NCT00783484

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.

Trial Health

87
On Track

Trial Health Score

Automated assessment based on enrollment pace, timeline, and geographic reach

Enrollment
37

participants targeted

Target at P50-P75 for phase_1 healthy-volunteers

Timeline
Completed

Started Oct 2008

Typical duration for phase_1 healthy-volunteers

Geographic Reach
1 country

1 active site

Status
completed

Health score is calculated from publicly available data and should be used for screening purposes only.

Trial Relationships

Click on a node to explore related trials.

Study Timeline

Key milestones and dates

Study Start

First participant enrolled

October 1, 2008

Completed
29 days until next milestone

First Submitted

Initial submission to the registry

October 30, 2008

Completed
1 day until next milestone

First Posted

Study publicly available on registry

October 31, 2008

Completed
6 months until next milestone

Primary Completion

Last participant's last visit for primary outcome

May 1, 2009

Completed
Same day until next milestone

Study Completion

Last participant's last visit for all outcomes

May 1, 2009

Completed
Last Updated

June 2, 2009

Status Verified

May 1, 2009

Enrollment Period

7 months

First QC Date

October 30, 2008

Last Update Submit

May 28, 2009

Conditions

Keywords

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

Outcome Measures

Primary Outcomes (2)

  • 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 Outcomes (2)

  • 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

Study Arms (6)

Cohort 1

EXPERIMENTAL

PF-03716539 crossover, single dose escalation (doses subject to change).

Drug: PF-03716539Other: Placebo

Cohort 2

EXPERIMENTAL

PF-03716539 crossover, single dose escalation (doses subject to change).

Drug: PF-03716539Other: Placebo

Cohort 3

EXPERIMENTAL

Midazolam-PF-03716539 drug-drug interaction (PF-03716539 doses subject to change).

Drug: MidazolamDrug: Midazolam + PF-03716539 (100 mg)Drug: Midazolam + PF-03716539 (50 mg)

Cohort 4

EXPERIMENTAL

Darunavir-PF-03716539 drug-drug interaction (PF-03716539 doses subject to change).

Drug: DarunavirDrug: Darunavir + PF-03716539

Cohort 5

EXPERIMENTAL

Maraviroc-PF-03716539 drug-drug interaction (PF-03716539 doses subject to change).

Drug: MaravirocDrug: Maraviroc +PF-03716539

Cohort 6

EXPERIMENTAL

Maraviroc-PF-03716539 drug-drug interaction (PF-03716539 200 mg).

Drug: MaravirocDrug: Maraviroc +PF-03716539

Interventions

PF-03716539 10 mg oral solution, single dose

Cohort 1
PlaceboOTHER

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

Cohort 1

Midazolam 1 mg IV, single dose

Cohort 3

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

Cohort 3

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

Cohort 3

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

Cohort 4

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

Cohort 4

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

Also known as: Selzentry
Cohort 5

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

Also known as: Selzentry
Cohort 5

Eligibility Criteria

Age18 Years - 55 Years
Sexall
Healthy VolunteersYes
Age GroupsAdult (18-64)

You may qualify if:

  • 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).

You may not qualify if:

  • 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.

Contact the study team to confirm eligibility.

Sponsors & Collaborators

Study Sites (1)

Pfizer Investigational Site

Brussels, 1070, Belgium

Location

Related Links

MeSH Terms

Interventions

MidazolamDarunavirMaraviroc

Intervention Hierarchy (Ancestors)

BenzodiazepinesBenzazepinesHeterocyclic Compounds, 2-RingHeterocyclic Compounds, Fused-RingHeterocyclic CompoundsSulfonamidesAmidesOrganic ChemicalsCarbamatesAcids, AcyclicCarboxylic AcidsSulfonesSulfur CompoundsFuransHeterocyclic Compounds, 1-RingCyclohexanesCycloparaffinsHydrocarbons, AlicyclicHydrocarbons, CyclicHydrocarbonsTriazolesAzoles

Study Officials

  • Pfizer CT.gov Call Center

    Pfizer

    STUDY DIRECTOR

Study Design

Study Type
interventional
Phase
phase 1
Allocation
RANDOMIZED
Masking
DOUBLE
Who Masked
PARTICIPANT, INVESTIGATOR
Purpose
TREATMENT
Intervention Model
CROSSOVER
Sponsor Type
INDUSTRY

Study Record Dates

First Submitted

October 30, 2008

First Posted

October 31, 2008

Study Start

October 1, 2008

Primary Completion

May 1, 2009

Study Completion

May 1, 2009

Last Updated

June 2, 2009

Record last verified: 2009-05

Locations