A Phase I Study To Estimate The Effect Of Ketoconazole And Omeprazole On The Pharmacokinetics Of Dimebon In Healthy Subjects Who Are Normal Or Poor CYP2D6 Metabolizers

Phase 1

Completed

• Conditions: Alzheimer's Disease; Huntington's Disease
• Interventions: Drug: Dimebon + Omeprazole; Drug: Dimebon alone; Drug: Dimebon + Ketoconazole

• Registration Number: NCT00931073
• Lead Sponsor: Pfizer

Brief Summary

This study will evaluate the potential for a drug-drug interaction of Dimebon with ketoconazole and omeprazole, potent inhibitors of the drug metabolizing enzymes CYP3A4 and CYP2C19, respectively.

Detailed Description

Not available

Study Timeline

• Study Start: 2009-07
• Study First Submitted: 2009-07-01
• Study First Submitted QC: 2009-07-01
• Study First Posted: 2009-07-02
• Primary Completion: 2009-10
• Study Completion: 2009-10
• Status Verified: 2009-11
• Last Update Submitted: 2009-11-17
• Last Update Posted: 2009-11-18

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 24

Inclusion Criteria

• Subjects who are willing and able to comply with scheduled visits, treatment plan, laboratory tests, and other study procedures.
• Subjects must have either a CYP2D6 EM (n=12) or PM (n=12) status based on genotyping at screening.
• Subjects must have a CYP2C19 EM status based on status at screening.

Exclusion Criteria

• Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease.
• Subjects with any history of a previous seizure or convulsion or significant head trauma.
• Subjects specifically allergic to imidazole antifungal agents.
• Subjects specifically allergic to omeprazole or other proton pump inhibitors.
• Any condition possibly affecting drug absorption (eg, gastrectomy).
• Subjects with hypersensitivity reactions to Dimebon or other antihistamines.
• Consumption of grapefruit or grapefruit containing products within 7 days prior to the first dose of study medication.
• Subjects currently taking omeprazole, other proton pump inhibitors, antacids, H2-blockers or CYP2C19 inhibitors.
• Pregnant or nursing females; females of childbearing potential who are unwilling or unable to use an acceptable method of nonhormonal contraception as outlined in this protocol from at least 14 days prior to the first dose of study medication.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
Period 3	Dimebon + Omeprazole	-
Period 1	Dimebon alone	-
Period 2	Dimebon + Ketoconazole	-

Primary Outcome Measures

Name	Time	Method
Dimebon alone: Dimebon PK in CYP2D6 EMs and PMs (Cmax, Tmax, AUCinf (as data permit), AUClast, and t1/2 (as data permit), CL/F (as data permit) and V/F (as data permit))	Period 1 Day 1
Dimebon + keto: Dimebon PK in CYP2D6 EMs and PMs (Cmax, Tmax, AUCinf (as data permit), AUClast, and t1/2 (as data permit), CL/F (as data permit) and V/F (as data permit))	Period 2 Day 4
Dimebon + omeprazole: Dimebon PK in CYP2D6 EMs and PMs (Cmax, Tmax, AUCinf (as data permit), AUClast, and t1/2 (as data permit), CL/F (as data permit) and V/F (as data permit))	Period 3 Day 5

Secondary Outcome Measures

Name	Time	Method
Dimebon alone: Safety and tolerability (AE's, ECG, vital signs, safety labs)	Period 1 Day 1-7
Dimebon + keto: Safety and tolerability (AE's, ECG, vital signs, safety labs)	Period 2 Day 1-12
Dimebon + omeprazole: Safety and tolerability (AE's, ECG, vital signs, safety labs)	Period 3 Day 1-13

Trial Locations

Locations (1)

Pfizer Investigational Site; 🇺🇸 Kalamazoo, Michigan, United States