A Phase 1, Randomized, Open-Label, Two-Way Crossover Study To Evaluate The Steady-State Effect Of Dimebon (PF 01913539) On The Single-Dose Pharmacokinetics And Pharmacodynamics Of Warfarin In Healthy Subjects
Study Details
Study Description
Brief Summary
This study will evaluate the potential drug-drug interaction of Dimebon with the FDA-recommended CYP2C9 substrate warfarin in healthy subjects. Conformance with the guidance includes general study design using a randomized, open label, single-dose warfarin, steady-state Dimebon, 2-sequence, 2-treatment, 2-period crossover design with a minimum 7-day washout period between treatments.
| Condition or Disease | Intervention/Treatment | Phase |
|---|---|---|
| Phase 1 |
Study Design
Arms and Interventions
| Arm | Intervention/Treatment |
|---|---|
| Other: A A: Warfarin alone |
Drug: Warfarin
A: a single oral dose of warfarin 25 mg administered on Day 1 of the relevant dosing period, as tablets.
|
| Other: B B: Dimebon and Warfarin co-administration |
Drug: Dimebon
B is oral doses of Dimebon 10 mg TID on Days 1 7 and Dimebon 20 mg TID on Days 8 17, with co administration of a single oral dose of warfarin 25 mg on Day 12 of the relevant dosing period, both as tablets
Drug: Warfarin
B is oral doses of Dimebon 10 mg TID on Days 1 7 and Dimebon 20 mg TID on Days 8 17, with co administration of a single oral dose of warfarin 25 mg on Day 12 of the relevant dosing period, both as tablets
|
Outcome Measures
Primary Outcome Measures
- Single dose pharmacokinetics (Cmax, AUCinf) of warfarin 25 mg with and without co-administration of steady-state Dimebon 20 mg TID in healthy adult subjects. [7+18 days]
- Single dose pharmacodynamics (INRmax, AUC-INR) of warfarin 25 mg with and without co-administration of steady-state Dimebon 20 mg TID in healthy adult subjects. [7+18 days]
- Safety and tolerability ( adverse event monitoring, physical examinations, vital signs, ECG's and clinical laboratory tests) of multiple doses of Dimebon 20 mg TID with a single dose of warfarin 25 mg in healthy adult subjects. [7+18 days]
Eligibility Criteria
Criteria
Inclusion Criteria:
-
Healthy male and/or female (non-childbearing potential) subjects between the ages of 18 and 55 years, inclusive (Healthy is defined as no clinically relevant abnormalities identified by a detailed medical history, full physical examination, including blood pressure and pulse rate measurement, 12 lead ECG and clinical laboratory tests).
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Prothrombin time (PT)/INR, and partial thromboplastin time (PTT).
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Plasma Protein C and Protein S activity (functional) within the normal reference range.
Exclusion Criteria:
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A known sensitivity or previous intolerance to Dimebon or warfarin.
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Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at time of dosing) disease or clinical findings at Screening.
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Subjects receiving warfarin for treatment of active thromboembolic events (ie, pulmonary embolism, deep vein thrombosis), as well as subjects anticoagulated with prosthetic heart valves.
Contacts and Locations
Locations
| Site | City | State | Country | Postal Code | |
|---|---|---|---|---|---|
| 1 | Pfizer Investigational Site | New Haven | Connecticut | United States | 06511 |
Sponsors and Collaborators
- Pfizer
- Medivation, Inc.
Investigators
- Study Director: Pfizer CT.gov Call Center, Pfizer
Study Documents (Full-Text)
None provided.More Information
Additional Information:
Publications
None provided.- B1451020