A Study To Evaluate The Safety, Tolerability And Pharmacokinetics Of Single Oral Doses Of PF-03716539 In Healthy Adult Subjects
This study has been completed.
Sponsor:
Pfizer
Information provided by:
Pfizer
ClinicalTrials.gov Identifier:
NCT00783484
First received: October 30, 2008
Last updated: May 28, 2009
Last verified: May 2009
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Purpose
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 | Intervention | Phase |
|---|---|---|
|
Healthy Volunteers |
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 |
Phase 1 |
| Study Type: | Interventional |
| Study Design: | Allocation: Randomized Endpoint Classification: Safety Study Intervention Model: Crossover Assignment Masking: Double Blind (Subject, 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 |
Resource links provided by NLM:
Further study details as provided by Pfizer:
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. [ Time Frame: 27 days ] [ Designated as safety issue: Yes ]
- To explore the pharmacokinetics of escalating single oral doses of PF 03716539 in healthy adult subjects. [ Time Frame: 6 days ] [ Designated as safety issue: No ]
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. [ Time Frame: 6 days ] [ Designated as safety issue: No ]
- To evaluate the potential of PF 03716539 to enhance or "boost" the pharmacokinetics of both darunavir and maraviroc. [ Time Frame: 8 days ] [ Designated as safety issue: No ]
| Enrollment: | 37 |
| Study Start Date: | October 2008 |
| Study Completion Date: | May 2009 |
| Primary Completion Date: | May 2009 (Final data collection date for primary outcome measure) |
| Arms | Assigned Interventions |
|---|---|
|
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 Name: Selzentry
Drug: Maraviroc +PF-03716539
Maraviroc 150 mg tablet, single dose plus PF-03716539 100 mg oral solution, single dose (Day 7)
Other Name: 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 Name: Selzentry
Drug: Maraviroc +PF-03716539
Maraviroc 225 mg tablet, single dose plus PF-03716539 200 mg oral solution, single dose (Day 7)
Other Name: Selzentry
|
Eligibility| Ages Eligible for Study: | 18 Years to 55 Years |
| Genders Eligible for Study: | Both |
| Accepts Healthy Volunteers: | Yes |
Criteria
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 More Information
Additional Information:
No publications provided
| Responsible Party: | Director, Clinical Trial Disclosure Group, Pfizer, Inc. |
| ClinicalTrials.gov Identifier: | NCT00783484 History of Changes |
| Other Study ID Numbers: | B0831001 |
| Study First Received: | October 30, 2008 |
| Last Updated: | May 28, 2009 |
| Health Authority: | Belgium: Federal Agency for Medicinal Products and Health Products |
Keywords provided by Pfizer:
|
First in Human (FIH), PF-03716539, PK enhancer |
Additional relevant MeSH terms:
|
Midazolam Darunavir Adjuvants, Anesthesia Central Nervous System Agents Therapeutic Uses Pharmacologic Actions Anti-Anxiety Agents Tranquilizing Agents Central Nervous System Depressants Physiological Effects of Drugs Psychotropic Drugs Hypnotics and Sedatives Anesthetics, Intravenous |
Anesthetics, General Anesthetics GABA Modulators GABA Agents Neurotransmitter Agents Molecular Mechanisms of Pharmacological Action HIV Protease Inhibitors Protease Inhibitors Enzyme Inhibitors Anti-HIV Agents Anti-Retroviral Agents Antiviral Agents Anti-Infective Agents |
ClinicalTrials.gov processed this record on May 23, 2013