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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.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Cohort 1 | Experimental | PF-03716539 crossover, single dose escalation (doses subject to change). |
|
| Cohort 2 | Experimental | PF-03716539 crossover, single dose escalation (doses subject to change). |
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| Cohort 3 | Experimental | Midazolam-PF-03716539 drug-drug interaction (PF-03716539 doses subject to change). |
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| Cohort 4 | Experimental | Darunavir-PF-03716539 drug-drug interaction (PF-03716539 doses subject to change). |
|
| Cohort 5 | Experimental | Maraviroc-PF-03716539 drug-drug interaction (PF-03716539 doses subject to change). |
|
| Cohort 6 |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| PF-03716539 | Drug | PF-03716539 10 mg oral solution, single dose |
| |
| Measure | Description | Time Frame |
|---|---|---|
| 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 |
| Measure | Description | Time Frame |
|---|---|---|
| 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. |
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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.
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| Name | Affiliation | Role |
|---|---|---|
| Pfizer CT.gov Call Center | Pfizer | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Pfizer Investigational Site | Brussels | 1070 | Belgium |
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| Label | URL |
|---|---|
| To obtain contact information for a study center near you, click here. | View source |
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| Experimental |
Maraviroc-PF-03716539 drug-drug interaction (PF-03716539 200 mg). |
|
| PF-03716539 |
| Drug |
PF-03716539 25 mg oral solution, single dose |
|
| PF-03716539 | Drug | PF-03716539 3 mg oral solution, single dose |
|
| Placebo | Other | Placebo for 3 mg, 10 mg and 25 mg of PF-03716539 (single dose) |
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| PF-03716539 | Drug | PF-03716539 100 mg oral solution, single dose |
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| PF-03716539 | Drug | PF-03716539 200 mg oral solution, single dose |
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| PF-03716539 | Drug | PF-03716539 50 mg oral solution, single dose |
|
| Placebo | Other | Placebo for 50 mg, 100 mg and 200 mg of PF-03716539 (single dose) |
|
| Midazolam | Drug | Midazolam 1 mg IV, single dose |
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| Midazolam + PF-03716539 (100 mg) | Drug | Midazolam 1 mg IV, single dose plus PF-03716539 100 mg oral solution, single dose |
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| Midazolam + PF-03716539 (50 mg) | Drug | Midazolam 1 mg IV, single dose plus PF-03716539 50 mg oral solution, single dose |
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| Darunavir | Drug | Darunavir 600 mg tablet twice daily for 9 days (Days 1-9) |
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| Darunavir + PF-03716539 | Drug | Darunavir 600 mg tablet, single dose plus PF-03716539 50 mg oral solution, single dose (Day 10) |
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| Maraviroc | Drug | Maraviroc 150 mg tablet once daily for 6 days (Days 1-6) |
|
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| Maraviroc +PF-03716539 | Drug | Maraviroc 150 mg tablet, single dose plus PF-03716539 100 mg oral solution, single dose (Day 7) |
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| Maraviroc | Drug | Maraviroc 225 mg tablet once daily for 6 days (Days 1-6) |
|
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| Maraviroc +PF-03716539 | Drug | Maraviroc 225 mg tablet, single dose plus PF-03716539 200 mg oral solution, single dose (Day 7) |
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|
| 8 days |
| ID | Term |
|---|---|
| D008874 | Midazolam |
| D000069454 | Darunavir |
| D000077592 | Maraviroc |
| ID | Term |
|---|---|
| D001569 | Benzodiazepines |
| D001552 | Benzazepines |
| D006574 | Heterocyclic Compounds, 2-Ring |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
| D006571 | Heterocyclic Compounds |
| D013449 | Sulfonamides |
| D000577 | Amides |
| D009930 | Organic Chemicals |
| D002219 | Carbamates |
| D000144 | Acids, Acyclic |
| D002264 | Carboxylic Acids |
| D013450 | Sulfones |
| D013457 | Sulfur Compounds |
| D005663 | Furans |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D003510 | Cyclohexanes |
| D003516 | Cycloparaffins |
| D006840 | Hydrocarbons, Alicyclic |
| D006844 | Hydrocarbons, Cyclic |
| D006838 | Hydrocarbons |
| D014230 | Triazoles |
| D001393 | Azoles |
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