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| ID | Type | Description | Link |
|---|---|---|---|
| 2010_531 |
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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.
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.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Fosaprepitant 150 mg | Experimental | Fosaprepitant 150 mg |
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| Aprepitant 165 mg | Experimental | Aprepitant 165 mg |
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| Aprepitant 250 mg | Experimental | Aprepitant 250 mg |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Fosaprepitant 150 mg | Drug | 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 |
| Measure | Description | Time Frame |
|---|---|---|
| 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 |
| Measure | Description | Time Frame |
|---|---|---|
| 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 |
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Inclusion Criteria:
Exclusion Criteria:
experiences related to EMENDâ„¢, dexamethasone, or ondansetron
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| Name | Affiliation | Role |
|---|---|---|
| Medical Monitor | Merck Sharp & Dohme LLC | Study Director |
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| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 22739139 | Result | 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. |
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Aprepitant 250 mg was not evaluated because the assessment of the positron emission tomography (PET) scan data (neurokinin 1 (NK1)-receptor occupancy values at 24 & 48 hours postdose) from fosaprepitant 150 mg & aprepitant 165 mg revealed that the protocol's hypothesis was met; therefore, it was not necessary to evaluate aprepitant 250 mg.
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| ID | Title | Description |
|---|---|---|
| FG000 | Fosaprepitant 150 mg | A single intravenous infusion of 150 mg fosaprepitant dimeglumine over 20 minutes, 15 minutes after consumption of a standard light breakfast meal on Day 1. |
| FG001 | Aprepitant 165 mg |
| Title | Milestones | Reasons Not Completed | |||||
|---|---|---|---|---|---|---|---|
| Overall Study |
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| Aprepitant 165 mg | Drug | a single oral 165 mg aprepitant capsule 15 minutes after consumption of a standard light breakfast meal |
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| Aprepitant 250 mg | Drug | a single oral 250 mg dose achieved by administering two 125 mg aprepitant capsules 15 minutes after consumption of a standard light breakfast meal |
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| 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. |
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| 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. |
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| Ondansetron | Drug | 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 |
|
| MK0999 | Drug | I.V. infusion of MK0999 containing ~100 MBq (~3 mCi) containing ≤ 5 ug of MK0999) |
|
A single oral 165 mg aprepitant capsule 15 minutes after consumption of a standard light breakfast meal on Day 1.
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| NOT COMPLETED |
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| ID | Title | Description |
|---|---|---|
| BG000 | Fosaprepitant 150 mg | A single intravenous infusion of 150 mg fosaprepitant dimeglumine over 20 minutes, 15 minutes after consumption of a standard light breakfast meal on Day 1. |
| BG001 | Aprepitant 165 mg | A single oral 165 mg aprepitant capsule 15 minutes after consumption of a standard light breakfast meal on Day 1. |
| BG002 | Total | Total of all reporting groups |
| Units | Counts |
|---|---|
| Participants |
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| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Age, Customized | Number | Participants |
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| Sex: Female, Male | Count of Participants | Participants |
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| Region of Enrollment | Number | participants |
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| Type | Title | Description | Population Description | Reporting Status | Anticipated Posting Date | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Time Frame | Units Analyzed | Denominator Units Selected | Arm/Group Information | Denominators | Classes | Analyses | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Primary | Brain NK1-receptor Occupancy at 24 Hours Post Dose | All participants with at least 1 successful post dose PET scan were included in the analysis population. | Posted | Geometric Mean | 95% Confidence Interval | Percent of occupancy | 24 hours post dose |
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| Primary | Brain NK1-receptor Occupancy at 48 Hours Post Dose | All participants with at least 1 successful postdose PET scan were included in the analysis population. | Posted | Geometric Mean | 95% Confidence Interval | Percent of occupancy | 48 hours post dose |
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| Secondary | Brain NK1-receptor Occupancy at the Time of the Maximum Concentration (Tmax) | All participants with at least 1 successful postdose PET scan were included in the analysis population. | Posted | Geometric Mean | 95% Confidence Interval | Percent of occupancy | 30 minutes after the end of the 20-minute infusion of fosaprepitant or at 4 hours after oral dosing of aprepitant |
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| Secondary | Brain NK1-receptor Occupancy at 120 Hours Post Dose | All participants with at least 1 successful postdose PET scan were included in the analysis population. | Posted | Geometric Mean | 95% Confidence Interval | Percent of occupancy | 120 hours post dose |
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| ID | Title | Description | Deaths (Affected) | Deaths (At Risk) | Serious Events (Affected) | Serious Events (At Risk) | Other Events (Affected) | Other Events (At Risk) |
|---|---|---|---|---|---|---|---|---|
| EG000 | Fosaprepitant 150 mg | A single intravenous infusion of 150 mg fosaprepitant dimeglumine over 20 minutes, 15 minutes after consumption of a standard light breakfast meal on Day 1. | 0 | 8 | 5 | 8 | ||
| EG001 | Aprepitant 165 mg | A single oral 165 mg aprepitant capsule 15 minutes after consumption of a standard light breakfast meal on Day 1. | 0 | 8 | 8 | 8 |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Vision blurred | Eye disorders | MedDRA 13.0 |
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| Visual impairment | Eye disorders | MedDRA 13.0 |
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| Abdominal distension | Gastrointestinal disorders | MedDRA 13.0 |
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| Abdominal pain | Gastrointestinal disorders | MedDRA 13.0 |
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| Constipation | Gastrointestinal disorders | MedDRA 13.0 |
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| Gastroesophageal reflux disease | Gastrointestinal disorders | MedDRA 13.0 |
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| Fatigue | General disorders | MedDRA 13.0 |
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| Influenza like illness | General disorders | MedDRA 13.0 |
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| Bronchitis | Infections and infestations | MedDRA 13.0 |
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| Neutrophil count decreased | Investigations | MedDRA 13.0 |
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| Positron emission tomogram abnormal | Investigations | MedDRA 13.0 |
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| Dizziness | Nervous system disorders | MedDRA 13.0 |
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| Dizziness postural | Nervous system disorders | MedDRA 13.0 |
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| Headache | Nervous system disorders | MedDRA 13.0 |
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| Insomnia | Psychiatric disorders | MedDRA 13.0 |
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| Cough | Respiratory, thoracic and mediastinal disorders | MedDRA 13.0 |
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| Dry throat | Respiratory, thoracic and mediastinal disorders | MedDRA 13.0 |
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| Dyspnea | Respiratory, thoracic and mediastinal disorders | MedDRA 13.0 |
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| Hiccups | Respiratory, thoracic and mediastinal disorders | MedDRA 13.0 |
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| Oropharyngeal pain | Respiratory, thoracic and mediastinal disorders | MedDRA 13.0 |
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| Acne | Skin and subcutaneous tissue disorders | MedDRA 13.0 |
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| Flushing | Vascular disorders | MedDRA 13.0 |
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The SPONSOR must have the opportunity to review all proposed abstracts, manuscripts, or presentations regarding this study 60 days prior to submission for publication/presentation. Any information identified by the SPONSOR as confidential must be deleted prior to submission. SPONSOR review can be expedited to meet publication guidelines.
| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Senior Vice President, Global Clinical Development | Merck Sharp & Dohme Corp. | ClinicalTrialsDisclosure@merck.com |
| ID | Term |
|---|---|
| D014839 | Vomiting |
| ID | Term |
|---|---|
| D012817 | Signs and Symptoms, Digestive |
| D012816 | Signs and Symptoms |
| D013568 | Pathological Conditions, Signs and Symptoms |
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| ID | Term |
|---|---|
| C579707 | fosaprepitant |
| D000077608 | Aprepitant |
| D003907 | Dexamethasone |
| D017294 | Ondansetron |
| ID | Term |
|---|---|
| D009025 | Morpholines |
| D010078 | Oxazines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D011246 | Pregnadienetriols |
| D011245 | Pregnadienes |
| D011278 | Pregnanes |
| D013256 | Steroids |
| D000072473 | Fused-Ring Compounds |
| D011083 | Polycyclic Compounds |
| D013259 | Steroids, Fluorinated |
| D007093 | Imidazoles |
| D001393 | Azoles |
| D002227 | Carbazoles |
| D007211 | Indoles |
| D006574 | Heterocyclic Compounds, 2-Ring |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
| D006575 | Heterocyclic Compounds, 3-Ring |
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| Title | Measurements |
|---|---|
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| > = 55 years |
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| Male |
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