Healthy
Conditions
Brief summary
The aim of the study is to evaluate safety, tolerability and pharmacokinetics in Asian and Caucasian healthy male volunteers administered BI 207127 NA.
Interventions
DRUGMatching placebo (low dose)
single dose of matching placebo
DRUGBI 207127 NA (medium dose)
Single does of BI 207127 NA
DRUGBI 207127 NA (low dose)
single dose of BI 207127 NA
DRUGMatching placebo (medium dose)
Single dose of matching placebo
DRUGBI 207127 NA (high dose)
Single dose of BI 207127 NA
DRUGMatching placebo (high dose)
Single dose of matching placebo
Sponsors
Boehringer Ingelheim
Study design
Allocation
RANDOMIZED
Intervention model
PARALLEL
Primary purpose
TREATMENT
Masking
DOUBLE
Eligibility
Sex/Gender
MALE
Age
20 Years to 50 Years
Healthy volunteers
Yes
Inclusion criteria
1. Healthy male volunteers 2. Chinese ethnicity or Japanese ethnicity or Caucasian 3. Body Mass Index (BMI) = 18.5 and BMI =25 kg/m2 for Japanese and Chinese, BMI =18.5 and BMI = 29.9 kg/m2 for Caucasians
Exclusion criteria
1. Any finding of the medical examination (including Blood pressure(BP), Pulse rate (PR) and Electrocardiogram (ECG)) deviating from normal and of clinical relevance 2. Any evidence of a clinically relevant concomitant disease 3. Intake of drugs with a long half-life (\> 24 hours) within at least one month or less than 10 half-lives of the respective drug prior to administration or during the trial
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Number of Subjects With Drug Related Adverse Events | From first administration of study drug (drug related AEs) until 14 days after end of trial visit, upto 17 days. | Number of subjects with investigator-defined drug-related adverse events (AEs). Tolerability assessment endpoint. The investigator assessed the possible causal relationship between all AEs and the investigational drug, considering all relevant factors, including pattern of reaction, temporal relationship, de-challenge or re-challenge, and confounding factors such as concomitant medication, concomitant diseases, and relevant history. |
| Number of Subjects With Adverse Events as Determined by Clinical Relevant Abnormalities for Vital Signs, Blood Chemistry, Haematology, Urinanalysis and ECG | From signing the informed consent (within 21 days before drug administration) until 14 days after end of trial visit, upto 38 days. | Clinical relevant abnormalities for vital signs, blood chemistry, haematology, urinanalysis and ECG. Tolerability assessment endpoint. New abnormal findings or worsening of baseline conditions were reported as adverse events. Adverse events were assessed through the entire trial, from signing the informed consent (within 21 days before drug administration) onwards through the observational phase until the end-of-trial-examination (within 14 days after last trial procedure). |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Cmax of Deleobuvir | -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration | Maximum measured concentration of the analyte in plasma (Deleobuvir). |
| AUC0-∞ of BI 208333 (Metabolite of Deleobuvir) | -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration | Area under the concentration-time curve of the analyte in plasma (BI 208333) over the time interval from 0 extrapolated to infinity. The descriptive statistics of the arms Japanese 400mg, Japanese 800mg and Chinese 400mg cannot be determined. The reason was that there were too few data to derive a terminal elimination rate constant (slope) to calculate AUC0-∞. |
| Tmax of BI 208333 (Metabolite of Deleobuvir) | -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration | Time from dosing to the maximum measured concentration of the analyte in plasma (BI 208333) . |
| Cmax of BI 208333 (Metabolite of Deleobuvir) | -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration | Maximum measured concentration of the analyte in plasma (BI 208333). |
| AUC0-∞ of CD 6168 (Metabolite of Deleobuvir) | -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration | Area under the concentration-time curve of the analyte in plasma (CD 6168) over the time interval from 0 extrapolated to infinity. The descriptive statistics of the arms Japanese 1200mg and Chinese 400mg cannot be determined. The reason was that there were too few data to derive a terminal elimination rate constant (slope) to calculate AUC0-∞. |
| AUC0-∞ of Deleobuvir | -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h (hours) after drug administration | Area under the concentration-time curve of the analyte in plasma (Deleobuvir) over the time interval from 0 extrapolated to infinity (AUC0-∞). |
| Cmax of CD 6168 (Metabolite of Deleobuvir) | -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration | Maximum measured concentration of the analyte in plasma (CD 6168). |
| AUC0-∞ of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration | Area under the concentration-time curve of the analyte in plasma (CD 6168 Acylglucuronide) over the time interval from 0 extrapolated to infinity. The descriptive statistics of the arms Japanese 400mg, Japanese 800mg, Japanese 1200mg and Chinese 400mg cannot be determined. The reason was that there were too few data to derive a terminal elimination rate constant (slope) to calculate AUC0-∞. |
| Tmax of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration | Time from dosing to the maximum measured concentration of the analyte in plasma (CD 6168 Acylglucuronide). The descriptive statistics of the arm Chinese 400mg cannot be determined due to limitation of available data above the below limit of quantification (BLQ). |
| Cmax of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration | Maximum measured concentration of the analyte in plasma (CD 6168 Acylglucuronide). The descriptive statistics of the arm Chinese 400mg cannot be determined due to limitation of available data above the below limit of quantification (BLQ). |
| Tmax of CD 6168 (Metabolite of Deleobuvir) | -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration | Time from dosing to the maximum measured concentration of the analyte in plasma (CD 6168). |
| Tmax of Deleobuvir | -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration | Time from dosing to the maximum measured concentration of the analyte in plasma (Deleobuvir). |
Countries
South Korea
Participant flow
Recruitment details
60 subjects were included (27 Chinese, 25 Japanese, and 8 Caucasian subjects). 24 Japanese and 24 Chinese subjects were randomised to 1 of 3 (rising) dose groups and received single oral doses of either 400mg, 800mg, or 1200mg of BI 207127 NA or of the respective placebo. Caucasian subjects were randomised to 1200 mg BI 207127 NA or placebo.
Pre-assignment details
The decision to proceed to the next higher dose group was based upon the safety of the preceding dose group. Caucasian subjects were randomised to receive either placebo or 1200 mg BI 207127 NA; this dose group could be started independently from the results of dose escalation in the Asian subjects.
Participants by arm
| Arm | Count |
|---|---|
| 1200 mg Deleobuvir (Caucasian Subjects) Caucasian subjects who received 1200 mg Deleobuvir.
Oral with 240 mL of water in fed condition. | 6 |
| Placebo (Caucasian Subjects) Caucasian subjects who received matching placebo.
Oral with 240 mL of water in fed condition. | 2 |
| 400 mg Deleobuvir (Japanese Subjects) Japanese subjects who received 400 mg Deleobuvir.
Oral with 240 mL of water in fed condition. | 6 |
| 800 mg Deleobuvir (Japanese Subjects) Japanese subjects who received 800 mg Deleobuvir.
Oral with 240 mL of water in fed condition. | 6 |
| 1200mg Deleobuvir (Japanese Subjects) Japanese subjects who received 1200 mg Deleobuvir.
Oral with 240 mL of water in fed condition. | 6 |
| Placebo (Japanese Subjects) Japanese subjects who received matching placebo.
Oral with 240 mL of water in fed condition. | 6 |
| 400 mg Deleobuvir (Chinese Subjects) Chinese subjects who received 400 mg Deleobuvir.
Oral with 240 mL of water in fed condition. | 6 |
| 800 mg Deleobuvir (Chinese Subjects) Chinese subjects who received 800 mg Deleobuvir.
Oral with 240 mL of water in fed condition. | 6 |
| 1200 mg Deleobuvir (Chinese Subjects) Chinese subjects who received 1200 mg Deleobuvir.
Oral with 240 mL of water in fed condition. | 6 |
| Placebo (Chinese Subjects) Chinese subjects who received matching placebo.
Oral with 240 mL of water in fed condition. | 6 |
| Total | 56 |
Withdrawals & dropouts
| Period | Reason | FG000 | FG001 | FG002 | FG003 | FG004 | FG005 | FG006 | FG007 | FG008 | FG009 |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study | failed screening visit | 0 | 0 | 1 | 0 | 0 | 0 | 1 | 1 | 0 | 1 |
Baseline characteristics
| Characteristic | Total | 1200 mg Deleobuvir (Caucasian Subjects) | Placebo (Caucasian Subjects) | 400 mg Deleobuvir (Japanese Subjects) | 800 mg Deleobuvir (Japanese Subjects) | 1200mg Deleobuvir (Japanese Subjects) | Placebo (Japanese Subjects) | 400 mg Deleobuvir (Chinese Subjects) | 800 mg Deleobuvir (Chinese Subjects) | 1200 mg Deleobuvir (Chinese Subjects) | Placebo (Chinese Subjects) |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Age, Continuous | 26.4 years STANDARD_DEVIATION 5.2 | 29.3 years STANDARD_DEVIATION 7 | 31.0 years STANDARD_DEVIATION 8.5 | 28.8 years STANDARD_DEVIATION 7 | 28.2 years STANDARD_DEVIATION 4.6 | 23.7 years STANDARD_DEVIATION 3.6 | 29.2 years STANDARD_DEVIATION 7.1 | 24.7 years STANDARD_DEVIATION 2.1 | 26.0 years STANDARD_DEVIATION 3.9 | 23.7 years STANDARD_DEVIATION 2.3 | 23.0 years STANDARD_DEVIATION 2.1 |
| Sex: Female, Male Female | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Sex: Female, Male Male | 56 Participants | 6 Participants | 2 Participants | 6 Participants | 6 Participants | 6 Participants | 6 Participants | 6 Participants | 6 Participants | 6 Participants | 6 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk | EG002 affected / at risk | EG003 affected / at risk |
|---|---|---|---|---|
| deaths Total, all-cause mortality | — / — | — / — | — / — | — / — |
| other Total, other adverse events | 5 / 14 | 1 / 12 | 2 / 12 | 14 / 18 |
| serious Total, serious adverse events | 0 / 14 | 0 / 12 | 0 / 12 | 0 / 18 |
Outcome results
Primary
Number of Subjects With Adverse Events as Determined by Clinical Relevant Abnormalities for Vital Signs, Blood Chemistry, Haematology, Urinanalysis and ECG
Clinical relevant abnormalities for vital signs, blood chemistry, haematology, urinanalysis and ECG. Tolerability assessment endpoint. New abnormal findings or worsening of baseline conditions were reported as adverse events. Adverse events were assessed through the entire trial, from signing the informed consent (within 21 days before drug administration) onwards through the observational phase until the end-of-trial-examination (within 14 days after last trial procedure).
Time frame: From signing the informed consent (within 21 days before drug administration) until 14 days after end of trial visit, upto 38 days.
Population: The treated set.
| Arm | Measure | Value (NUMBER) |
|---|---|---|
| 1200 mg Deleobuvir (Caucasian Subjects) | Number of Subjects With Adverse Events as Determined by Clinical Relevant Abnormalities for Vital Signs, Blood Chemistry, Haematology, Urinanalysis and ECG | 0 participants |
| Placebo (Caucasian Subjects) | Number of Subjects With Adverse Events as Determined by Clinical Relevant Abnormalities for Vital Signs, Blood Chemistry, Haematology, Urinanalysis and ECG | 0 participants |
| 400 mg Deleobuvir (Japanese Subjects) | Number of Subjects With Adverse Events as Determined by Clinical Relevant Abnormalities for Vital Signs, Blood Chemistry, Haematology, Urinanalysis and ECG | 0 participants |
| 800 mg Deleobuvir (Japanese Subjects) | Number of Subjects With Adverse Events as Determined by Clinical Relevant Abnormalities for Vital Signs, Blood Chemistry, Haematology, Urinanalysis and ECG | 0 participants |
| 1200mg Deleobuvir (Japanese Subjects) | Number of Subjects With Adverse Events as Determined by Clinical Relevant Abnormalities for Vital Signs, Blood Chemistry, Haematology, Urinanalysis and ECG | 0 participants |
| Placebo (Japanese Subjects) | Number of Subjects With Adverse Events as Determined by Clinical Relevant Abnormalities for Vital Signs, Blood Chemistry, Haematology, Urinanalysis and ECG | 0 participants |
| 400 mg Deleobuvir (Chinese Subjects) | Number of Subjects With Adverse Events as Determined by Clinical Relevant Abnormalities for Vital Signs, Blood Chemistry, Haematology, Urinanalysis and ECG | 0 participants |
| 800 mg Deleobuvir (Chinese Subjects) | Number of Subjects With Adverse Events as Determined by Clinical Relevant Abnormalities for Vital Signs, Blood Chemistry, Haematology, Urinanalysis and ECG | 0 participants |
| 1200 mg Deleobuvir (Chinese Subjects) | Number of Subjects With Adverse Events as Determined by Clinical Relevant Abnormalities for Vital Signs, Blood Chemistry, Haematology, Urinanalysis and ECG | 0 participants |
| Placebo (Chinese Subjects) | Number of Subjects With Adverse Events as Determined by Clinical Relevant Abnormalities for Vital Signs, Blood Chemistry, Haematology, Urinanalysis and ECG | 0 participants |
Primary
Number of Subjects With Drug Related Adverse Events
Number of subjects with investigator-defined drug-related adverse events (AEs). Tolerability assessment endpoint. The investigator assessed the possible causal relationship between all AEs and the investigational drug, considering all relevant factors, including pattern of reaction, temporal relationship, de-challenge or re-challenge, and confounding factors such as concomitant medication, concomitant diseases, and relevant history.
Time frame: From first administration of study drug (drug related AEs) until 14 days after end of trial visit, upto 17 days.
Population: Treated set (full analysis set according to the International Conference on Harmonization (ICH) E9 guideline): all subjects who were dispensed trial medication and were documented to have taken at least 1 dose of investigational treatment.
| Arm | Measure | Value (NUMBER) |
|---|---|---|
| 1200 mg Deleobuvir (Caucasian Subjects) | Number of Subjects With Drug Related Adverse Events | 5 Participants |
| Placebo (Caucasian Subjects) | Number of Subjects With Drug Related Adverse Events | 1 Participants |
| 400 mg Deleobuvir (Japanese Subjects) | Number of Subjects With Drug Related Adverse Events | 0 Participants |
| 800 mg Deleobuvir (Japanese Subjects) | Number of Subjects With Drug Related Adverse Events | 0 Participants |
| 1200mg Deleobuvir (Japanese Subjects) | Number of Subjects With Drug Related Adverse Events | 5 Participants |
| Placebo (Japanese Subjects) | Number of Subjects With Drug Related Adverse Events | 2 Participants |
| 400 mg Deleobuvir (Chinese Subjects) | Number of Subjects With Drug Related Adverse Events | 1 Participants |
| 800 mg Deleobuvir (Chinese Subjects) | Number of Subjects With Drug Related Adverse Events | 2 Participants |
| 1200 mg Deleobuvir (Chinese Subjects) | Number of Subjects With Drug Related Adverse Events | 4 Participants |
| Placebo (Chinese Subjects) | Number of Subjects With Drug Related Adverse Events | 2 Participants |
Secondary
AUC0-∞ of BI 208333 (Metabolite of Deleobuvir)
Area under the concentration-time curve of the analyte in plasma (BI 208333) over the time interval from 0 extrapolated to infinity. The descriptive statistics of the arms Japanese 400mg, Japanese 800mg and Chinese 400mg cannot be determined. The reason was that there were too few data to derive a terminal elimination rate constant (slope) to calculate AUC0-∞.
Time frame: -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration
Population: The PK analysis set.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 1200 mg Deleobuvir (Caucasian Subjects) | AUC0-∞ of BI 208333 (Metabolite of Deleobuvir) | 12.7 µmol*h/L | Geometric Coefficient of Variation 54.6 |
| Placebo (Caucasian Subjects) | AUC0-∞ of BI 208333 (Metabolite of Deleobuvir) | 10.1 µmol*h/L | Geometric Coefficient of Variation 54.2 |
| 400 mg Deleobuvir (Japanese Subjects) | AUC0-∞ of BI 208333 (Metabolite of Deleobuvir) | 5.97 µmol*h/L | Geometric Coefficient of Variation 23.9 |
| 800 mg Deleobuvir (Japanese Subjects) | AUC0-∞ of BI 208333 (Metabolite of Deleobuvir) | 9.01 µmol*h/L | Geometric Coefficient of Variation 186 |
Secondary
AUC0-∞ of CD 6168 Acylglucuronide (Metabolite of Deleobuvir)
Area under the concentration-time curve of the analyte in plasma (CD 6168 Acylglucuronide) over the time interval from 0 extrapolated to infinity. The descriptive statistics of the arms Japanese 400mg, Japanese 800mg, Japanese 1200mg and Chinese 400mg cannot be determined. The reason was that there were too few data to derive a terminal elimination rate constant (slope) to calculate AUC0-∞.
Time frame: -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration
Population: The PK analysis set.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 1200 mg Deleobuvir (Caucasian Subjects) | AUC0-∞ of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | 1.27 µmol*h/L | Geometric Coefficient of Variation 114 |
| Placebo (Caucasian Subjects) | AUC0-∞ of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | 0.56 µmol*h/L | Geometric Coefficient of Variation 17.5 |
| 400 mg Deleobuvir (Japanese Subjects) | AUC0-∞ of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | 1.01 µmol*h/L | Geometric Coefficient of Variation 50.2 |
Secondary
AUC0-∞ of CD 6168 (Metabolite of Deleobuvir)
Area under the concentration-time curve of the analyte in plasma (CD 6168) over the time interval from 0 extrapolated to infinity. The descriptive statistics of the arms Japanese 1200mg and Chinese 400mg cannot be determined. The reason was that there were too few data to derive a terminal elimination rate constant (slope) to calculate AUC0-∞.
Time frame: -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration
Population: The PK analysis set.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 1200 mg Deleobuvir (Caucasian Subjects) | AUC0-∞ of CD 6168 (Metabolite of Deleobuvir) | 15.8 µmol*h/L | Geometric Coefficient of Variation 125 |
| Placebo (Caucasian Subjects) | AUC0-∞ of CD 6168 (Metabolite of Deleobuvir) | 4.48 µmol*h/L | Geometric Coefficient of Variation 85.8 |
| 400 mg Deleobuvir (Japanese Subjects) | AUC0-∞ of CD 6168 (Metabolite of Deleobuvir) | 11.0 µmol*h/L | Geometric Coefficient of Variation 55.3 |
| 800 mg Deleobuvir (Japanese Subjects) | AUC0-∞ of CD 6168 (Metabolite of Deleobuvir) | 12.0 µmol*h/L | Geometric Coefficient of Variation 25.1 |
| 1200mg Deleobuvir (Japanese Subjects) | AUC0-∞ of CD 6168 (Metabolite of Deleobuvir) | 22.2 µmol*h/L | Geometric Coefficient of Variation 38.9 |
Secondary
AUC0-∞ of Deleobuvir
Area under the concentration-time curve of the analyte in plasma (Deleobuvir) over the time interval from 0 extrapolated to infinity (AUC0-∞).
Time frame: -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h (hours) after drug administration
Population: The pharmacokinetic (PK) analysis set: all evaluable subjects of the treated set who provided at least 1 observation for at least 1 PK endpoint without important protocol violations relevant to the evaluation of PK.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 1200 mg Deleobuvir (Caucasian Subjects) | AUC0-∞ of Deleobuvir | 61.2 µmol*h/L | Geometric Coefficient of Variation 45.5 |
| Placebo (Caucasian Subjects) | AUC0-∞ of Deleobuvir | 14.0 µmol*h/L | Geometric Coefficient of Variation 56.1 |
| 400 mg Deleobuvir (Japanese Subjects) | AUC0-∞ of Deleobuvir | 31.4 µmol*h/L | Geometric Coefficient of Variation 52.3 |
| 800 mg Deleobuvir (Japanese Subjects) | AUC0-∞ of Deleobuvir | 48.2 µmol*h/L | Geometric Coefficient of Variation 39.1 |
| 1200mg Deleobuvir (Japanese Subjects) | AUC0-∞ of Deleobuvir | 8.7 µmol*h/L | Geometric Coefficient of Variation 78.7 |
| Placebo (Japanese Subjects) | AUC0-∞ of Deleobuvir | 42.6 µmol*h/L | Geometric Coefficient of Variation 28.2 |
| 400 mg Deleobuvir (Chinese Subjects) | AUC0-∞ of Deleobuvir | 72.0 µmol*h/L | Geometric Coefficient of Variation 55.9 |
Secondary
Cmax of BI 208333 (Metabolite of Deleobuvir)
Maximum measured concentration of the analyte in plasma (BI 208333).
Time frame: -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration
Population: The PK analysis set.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 1200 mg Deleobuvir (Caucasian Subjects) | Cmax of BI 208333 (Metabolite of Deleobuvir) | 1.82 µmol/L | Geometric Coefficient of Variation 42.8 |
| Placebo (Caucasian Subjects) | Cmax of BI 208333 (Metabolite of Deleobuvir) | 0.59 µmol/L | Geometric Coefficient of Variation 43.6 |
| 400 mg Deleobuvir (Japanese Subjects) | Cmax of BI 208333 (Metabolite of Deleobuvir) | 0.92 µmol/L | Geometric Coefficient of Variation 54.2 |
| 800 mg Deleobuvir (Japanese Subjects) | Cmax of BI 208333 (Metabolite of Deleobuvir) | 1.32 µmol/L | Geometric Coefficient of Variation 55 |
| 1200mg Deleobuvir (Japanese Subjects) | Cmax of BI 208333 (Metabolite of Deleobuvir) | 0.58 µmol/L | Geometric Coefficient of Variation 26.8 |
| Placebo (Japanese Subjects) | Cmax of BI 208333 (Metabolite of Deleobuvir) | 0.86 µmol/L | Geometric Coefficient of Variation 38.9 |
| 400 mg Deleobuvir (Chinese Subjects) | Cmax of BI 208333 (Metabolite of Deleobuvir) | 1.19 µmol/L | Geometric Coefficient of Variation 104 |
Secondary
Cmax of CD 6168 Acylglucuronide (Metabolite of Deleobuvir)
Maximum measured concentration of the analyte in plasma (CD 6168 Acylglucuronide). The descriptive statistics of the arm Chinese 400mg cannot be determined due to limitation of available data above the below limit of quantification (BLQ).
Time frame: -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration
Population: The PK analysis set.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 1200 mg Deleobuvir (Caucasian Subjects) | Cmax of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | 0.13 µmol/L | Geometric Coefficient of Variation 62.3 |
| Placebo (Caucasian Subjects) | Cmax of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | 0.03 µmol/L | Geometric Coefficient of Variation 38 |
| 400 mg Deleobuvir (Japanese Subjects) | Cmax of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | 0.08 µmol/L | Geometric Coefficient of Variation 48.2 |
| 800 mg Deleobuvir (Japanese Subjects) | Cmax of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | 0.11 µmol/L | Geometric Coefficient of Variation 128 |
| 1200mg Deleobuvir (Japanese Subjects) | Cmax of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | 0.05 µmol/L | Geometric Coefficient of Variation 29 |
| Placebo (Japanese Subjects) | Cmax of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | 0.07 µmol/L | Geometric Coefficient of Variation 91.6 |
Secondary
Cmax of CD 6168 (Metabolite of Deleobuvir)
Maximum measured concentration of the analyte in plasma (CD 6168).
Time frame: -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration
Population: The PK analysis set.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 1200 mg Deleobuvir (Caucasian Subjects) | Cmax of CD 6168 (Metabolite of Deleobuvir) | 2.31 µmol/L | Geometric Coefficient of Variation 80.7 |
| Placebo (Caucasian Subjects) | Cmax of CD 6168 (Metabolite of Deleobuvir) | 0.57 µmol/L | Geometric Coefficient of Variation 43.6 |
| 400 mg Deleobuvir (Japanese Subjects) | Cmax of CD 6168 (Metabolite of Deleobuvir) | 1.39 µmol/L | Geometric Coefficient of Variation 34.3 |
| 800 mg Deleobuvir (Japanese Subjects) | Cmax of CD 6168 (Metabolite of Deleobuvir) | 2.65 µmol/L | Geometric Coefficient of Variation 32.2 |
| 1200mg Deleobuvir (Japanese Subjects) | Cmax of CD 6168 (Metabolite of Deleobuvir) | 0.35 µmol/L | Geometric Coefficient of Variation 109 |
| Placebo (Japanese Subjects) | Cmax of CD 6168 (Metabolite of Deleobuvir) | 1.66 µmol/L | Geometric Coefficient of Variation 18.2 |
| 400 mg Deleobuvir (Chinese Subjects) | Cmax of CD 6168 (Metabolite of Deleobuvir) | 2.50 µmol/L | Geometric Coefficient of Variation 30.9 |
Secondary
Cmax of Deleobuvir
Maximum measured concentration of the analyte in plasma (Deleobuvir).
Time frame: -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration
Population: The PK analysis set.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 1200 mg Deleobuvir (Caucasian Subjects) | Cmax of Deleobuvir | 11.8 µmol/L | Geometric Coefficient of Variation 42 |
| Placebo (Caucasian Subjects) | Cmax of Deleobuvir | 3.2 µmol/L | Geometric Coefficient of Variation 63.9 |
| 400 mg Deleobuvir (Japanese Subjects) | Cmax of Deleobuvir | 6.41 µmol/L | Geometric Coefficient of Variation 47.4 |
| 800 mg Deleobuvir (Japanese Subjects) | Cmax of Deleobuvir | 8.26 µmol/L | Geometric Coefficient of Variation 37.7 |
| 1200mg Deleobuvir (Japanese Subjects) | Cmax of Deleobuvir | 2.32 µmol/L | Geometric Coefficient of Variation 75.5 |
| Placebo (Japanese Subjects) | Cmax of Deleobuvir | 8.89 µmol/L | Geometric Coefficient of Variation 24.1 |
| 400 mg Deleobuvir (Chinese Subjects) | Cmax of Deleobuvir | 12.9 µmol/L | Geometric Coefficient of Variation 51.3 |
Secondary
Tmax of BI 208333 (Metabolite of Deleobuvir)
Time from dosing to the maximum measured concentration of the analyte in plasma (BI 208333) .
Time frame: -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration
Population: The PK analysis set.
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| 1200 mg Deleobuvir (Caucasian Subjects) | Tmax of BI 208333 (Metabolite of Deleobuvir) | 6.00 h |
| Placebo (Caucasian Subjects) | Tmax of BI 208333 (Metabolite of Deleobuvir) | 6.00 h |
| 400 mg Deleobuvir (Japanese Subjects) | Tmax of BI 208333 (Metabolite of Deleobuvir) | 6.00 h |
| 800 mg Deleobuvir (Japanese Subjects) | Tmax of BI 208333 (Metabolite of Deleobuvir) | 6.00 h |
| 1200mg Deleobuvir (Japanese Subjects) | Tmax of BI 208333 (Metabolite of Deleobuvir) | 5.01 h |
| Placebo (Japanese Subjects) | Tmax of BI 208333 (Metabolite of Deleobuvir) | 6.00 h |
| 400 mg Deleobuvir (Chinese Subjects) | Tmax of BI 208333 (Metabolite of Deleobuvir) | 6.00 h |
Secondary
Tmax of CD 6168 Acylglucuronide (Metabolite of Deleobuvir)
Time from dosing to the maximum measured concentration of the analyte in plasma (CD 6168 Acylglucuronide). The descriptive statistics of the arm Chinese 400mg cannot be determined due to limitation of available data above the below limit of quantification (BLQ).
Time frame: -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration
Population: The PK analysis set.
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| 1200 mg Deleobuvir (Caucasian Subjects) | Tmax of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | 7.01 h |
| Placebo (Caucasian Subjects) | Tmax of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | 8.00 h |
| 400 mg Deleobuvir (Japanese Subjects) | Tmax of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | 9.98 h |
| 800 mg Deleobuvir (Japanese Subjects) | Tmax of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | 10.00 h |
| 1200mg Deleobuvir (Japanese Subjects) | Tmax of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | 6.00 h |
| Placebo (Japanese Subjects) | Tmax of CD 6168 Acylglucuronide (Metabolite of Deleobuvir) | 8.00 h |
Secondary
Tmax of CD 6168 (Metabolite of Deleobuvir)
Time from dosing to the maximum measured concentration of the analyte in plasma (CD 6168).
Time frame: -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration
Population: The PK analysis set.
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| 1200 mg Deleobuvir (Caucasian Subjects) | Tmax of CD 6168 (Metabolite of Deleobuvir) | 6.01 h |
| Placebo (Caucasian Subjects) | Tmax of CD 6168 (Metabolite of Deleobuvir) | 7.00 h |
| 400 mg Deleobuvir (Japanese Subjects) | Tmax of CD 6168 (Metabolite of Deleobuvir) | 6.00 h |
| 800 mg Deleobuvir (Japanese Subjects) | Tmax of CD 6168 (Metabolite of Deleobuvir) | 9.98 h |
| 1200mg Deleobuvir (Japanese Subjects) | Tmax of CD 6168 (Metabolite of Deleobuvir) | 6.00 h |
| Placebo (Japanese Subjects) | Tmax of CD 6168 (Metabolite of Deleobuvir) | 5.50 h |
| 400 mg Deleobuvir (Chinese Subjects) | Tmax of CD 6168 (Metabolite of Deleobuvir) | 7.00 h |
Secondary
Tmax of Deleobuvir
Time from dosing to the maximum measured concentration of the analyte in plasma (Deleobuvir).
Time frame: -2:00, 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 h after drug administration
Population: The PK analysis set.
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| 1200 mg Deleobuvir (Caucasian Subjects) | Tmax of Deleobuvir | 6.01 h |
| Placebo (Caucasian Subjects) | Tmax of Deleobuvir | 4.51 h |
| 400 mg Deleobuvir (Japanese Subjects) | Tmax of Deleobuvir | 5.50 h |
| 800 mg Deleobuvir (Japanese Subjects) | Tmax of Deleobuvir | 5.00 h |
| 1200mg Deleobuvir (Japanese Subjects) | Tmax of Deleobuvir | 4.50 h |
| Placebo (Japanese Subjects) | Tmax of Deleobuvir | 5.00 h |
| 400 mg Deleobuvir (Chinese Subjects) | Tmax of Deleobuvir | 5.50 h |