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

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

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT00783484

Enrollment

Registered

2008-10-31

Start date

2008-10-31

Completion date

2009-05-31

Last updated

2009-06-02

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy Volunteers

Keywords

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

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.

Interventions

DRUGPF-03716539

PF-03716539 10 mg oral solution, single dose

OTHERPlacebo

Placebo for 3 mg, 10 mg and 25 mg of PF-03716539 (single dose)

DRUGMidazolam

Midazolam 1 mg IV, single dose

DRUGMidazolam + PF-03716539 (100 mg)

Midazolam 1 mg IV, single dose plus PF-03716539 100 mg oral solution, single dose

DRUGMidazolam + PF-03716539 (50 mg)

Midazolam 1 mg IV, single dose plus PF-03716539 50 mg oral solution, single dose

DRUGDarunavir

Darunavir 600 mg tablet twice daily for 9 days (Days 1-9)

DRUGDarunavir + PF-03716539

Darunavir 600 mg tablet, single dose plus PF-03716539 50 mg oral solution, single dose (Day 10)

DRUGMaraviroc

Maraviroc 150 mg tablet once daily for 6 days (Days 1-6)

DRUGMaraviroc +PF-03716539

Maraviroc 150 mg tablet, single dose plus PF-03716539 100 mg oral solution, single dose (Day 7)

Study design

Allocation

RANDOMIZED

Intervention model

CROSSOVER

Primary purpose

TREATMENT

Masking

DOUBLE (Subject, Investigator)

Eligibility

Sex/Gender

ALL

Age

18 Years to 55 Years

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.

Design outcomes

Primary

Measure	Time frame
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

Measure	Time frame
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

Countries

Belgium

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026