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NCT Number: NCT00931073

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

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.

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Key information

Conditions

Alzheimer's Disease Alzheimer Disease Basal Ganglia Diseases Brain Diseases Central Nervous System Diseases Chorea Cognition Disorders Congenital, Hereditary, and Neonatal Diseases and Abnormalities Dementia Dyskinesias Genetic Diseases, Inborn Heredodegenerative Disorders, Nervous System Huntington Disease Huntington's Disease Mental Disorders Movement Disorders Nervous System Diseases Neurocognitive Disorders Neurodegenerative Diseases Tauopathies

Age range

18 year–55 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

Pfizer Investigational Site

Kalamazoo, Michigan, 49007, United States

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

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.

Treatment and study plan

Dimebon alone

Drug

Pharmacokinetics of a single oral dose of 10 mg Dimebon (tablet) will be assessed in subjects with a CYP2D6 extensive and poor metabolizer status based on genotyping as screening

Dimebon + Ketoconazole

Drug

Pharmacokinetics of a single oral dose of 10 mg Dimebon (tablet) will be assessed on Day 4 during the daily administration of ketoconazole (400 mg, Day 1-11) in subjects with a CYP2D6 extensive and poor metabolizer status based on genotyping as screening

Dimebon + Omeprazole

Drug

Pharmacokinetics of a single oral dose of 10 mg Dimebon (tablet) will be assessed on Day 5 during the daily administration of omeprazole(40 mg, Day 1-12) in subjects with a CYP2D6 extensive and poor metabolizer status based on genotyping as screening

Primary outcomes

  1. 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

  2. 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

  3. 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

Secondary outcomes

  1. Dimebon alone: Safety and tolerability (AE's, ECG, vital signs, safety labs)

    Time frame: Period 1 Day 1-7

  2. Dimebon + keto: Safety and tolerability (AE's, ECG, vital signs, safety labs)

    Time frame: Period 2 Day 1-12

  3. Dimebon + omeprazole: Safety and tolerability (AE's, ECG, vital signs, safety labs)

    Time frame: Period 3 Day 1-13

Sponsors and collaborators

Lead sponsor

Pfizer

Industry

Collaborators

  • Medivation, Inc.

Registry information

Official study 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

Important dates

Study start
2009
Primary completion
2009
Study completion
2009
First posted
Jul 2, 2009
Registry last updated
Nov 18, 2009

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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