Trial Outcomes & Findings for Open Label Single Dose Phase I Trial of BI 201335 to Study Pharmacokinetics and Safety in Patients With Compensated Liver Cirrhosis (NCT NCT01909778)
NCT ID: NCT01909778
Last Updated: 2015-08-10
Results Overview
Area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity (AUC 0-∞).
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
2 participants
Primary outcome timeframe
-0:15, 1:00, 2:00, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 16:00, 20:00, 24:00, 48:00, 72:00, 96:00, 120:00 h (hours) after drug administration on day 1 and day 15
Results posted on
2015-08-10
Participant Flow
Participant milestones
| Measure |
All Subjects
The trial was a nonrandomised, open-label, 2-period fixed-sequence trial to evaluate two single oral doses of Faldaprevir, separated by 14 days washout period. The dose levels were 120 mg first, 240 mg second.
A number of 12 entered patients with compensated liver cirrhosis was planned.
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|---|---|
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Overall Study
STARTED
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2
|
|
Overall Study
COMPLETED
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1
|
|
Overall Study
NOT COMPLETED
|
1
|
Reasons for withdrawal
| Measure |
All Subjects
The trial was a nonrandomised, open-label, 2-period fixed-sequence trial to evaluate two single oral doses of Faldaprevir, separated by 14 days washout period. The dose levels were 120 mg first, 240 mg second.
A number of 12 entered patients with compensated liver cirrhosis was planned.
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|---|---|
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Overall Study
failed screening
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1
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Baseline Characteristics
Open Label Single Dose Phase I Trial of BI 201335 to Study Pharmacokinetics and Safety in Patients With Compensated Liver Cirrhosis
Baseline characteristics by cohort
| Measure |
All Subjects
n=2 Participants
The trial was a nonrandomised, open-label, 2-period fixed-sequence trial to evaluate two single oral doses of Faldaprevir, separated by 14 days washout period. The dose levels were 120 mg and 240 mg.
A number of 12 entered patients with compensated liver cirrhosis was planned.
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|---|---|
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Age, Categorical
<=18 years
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0 Participants
n=99 Participants
|
|
Age, Categorical
Between 18 and 65 years
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2 Participants
n=99 Participants
|
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Age, Categorical
>=65 years
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0 Participants
n=99 Participants
|
|
Sex: Female, Male
Female
|
1 Participants
n=99 Participants
|
|
Sex: Female, Male
Male
|
1 Participants
n=99 Participants
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PRIMARY outcome
Timeframe: -0:15, 1:00, 2:00, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 16:00, 20:00, 24:00, 48:00, 72:00, 96:00, 120:00 h (hours) after drug administration on day 1 and day 15Population: Only one patient was treated and completed this study; he was the only patient analysed.
Area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity (AUC 0-∞).
Outcome measures
| Measure |
Low Dose of Faldaprevir (Period 1)
n=1 Participants
single dose of 120 mg Faldaprevir soft gel capsule.
|
High Dose of Faldaprevir (Period 2)
n=1 Participants
single dose of 240 mg Faldaprevir soft gel capsule after a wash-out period of at least 14 days.
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|---|---|---|
|
AUC 0-∞
|
7240 h*ng/mL
|
24700 h*ng/mL
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PRIMARY outcome
Timeframe: -0:15, 1:00, 2:00, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 16:00, 20:00, 24:00, 48:00, 72:00, 96:00, 120:00 h after drug administration on day 1 and day 15Population: Only one patient was treated and completed this study; he was the only patient analysed.
Maximum plasma concentration (Cmax). Individual Cmax values will be directly determined from the plasma concentration time profiles.
Outcome measures
| Measure |
Low Dose of Faldaprevir (Period 1)
n=1 Participants
single dose of 120 mg Faldaprevir soft gel capsule.
|
High Dose of Faldaprevir (Period 2)
n=1 Participants
single dose of 240 mg Faldaprevir soft gel capsule after a wash-out period of at least 14 days.
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|---|---|---|
|
Cmax
|
308 ng/mL
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999 ng/mL
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SECONDARY outcome
Timeframe: -0:15, 1:00, 2:00, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 16:00, 20:00, 24:00, 48:00, 72:00, 96:00, 120:00 h after drug administration on day 1 and day 15Population: Only one patient was treated and completed this study; he was the only patient analysed.
Time at which the maximum plasma concentration occurs (tmax). Individual tmax values will be directly determined from the plasma concentration time profiles.
Outcome measures
| Measure |
Low Dose of Faldaprevir (Period 1)
n=1 Participants
single dose of 120 mg Faldaprevir soft gel capsule.
|
High Dose of Faldaprevir (Period 2)
n=1 Participants
single dose of 240 mg Faldaprevir soft gel capsule after a wash-out period of at least 14 days.
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|---|---|---|
|
Tmax
|
8.00 hours
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8.00 hours
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SECONDARY outcome
Timeframe: -0:15, 1:00, 2:00, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 16:00, 20:00, 24:00, 48:00, 72:00, 96:00, 120:00 h after drug administration on day 1 and day 15Population: Only one patient was treated and completed this study; he was the only patient analysed.
Area under the concentration-time curve over the time interval from 0 to the last quantifiable plasma concentration (AUC0-tz).
Outcome measures
| Measure |
Low Dose of Faldaprevir (Period 1)
n=1 Participants
single dose of 120 mg Faldaprevir soft gel capsule.
|
High Dose of Faldaprevir (Period 2)
n=1 Participants
single dose of 240 mg Faldaprevir soft gel capsule after a wash-out period of at least 14 days.
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|---|---|---|
|
AUC0-tz
|
6770 h*ng/mL
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23900 h*ng/mL
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SECONDARY outcome
Timeframe: -0:15, 1:00, 2:00, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 16:00, 20:00, 24:00, 48:00, 72:00, 96:00, 120:00 h after drug administration on day 1 and day 15Population: Only one patient was treated and completed this study; he was the only patient analysed.
Elimination half-life (t1/2). The terminal half-life will be calculated from the terminal rate constant.
Outcome measures
| Measure |
Low Dose of Faldaprevir (Period 1)
n=1 Participants
single dose of 120 mg Faldaprevir soft gel capsule.
|
High Dose of Faldaprevir (Period 2)
n=1 Participants
single dose of 240 mg Faldaprevir soft gel capsule after a wash-out period of at least 14 days.
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|---|---|---|
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t1/2
|
33.8 hours
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26.8 hours
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SECONDARY outcome
Timeframe: -0:15, 1:00, 2:00, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 16:00, 20:00, 24:00, 48:00, 72:00, 96:00, 120:00 h after drug administration on day 1 and day 15Population: Only one patient was treated and completed this study; he was the only patient analysed.
Apparent clearance of the analyte in plasma following extravascular administration (CL/F). The apparent clearance after oral administration will be determined according to the following equation: CL or CL/F=dose/AUC0-∞. (F=absolute bioavailability factor)
Outcome measures
| Measure |
Low Dose of Faldaprevir (Period 1)
n=1 Participants
single dose of 120 mg Faldaprevir soft gel capsule.
|
High Dose of Faldaprevir (Period 2)
n=1 Participants
single dose of 240 mg Faldaprevir soft gel capsule after a wash-out period of at least 14 days.
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|---|---|---|
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CL/F
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276 mL/min
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162 mL/min
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SECONDARY outcome
Timeframe: -0:15, 1:00, 2:00, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 16:00, 20:00, 24:00, 48:00, 72:00, 96:00, 120:00 h after drug administration on day 1 and day 15Population: Only one patient was treated and completed this study; he was the only patient analysed.
Apparent volume of distribution during the terminal phase (Vz/F) following an extravascular dose (at steady state).
Outcome measures
| Measure |
Low Dose of Faldaprevir (Period 1)
n=1 Participants
single dose of 120 mg Faldaprevir soft gel capsule.
|
High Dose of Faldaprevir (Period 2)
n=1 Participants
single dose of 240 mg Faldaprevir soft gel capsule after a wash-out period of at least 14 days.
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|---|---|---|
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Vz/F
|
809 Liter
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376 Liter
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SECONDARY outcome
Timeframe: -0:15, 1:00, 2:00, 3:00, 4:00, 5:00, 6:00, 8:00, 12:00, 16:00, 20:00, 24:00, 48:00, 72:00, 96:00, 120:00 h after drug administration on day 1 and day 15Population: Only one patient was treated and completed this study; he was the only patient analysed.
Mean residence time of the analyte in the body after oral administration (MRTpo).
Outcome measures
| Measure |
Low Dose of Faldaprevir (Period 1)
n=1 Participants
single dose of 120 mg Faldaprevir soft gel capsule.
|
High Dose of Faldaprevir (Period 2)
n=1 Participants
single dose of 240 mg Faldaprevir soft gel capsule after a wash-out period of at least 14 days.
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|---|---|---|
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MRTpo
|
39.3 hours
Standard Deviation NA
Not calculable as only one participant analysed.
|
31.6 hours
Standard Deviation NA
Not calculable as only one participant analysed.
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SECONDARY outcome
Timeframe: Day 6 of period 1 and 2Population: Only one patient was treated and completed this study; he was the only patient analysed.
The investigator has assessed tolerability based on adverse events and the laboratory evaluation. Tolerability was assessed by the investigator according to the categories 1="good", 2="satisfactory", 3="not satisfactory", and 4="bad".
Outcome measures
| Measure |
Low Dose of Faldaprevir (Period 1)
n=1 Participants
single dose of 120 mg Faldaprevir soft gel capsule.
|
High Dose of Faldaprevir (Period 2)
n=1 Participants
single dose of 240 mg Faldaprevir soft gel capsule after a wash-out period of at least 14 days.
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|---|---|---|
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Assessment of Tolerability by Investigator
|
1 units on a scale
|
1 units on a scale
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SECONDARY outcome
Timeframe: from intake of the second dose Faldaprevir up to 9 daysPopulation: Only one patient was treated and completed this study; he was the only patient analyzed.
Clinical Relevant Abnormalities for Vital Signs, Blood Chemistry, Haematology, Urinanalysis and ECG. New abnormal findings or worsening of baseline conditions were reported as Adverse Events.
Outcome measures
| Measure |
Low Dose of Faldaprevir (Period 1)
n=1 Participants
single dose of 120 mg Faldaprevir soft gel capsule.
|
High Dose of Faldaprevir (Period 2)
n=1 Participants
single dose of 240 mg Faldaprevir soft gel capsule after a wash-out period of at least 14 days.
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|---|---|---|
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Clinical Relevant Abnormalities for Vital Signs, Blood Chemistry, Haematology, Urinanalysis and ECG
|
0 participants
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0 participants
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Adverse Events
Low Dose of Faldaprevir (Period 1)
Serious events: 0 serious events
Other events: 1 other events
Deaths: 0 deaths
High Dose of Faldaprevir (Period 2)
Serious events: 0 serious events
Other events: 1 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Low Dose of Faldaprevir (Period 1)
n=1 participants at risk
single dose of 120 mg Faldaprevir soft gel capsule.
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High Dose of Faldaprevir (Period 2)
n=1 participants at risk
single dose of 240 mg Faldaprevir soft gel capsule after a wash-out period of at least 14 days.
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|---|---|---|
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Gastrointestinal disorders
Abdominal pain
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100.0%
1/1 • From intake of the second dose Faldaprevir up to 9 days. Patients were required to report spontaneously any adverse events (AEs) as well as the time of onset, duration and intensity of these events.
In addition, each patient was assessed by an investigator at any measurement time point as well as at the end of observation and whenever necessary as deemed by the investigator. Assessment was made using non-specific questions such as "How do you feel?". Specific questions were asked wherever required or useful to more precisely describe an AE.
|
100.0%
1/1 • From intake of the second dose Faldaprevir up to 9 days. Patients were required to report spontaneously any adverse events (AEs) as well as the time of onset, duration and intensity of these events.
In addition, each patient was assessed by an investigator at any measurement time point as well as at the end of observation and whenever necessary as deemed by the investigator. Assessment was made using non-specific questions such as "How do you feel?". Specific questions were asked wherever required or useful to more precisely describe an AE.
|
|
Gastrointestinal disorders
Nausea
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100.0%
1/1 • From intake of the second dose Faldaprevir up to 9 days. Patients were required to report spontaneously any adverse events (AEs) as well as the time of onset, duration and intensity of these events.
In addition, each patient was assessed by an investigator at any measurement time point as well as at the end of observation and whenever necessary as deemed by the investigator. Assessment was made using non-specific questions such as "How do you feel?". Specific questions were asked wherever required or useful to more precisely describe an AE.
|
100.0%
1/1 • From intake of the second dose Faldaprevir up to 9 days. Patients were required to report spontaneously any adverse events (AEs) as well as the time of onset, duration and intensity of these events.
In addition, each patient was assessed by an investigator at any measurement time point as well as at the end of observation and whenever necessary as deemed by the investigator. Assessment was made using non-specific questions such as "How do you feel?". Specific questions were asked wherever required or useful to more precisely describe an AE.
|
|
Gastrointestinal disorders
Diarrhoea
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100.0%
1/1 • From intake of the second dose Faldaprevir up to 9 days. Patients were required to report spontaneously any adverse events (AEs) as well as the time of onset, duration and intensity of these events.
In addition, each patient was assessed by an investigator at any measurement time point as well as at the end of observation and whenever necessary as deemed by the investigator. Assessment was made using non-specific questions such as "How do you feel?". Specific questions were asked wherever required or useful to more precisely describe an AE.
|
0.00%
0/1 • From intake of the second dose Faldaprevir up to 9 days. Patients were required to report spontaneously any adverse events (AEs) as well as the time of onset, duration and intensity of these events.
In addition, each patient was assessed by an investigator at any measurement time point as well as at the end of observation and whenever necessary as deemed by the investigator. Assessment was made using non-specific questions such as "How do you feel?". Specific questions were asked wherever required or useful to more precisely describe an AE.
|
|
General disorders
Fatigue
|
100.0%
1/1 • From intake of the second dose Faldaprevir up to 9 days. Patients were required to report spontaneously any adverse events (AEs) as well as the time of onset, duration and intensity of these events.
In addition, each patient was assessed by an investigator at any measurement time point as well as at the end of observation and whenever necessary as deemed by the investigator. Assessment was made using non-specific questions such as "How do you feel?". Specific questions were asked wherever required or useful to more precisely describe an AE.
|
100.0%
1/1 • From intake of the second dose Faldaprevir up to 9 days. Patients were required to report spontaneously any adverse events (AEs) as well as the time of onset, duration and intensity of these events.
In addition, each patient was assessed by an investigator at any measurement time point as well as at the end of observation and whenever necessary as deemed by the investigator. Assessment was made using non-specific questions such as "How do you feel?". Specific questions were asked wherever required or useful to more precisely describe an AE.
|
|
Nervous system disorders
Disturbance in attention
|
0.00%
0/1 • From intake of the second dose Faldaprevir up to 9 days. Patients were required to report spontaneously any adverse events (AEs) as well as the time of onset, duration and intensity of these events.
In addition, each patient was assessed by an investigator at any measurement time point as well as at the end of observation and whenever necessary as deemed by the investigator. Assessment was made using non-specific questions such as "How do you feel?". Specific questions were asked wherever required or useful to more precisely describe an AE.
|
100.0%
1/1 • From intake of the second dose Faldaprevir up to 9 days. Patients were required to report spontaneously any adverse events (AEs) as well as the time of onset, duration and intensity of these events.
In addition, each patient was assessed by an investigator at any measurement time point as well as at the end of observation and whenever necessary as deemed by the investigator. Assessment was made using non-specific questions such as "How do you feel?". Specific questions were asked wherever required or useful to more precisely describe an AE.
|
|
Skin and subcutaneous tissue disorders
Sweating
|
0.00%
0/1 • From intake of the second dose Faldaprevir up to 9 days. Patients were required to report spontaneously any adverse events (AEs) as well as the time of onset, duration and intensity of these events.
In addition, each patient was assessed by an investigator at any measurement time point as well as at the end of observation and whenever necessary as deemed by the investigator. Assessment was made using non-specific questions such as "How do you feel?". Specific questions were asked wherever required or useful to more precisely describe an AE.
|
100.0%
1/1 • From intake of the second dose Faldaprevir up to 9 days. Patients were required to report spontaneously any adverse events (AEs) as well as the time of onset, duration and intensity of these events.
In addition, each patient was assessed by an investigator at any measurement time point as well as at the end of observation and whenever necessary as deemed by the investigator. Assessment was made using non-specific questions such as "How do you feel?". Specific questions were asked wherever required or useful to more precisely describe an AE.
|
|
Gastrointestinal disorders
Soft stools
|
0.00%
0/1 • From intake of the second dose Faldaprevir up to 9 days. Patients were required to report spontaneously any adverse events (AEs) as well as the time of onset, duration and intensity of these events.
In addition, each patient was assessed by an investigator at any measurement time point as well as at the end of observation and whenever necessary as deemed by the investigator. Assessment was made using non-specific questions such as "How do you feel?". Specific questions were asked wherever required or useful to more precisely describe an AE.
|
100.0%
1/1 • From intake of the second dose Faldaprevir up to 9 days. Patients were required to report spontaneously any adverse events (AEs) as well as the time of onset, duration and intensity of these events.
In addition, each patient was assessed by an investigator at any measurement time point as well as at the end of observation and whenever necessary as deemed by the investigator. Assessment was made using non-specific questions such as "How do you feel?". Specific questions were asked wherever required or useful to more precisely describe an AE.
|
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 Boehringer Ingelheim (BI) acknowledges that investigators have the right to publish the study results. Investigators shall provide BI with a copy of any publication or presentation for review prior to any submission. Such review will be done with regard to proprietary information, information related to patentable inventions, medical, scientific, and statistical accuracy within 60 days. BI may request a delay of the publication in order to protect BI's intellectual property rights.
- Publication restrictions are in place
Restriction type: OTHER