Aprepitant and Fosaprepitant Time-on-Target PET (Positron Emission Tomography) Study (0869-183)
Phase 1
Completed
- Conditions
- Chemotherapy-Induced Nausea and Vomiting (CINV)
- Interventions
- Registration Number
- NCT01111851
- Lead Sponsor
- Merck Sharp & Dohme LLC
- Brief Summary
This study will evaluate if the mean value of brain neurokinin 1 (NK1)-receptor occupancy of participants treated with aprepitant is similar to that of participants treated with fosaprepitant at certain timepoints.
- Detailed Description
The third arm of the study (Aprepitant 250 mg) will only be conducted if the real-time assessment of the NK1-receptor occupancy data between fosaprepitant 150 mg \& aprepitant 165 mg reveals that the primary hypothesis will not be supported.
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- All
- Target Recruitment
- 16
Inclusion Criteria
- Generally healthy
- Female participants must be of non-childbearing potential
- Non-smoker or has not used nicotine or nicotine-containing products for at least 6 months
Exclusion Criteria
- History of a clinically significant psychiatric disorder over the last 5 to 10 years
- History of stroke, chronic seizures, or major neurological disorder
- History of clinically significant endocrine, gastrointestinal, cardiovascular, hematological, hepatic, immunological, renal, respiratory, or genitourinary abnormalities or diseases
- History of neoplastic disease
- Excessive consumption of alcohol (3 drinks/day) or caffeinated beverages (6 servings/day)
- Major surgery, donated or lost 1 unit of blood within 4 weeks
- Participated in another investigational study within 4 weeks
- History of significant drug allergy or any clinically significant adverse
experiences related to EMENDâ„¢, dexamethasone, or ondansetron
- History of significant multiple and/or severe allergies
- History of anaphylactic reaction or significant intolerability to prescription or non-prescription drugs or food
- Current drug/alcohol abuse, or history of such within 2 years
- Participation in a PET study or other study involving administration of a radioactive substance or ionizing radiation within the prior 12 months
- Extensive radiological examination within the prior 12 months
- Magnetizable metal prostheses or devices (Magnetic Resonance Imaging (MRI) hazard)
- History of claustrophobia
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- PARALLEL
- Arm && Interventions
Group Intervention Description Aprepitant 165 mg Dexamethasone (12-8-16-16 mg) Aprepitant 165 mg Aprepitant 250 mg Dexamethasone (12-8-8-16 mg) Aprepitant 250 mg Fosaprepitant 150 mg Ondansetron Fosaprepitant 150 mg Aprepitant 165 mg Aprepitant 165 mg Aprepitant 165 mg Fosaprepitant 150 mg Fosaprepitant 150 mg Fosaprepitant 150 mg Fosaprepitant 150 mg Dexamethasone (12-8-16-16 mg) Fosaprepitant 150 mg Fosaprepitant 150 mg MK0999 Fosaprepitant 150 mg Aprepitant 165 mg MK0999 Aprepitant 165 mg Aprepitant 250 mg MK0999 Aprepitant 250 mg Aprepitant 250 mg Aprepitant 250 mg Aprepitant 250 mg Aprepitant 250 mg Ondansetron Aprepitant 250 mg Aprepitant 165 mg Ondansetron Aprepitant 165 mg
- Primary Outcome Measures
Name Time Method Brain NK1-receptor Occupancy at 24 Hours Post Dose 24 hours post dose Brain NK1-receptor Occupancy at 48 Hours Post Dose 48 hours post dose
- Secondary Outcome Measures
Name Time Method Brain NK1-receptor Occupancy at the Time of the Maximum Concentration (Tmax) 30 minutes after the end of the 20-minute infusion of fosaprepitant or at 4 hours after oral dosing of aprepitant Brain NK1-receptor Occupancy at 120 Hours Post Dose 120 hours post dose