A Study To Evaluate The Safety, Tolerability And Pharmacokinetics Of Single Oral Doses Of PF-03716539 In Healthy Adult Subjects
- Conditions
- Healthy Volunteers
- Interventions
- Registration Number
- NCT00783484
- Lead Sponsor
- Pfizer
- 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.
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- All
- Target Recruitment
- 37
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).
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.
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- CROSSOVER
- Arm && Interventions
Group Intervention Description Cohort 3 Midazolam + PF-03716539 (50 mg) Midazolam-PF-03716539 drug-drug interaction (PF-03716539 doses subject to change). Cohort 1 Placebo PF-03716539 crossover, single dose escalation (doses subject to change). Cohort 2 Placebo PF-03716539 crossover, single dose escalation (doses subject to change). Cohort 3 Midazolam + PF-03716539 (100 mg) Midazolam-PF-03716539 drug-drug interaction (PF-03716539 doses subject to change). Cohort 1 PF-03716539 PF-03716539 crossover, single dose escalation (doses subject to change). Cohort 6 Maraviroc +PF-03716539 Maraviroc-PF-03716539 drug-drug interaction (PF-03716539 200 mg). Cohort 2 PF-03716539 PF-03716539 crossover, single dose escalation (doses subject to change). Cohort 5 Maraviroc +PF-03716539 Maraviroc-PF-03716539 drug-drug interaction (PF-03716539 doses subject to change). Cohort 4 Darunavir + PF-03716539 Darunavir-PF-03716539 drug-drug interaction (PF-03716539 doses subject to change). Cohort 4 Darunavir Darunavir-PF-03716539 drug-drug interaction (PF-03716539 doses subject to change). Cohort 3 Midazolam Midazolam-PF-03716539 drug-drug interaction (PF-03716539 doses subject to change). Cohort 5 Maraviroc Maraviroc-PF-03716539 drug-drug interaction (PF-03716539 doses subject to change). Cohort 6 Maraviroc Maraviroc-PF-03716539 drug-drug interaction (PF-03716539 200 mg).
- Primary Outcome Measures
Name Time Method 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
Name Time Method To evaluate the potential of PF 03716539 to enhance or "boost" the pharmacokinetics of both darunavir and maraviroc. 8 days To assess the potency of PF 03716539 for CYP3A4 inhibition utilizing single dose IV midazolam as a probe substrate for CYP3A4/5. 6 days
Trial Locations
- Locations (1)
Pfizer Investigational Site
🇧🇪Bruxelles, Belgium