A Study To Evaluate The Safety, Tolerability And Pharmacokinetics Of Single Oral Doses Of PF-03716539 In Healthy Adult Subjects

Sponsor

Pfizer (Industry)

Overall Status

Completed

CT.gov ID

NCT00783484

Collaborator

(none)

Enrollment

Location

Arms

Duration (Months)

5.3

Patients Per Site Per Month

Study Details

Study Description

Brief Summary

First in human study to evaluate the safety, tolerability, and pharmacokinetics of PF-03716539. The potential of PF-03716539 to increase the concentrations of midazolam, darunavir and maraviroc will also be evaluated.

Condition or Disease	Intervention/Treatment	Phase
Healthy Volunteers	Drug: PF-03716539 Drug: PF-03716539 Drug: PF-03716539 Other: Placebo Drug: PF-03716539 Drug: PF-03716539 Drug: PF-03716539 Other: Placebo Drug: Midazolam Drug: Midazolam + PF-03716539 (100 mg) Drug: Midazolam + PF-03716539 (50 mg) Drug: Darunavir Drug: Darunavir + PF-03716539 Drug: Maraviroc Drug: Maraviroc +PF-03716539 Drug: Maraviroc Drug: Maraviroc +PF-03716539	Phase 1

Study Design

Study Type:

Interventional

Actual Enrollment :

37 participants

Allocation:

Randomized

Intervention Model:

Crossover Assignment

Masking:

Double (Participant, Investigator)

Primary Purpose:

Treatment

Official Title:

A Double-Blind (3rd Party Open), Placebo-Controlled, Crossover, Dose Escalating Study To Evaluate The Safety, Tolerability And Pharmacokinetics Of Single Oral Doses Of PF-03716539, To Assess The Potential Of PF-03716539 To Inhibit CYP3A4 (In Vivo) And To Evaluate The Drug Interaction Potential Between PF-03716539 And Darunavir Or Maraviroc In Healthy Adult Subjects

Study Start Date :

Oct 1, 2008

Actual Primary Completion Date :

May 1, 2009

Actual Study Completion Date :

May 1, 2009

Arms and Interventions

Arm	Intervention/Treatment
Experimental: Cohort 1 PF-03716539 crossover, single dose escalation (doses subject to change).	Drug: PF-03716539 PF-03716539 10 mg oral solution, single dose Drug: PF-03716539 PF-03716539 25 mg oral solution, single dose Drug: PF-03716539 PF-03716539 3 mg oral solution, single dose Other: Placebo Placebo for 3 mg, 10 mg and 25 mg of PF-03716539 (single dose)
Experimental: Cohort 2 PF-03716539 crossover, single dose escalation (doses subject to change).	Drug: PF-03716539 PF-03716539 100 mg oral solution, single dose Drug: PF-03716539 PF-03716539 200 mg oral solution, single dose Drug: PF-03716539 PF-03716539 50 mg oral solution, single dose Other: Placebo Placebo for 50 mg, 100 mg and 200 mg of PF-03716539 (single dose)
Experimental: Cohort 3 Midazolam-PF-03716539 drug-drug interaction (PF-03716539 doses subject to change).	Drug: Midazolam Midazolam 1 mg IV, single dose Drug: Midazolam + PF-03716539 (100 mg) Midazolam 1 mg IV, single dose plus PF-03716539 100 mg oral solution, single dose Drug: Midazolam + PF-03716539 (50 mg) Midazolam 1 mg IV, single dose plus PF-03716539 50 mg oral solution, single dose
Experimental: Cohort 4 Darunavir-PF-03716539 drug-drug interaction (PF-03716539 doses subject to change).	Drug: Darunavir Darunavir 600 mg tablet twice daily for 9 days (Days 1-9) Drug: Darunavir + PF-03716539 Darunavir 600 mg tablet, single dose plus PF-03716539 50 mg oral solution, single dose (Day 10)
Experimental: Cohort 5 Maraviroc-PF-03716539 drug-drug interaction (PF-03716539 doses subject to change).	Drug: Maraviroc Maraviroc 150 mg tablet once daily for 6 days (Days 1-6) Other Names: Selzentry Drug: Maraviroc +PF-03716539 Maraviroc 150 mg tablet, single dose plus PF-03716539 100 mg oral solution, single dose (Day 7) Other Names: Selzentry
Experimental: Cohort 6 Maraviroc-PF-03716539 drug-drug interaction (PF-03716539 200 mg).	Drug: Maraviroc Maraviroc 225 mg tablet once daily for 6 days (Days 1-6) Other Names: Selzentry Drug: Maraviroc +PF-03716539 Maraviroc 225 mg tablet, single dose plus PF-03716539 200 mg oral solution, single dose (Day 7) Other Names: Selzentry

Outcome Measures

Primary Outcome Measures

To evaluate the safety and tolerability of escalating single oral doses of PF 03716539 administered as Extemporaneous Powder for Solution (EPS) in healthy adult subjects. [27 days]
To explore the pharmacokinetics of escalating single oral doses of PF 03716539 in healthy adult subjects. [6 days]

Secondary Outcome Measures

To assess the potency of PF 03716539 for CYP3A4 inhibition utilizing single dose IV midazolam as a probe substrate for CYP3A4/5. [6 days]
To evaluate the potential of PF 03716539 to enhance or "boost" the pharmacokinetics of both darunavir and maraviroc. [8 days]

Eligibility Criteria

Criteria

Ages Eligible for Study:

18 Years to 55 Years

Sexes Eligible for Study:

All

Accepts Healthy Volunteers:

Yes

Inclusion Criteria:

Healthy male and/or female subjects between the ages of 18 and 55 years, inclusive.

Body Mass Index (BMI) of approximately 18 to 30 kg/m2. Total body weight >50 kg (110 lbs).

Exclusion Criteria:

Pregnant or nursing females. females of childbearing potential. Evidence or history of clinically significant hematological, renal (including kidney stones), endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at time of dosing) or clinical findings at screening.

Treatment with an investigational drug within 30 days (or determined by the local requirement, whichever is longer) or 5 half-lives preceding the first dose of study medication.

Contacts and Locations

Locations

	Site	City	State	Country	Postal Code
1	Pfizer Investigational Site	Bruxelles		Belgium	1070

Sponsors and Collaborators

Pfizer

Investigators

Study Director: Pfizer CT.gov Call Center, Pfizer

Study Documents (Full-Text)

None provided.

More Information

Additional Information:

To obtain contact information for a study center near you, click here.

Publications

None provided.

Responsible Party:

, ,

ClinicalTrials.gov Identifier:

NCT00783484

Other Study ID Numbers:

B0831001

First Posted:

Oct 31, 2008

Last Update Posted:

Jun 2, 2009

Last Verified:

May 1, 2009

Keywords provided by , ,

First in Human (FIH), PF-03716539, PK enhancer

Additional relevant MeSH terms:

Maraviroc

Darunavir

Midazolam

Study Results

No Results Posted as of Jun 2, 2009