Trial Outcomes & Findings for Bioavailability of 3 Different Formulations of BI 207127 in Healthy Male Volunteers (NCT NCT01535638)
NCT ID: NCT01535638
Last Updated: 2016-04-11
Results Overview
Area under the concentration-time curve of Deleobuvir in plasma over the time interval from 0 extrapolated to infinity (AUC0-∞). The measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities.
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
18 participants
Primary outcome timeframe
1:00 (h) hour before drug administration and 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00, 48:00 h after drug administration
Results posted on
2016-04-11
Participant Flow
Participant milestones
| Measure |
Trial Formulation II / Final Formulation (FF) / FF Modified
In this sequence group the treatments (600 mg Deleobuvir in different formulations, single dose) are administered in the order Trial Formulation (TF) II, Final Formulation (FF) and FF modified. There was a wash out period of at least 6 days between each drug administration.
|
Trial Formulation II / Final Formulation (FF) Modified / FF
In this sequence group the treatments (600 mg Deleobuvir in different formulations, single dose) are administered in the order Trial Formulation II, Final Formulation modified and Final Formulation. There was a wash out period of at least 6 days between each drug administration.
|
Final Formulation (FF) / Trial Formulation II / FF Modified
In this sequence group the treatments (600 mg Deleobuvir in different formulations, single dose) are administered in the order Final Formulation, Trial Formulation II and Final Formulation modified. There was a wash out period of at least 6 days between each drug administration.
|
Final Formulation (FF) / FF Modified / Trial Formulation II
In this sequence group the treatments (600 mg Deleobuvir in different formulations, single dose) are administered in the order Final Formulation, Final Formulation modified and Trial Formulation II. There was a wash out period of at least 6 days between each drug administration.
|
Final Formulation (FF) Modified / Trial Formulation II / FF
In this sequence group the treatments (600 mg Deleobuvir in different formulations, single dose) are administered in the order Final Formulation modified, Trial Formulation II and Final Formulation. There was a wash out period of at least 6 days between each drug administration.
|
Final Formulation (FF) Modified / FF / Trial Formulation II
In this sequence group the treatments (600 mg Deleobuvir in different formulations, single dose) are administered in the order Final Formulation modified, Final Formulation and Trial Formulation II. There was a wash out period of at least 6 days between each drug administration.
|
|---|---|---|---|---|---|---|
|
Treatment 1 (Single Dose)
STARTED
|
3
|
3
|
3
|
3
|
3
|
3
|
|
Treatment 1 (Single Dose)
COMPLETED
|
3
|
3
|
3
|
3
|
3
|
2
|
|
Treatment 1 (Single Dose)
NOT COMPLETED
|
0
|
0
|
0
|
0
|
0
|
1
|
|
Treatment 2 (Single Dose)
STARTED
|
3
|
3
|
3
|
3
|
3
|
2
|
|
Treatment 2 (Single Dose)
COMPLETED
|
3
|
3
|
3
|
3
|
3
|
2
|
|
Treatment 2 (Single Dose)
NOT COMPLETED
|
0
|
0
|
0
|
0
|
0
|
0
|
|
Treatment 3 (Single Dose)
STARTED
|
3
|
3
|
3
|
3
|
3
|
2
|
|
Treatment 3 (Single Dose)
COMPLETED
|
3
|
3
|
3
|
2
|
3
|
2
|
|
Treatment 3 (Single Dose)
NOT COMPLETED
|
0
|
0
|
0
|
1
|
0
|
0
|
Reasons for withdrawal
| Measure |
Trial Formulation II / Final Formulation (FF) / FF Modified
In this sequence group the treatments (600 mg Deleobuvir in different formulations, single dose) are administered in the order Trial Formulation (TF) II, Final Formulation (FF) and FF modified. There was a wash out period of at least 6 days between each drug administration.
|
Trial Formulation II / Final Formulation (FF) Modified / FF
In this sequence group the treatments (600 mg Deleobuvir in different formulations, single dose) are administered in the order Trial Formulation II, Final Formulation modified and Final Formulation. There was a wash out period of at least 6 days between each drug administration.
|
Final Formulation (FF) / Trial Formulation II / FF Modified
In this sequence group the treatments (600 mg Deleobuvir in different formulations, single dose) are administered in the order Final Formulation, Trial Formulation II and Final Formulation modified. There was a wash out period of at least 6 days between each drug administration.
|
Final Formulation (FF) / FF Modified / Trial Formulation II
In this sequence group the treatments (600 mg Deleobuvir in different formulations, single dose) are administered in the order Final Formulation, Final Formulation modified and Trial Formulation II. There was a wash out period of at least 6 days between each drug administration.
|
Final Formulation (FF) Modified / Trial Formulation II / FF
In this sequence group the treatments (600 mg Deleobuvir in different formulations, single dose) are administered in the order Final Formulation modified, Trial Formulation II and Final Formulation. There was a wash out period of at least 6 days between each drug administration.
|
Final Formulation (FF) Modified / FF / Trial Formulation II
In this sequence group the treatments (600 mg Deleobuvir in different formulations, single dose) are administered in the order Final Formulation modified, Final Formulation and Trial Formulation II. There was a wash out period of at least 6 days between each drug administration.
|
|---|---|---|---|---|---|---|
|
Treatment 1 (Single Dose)
Protocol Violation
|
0
|
0
|
0
|
0
|
0
|
1
|
|
Treatment 3 (Single Dose)
Protocol Violation
|
0
|
0
|
0
|
1
|
0
|
0
|
Baseline Characteristics
Bioavailability of 3 Different Formulations of BI 207127 in Healthy Male Volunteers
Baseline characteristics by cohort
| Measure |
All Subjects
n=18 Participants
This study was conducted in healthy male subjects as open-label, single-dose, randomised three-way crossover trial to investigate relative bioavailability. Each subject was planned to receive all 3 treatments in a randomly assigned order. The treatments were 3 single doses of 600 mg (3 film-coated tablets à 200 mg each) of Deleobuvir, either as TF II (trial formulation 2) formulation, FF (final formulation) formulation or as FF modified formulation.
|
|---|---|
|
Age, Continuous
|
40.0 years
STANDARD_DEVIATION 6.2 • n=5 Participants
|
|
Sex: Female, Male
Female
|
0 Participants
n=5 Participants
|
|
Sex: Female, Male
Male
|
18 Participants
n=5 Participants
|
PRIMARY outcome
Timeframe: 1:00 (h) hour before drug administration and 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00, 48:00 h after drug administrationPopulation: The pharmacokinetic set (PKS) included all subjects in the treated set who provided at least one observation for at least one primary (PK) endpoint without important protocol violations relevant to the evaluation of PK and no vomiting must have occurred at or before two times the median tmax.
Area under the concentration-time curve of Deleobuvir in plasma over the time interval from 0 extrapolated to infinity (AUC0-∞). The measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities.
Outcome measures
| Measure |
Deleobuvir Trial Formulation II
n=13 Participants
Trial formulation II film-coated tablets.
600 mg Deleobuvir (3 tablets à 200 mg). Oral administration with 240 mL water directly after a standard normal breakfast.
|
Deleobuvir Final Formulation
n=15 Participants
Final formulation film-coated tablets.
600 mg Deleobuvir (3 tablets à 200 mg). Oral administration with 240 mL water directly after a standard normal breakfast.
|
Deleobuvir Final Formulation Modified
n=14 Participants
Final formulation modified film-coated tablets.
600 mg Deleobuvir (3 tablets à 200 mg). Oral administration with 240 mL water directly after a standard normal breakfast.
|
|---|---|---|---|
|
AUC0-∞
|
10600 nmol*h/L
Geometric Coefficient of Variation 45.0
|
12400 nmol*h/L
Geometric Coefficient of Variation 57.3
|
13600 nmol*h/L
Geometric Coefficient of Variation 66.0
|
PRIMARY outcome
Timeframe: 1:00 h before drug administration and 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00, 48:00 h after drug administrationPopulation: The pharmacokinetic set (PKS).
Maximum measured concentration of Deleobuvir in plasma. The measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities.
Outcome measures
| Measure |
Deleobuvir Trial Formulation II
n=13 Participants
Trial formulation II film-coated tablets.
600 mg Deleobuvir (3 tablets à 200 mg). Oral administration with 240 mL water directly after a standard normal breakfast.
|
Deleobuvir Final Formulation
n=15 Participants
Final formulation film-coated tablets.
600 mg Deleobuvir (3 tablets à 200 mg). Oral administration with 240 mL water directly after a standard normal breakfast.
|
Deleobuvir Final Formulation Modified
n=14 Participants
Final formulation modified film-coated tablets.
600 mg Deleobuvir (3 tablets à 200 mg). Oral administration with 240 mL water directly after a standard normal breakfast.
|
|---|---|---|---|
|
Cmax
|
2460 nmol/L
Geometric Coefficient of Variation 48.3
|
2990 nmol/L
Geometric Coefficient of Variation 53.6
|
3070 nmol/L
Geometric Coefficient of Variation 73.1
|
Adverse Events
Deleobuvir Trial Formulation II
Serious events: 0 serious events
Other events: 4 other events
Deaths: 0 deaths
Deleobuvir Final Formulation
Serious events: 0 serious events
Other events: 4 other events
Deaths: 0 deaths
Deleobuvir Final Formulation Modified
Serious events: 0 serious events
Other events: 3 other events
Deaths: 0 deaths
Deleobuvir (Total)
Serious events: 0 serious events
Other events: 7 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Deleobuvir Trial Formulation II
n=16 participants at risk
Trial formulation II film-coated tablets.
600 mg Deleobuvir (3 tablets à 200 mg). Oral administration with 240 mL water directly after a standard normal breakfast.
|
Deleobuvir Final Formulation
n=17 participants at risk
Final formulation film-coated tablets.
600 mg Deleobuvir (3 tablets à 200 mg). Oral administration with 240 mL water directly after a standard normal breakfast.
|
Deleobuvir Final Formulation Modified
n=18 participants at risk
Final formulation modified film-coated tablets.
600 mg Deleobuvir (3 tablets à 200 mg). Oral administration with 240 mL water directly after a standard normal breakfast.
|
Deleobuvir (Total)
n=18 participants at risk
All subjects while on treatment with Deleobuvir, i.e. there is no distinction between the 3 formulations.
|
|---|---|---|---|---|
|
Nervous system disorders
Headache
|
18.8%
3/16 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
23.5%
4/17 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
11.1%
2/18 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
27.8%
5/18 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
|
Nervous system disorders
Dizziness
|
6.2%
1/16 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
0.00%
0/17 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
0.00%
0/18 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
5.6%
1/18 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
|
Respiratory, thoracic and mediastinal disorders
Oropharyngeal pain
|
0.00%
0/16 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
0.00%
0/17 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
5.6%
1/18 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
5.6%
1/18 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
|
Gastrointestinal disorders
Nausea
|
6.2%
1/16 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
5.9%
1/17 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
5.6%
1/18 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
5.6%
1/18 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
|
Gastrointestinal disorders
Vomiting
|
6.2%
1/16 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
0.00%
0/17 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
0.00%
0/18 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
5.6%
1/18 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
|
General disorders
Fatigue
|
6.2%
1/16 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
0.00%
0/17 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
0.00%
0/18 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
5.6%
1/18 • Adverse events (AE) occurring up to 2 days (48 h) after single intake of Deleobuvir tablets were assigned to the respective treatment period.
The volunteers were required to report spontaneously any AEs (and time of onset, duration, intensity). In addition, each volunteer was assessed regularly by the medical staff throughout the clinical trial (including prior to discharge from the trial centre) as well as at the end of observation and whenever necessary as deemed by the investigator.
|
Additional Information
Boehringer Ingelheim Call Center
Boehringer Ingelheim Pharmaceuticals
Phone: 1-800-243-0127
Email: [email protected]
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place