of Variation) [Hour*micrograms per milliliter]
18.9
(80.0)
19.5
(56.6)
6.76
(49.3)
31. Secondary Outcome
Title AUC (0-24) of Ritonavir Following QHS Dosing
Description Blood samples were collected at indicated time points to assess AUC (0-24) of ritonavir following QHS dosing. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 8.
Time Frame Day 8: pre-evening dose, 1,2,3,4,5,6,8 hours

Outcome Measure Data

Analysis Population Description
PK Population
Arm/Group Title BMS-663068 1200 mg QHS + RTV 100 mg QHS
Arm/Group Description All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8.
Measure Participants 9
Geometric Mean (Geometric Coefficient of Variation) [Hour*micrograms per milliliter]
6.13
(94.3)
32. Secondary Outcome
Title Accumulation Index of Ritonavir Following Q12H Dosing
Description Blood samples were collected at indicated time points to assess Accumulation Index of ritonavir following Q12H dosing. AI was calculated as ratio of AUC(tau) at steady-state to AUC(tau) after the first dose. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 8 morning dose (AM).
Time Frame Day 8: pre-morning dose, 1,2,3,4,5,6,8,12 hours; Day 8: 13,14,15,16,17,18,20 hours

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed.
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8.
Measure Participants 9 10 10
Geometric Mean (Geometric Coefficient of Variation) [Ratio of AUC]
3.58
(64.0)
4.41
(41.7)
3.62
(39.8)
33. Secondary Outcome
Title Accumulation Index of Ritonavir Following QHS Dosing
Description Blood samples were collected at indicated time points to assess Accumulation Index of ritonavir following QHS dosing. AI was calculated as ratio of AUC(tau) at steady-state to AUC(tau) after the first dose. Pharmacokinetic parameter values were derived by non-compartmental methods. Geometric mean and geometric coefficient of variation are presented for Day 8 evening dose (PM).
Time Frame Day 8: pre-evening dose, 1,2,3,4,5,6,8 hours

Outcome Measure Data

Analysis Population Description
PK Population. Only those participants with data available at the specified time points were analyzed.
Arm/Group Title BMS-663068 1200 mg QHS + RTV 100 mg QHS
Arm/Group Description All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8.
Measure Participants 9
Geometric Mean (Geometric Coefficient of Variation) [Ratio of AUC]
2.19
(16.2)

Adverse Events

Time Frame Serious adverse events (SAEs) and Non-serious adverse events (Non-SAEs) were collected from the start of the study treatment up to 50 days.
Adverse Event Reporting Description SAEs and Non-SAEs were reported by treatment for the Safety Population which comprised of all randomized participants who used the trial medication at least once.
Arm/Group Title BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg QHS + RTV 100 mg QHS BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Arm/Group Description All participants received BMS-663068 600 milligram (mg) and Ritonavir (RTV) 100 mg every 12 hours (Q12H) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg every night (quaque hora somni [QHS]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg and RTV 100 mg Q12H from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H and RTV 100 mg every 24 hours in the morning (quaque ante meridiem [QAM]) from Day 1 to Day 8. All participants received BMS-663068 1200 mg Q12H from Day 1 to Day 8.
All Cause Mortality
BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg QHS + RTV 100 mg QHS BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Affected / at Risk (%) # Events Affected / at Risk (%) # Events Affected / at Risk (%) # Events Affected / at Risk (%) # Events Affected / at Risk (%) # Events
Total 0/10 (0%) 0/10 (0%) 0/10 (0%) 0/10 (0%) 0/10 (0%)
Serious Adverse Events
BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg QHS + RTV 100 mg QHS BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Affected / at Risk (%) # Events Affected / at Risk (%) # Events Affected / at Risk (%) # Events Affected / at Risk (%) # Events Affected / at Risk (%) # Events
Total 0/10 (0%) 0/10 (0%) 0/10 (0%) 0/10 (0%) 0/10 (0%)
Other (Not Including Serious) Adverse Events
BMS-663068 600 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg QHS + RTV 100 mg QHS BMS-663068 1200 mg Q12H + RTV 100 mg Q12H BMS-663068 1200 mg Q12H + RTV 100 mg QAM BMS-663068 1200 mg Q12H
Affected / at Risk (%) # Events Affected / at Risk (%) # Events Affected / at Risk (%) # Events Affected / at Risk (%) # Events Affected / at Risk (%) # Events
Total 8/10 (80%) 5/10 (50%) 9/10 (90%) 8/10 (80%) 9/10 (90%)
Cardiac disorders
PALPITATIONS 1/10 (10%) 0/10 (0%) 0/10 (0%) 0/10 (0%) 0/10 (0%)
Eye disorders
EYE PRURITUS 0/10 (0%) 0/10 (0%) 1/10 (10%) 0/10 (0%) 0/10 (0%)
Gastrointestinal disorders
ABDOMINAL PAIN 0/10 (0%) 0/10 (0%) 0/10 (0%) 0/10 (0%) 1/10 (10%)
DIARRHOEA 1/10 (10%) 0/10 (0%) 0/10 (0%) 1/10 (10%) 2/10 (20%)
NAUSEA 0/10 (0%) 0/10 (0%) 1/10 (10%) 0/10 (0%) 0/10 (0%)
TOOTHACHE 0/10 (0%) 0/10 (0%) 2/10 (20%) 0/10 (0%) 0/10 (0%)
General disorders
ASTHENIA 1/10 (10%) 0/10 (0%) 1/10 (10%) 0/10 (0%) 0/10 (0%)
CHEST PAIN 0/10 (0%) 0/10 (0%) 0/10 (0%) 0/10 (0%) 1/10 (10%)
DISCOMFORT 0/10 (0%) 1/10 (10%) 0/10 (0%) 0/10 (0%) 0/10 (0%)
FATIGUE 1/10 (10%) 0/10 (0%) 1/10 (10%) 1/10 (10%) 0/10 (0%)
INFLUENZA LIKE ILLNESS 0/10 (0%) 1/10 (10%) 0/10 (0%) 0/10 (0%) 0/10 (0%)
Infections and infestations
ABSCESS JAW 0/10 (0%) 0/10 (0%) 1/10 (10%) 0/10 (0%) 0/10 (0%)
GONORRHOEA 0/10 (0%) 0/10 (0%) 0/10 (0%) 0/10 (0%) 1/10 (10%)
NASOPHARYNGITIS 1/10 (10%) 0/10 (0%) 3/10 (30%) 2/10 (20%) 0/10 (0%)
RHINITIS 1/10 (10%) 0/10 (0%) 0/10 (0%) 0/10 (0%) 0/10 (0%)
Musculoskeletal and connective tissue disorders
ARTHRALGIA 0/10 (0%) 0/10 (0%) 1/10 (10%) 0/10 (0%) 0/10 (0%)
BACK PAIN 0/10 (0%) 0/10 (0%) 1/10 (10%) 0/10 (0%) 0/10 (0%)
FLANK PAIN 0/10 (0%) 0/10 (0%) 0/10 (0%) 0/10 (0%) 1/10 (10%)
MYALGIA 0/10 (0%) 0/10 (0%) 1/10 (10%) 0/10 (0%) 0/10 (0%)
PAIN IN EXTREMITY 0/10 (0%) 0/10 (0%) 1/10 (10%) 0/10 (0%) 0/10 (0%)
Nervous system disorders
DIZZINESS 1/10 (10%) 0/10 (0%) 0/10 (0%) 0/10 (0%) 0/10 (0%)
HEADACHE 4/10 (40%) 3/10 (30%) 4/10 (40%) 3/10 (30%) 4/10 (40%)
NEURALGIA 0/10 (0%) 1/10 (10%) 0/10 (0%) 0/10 (0%) 0/10 (0%)
PRESYNCOPE 1/10 (10%) 0/10 (0%) 0/10 (0%) 1/10 (10%) 0/10 (0%)
SYNCOPE 0/10 (0%) 0/10 (0%) 1/10 (10%) 0/10 (0%) 0/10 (0%)
Psychiatric disorders
DISORIENTATION 1/10 (10%) 0/10 (0%) 1/10 (10%) 0/10 (0%) 2/10 (20%)
LISTLESS 1/10 (10%) 0/10 (0%) 0/10 (0%) 0/10 (0%) 0/10 (0%)
Renal and urinary disorders
MICTURITION URGENCY 1/10 (10%) 1/10 (10%) 1/10 (10%) 1/10 (10%) 3/10 (30%)
Respiratory, thoracic and mediastinal disorders
DYSPNOEA 1/10 (10%) 0/10 (0%) 0/10 (0%) 0/10 (0%) 0/10 (0%)
Skin and subcutaneous tissue disorders
BLISTER 1/10 (10%) 0/10 (0%) 0/10 (0%) 0/10 (0%) 0/10 (0%)
DRY SKIN 1/10 (10%) 0/10 (0%) 0/10 (0%) 0/10 (0%) 0/10 (0%)
ERYTHEMA 1/10 (10%) 0/10 (0%) 0/10 (0%) 2/10 (20%) 1/10 (10%)
HYPERHIDROSIS 0/10 (0%) 0/10 (0%) 1/10 (10%) 0/10 (0%) 0/10 (0%)
PRURITUS 0/10 (0%) 0/10 (0%) 0/10 (0%) 1/10 (10%) 0/10 (0%)
RASH 2/10 (20%) 1/10 (10%) 2/10 (20%) 1/10 (10%) 2/10 (20%)
RASH PRURITIC 1/10 (10%) 0/10 (0%) 1/10 (10%) 0/10 (0%) 0/10 (0%)

Limitations/Caveats

[Not Specified]

More Information

Certain Agreements

Principal Investigators are NOT employed by the organization sponsoring the study.

GSK agreements may vary with individual investigators, but will not prohibit any investigator from publishing. GSK supports the publication of results from all centers of a multi-center trial but requests that reports based on single-site data not precede the primary publication of the entire clinical trial.

Results Point of Contact

Name/Title GSK Response Center
Organization GlaxoSmithKline
Phone 866-435-7343
Email GSKClinicalSupportHD@gsk.com
Responsible Party:
ViiV Healthcare
ClinicalTrials.gov Identifier:
NCT01009814
Other Study ID Numbers:
  • 206267
  • AI438-006
First Posted:
Nov 9, 2009
Last Update Posted:
Jan 3, 2020
Last Verified:
Oct 1, 2019