Healthy
Conditions
Brief summary
The aim of the trial is to assess the bioavailability of Faldaprevir soft capsule with single oral dose and multiple oral doses in Chinese subjects
Interventions
DRUGfaldaprevir(high dose)
faldaprevir(high dose) will be taken by 1 day single use and 10 days multiple use. the subjects will be assigned to high dose treatment in random order
DRUGFaldaprevir(low dose)
faldaprevir(low dose) will be taken by 1 day single use and 10 days multiple use. the subjects will be assigned to low dose treatment in random order
Sponsors
Boehringer Ingelheim
Study design
Allocation
RANDOMIZED
Intervention model
PARALLEL
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 45 Years
Healthy volunteers
Yes
Inclusion criteria
Healthy male and female subjects
Exclusion criteria
Any relevant deviation from healthy conditionsAny relevant deviation from healthy conditions
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Cmax,ss (After Multiple Dosing) | Before drug administration and 24 hours(h), 48,72,96,120,144,168,192,216,216.5,217,218,219,220,222,224,228, 240 h after first administration of Faldaprevir | C(max,ss) is defined as maximum measured concentration of Faldaprevir in plasma at steady state over a uniform dosing interval tau. |
| AUC(Tau,ss) (After Multiple Dosing) | Before drug administration and 24 hours(h), 48,72,96,120,144,168,192,216,216.5,217,218,219,220,222,224,228,240 h after first administration of Faldaprevir | AUC(tau,ss) is defined as area under the concentration-time curve of Faldaprevir in plasma at steady state over a uniform dosing interval tau. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Cmax (After Single Dosing) | Before drug administration and 0.5 hours(h), 1,1.5,2,3,4,6,8,12,24,48,72,96h after administration of Faldaprevir | Cmax is defined as maximum measured concentration of Faldaprevir in plasma. |
| AUC(0-tz) (After Single Dosing) | Before drug administration and 0.5 hours(h), 1,1.5,2,3,4,6,8,12,24,48,72,96h after administration of Faldaprevir | AUC (0-tz) is defined as area under the concentration-time curve of the analyte in plasma over the respective time interval, where t and z define beginning and end times of the time interval. |
| t(1/2,ss) (After Multiple Dosing) | Before drug administration and 24 hours(h), 48,72,96,120,144,168,192,216,216.5,217,218,219,220,222,224,228,240 h after first administration of Faldaprevir | t(1/2,ss) is defined as the terminal half-life of Faldaprevir in plasma at steady state. |
| Tmax,ss (After Multiple Dosing) | Before drug administration and 24 hours(h), 48,72,96,120,144,168,192,216,216.5,217,218,219,220,222,224,228, 240 h after first administration of Faldaprevir | tmax,ss is defined as the time from last dosing to the maximum measured concentration of Faldaprevir in plasma at steady state |
Countries
China
Participant flow
Participants by arm
| Arm | Count |
|---|---|
| Faldaprevir 120 mg Oral administration of Faldaprevir 120 mg (BI 201335) soft gel capsule.
The study was divided into two phases, the first being a single dose and the second a multiple dose.
During the single dose treatment (days 1-5), subjects received one single dose in the morning of day 1.
During the multiple dose treatment (days 6-15), subjects received multiple oral doses of faldaprevir once daily from day 6 to day 15. | 10 |
| Faldaprevir 240 mg Oral administration of Faldaprevir 240 mg (BI 201335) soft gel capsule
The study was divided into two phases, the first being a single dose and the second a multiple dose.
During the single dose treatment (days 1-5), subjects received one single dose in the morning of day 1.
During the multiple dose treatment (days 6-15), subjects received multiple oral doses of faldaprevir once daily from day 6 to day 15. | 15 |
| Total | 25 |
Withdrawals & dropouts
| Period | Reason | FG000 | FG001 |
|---|---|---|---|
| Overall Study | Adverse Event | 0 | 3 |
Baseline characteristics
| Characteristic | Faldaprevir 120 mg | Faldaprevir 240 mg | Total |
|---|---|---|---|
| Age, Continuous | 25.3 years STANDARD_DEVIATION 4.5 | 24.8 years STANDARD_DEVIATION 5.7 | 25.0 years STANDARD_DEVIATION 5.2 |
| Sex: Female, Male Female | 5 Participants | 8 Participants | 13 Participants |
| Sex: Female, Male Male | 5 Participants | 7 Participants | 12 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 | 7 / 10 | 10 / 10 | 13 / 15 | 13 / 13 |
| serious Total, serious adverse events | 0 / 10 | 0 / 10 | 0 / 15 | 0 / 13 |
Outcome results
Primary
AUC(Tau,ss) (After Multiple Dosing)
AUC(tau,ss) is defined as area under the concentration-time curve of Faldaprevir in plasma at steady state over a uniform dosing interval tau.
Time frame: Before drug administration and 24 hours(h), 48,72,96,120,144,168,192,216,216.5,217,218,219,220,222,224,228,240 h after first administration of Faldaprevir
Population: Pharmacokinetic analysis set (PKS): This set included all subjects in TS who provided at least one PK endpoint and had no important protocol violations relevant to the evaluation of PK and provided no emesis with onset at or before twice the median t max .
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Faldaprevir 120 mg | AUC(Tau,ss) (After Multiple Dosing) | 36200 ng*h/mL | Geometric Coefficient of Variation 48.5 |
| Faldaprevir 240 mg | AUC(Tau,ss) (After Multiple Dosing) | 199000 ng*h/mL | Geometric Coefficient of Variation 49.5 |
Primary
Cmax,ss (After Multiple Dosing)
C(max,ss) is defined as maximum measured concentration of Faldaprevir in plasma at steady state over a uniform dosing interval tau.
Time frame: Before drug administration and 24 hours(h), 48,72,96,120,144,168,192,216,216.5,217,218,219,220,222,224,228, 240 h after first administration of Faldaprevir
Population: Pharmacokinetic analysis set (PKS): This set included all subjects in TS who provided at least one Pharmacokinetic (PK) endpoint and had no important protocol violations relevant to the evaluation of PK and provided no emesis with onset at or before twice the median t max .
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Faldaprevir 120 mg | Cmax,ss (After Multiple Dosing) | 3270 ng/mL | Geometric Coefficient of Variation 44 |
| Faldaprevir 240 mg | Cmax,ss (After Multiple Dosing) | 14200 ng/mL | Geometric Coefficient of Variation 35.5 |
Secondary
AUC(0-tz) (After Single Dosing)
AUC (0-tz) is defined as area under the concentration-time curve of the analyte in plasma over the respective time interval, where t and z define beginning and end times of the time interval.
Time frame: Before drug administration and 0.5 hours(h), 1,1.5,2,3,4,6,8,12,24,48,72,96h after administration of Faldaprevir
Population: Pharmacokinetic analysis set (PKS): This set included all subjects in TS who provided at least one PK endpoint and had no important protocol violations relevant to the evaluation of PK and provided no emesis with onset at or before twice the median t max .
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Faldaprevir 120 mg | AUC(0-tz) (After Single Dosing) | 14600 ng*h/mL | Geometric Coefficient of Variation 38.9 |
| Faldaprevir 240 mg | AUC(0-tz) (After Single Dosing) | 37900 ng*h/mL | Geometric Coefficient of Variation 45.5 |
Secondary
Cmax (After Single Dosing)
Cmax is defined as maximum measured concentration of Faldaprevir in plasma.
Time frame: Before drug administration and 0.5 hours(h), 1,1.5,2,3,4,6,8,12,24,48,72,96h after administration of Faldaprevir
Population: Pharmacokinetic analysis set (PKS): This set included all subjects in TS who provided at least one PK endpoint and had no important protocol violations relevant to the evaluation of PK and provided no emesis with onset at or before twice the median t max .
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Faldaprevir 120 mg | Cmax (After Single Dosing) | 664 ng/mL | Geometric Coefficient of Variation 48.7 |
| Faldaprevir 240 mg | Cmax (After Single Dosing) | 2060 ng/mL | Geometric Coefficient of Variation 44.3 |
Secondary
t(1/2,ss) (After Multiple Dosing)
t(1/2,ss) is defined as the terminal half-life of Faldaprevir in plasma at steady state.
Time frame: Before drug administration and 24 hours(h), 48,72,96,120,144,168,192,216,216.5,217,218,219,220,222,224,228,240 h after first administration of Faldaprevir
Population: Pharmacokinetic analysis set (PKS): This set included all subjects in TS who provided at least one PK endpoint and had no important protocol violations relevant to the evaluation of PK and provided no emesis with onset at or before twice the median t max .
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Faldaprevir 120 mg | t(1/2,ss) (After Multiple Dosing) | 31.2 hour | Geometric Coefficient of Variation 9.27 |
| Faldaprevir 240 mg | t(1/2,ss) (After Multiple Dosing) | 20.0 hour | Geometric Coefficient of Variation 23.6 |
Secondary
Tmax,ss (After Multiple Dosing)
tmax,ss is defined as the time from last dosing to the maximum measured concentration of Faldaprevir in plasma at steady state
Time frame: Before drug administration and 24 hours(h), 48,72,96,120,144,168,192,216,216.5,217,218,219,220,222,224,228, 240 h after first administration of Faldaprevir
Population: Pharmacokinetic analysis set (PKS): This set included all subjects in TS who provided at least one PK endpoint and had no important protocol violations relevant to the evaluation of PK and provided no emesis with onset at or before twice the median t max .
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Faldaprevir 120 mg | Tmax,ss (After Multiple Dosing) | 2.85 hour | Geometric Coefficient of Variation 33.6 |
| Faldaprevir 240 mg | Tmax,ss (After Multiple Dosing) | 2.44 hour | Geometric Coefficient of Variation 29.8 |