Trial Outcomes & Findings for A Study to Assess the Bioequivalence of Aprepitant and Fosaprepitant and the Effect of Food on Aprepitant Bioavailability (0869-165) (NCT NCT00945321)
NCT ID: NCT00945321
Last Updated: 2015-01-28
Results Overview
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
42 participants
Primary outcome timeframe
Through 72 Hours Postdose
Results posted on
2015-01-28
Participant Flow
Participant milestones
| Measure |
A/B/C/D
Treatment A: 165 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment B: 185 mg aprepitant Final Market Composition capsule in the fasted state/Treatment C: 150 mg fosaprepitant dimeglumine intravenous infusion in the fasted state/ Treatment D: 165 mg aprepitant Final Market Composition capsule in the fed state.
(The first 12 subjects in this treatment group received a standard high-fat breakfast. The rest of the subjects (9) in this treatment group received a standard light breakfast)
|
B/C/A/D
Treatment B: 185 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment C: 150 mg fosaprepitant dimeglumine intravenous infusion in the fasted state/ Treatment A: 165 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment D: 165 mg aprepitant Final Market Composition capsule in the fed state.
(The first 12 subjects in this treatment group received a standard high-fat breakfast. The rest of the subjects (9) in this treatment group received a standard light breakfast)
|
C/A/B/D
Treatment C: 150 mg fosaprepitant dimeglumine intravenous infusion in the fasted state/ Treatment A: 165 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment B: 185 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment D: 165 mg aprepitant Final Market Composition capsule in the fed state.
(The first 12 subjects in this treatment group received a standard high-fat breakfast. The rest of the subjects (9) in this treatment group received a standard light breakfast)
|
A/C/B/E
Treatment A: 165 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment C: 150 mg fosaprepitant dimeglumine intravenous infusion in the fasted state/ Treatment B: 185 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment E: 185 mg aprepitant Final Market Composition capsule in the fed state.
(The first 11 subjects in this treatment group received a standard high-fat breakfast. The rest of the subjects (9) in this treatment group received a standard light breakfast)
|
B/A/C/E
Treatment B: 185 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment A: 165 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment C: 150 mg fosaprepitant dimeglumine intravenous infusion in the fasted state/ Treatment E: 185 mg aprepitant Final Market Composition capsule in the fed state.
(The first 11 subjects in this treatment group received a standard high-fat breakfast. The rest of the subjects (9) in this treatment group received a standard light breakfast)
|
C/B/A/E
Treatment C: 150 mg fosaprepitant dimeglumine intravenous infusion in the fasted state/ Treatment B: 185 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment A: 165 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment E: 185 mg aprepitant Final Market Composition capsule in the fed state.
(The first 11 subjects in this treatment group received a standard high-fat breakfast. The rest of the subjects (9) in this treatment group received a standard light breakfast)
|
|---|---|---|---|---|---|---|
|
Period 1
STARTED
|
7
|
7
|
7
|
7
|
7
|
7
|
|
Period 1
COMPLETED
|
7
|
7
|
7
|
7
|
6
|
7
|
|
Period 1
NOT COMPLETED
|
0
|
0
|
0
|
0
|
1
|
0
|
|
Period 2
STARTED
|
7
|
7
|
7
|
7
|
6
|
7
|
|
Period 2
COMPLETED
|
7
|
7
|
7
|
7
|
6
|
7
|
|
Period 2
NOT COMPLETED
|
0
|
0
|
0
|
0
|
0
|
0
|
|
Period 3
STARTED
|
7
|
7
|
7
|
7
|
6
|
7
|
|
Period 3
COMPLETED
|
7
|
7
|
7
|
7
|
6
|
7
|
|
Period 3
NOT COMPLETED
|
0
|
0
|
0
|
0
|
0
|
0
|
|
Period 4
STARTED
|
7
|
7
|
7
|
7
|
6
|
7
|
|
Period 4
COMPLETED
|
7
|
7
|
7
|
7
|
6
|
6
|
|
Period 4
NOT COMPLETED
|
0
|
0
|
0
|
0
|
0
|
1
|
Reasons for withdrawal
| Measure |
A/B/C/D
Treatment A: 165 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment B: 185 mg aprepitant Final Market Composition capsule in the fasted state/Treatment C: 150 mg fosaprepitant dimeglumine intravenous infusion in the fasted state/ Treatment D: 165 mg aprepitant Final Market Composition capsule in the fed state.
(The first 12 subjects in this treatment group received a standard high-fat breakfast. The rest of the subjects (9) in this treatment group received a standard light breakfast)
|
B/C/A/D
Treatment B: 185 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment C: 150 mg fosaprepitant dimeglumine intravenous infusion in the fasted state/ Treatment A: 165 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment D: 165 mg aprepitant Final Market Composition capsule in the fed state.
(The first 12 subjects in this treatment group received a standard high-fat breakfast. The rest of the subjects (9) in this treatment group received a standard light breakfast)
|
C/A/B/D
Treatment C: 150 mg fosaprepitant dimeglumine intravenous infusion in the fasted state/ Treatment A: 165 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment B: 185 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment D: 165 mg aprepitant Final Market Composition capsule in the fed state.
(The first 12 subjects in this treatment group received a standard high-fat breakfast. The rest of the subjects (9) in this treatment group received a standard light breakfast)
|
A/C/B/E
Treatment A: 165 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment C: 150 mg fosaprepitant dimeglumine intravenous infusion in the fasted state/ Treatment B: 185 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment E: 185 mg aprepitant Final Market Composition capsule in the fed state.
(The first 11 subjects in this treatment group received a standard high-fat breakfast. The rest of the subjects (9) in this treatment group received a standard light breakfast)
|
B/A/C/E
Treatment B: 185 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment A: 165 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment C: 150 mg fosaprepitant dimeglumine intravenous infusion in the fasted state/ Treatment E: 185 mg aprepitant Final Market Composition capsule in the fed state.
(The first 11 subjects in this treatment group received a standard high-fat breakfast. The rest of the subjects (9) in this treatment group received a standard light breakfast)
|
C/B/A/E
Treatment C: 150 mg fosaprepitant dimeglumine intravenous infusion in the fasted state/ Treatment B: 185 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment A: 165 mg aprepitant Final Market Composition capsule in the fasted state/ Treatment E: 185 mg aprepitant Final Market Composition capsule in the fed state.
(The first 11 subjects in this treatment group received a standard high-fat breakfast. The rest of the subjects (9) in this treatment group received a standard light breakfast)
|
|---|---|---|---|---|---|---|
|
Period 1
Adverse Event
|
0
|
0
|
0
|
0
|
1
|
0
|
|
Period 4
Lost to Follow-up
|
0
|
0
|
0
|
0
|
0
|
1
|
Baseline Characteristics
A Study to Assess the Bioequivalence of Aprepitant and Fosaprepitant and the Effect of Food on Aprepitant Bioavailability (0869-165)
Baseline characteristics by cohort
| Measure |
All Participants
n=42 Participants
All randomized patients.
|
|---|---|
|
Age, Continuous
|
27.8 years
n=5 Participants
|
|
Sex: Female, Male
Female
|
10 Participants
n=5 Participants
|
|
Sex: Female, Male
Male
|
32 Participants
n=5 Participants
|
|
Height
|
172.9 Centimeters
n=5 Participants
|
|
Weight
|
74.2 Kilograms
n=5 Participants
|
PRIMARY outcome
Timeframe: Through 72 Hours PostdosePopulation: All subjects excluding one subject who dropped from the study after Period 1 due to accidental overdose were included in the pharmacokinetic (PK) analysis.
Outcome measures
| Measure |
165 mg Aprepitant (Fasted State)
n=41 Participants
165 mg aprepitant Final Market Composition capsule in the fasted state
|
185 mg Aprepitant (Fasted State)
n=41 Participants
185 mg aprepitant Final Market Composition capsule in the fasted state
|
150 mg Fosaprepitant Dimeglumine (Fasted State)
n=41 Participants
150 mg fosaprepitant dimeglumine intravenous infusion in the fasted state
|
165 mg Aprepitant (Light)
n=9 Participants
165 mg aprepitant Final Market Composition capsule in the fed state.
(The subjects (9) in this treatment group received a standard light breakfast.)
|
165 mg Aprepitant (High-Fat)
n=12 Participants
165 mg aprepitant Final Market Composition capsule in the fed state.
(The (12) subjects in this treatment group received a standard high-fat breakfast.)
|
185 mg Aprepitant (Light)
n=9 Participants
185 mg aprepitant Final Market Composition capsule in the fed state.
(The subjects (9) in this treatment group received a standard light breakfast.)
|
185 mg Aprepitant (High-Fat)
n=11 Participants
185 mg aprepitant Final Market Composition capsule in the fed state.
(The (12) subjects in this treatment group received a standard high-fat breakfast.)
|
|---|---|---|---|---|---|---|---|
|
Area Under the Curve (AUC(0 to Infinity)) Following Single Dose Administration of Aprepitant 165 mg or 185 mg and Fosaprepitant 150 mg
|
34589 ng•hr/mL
Standard Deviation 39.7
|
39053 ng•hr/mL
Standard Deviation 37.5
|
37375 ng•hr/mL
Standard Deviation 39.5
|
37795 ng•hr/mL
Standard Deviation 48.4
|
50172 ng•hr/mL
Standard Deviation 22.0
|
51146 ng•hr/mL
Standard Deviation 27.2
|
60578 ng•hr/mL
Standard Deviation 57.5
|
PRIMARY outcome
Timeframe: Through 72 Hours PostdosePopulation: All subjects excluding one subject who dropped from the study after Period 1 due to accidental overdose were included in the pharmacokinetic (PK) analysis.
Outcome measures
| Measure |
165 mg Aprepitant (Fasted State)
n=41 Participants
165 mg aprepitant Final Market Composition capsule in the fasted state
|
185 mg Aprepitant (Fasted State)
n=41 Participants
185 mg aprepitant Final Market Composition capsule in the fasted state
|
150 mg Fosaprepitant Dimeglumine (Fasted State)
n=9 Participants
150 mg fosaprepitant dimeglumine intravenous infusion in the fasted state
|
165 mg Aprepitant (Light)
n=12 Participants
165 mg aprepitant Final Market Composition capsule in the fed state.
(The subjects (9) in this treatment group received a standard light breakfast.)
|
165 mg Aprepitant (High-Fat)
n=9 Participants
165 mg aprepitant Final Market Composition capsule in the fed state.
(The (12) subjects in this treatment group received a standard high-fat breakfast.)
|
185 mg Aprepitant (Light)
n=11 Participants
185 mg aprepitant Final Market Composition capsule in the fed state.
(The subjects (9) in this treatment group received a standard light breakfast.)
|
185 mg Aprepitant (High-Fat)
185 mg aprepitant Final Market Composition capsule in the fed state.
(The (12) subjects in this treatment group received a standard high-fat breakfast.)
|
|---|---|---|---|---|---|---|---|
|
Peak Plasma Concentration (Cmax) Following Single Dose Administration of Aprepitant 165 mg or 185 mg and Fosaprepitant 150 mg.
|
1738 ng/mL
Standard Error 30.8
|
1636 ng/mL
Standard Error 31.2
|
1870 ng/mL
Standard Error 33.3
|
2362 ng/mL
Standard Error 38.5
|
2116 ng/mL
Standard Error 14.8
|
1995 ng/mL
Standard Error 35.2
|
—
|
Adverse Events
165 mg Aprepitant
Serious events: 0 serious events
Other events: 12 other events
Deaths: 0 deaths
185 mg Aprepitant
Serious events: 1 serious events
Other events: 13 other events
Deaths: 0 deaths
150 mg Fosaprepitant Dimeglumine
Serious events: 0 serious events
Other events: 15 other events
Deaths: 0 deaths
165 mg Aprepitant (Fed State)
Serious events: 0 serious events
Other events: 6 other events
Deaths: 0 deaths
185 mg Aprepitant (Fed State)
Serious events: 0 serious events
Other events: 3 other events
Deaths: 0 deaths
Serious adverse events
| Measure |
165 mg Aprepitant
n=41 participants at risk
165 mg aprepitant Final Market Composition capsule in the fasted state
|
185 mg Aprepitant
n=42 participants at risk
185 mg aprepitant Final Market Composition capsule in the fasted state
|
150 mg Fosaprepitant Dimeglumine
n=41 participants at risk
150 mg fosaprepitant dimeglumine intravenous infusion in the fasted state
|
165 mg Aprepitant (Fed State)
n=21 participants at risk
165 mg aprepitant Final Market Composition capsule in the fed
state. (The first 12 subjects in this treatment group received a standard high-fat breakfast. The rest of the
subjects (9) in this treatment group received a standard light breakfast)
|
185 mg Aprepitant (Fed State)
n=20 participants at risk
185 mg aprepitant Final Market Composition capsule in the fed state.
(The first 11 subjects in this treatment group received a standard high-fat breakfast. The rest of the subjects (9) in this treatment group received a standard light breakfast)
|
|---|---|---|---|---|---|
|
Injury, poisoning and procedural complications
Accidental Overdose
|
0.00%
0/41
|
2.4%
1/42
|
0.00%
0/41
|
0.00%
0/21
|
0.00%
0/20
|
Other adverse events
| Measure |
165 mg Aprepitant
n=41 participants at risk
165 mg aprepitant Final Market Composition capsule in the fasted state
|
185 mg Aprepitant
n=42 participants at risk
185 mg aprepitant Final Market Composition capsule in the fasted state
|
150 mg Fosaprepitant Dimeglumine
n=41 participants at risk
150 mg fosaprepitant dimeglumine intravenous infusion in the fasted state
|
165 mg Aprepitant (Fed State)
n=21 participants at risk
165 mg aprepitant Final Market Composition capsule in the fed
state. (The first 12 subjects in this treatment group received a standard high-fat breakfast. The rest of the
subjects (9) in this treatment group received a standard light breakfast)
|
185 mg Aprepitant (Fed State)
n=20 participants at risk
185 mg aprepitant Final Market Composition capsule in the fed state.
(The first 11 subjects in this treatment group received a standard high-fat breakfast. The rest of the subjects (9) in this treatment group received a standard light breakfast)
|
|---|---|---|---|---|---|
|
Eye disorders
Eye Movement Disorder
|
0.00%
0/41
|
2.4%
1/42
|
0.00%
0/41
|
0.00%
0/21
|
0.00%
0/20
|
|
Gastrointestinal disorders
Abdominal Pain
|
0.00%
0/41
|
0.00%
0/42
|
2.4%
1/41
|
0.00%
0/21
|
0.00%
0/20
|
|
Gastrointestinal disorders
Abdominal Pain Upper
|
0.00%
0/41
|
2.4%
1/42
|
0.00%
0/41
|
4.8%
1/21
|
0.00%
0/20
|
|
Gastrointestinal disorders
Diarrhoea
|
0.00%
0/41
|
0.00%
0/42
|
0.00%
0/41
|
4.8%
1/21
|
0.00%
0/20
|
|
Gastrointestinal disorders
Nausea
|
0.00%
0/41
|
2.4%
1/42
|
0.00%
0/41
|
0.00%
0/21
|
0.00%
0/20
|
|
Gastrointestinal disorders
Vomiting
|
0.00%
0/41
|
2.4%
1/42
|
0.00%
0/41
|
0.00%
0/21
|
0.00%
0/20
|
|
General disorders
Chest Discomfort
|
0.00%
0/41
|
0.00%
0/42
|
2.4%
1/41
|
0.00%
0/21
|
0.00%
0/20
|
|
General disorders
Chest Pain
|
0.00%
0/41
|
0.00%
0/42
|
0.00%
0/41
|
4.8%
1/21
|
0.00%
0/20
|
|
General disorders
Infusion Site Erythema
|
0.00%
0/41
|
0.00%
0/42
|
2.4%
1/41
|
0.00%
0/21
|
0.00%
0/20
|
|
General disorders
Infusion Site Induration
|
0.00%
0/41
|
2.4%
1/42
|
4.9%
2/41
|
0.00%
0/21
|
0.00%
0/20
|
|
General disorders
Infusion Site Mass
|
0.00%
0/41
|
0.00%
0/42
|
0.00%
0/41
|
4.8%
1/21
|
0.00%
0/20
|
|
General disorders
Puncture Site Indurations
|
0.00%
0/41
|
0.00%
0/42
|
0.00%
0/41
|
4.8%
1/21
|
0.00%
0/20
|
|
Infections and infestations
Nasopharyngitis
|
2.4%
1/41
|
4.8%
2/42
|
0.00%
0/41
|
4.8%
1/21
|
0.00%
0/20
|
|
Injury, poisoning and procedural complications
Procedureal Dizziness
|
0.00%
0/41
|
2.4%
1/42
|
0.00%
0/41
|
0.00%
0/21
|
0.00%
0/20
|
|
Musculoskeletal and connective tissue disorders
Myalgia
|
2.4%
1/41
|
0.00%
0/42
|
0.00%
0/41
|
0.00%
0/21
|
0.00%
0/20
|
|
Nervous system disorders
Dizziness
|
7.3%
3/41
|
7.1%
3/42
|
2.4%
1/41
|
0.00%
0/21
|
0.00%
0/20
|
|
Nervous system disorders
Headache
|
22.0%
9/41
|
14.3%
6/42
|
14.6%
6/41
|
4.8%
1/21
|
5.0%
1/20
|
|
Nervous system disorders
Somnolence
|
0.00%
0/41
|
0.00%
0/42
|
0.00%
0/41
|
9.5%
2/21
|
5.0%
1/20
|
|
Respiratory, thoracic and mediastinal disorders
Nasal Congestion
|
4.9%
2/41
|
0.00%
0/42
|
4.9%
2/41
|
0.00%
0/21
|
0.00%
0/20
|
|
Respiratory, thoracic and mediastinal disorders
Oropharyngial Pain
|
0.00%
0/41
|
0.00%
0/42
|
2.4%
1/41
|
0.00%
0/21
|
5.0%
1/20
|
|
Skin and subcutaneous tissue disorders
Ecchymosis
|
0.00%
0/41
|
2.4%
1/42
|
0.00%
0/41
|
0.00%
0/21
|
0.00%
0/20
|
|
Skin and subcutaneous tissue disorders
Hyperhidrosis
|
0.00%
0/41
|
2.4%
1/42
|
0.00%
0/41
|
0.00%
0/21
|
0.00%
0/20
|
|
Vascular disorders
Vein Pain
|
0.00%
0/41
|
0.00%
0/42
|
2.4%
1/41
|
0.00%
0/21
|
0.00%
0/20
|
Additional Information
Senior Vice President, Global Clinical Development
Merck Sharp & Dohme Corp.
Phone: 1-800-672-6372
Email: [email protected]
Results disclosure agreements
- Principal investigator is a sponsor employee Merck agreements may vary with individual investigators, but will not prohibit any investigator from publishing. Merck supports the publication of results from all centers of a multi-center trial but requests that reports based on single-site data not precede the primary publication of the entire clinical trial.
- Publication restrictions are in place
Restriction type: OTHER