A Phase 1 Clinical Study to Investigate the Pharmacokinetics and Safety/Tolerability of SA001 in Healthy Male Volunteers
Study Details
Study Description
Brief Summary
The purpose of this phase1 study is to investigate the pharmacokinetics, safety and tolerability of a single oral dose of SA001 and its active metabolite in healthy male volunteers.
Condition or Disease | Intervention/Treatment | Phase |
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Phase 1 |
Detailed Description
This study consists of Part 1 followed Part 2.
Part 1 (Dose escalation study, SA001 60mg~300mg dose group) The part 1 is a dose escalation study. The starting dose is SA001 60mg, and the maximum dose is 300mg. Each dose group is assigned to SA001 or Placebo in a ratio of 3:1. The pharmacokinetics, safety and tolerability of SA001 and its metabolite are investigated after a single oral administration on the fasting state.
Part 2 (Single dose and food effect study, SA001 120mg and 300mg dose group) The purpose of this part 2 is to evaluate the food effect of a high-fat diets(HFDs) on the single oral dose pharmacokinetics of SA001 and its metabolite.
Study Design
Arms and Interventions
Arm | Intervention/Treatment |
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Experimental: Cohort 1 (SA001 60mg or Placebo) 6 subjects receiving a single dose of 60mg SA001 and 2 subjects receiving placebo |
Drug: SA001 60mg or Placebo
Study Drug: SA001 60mg
Comparator: Placebo
Cohort 1 in the part 1 (Dose escalation study)
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Experimental: Cohort 2 (SA001 120mg or Placebo) 6 subjects receiving a single dose of 120mg SA001 and 2 subjects receiving placebo |
Drug: SA001 120mg or Placebo
Study Drug: SA001 120mg
Comparator: Placebo
Cohort 2 in the part 1 (Dose escalation study) and part 2 (Food effect study)
|
Experimental: Cohort 3 (SA001 180mg or Placebo) 6 subjects receiving a single dose of 180mg SA001 and 2 subjects receiving placebo |
Drug: SA001 180mg or Placebo
Study Drug: SA001 180mg
Comparator: Placebo
Cohort 3 in the part 1 (Dose escalation study)
|
Experimental: Cohort 4 (SA001 240mg or Placebo) 6 subjects receiving a single dose of 240mg SA001 and 2 subjects receiving placebo |
Drug: SA001 240mg or Placebo
Study Drug: SA001 240mg
Comparator: Placebo
Cohort 4 in the part 1 (Dose escalation study)
|
Experimental: Cohort 5 (SA001 300mg or Placebo) 6 subjects receiving a single dose of 300mg SA001 and 2 subjects receiving placebo |
Drug: SA001 300mg or Placebo
Study Drug: SA001 300mg
Comparator: Placebo
Cohort 5 in the part 1(Dose escalation study) and part 2 (Food effect study)
|
Outcome Measures
Primary Outcome Measures
- The incidence of treated related adverse event [Part1: Day-2(administration) to approximately Day 15 (Post study visit)]
Safety/Tolerability Assessment in the part 1
Secondary Outcome Measures
- Area under the curve (AUC) from time 0 to the time of the last quantifiable concentration (AUC0-tlast) of SA001 and its metabolite [Part1: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose, Part2: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose]
- Area under the curve (AUC) from time 0 extrapolated to infinity (AUC0-∞) of SA001 and its metabolite [Part1: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose, Part2: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose]
- Maximum observed plasma concentration (Cmax) of SA001 and its metabolite [Part1: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose, Part2: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose]
- Time to reach the maximum observed plasma concentration (tmax) of SA001 and its metabolite [Part1: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose, Part2: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose]
- t1/2 of SA001 and its metabolite [Part1: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose, Part2: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose]
- CL/F of SA001 and its metabolite [Part1: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose, Part2: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose]
- Vz/F of SA001 and its metabolite [Part1: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose, Part2: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose]
- CLR of SA001 and its metabolite [Part1: predose and 0 ~ 4, 4 ~ 8, 8 ~ 12, 12 ~ 24, 24 ~ 32 and 32 ~ 48 hours postdose, Part2: predose and 0 ~ 4, 4 ~ 8, 8 ~ 12, 12 ~ 24, 24 ~ 32 and 32 ~ 48 hours postdose]
CLR = Ae / AUCinf (Ae: total amount excreted in the urine)
- Fraction recovered unchanged in urine (FR) of SA001 and its metabolite [Part1: predose and 0 ~ 4, 4 ~ 8, 8 ~ 12, 12 ~ 24, 24 ~ 32 and 32 ~ 48 hours postdose, Part2: predose and 0 ~ 4, 4 ~ 8, 8 ~ 12, 12 ~ 24, 24 ~ 32 and 32 ~ 48 hours postdose]
Eligibility Criteria
Criteria
Inclusion Criteria:
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19 years to 45 years (Healthy male Korean)
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Body weight of 55 to 90kg; and BMI of 18.0 to 27.0 kg/m^2
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Subject who voluntarily agrees to participate in this study and has given a written informed consent, after fully understanding the detailed explanation of this study
Exclusion Criteria:
- Subject with a disease history of any clinically significant condition as below.
- Liver, Kidney, nervous system, immune system, respiratory system, endocrine system, tumor, cardiovascular disease or mental illness (mood disorder or obsessive-compulsive disorder etc.) etc.
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Subject with a history of gastrointestinal disease (Crohn's disease, ulcer, acute or chronic pancreatitis, etc.) or gastrointestinal surgery (except simple appendicectomy or hernia surgery) that may affect the absorption of the study drug
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Subject with a history of clinically significant hypersensitivity or hypersensitivity reactions to drugs (aspirin, antibiotics, etc.)
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Serum ALT(SGPT)/AST(SGOT) >1.5×institutional upper limit normal (ULN)
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eGFR< 90mL/min/1.73m^2
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Systolic blood pressure <100 mmHg or >160 mmHg
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Diastolic blood pressure <60 mmHg or >100 mmHg
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Inadequate cardiac function confirmed by 12-lead ECG findings at screening as followings:
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QTcF > 430msec (males)
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PR interval > 200msec or < 110msec
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QRS complex > 120msec
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Evidence of 2nd- or 3rd-degree atrioventricular (AV) block
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Pathologic Q waves (defined as Q-wave > 40msec or depth > 0.5mV)
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Evidence of ventricular preexicitation, left bundle branch block (LBBB), right bundle branch block (RBBB, Incomplete RBBB)
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Subject with risk factors for Torsade de pointes such as long QT syndrome, family history of sudden death, heart failure, hypokalemia, and arrhythmias
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Subject with a history of drug abuse within 60 days prior to screening or who is positive for drugs of abuse in urine tests at screening
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Subject who received any prescription drug or herbal medicine within 14 days prior to the first administration of the Investigational product
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Subject who received any drugs such as
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Prescription drug or herbal medicine within 14 days prior to the first administration of the investigational products
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Over the counter (OTC) or vitamin within 7 days prior to the first administration of the investigational products
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Subject who received other investigational products within 90 days prior to the first administration of the investigational products
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Subject who continuously drink alcohol (more than 21 units/week, 1 unit = 10 g of pure alcohol) or cannot abstain from alcohol during the study period
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Subject with history of smoking within 90 days prior to the first administration of the investigational products
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Subject who cannot prohibit grapefruit/ caffeine-containing foods during the study period from 3 days before the first administration of the investigational products
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Man of reproductive potential not willing to use contraceptive measures during the study period
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Subject not eligible for study participation in the opinion of the investigator
Contacts and Locations
Locations
Site | City | State | Country | Postal Code | |
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1 | Seoul National University Hospital | Seoul | Korea, Republic of |
Sponsors and Collaborators
- Samjin Pharmaceutical Co., Ltd.
Investigators
- Principal Investigator: Kyung-sang Yu, M.D., Ph.D., M.B.A, Seoul National University College of Medicine / Seoul National University Hospital
Study Documents (Full-Text)
None provided.More Information
Publications
None provided.- SJSA001