Trial Outcomes & Findings for Investigation of Food Effect and Gastric ph Increase on the Bioavailability of Faldapravir (NCT NCT01694706)
NCT ID: NCT01694706
Last Updated: 2015-07-30
Results Overview
Area under the concentration-time curve of the faldaprevir in plasma over the time interval from 0 extrapolated to infinity In this endpoint, the "measured values" show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities.
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
15 participants
Primary outcome timeframe
1.5 hours (h) before drug administration and 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, 96h and 120h after drug administration
Results posted on
2015-07-30
Participant Flow
This was a randomised open label, 3-way cross over study with three sequences. Faldaprevir administrations in each treatment period were separated by washout period of at least 14 days.
Participant milestones
| Measure |
Faldaprevir/Faldaprevir+ OMP/Faldaprevir Fed
Faldaprevir: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally following an overnight or at least 10 hours (h) fast prior the drug administration.
Faldaprevir+ OMP: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was coadministered orally with 40 mg Omeprazole following an overnight or at least 10 hours (h) fast prior the drug administration following multiple dosing of 40 mg omeprazole once daily for 4 days prior the first dose of faldaprevir.
Faldaprevir fed: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally 30 minutes (min) after a standard high-fat, high-caloric meal was served. The meal had to be completely consumed within 25 min or less.
|
Faldaprevir Fed/ Faldaprevir/ Faldaprevir+ OMP
Faldaprevir fed: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally 30 minutes (min) after a standard high-fat, high-caloric meal was served. The meal had to be completely consumed within 25 min or less.
Faldaprevir: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally following an overnight or at least 10 hours (h) fast prior the drug administration (Reference treatment)
faldaprevir+ OMP: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was coadministered orally with 40 mg Omeprazole following an overnight or at least 10 hours (h) fast prior the drug administration following multiple dosing of 40 mg omeprazole once daily for 4 days prior the first dose of faldaprevir.
|
Faldaprevir+ OMP/ Faldaprevir Fed/ Faldaprevir
Faldaprevir+ OMP: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was coadministered orally with 40 mg Omeprazole following an overnight or at least 10 hours (h) fast prior the drug administration following multiple dosing of 40 mg omeprazole once daily for 4 days prior the first dose of faldaprevir.
Faldaprevir fed: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally 30 minutes (min) after a standard high-fat, high-caloric meal was served. The meal had to be completely consumed within 25 min or less.
Faldaprevir: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally following an overnight or at least 10 hours (h) fast prior the drug administration
|
|---|---|---|---|
|
Overall Study
STARTED
|
5
|
5
|
5
|
|
Overall Study
Received Faldaprevir
|
5
|
5
|
5
|
|
Overall Study
Received Faldaprevir +OMP
|
5
|
5
|
5
|
|
Overall Study
Received Faldaprevir Fed
|
4
|
5
|
5
|
|
Overall Study
COMPLETED
|
4
|
4
|
5
|
|
Overall Study
NOT COMPLETED
|
1
|
1
|
0
|
Reasons for withdrawal
| Measure |
Faldaprevir/Faldaprevir+ OMP/Faldaprevir Fed
Faldaprevir: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally following an overnight or at least 10 hours (h) fast prior the drug administration.
Faldaprevir+ OMP: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was coadministered orally with 40 mg Omeprazole following an overnight or at least 10 hours (h) fast prior the drug administration following multiple dosing of 40 mg omeprazole once daily for 4 days prior the first dose of faldaprevir.
Faldaprevir fed: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally 30 minutes (min) after a standard high-fat, high-caloric meal was served. The meal had to be completely consumed within 25 min or less.
|
Faldaprevir Fed/ Faldaprevir/ Faldaprevir+ OMP
Faldaprevir fed: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally 30 minutes (min) after a standard high-fat, high-caloric meal was served. The meal had to be completely consumed within 25 min or less.
Faldaprevir: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally following an overnight or at least 10 hours (h) fast prior the drug administration (Reference treatment)
faldaprevir+ OMP: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was coadministered orally with 40 mg Omeprazole following an overnight or at least 10 hours (h) fast prior the drug administration following multiple dosing of 40 mg omeprazole once daily for 4 days prior the first dose of faldaprevir.
|
Faldaprevir+ OMP/ Faldaprevir Fed/ Faldaprevir
Faldaprevir+ OMP: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was coadministered orally with 40 mg Omeprazole following an overnight or at least 10 hours (h) fast prior the drug administration following multiple dosing of 40 mg omeprazole once daily for 4 days prior the first dose of faldaprevir.
Faldaprevir fed: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally 30 minutes (min) after a standard high-fat, high-caloric meal was served. The meal had to be completely consumed within 25 min or less.
Faldaprevir: Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally following an overnight or at least 10 hours (h) fast prior the drug administration
|
|---|---|---|---|
|
Overall Study
Adverse Event
|
0
|
1
|
0
|
|
Overall Study
other reason not defined above
|
1
|
0
|
0
|
Baseline Characteristics
Investigation of Food Effect and Gastric ph Increase on the Bioavailability of Faldapravir
Baseline characteristics by cohort
| Measure |
Entire Study Population
n=15 Participants
All subjects received all tested treatments in a randomised, open label, 3-way cross over study. The treatments were:
Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally following an overnight or at least 10 hours (h) fast prior the drug administration (Reference treatment)
Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally 30 minutes (min) after a standard high-fat, high-caloric meal was served. The meal had to be completely consumed within 25 min or less.
Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was coadministered orally with 40 mg Omeprazole following an overnight or at least 10 hours (h) fast prior the drug administration following multiple dosing of 40 mg omeprazole once daily for 4 days prior the first dose of faldaprevir.
Drug administrations were separated by a washout period of at least 14 days
|
|---|---|
|
Age, Continuous
|
34.7 years
STANDARD_DEVIATION 8.2 • n=5 Participants
|
|
Sex: Female, Male
Female
|
7 Participants
n=5 Participants
|
|
Sex: Female, Male
Male
|
8 Participants
n=5 Participants
|
PRIMARY outcome
Timeframe: 1.5 hours (h) before drug administration and 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, 96h and 120h after drug administrationPopulation: Pharmacokinetic (PK) set: Included all treated subjects that provided at least 1 observation for at least 1 primary endpoint without important protocol violations with respect to the statistical evaluation of the pharmacokinetic endpoints.
Area under the concentration-time curve of the faldaprevir in plasma over the time interval from 0 extrapolated to infinity In this endpoint, the "measured values" show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities.
Outcome measures
| Measure |
Faldaprevir in Fasting
n=14 Participants
Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally following an overnight or at least 10 hours (h) fast prior the drug administration (Reference treatment)
|
Faldaprevir After a High-fat Meal
n=14 Participants
Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally 30 minutes (min) after a standard high-fat, high-caloric meal was served. The meal had to be completely consumed within 25 min or less
|
Faldaprevir and Omeprazole
n=14 Participants
Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was coadministered orally with 40 mg Omeprazole following an overnight or at least 10 hours (h) fast prior the drug administration following multiple dosing of 40 mg omeprazole once daily for 4 days prior the first dose of faldaprevir
|
|---|---|---|---|
|
Faldaprevir: Area Under the Curve Over the Time Interval From 0 Extrapolated to Infinity (AUC 0-infinity)
|
37900 [ng*h/mL]
Geometric Coefficient of Variation 67.2
|
48200 [ng*h/mL]
Geometric Coefficient of Variation 41.7
|
36000 [ng*h/mL]
Geometric Coefficient of Variation 63.4
|
PRIMARY outcome
Timeframe: 1.5 hours (h) before drug administration and 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, 96h and 120h after drug administrationPopulation: PK set
Maximum measured concentration of the faldaprevir in plasma In this endpoint, the "measured values" show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities.
Outcome measures
| Measure |
Faldaprevir in Fasting
n=14 Participants
Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally following an overnight or at least 10 hours (h) fast prior the drug administration (Reference treatment)
|
Faldaprevir After a High-fat Meal
n=14 Participants
Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally 30 minutes (min) after a standard high-fat, high-caloric meal was served. The meal had to be completely consumed within 25 min or less
|
Faldaprevir and Omeprazole
n=14 Participants
Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was coadministered orally with 40 mg Omeprazole following an overnight or at least 10 hours (h) fast prior the drug administration following multiple dosing of 40 mg omeprazole once daily for 4 days prior the first dose of faldaprevir
|
|---|---|---|---|
|
Faldaprevir: Maximum Measured Concentration (Cmax)
|
2030 ng/mL
Geometric Coefficient of Variation 140
|
2600 ng/mL
Geometric Coefficient of Variation 57.5
|
1920 ng/mL
Geometric Coefficient of Variation 122
|
SECONDARY outcome
Timeframe: 1.5 hours (h) before drug administration and 0.5h, 1h, 1.5h, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, 96h and 120h after drug administrationPopulation: PK set
Area under the concentration-time curve of the faldaprevir in plasma over the time interval from 0 to the last quantifiable drug plasma concentration In this endpoint, the "measured values" show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities.
Outcome measures
| Measure |
Faldaprevir in Fasting
n=14 Participants
Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally following an overnight or at least 10 hours (h) fast prior the drug administration (Reference treatment)
|
Faldaprevir After a High-fat Meal
n=14 Participants
Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally 30 minutes (min) after a standard high-fat, high-caloric meal was served. The meal had to be completely consumed within 25 min or less
|
Faldaprevir and Omeprazole
n=14 Participants
Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was coadministered orally with 40 mg Omeprazole following an overnight or at least 10 hours (h) fast prior the drug administration following multiple dosing of 40 mg omeprazole once daily for 4 days prior the first dose of faldaprevir
|
|---|---|---|---|
|
Faldaprevir: Area Under the Curve 0 to the Last Quantifiable Data Point (AUC0-tz)
|
36300 ng*h/mL
Geometric Coefficient of Variation 70.3
|
46400 ng*h/mL
Geometric Coefficient of Variation 42.6
|
34400 ng*h/mL
Geometric Coefficient of Variation 65.6
|
Adverse Events
Faldaprevir in Fasting
Serious events: 0 serious events
Other events: 4 other events
Deaths: 0 deaths
Faldaprevir After a High-fat Meal
Serious events: 0 serious events
Other events: 4 other events
Deaths: 0 deaths
Faldaprevir and Omeprazole
Serious events: 0 serious events
Other events: 4 other events
Deaths: 0 deaths
Omeprazole
Serious events: 0 serious events
Other events: 0 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Faldaprevir in Fasting
n=15 participants at risk
Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally following an overnight or at least 10 hours (h) fast prior the drug administration (Reference treatment)
|
Faldaprevir After a High-fat Meal
n=14 participants at risk
Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was administered orally 30 minutes (min) after a standard high-fat, high-caloric meal was served. The meal had to be completely consumed within 25 min or less
|
Faldaprevir and Omeprazole
n=14 participants at risk
Single dose of 240 mg faldaprevir in a form of two soft gelatin capsules was coadministered orally with 40 mg Omeprazole following an overnight or at least 10 hours (h) fast
|
Omeprazole
n=15 participants at risk
40 mg omeprazole once daily for 4 days prior the first dose of faldaprevir
|
|---|---|---|---|---|
|
Gastrointestinal disorders
Abdominal pain upper
|
0.00%
0/15 • From first drug administration until the end of trial visit, up until 20 days
|
7.1%
1/14 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/14 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/15 • From first drug administration until the end of trial visit, up until 20 days
|
|
Gastrointestinal disorders
Diarrhoea
|
13.3%
2/15 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/14 • From first drug administration until the end of trial visit, up until 20 days
|
14.3%
2/14 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/15 • From first drug administration until the end of trial visit, up until 20 days
|
|
Gastrointestinal disorders
Nausea
|
0.00%
0/15 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/14 • From first drug administration until the end of trial visit, up until 20 days
|
7.1%
1/14 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/15 • From first drug administration until the end of trial visit, up until 20 days
|
|
Gastrointestinal disorders
Vomiting
|
6.7%
1/15 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/14 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/14 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/15 • From first drug administration until the end of trial visit, up until 20 days
|
|
Infections and infestations
Rhinitis
|
0.00%
0/15 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/14 • From first drug administration until the end of trial visit, up until 20 days
|
7.1%
1/14 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/15 • From first drug administration until the end of trial visit, up until 20 days
|
|
Musculoskeletal and connective tissue disorders
Arthritis
|
6.7%
1/15 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/14 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/14 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/15 • From first drug administration until the end of trial visit, up until 20 days
|
|
Nervous system disorders
Headache
|
6.7%
1/15 • From first drug administration until the end of trial visit, up until 20 days
|
14.3%
2/14 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/14 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/15 • From first drug administration until the end of trial visit, up until 20 days
|
|
Respiratory, thoracic and mediastinal disorders
Asthma
|
0.00%
0/15 • From first drug administration until the end of trial visit, up until 20 days
|
7.1%
1/14 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/14 • From first drug administration until the end of trial visit, up until 20 days
|
0.00%
0/15 • From first drug administration until the end of trial visit, up until 20 days
|
Additional Information
Boehringer Ingelheim Call Center
Boehringer Ingelheim
Phone: 1-800-243-0127
Email: [email protected]
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place