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

Healthy Volunteers Clinical Trial

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

Clinical Trial Details — Status: Completed

Administrative data

• NCT number: NCT00783484
• Other study ID #: B0831001
• Status: Completed
• Phase: Phase 1
• First received: October 30, 2008
• Last updated: May 28, 2009
• Start date: October 2008
• Est. completion date: May 2009

Study information

• Verified date: May 2009
• Source: Pfizer
• Contact: n/a
• Is FDA regulated: No
• Health authority: Belgium: Federal Agency for Medicinal Products and Health Products
• Study type: Interventional

Clinical Trial 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.

Recruitment information / eligibility

• Status: Completed
• Enrollment: 37
• Est. completion date: May 2009
• Est. primary completion date: May 2009
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: Both
• Age group: 18 Years to 55 Years

Eligibility

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.

Study Design

Allocation: Randomized, Endpoint Classification: Safety Study, Intervention Model: Crossover Assignment, Masking: Double Blind (Subject, Investigator), Primary Purpose: Treatment

Related Conditions & MeSH terms

• Healthy Volunteers

Intervention

Drug:
• PF-03716539
PF-03716539 10 mg oral solution, single dose
• PF-03716539
PF-03716539 25 mg oral solution, single dose
• 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)

Drug:
• PF-03716539
PF-03716539 100 mg oral solution, single dose
• PF-03716539
PF-03716539 200 mg oral solution, single dose
• 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)

Drug:
• Midazolam
Midazolam 1 mg IV, single dose
• Midazolam + PF-03716539 (100 mg)
Midazolam 1 mg IV, single dose plus PF-03716539 100 mg oral solution, single dose
• Midazolam + PF-03716539 (50 mg)
Midazolam 1 mg IV, single dose plus PF-03716539 50 mg oral solution, single dose
• Darunavir
Darunavir 600 mg tablet twice daily for 9 days (Days 1-9)
• Darunavir + PF-03716539
Darunavir 600 mg tablet, single dose plus PF-03716539 50 mg oral solution, single dose (Day 10)
• Maraviroc
Maraviroc 150 mg tablet once daily for 6 days (Days 1-6)
• Maraviroc +PF-03716539
Maraviroc 150 mg tablet, single dose plus PF-03716539 100 mg oral solution, single dose (Day 7)
• Maraviroc
Maraviroc 225 mg tablet once daily for 6 days (Days 1-6)
• Maraviroc +PF-03716539
Maraviroc 225 mg tablet, single dose plus PF-03716539 200 mg oral solution, single dose (Day 7)

Locations

Country	Name	City	State
Belgium	Pfizer Investigational Site	Bruxelles

Sponsors (1)

Lead Sponsor	Collaborator
Pfizer

Country where clinical trial is conducted

Belgium, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	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	Yes
Primary	To explore the pharmacokinetics of escalating single oral doses of PF 03716539 in healthy adult subjects.		6 days	No
Secondary	To assess the potency of PF 03716539 for CYP3A4 inhibition utilizing single dose IV midazolam as a probe substrate for CYP3A4/5.		6 days	No
Secondary	To evaluate the potential of PF 03716539 to enhance or "boost" the pharmacokinetics of both darunavir and maraviroc.		8 days	No

External Links

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