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

• Register: ClinicalTrials.gov
• Last refreshed on: 19 February 2015
• Main ID: NCT00931073
• Date of registration: 01/07/2009
• Prospective Registration: Yes
• Primary sponsor: Pfizer
• Public title: 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
• Scientific title: A Phase I, Open-Label, Three-Period, Fixed-Sequence Study To Estimate The Steady-State Effect Of Ketoconazole And Omeprazole On The Single-Dose Pharmacokinetics Of Dimebon [PF-01913539] In Healthy CYP2D6 EM And PM Subjects
• Date of first enrolment: July 2009
• Target sample size: 24
• Recruitment status: Completed
• URL: http://clinicaltrials.gov/show/NCT00931073
• Study type: Interventional
• Study design: Allocation: Non-Randomized, Endpoint Classification: Pharmacokinetics Study, Intervention Model: Crossover Assignment, Masking: Open Label
• Phase: Phase 1

Countries of recruitment

United States

Contacts

• Name: Pfizer CT.gov Call Center
• Affiliation: Pfizer

Key inclusion & exclusion criteria

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.



Age minimum: 18 Years
Age maximum: 55 Years
Gender: Both

Health Condition(s) or Problem(s) studied

Alzheimer's Disease

Huntington's Disease

Intervention(s)

Drug: Dimebon + Omeprazole

Drug: Dimebon + Ketoconazole

Drug: Dimebon alone

Primary Outcome(s)

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)) [Time Frame: 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)) [Time Frame: Period 3 Day 5]

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)) [Time Frame: Period 1 Day 1]

Secondary Outcome(s)

Dimebon alone: Safety and tolerability (AE's, ECG, vital signs, safety labs) [Time Frame: Period 1 Day 1-7]

Dimebon + keto: Safety and tolerability (AE's, ECG, vital signs, safety labs) [Time Frame: Period 2 Day 1-12]

Dimebon + omeprazole: Safety and tolerability (AE's, ECG, vital signs, safety labs) [Time Frame: Period 3 Day 1-13]

Secondary ID(s)

B1451017

Source(s) of Monetary Support

Please refer to primary and secondary sponsors

Secondary Sponsor(s)

Medivation, Inc.