NCT01111851

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.

Trial Health

100
On Track

Trial Health Score

Automated assessment based on enrollment pace, timeline, and geographic reach

Enrollment
16

participants targeted

Target at below P25 for phase_1

Timeline
Completed

Started Apr 2010

Shorter than P25 for phase_1

Status
completed

Health score is calculated from publicly available data and should be used for screening purposes only.

Trial Relationships

Click on a node to explore related trials.

Study Timeline

Key milestones and dates

Study Start

First participant enrolled

April 1, 2010

Completed
25 days until next milestone

First Submitted

Initial submission to the registry

April 26, 2010

Completed
2 days until next milestone

First Posted

Study publicly available on registry

April 28, 2010

Completed
5 months until next milestone

Primary Completion

Last participant's last visit for primary outcome

October 1, 2010

Completed
Same day until next milestone

Study Completion

Last participant's last visit for all outcomes

October 1, 2010

Completed
1.1 years until next milestone

Results Posted

Study results publicly available

November 3, 2011

Completed
Last Updated

February 25, 2015

Status Verified

February 1, 2015

Enrollment Period

6 months

First QC Date

April 26, 2010

Results QC Date

September 29, 2011

Last Update Submit

February 6, 2015

Conditions

Chemotherapy-Induced Nausea and Vomiting (CINV)

Keywords

NK1-receptor occupancy

Outcome Measures

Primary Outcomes (2)

  • 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 Outcomes (2)

  • 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

Study Arms (3)

Fosaprepitant 150 mg

EXPERIMENTAL

Fosaprepitant 150 mg

Drug: Fosaprepitant 150 mgDrug: Dexamethasone (12-8-16-16 mg)Drug: OndansetronDrug: MK0999

Aprepitant 165 mg

EXPERIMENTAL

Aprepitant 165 mg

Drug: Aprepitant 165 mgDrug: Dexamethasone (12-8-16-16 mg)Drug: OndansetronDrug: MK0999

Aprepitant 250 mg

EXPERIMENTAL

Aprepitant 250 mg

Drug: Aprepitant 250 mgDrug: Dexamethasone (12-8-8-16 mg)Drug: OndansetronDrug: MK0999

Interventions

Fosaprepitant 150 mgDRUG

a single intravenous infusion of 150 mg fosaprepitant dimeglumine over 20 minutes on Day 1 15 minutes after consumption of a standard light breakfast meal

Also known as: MK0517
Fosaprepitant 150 mg
Aprepitant 165 mgDRUG

a single oral 165 mg aprepitant capsule 15 minutes after consumption of a standard light breakfast meal

Also known as: MK0869
Aprepitant 165 mg
Aprepitant 250 mgDRUG

a single oral 250 mg dose achieved by administering two 125 mg aprepitant capsules 15 minutes after consumption of a standard light breakfast meal

Also known as: MK0869
Aprepitant 250 mg
Dexamethasone (12-8-16-16 mg)DRUG

Dexamethasone 12 mg will be administered orally 30 minutes after the start of fosaprepitant dimeglumine or 30 minutes after aprepitant on Day 1; Oral doses of dexamethasone will be administered on Day 2 (8 mg), Day 3 (8 mg twice daily), and Day 4 (8 mg twice daily) with or without a meal.

Also known as: Dexamethasone
Aprepitant 165 mgFosaprepitant 150 mg
Dexamethasone (12-8-8-16 mg)DRUG

Dexamethasone 12 mg will be administered orally 30 minutes after after aprepitant on Day 1; Oral doses of dexamethasone will be administered on Day 2 (8 mg), Day 3 (8 mg), and Day 4 (8 mg twice daily) with or without a meal.

Also known as: Dexamethasone
Aprepitant 250 mg
OndansetronDRUG

The intravenous (I.V.) infusion of ondansetron 32 mg will begin 30 minutes after the start of fosaprepitant dimeglumine or 30 minutes after aprepitant on Day 1 and will be administered as a 15-minute infusion

Aprepitant 165 mgAprepitant 250 mgFosaprepitant 150 mg
MK0999DRUG

I.V. infusion of MK0999 containing \~100 MBq (\~3 mCi) containing ≤ 5 ug of MK0999)

Aprepitant 165 mgAprepitant 250 mgFosaprepitant 150 mg

Eligibility Criteria

Age18 Years - 55 Years
Sexall
Healthy VolunteersYes
Age GroupsAdult (18-64)

You may qualify if:

  • 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

You may not qualify if:

  • 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 EMEND™, 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)
  • +1 more criteria

Contact the study team to confirm eligibility.

Sponsors & Collaborators

Related Publications (1)

  • Van Laere K, De Hoon J, Bormans G, Koole M, Derdelinckx I, De Lepeleire I, Declercq R, Sanabria Bohorquez SM, Hamill T, Mozley PD, Tatosian D, Xie W, Liu Y, Liu F, Zappacosta P, Mahon C, Butterfield KL, Rosen LB, Murphy MG, Hargreaves RJ, Wagner JA, Shadle CR. Equivalent dynamic human brain NK1-receptor occupancy following single-dose i.v. fosaprepitant vs. oral aprepitant as assessed by PET imaging. Clin Pharmacol Ther. 2012 Aug;92(2):243-50. doi: 10.1038/clpt.2012.62. Epub 2012 Jun 27.

    PMID: 22739139RESULT

MeSH Terms

Conditions

Vomiting

Interventions

fosaprepitantAprepitantDexamethasoneOndansetron

Condition Hierarchy (Ancestors)

Signs and Symptoms, DigestiveSigns and SymptomsPathological Conditions, Signs and Symptoms

Intervention Hierarchy (Ancestors)

MorpholinesOxazinesHeterocyclic Compounds, 1-RingHeterocyclic CompoundsPregnadienetriolsPregnadienesPregnanesSteroidsFused-Ring CompoundsPolycyclic CompoundsSteroids, FluorinatedImidazolesAzolesCarbazolesIndolesHeterocyclic Compounds, 2-RingHeterocyclic Compounds, Fused-RingHeterocyclic Compounds, 3-Ring

Results Point of Contact

Title
Senior Vice President, Global Clinical Development
Organization
Merck Sharp & Dohme Corp.
ClinicalTrialsDisclosure@merck.com

Study Officials

  • Medical Monitor

    Merck Sharp & Dohme LLC

    STUDY DIRECTOR

Publication Agreements

PI is Sponsor Employee
No
Restriction Type
OTHER
Restrictive Agreement
Yes

Study Design

Study Type
interventional
Phase
phase 1
Allocation
RANDOMIZED
Masking
NONE
Purpose
TREATMENT
Intervention Model
PARALLEL
Sponsor Type
INDUSTRY
Responsible Party
SPONSOR

Study Record Dates

First Submitted

April 26, 2010

First Posted

April 28, 2010

Study Start

April 1, 2010

Primary Completion

October 1, 2010

Study Completion

October 1, 2010

Last Updated

February 25, 2015

Results First Posted

November 3, 2011

Record last verified: 2015-02