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:
Information provided by:
Pfizer
ClinicalTrials.gov Identifier:
NCT00783484
First received: October 30, 2008
Last updated: May 28, 2009
Last verified: May 2009
  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
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the Contacts provided below. For general information, see Learn About Clinical Studies.

Please refer to this study by its ClinicalTrials.gov identifier: NCT00783484

Locations
Belgium
Pfizer Investigational Site
Bruxelles, Belgium, 1070
Sponsors and Collaborators
Pfizer
Investigators
Study Director: Pfizer CT.gov Call Center Pfizer
  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 July 13, 2014