Healthy
Conditions
Brief summary
The aim of this study is to investigate the safety and tolerability of BI 655130 in healthy male subjects following single rising low, medium and high doses.
Interventions
DRUGPlacebo
Sponsors
Boehringer Ingelheim
Study design
Allocation
RANDOMIZED
Intervention model
PARALLEL
Primary purpose
TREATMENT
Masking
SINGLE (Subject)
Eligibility
Sex/Gender
MALE
Age
18 Years to 45 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy male subjects according to the investigators assessment, based on a complete medical history including a physical examination, vital signs (BP - Blood Pressure, PR - Puls Rate), 12-lead ECG (Electrocardiogram), and clinical laboratory tests * Age of 18 to 45 years (incl.) * BMI (Body Mass Index) of 18.5 to 29.9 kg/m2 (incl.) * Signed and dated written informed consent prior to admission to the study in accordance with GCP and local legislation
Exclusion criteria
* Any finding in the medical examination (including BP - Blood Pressure, PR - Pulse Rate or ECG - Electrocardiogram) is deviating from normal and judged as clinically relevant by the investigator * Repeated measurement of systolic blood pressure outside the range of 90 to 140 mmHg, diastolic blood pressure outside the range of 50 to 90 mmHg, or pulse rate outside the range of 45 to 90 bpm * Any laboratory value outside the reference range that the investigator considers to be of clinical relevance * Any evidence of a concomitant disease judged as clinically relevant by the investigator * Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders * Cholecystectomy and/or surgery of the gastrointestinal tract (except appendectomy and simple hernia repair) * Diseases of the central nervous system (including but not limited to any kind of seizures or stroke), and other relevant neurological or psychiatric disorders * Further
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Percentage of Subjects With Drug Related Adverse Events | Adverse events reported until the end-of-trial examination; up to day 74 | Percentage of subjects with drug related adverse events are presented. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Maximum Measured Concentration of BI 655130 in Plasma (Cmax) | -2 hours (h) before and 0.5h, 1h, 2h, 3h, 4h, 8h, 12h, 24h, 48h, 72h, 96h, 168h, 336h, 504h, 672h, 840h, 1008h, 1344h, 1680h after drug administration | Maximum measured concentration of BI 655130 in plasma (Cmax) is presented. |
| Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) | -2 hours (h) before and 0.5h, 1h, 2h, 3h, 4h, 8h, 12h, 24h, 48h, 72h, 96h, 168h, 336h, 504h, 672h, 840h, 1008h, 1344h, 1680h after drug administration | Area under the concentration-time curve of the BI 655130 in plasma over the time interval from 0 extrapolated to infinity (AUC0-∞) is presented. Reliable values of AUC0-∞ could not be calculated because concentrations were too high at the last PK sample collected 1680h after drug administration. AUC0-tz was utilized for the dose proportionality analyses instead of AUC0-∞. |
| Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 to the Last Measurable Plasma Concentration (AUC0-tz) | -2 hours (h) before and 0.5h, 1h, 2h, 3h, 4h, 8h, 12h, 24h, 48h, 72h, 96h, 168h, 336h, 504h, 672h, 840h, 1008h, 1344h, 1680h after drug administration | Area under the concentration-time curve of the BI 655130 in plasma over the time interval from 0 to the last measurable plasma concentration (AUC0-tz) is presented. |
Countries
Belgium
Participant flow
Recruitment details
A total of 78 subjects were randomised to 11 sequential dose groups (including an unplanned dose group). All subjects completed the trial according to the protocol. 3 subjects were not dosed as planned: they received 0.050 mg/kg BI 655130 instead of the planned 0.100 mg/kg BI 655130.
Pre-assignment details
A total of 80 subjects were planned to be included in 10 sequential dose groups, each consisting of 8 subjects (6 on BI 655130 and 2 on placebo). However, 1 additional dose group was introduced to accommodate for a dosing error administration of 0.050 mg/kg instead of 0.100 mg/kg;
Participants by arm
| Arm | Count |
|---|---|
| 0.001 mg/kg BI 655130 (Dose Group 1) Male healthy volunteers received single dose of 0.001 milligrams/kilograms (mg/kg) BI 655130 as concentrate for solution for Intravenous (IV) 30 min infusion | 6 |
| 0.003 mg/kg BI 655130 (Dose Group 2) Male healthy volunteers received single dose of 0.003 mg/kg BI 655130 as concentrate for solution for IV 30 min infusion | 6 |
| 0.010 mg/kg BI 655130 (Dose Group 3) Male healthy volunteers received single dose of 0.010 mg/kg BI 655130 as concentrate for solution for IV 30 min infusion | 6 |
| 0.030 mg/kg BI 655130 (Dose Group 4) Male healthy volunteers received single dose of 0.030 mg/kg BI 655130 as concentrate for solution for IV 30 min infusion | 6 |
| 0.100 mg/kg BI 655130 (Dose Group 5) Male healthy volunteers received single dose of 0.100 mg/kg BI 655130 as concentrate for solution for IV 30 min infusion | 5 |
| 0.300 mg/kg BI 655130 (Dose Group 6) Male healthy volunteers received single dose of0.300 mg/kg BI 655130 as concentrate for solution for IV 30 min infusion | 4 |
| 1 mg/kg BI 655130 (Dose Group 7) Male healthy volunteers received single dose of 1 mg/kg BI 655130 as concentrate for solution for IV 30 min infusion | 6 |
| 3 mg/kg BI 655130 (Dose Group 8) Male healthy volunteers received single dose of 3 mg/kg BI 655130 as concentrate for solution for IV 30 min infusion | 6 |
| 6 mg/kg BI 655130 (Dose Group 9) Male healthy volunteers received single dose of 6 mg/kg BI 655130 as concentrate for solution for IV 30 min infusion | 6 |
| 10 mg/kg BI 655130 (Dose Group 10) Male healthy volunteers received single dose of 10 mg/kg BI 655130 as concentrate for solution for IV 30 min infusion | 4 |
| 0.050 mg/kg BI 655130 (Unplanned) Male healthy volunteers received single dose of 0.050 mg/kg BI 655130 as concentrate for solution for IV 30 min infusion (unit strength: 20 milligrams/milliLitres (mg/mL). This separate group (unplanned) was introduced to accommodate subjects who had been wrongly administered 0.050 mg/kg BI 655130 instead of the planned 0.100 mg/kg BI 655130 | 3 |
| Placebo Male healthy volunteers received single dose of matching placebo as concentrate for solution for IV 30 min infusion. | 20 |
| Total | 78 |
Baseline characteristics
| Characteristic | 0.050 mg/kg BI 655130 (Unplanned) | Total | Placebo | 0.001 mg/kg BI 655130 (Dose Group 1) | 0.003 mg/kg BI 655130 (Dose Group 2) | 0.010 mg/kg BI 655130 (Dose Group 3) | 0.030 mg/kg BI 655130 (Dose Group 4) | 0.100 mg/kg BI 655130 (Dose Group 5) | 0.300 mg/kg BI 655130 (Dose Group 6) | 1 mg/kg BI 655130 (Dose Group 7) | 3 mg/kg BI 655130 (Dose Group 8) | 6 mg/kg BI 655130 (Dose Group 9) | 10 mg/kg BI 655130 (Dose Group 10) |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Age, Continuous | 31.0 years STANDARD_DEVIATION 7 | 33.1 years STANDARD_DEVIATION 7.7 | 34.2 years STANDARD_DEVIATION 8.5 | 25.5 years STANDARD_DEVIATION 5 | 33.2 years STANDARD_DEVIATION 8.1 | 33.2 years STANDARD_DEVIATION 8.7 | 31.2 years STANDARD_DEVIATION 8 | 40.0 years STANDARD_DEVIATION 2.5 | 33.5 years STANDARD_DEVIATION 2.6 | 32.5 years STANDARD_DEVIATION 7.7 | 34.2 years STANDARD_DEVIATION 6.5 | 36.0 years STANDARD_DEVIATION 9.9 | 29.8 years STANDARD_DEVIATION 5.6 |
| Ethnicity (NIH/OMB) Hispanic or Latino | 0 Participants | 1 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 1 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Ethnicity (NIH/OMB) Not Hispanic or Latino | 3 Participants | 77 Participants | 20 Participants | 6 Participants | 6 Participants | 6 Participants | 6 Participants | 4 Participants | 4 Participants | 6 Participants | 6 Participants | 6 Participants | 4 Participants |
| Ethnicity (NIH/OMB) Unknown or Not Reported | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) American Indian or Alaska Native | 0 Participants | 1 Participants | 1 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Asian | 0 Participants | 1 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 1 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Black or African American | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) More than one race | 0 Participants | 0 Participants | 00 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Native Hawaiian or Other Pacific Islander | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Unknown or Not Reported | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) White | 3 Participants | 76 Participants | 19 Participants | 6 Participants | 6 Participants | 6 Participants | 6 Participants | 5 Participants | 4 Participants | 6 Participants | 5 Participants | 6 Participants | 4 Participants |
| 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 | 0 Participants | 0 Participants |
| Sex: Female, Male Male | 3 Participants | 78 Participants | 20 Participants | 6 Participants | 6 Participants | 6 Participants | 6 Participants | 5 Participants | 4 Participants | 6 Participants | 6 Participants | 6 Participants | 4 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk | EG002 affected / at risk | EG003 affected / at risk | EG004 affected / at risk | EG005 affected / at risk | EG006 affected / at risk | EG007 affected / at risk | EG008 affected / at risk | EG009 affected / at risk | EG010 affected / at risk | EG011 affected / at risk |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| deaths Total, all-cause mortality | — / — | — / — | — / — | — / — | — / — | — / — | — / — | — / — | — / — | — / — | — / — | — / — |
| other Total, other adverse events | 11 / 20 | 2 / 6 | 4 / 6 | 5 / 6 | 5 / 6 | 4 / 5 | 2 / 4 | 5 / 6 | 3 / 6 | 3 / 6 | 1 / 4 | 2 / 3 |
| serious Total, serious adverse events | 0 / 20 | 0 / 6 | 0 / 6 | 0 / 6 | 0 / 6 | 0 / 5 | 0 / 4 | 0 / 6 | 0 / 6 | 0 / 6 | 0 / 4 | 0 / 3 |
Outcome results
Primary
Percentage of Subjects With Drug Related Adverse Events
Percentage of subjects with drug related adverse events are presented.
Time frame: Adverse events reported until the end-of-trial examination; up to day 74
Population: Treated set
| Arm | Measure | Value (NUMBER) |
|---|---|---|
| 0.001 mg/kg BI 655130 (Dose Group 1) | Percentage of Subjects With Drug Related Adverse Events | 16.7 percentage of participants |
| 0.003 mg/kg BI 655130 (Dose Group 2) | Percentage of Subjects With Drug Related Adverse Events | 16.7 percentage of participants |
| 0.010 mg/kg BI 655130 (Dose Group 3) | Percentage of Subjects With Drug Related Adverse Events | 33.3 percentage of participants |
| 0.030 mg/kg BI 655130 (Dose Group 4) | Percentage of Subjects With Drug Related Adverse Events | 0.0 percentage of participants |
| 0.100 mg/kg BI 655130 (Dose Group 5) | Percentage of Subjects With Drug Related Adverse Events | 0.0 percentage of participants |
| 0.300 mg/kg BI 655130 (Dose Group 6) | Percentage of Subjects With Drug Related Adverse Events | 0.0 percentage of participants |
| 1 mg/kg BI 655130 (Dose Group 7) | Percentage of Subjects With Drug Related Adverse Events | 16.7 percentage of participants |
| 3 mg/kg BI 655130 (Dose Group 8) | Percentage of Subjects With Drug Related Adverse Events | 0.0 percentage of participants |
| 6 mg/kg BI 655130 (Dose Group 9) | Percentage of Subjects With Drug Related Adverse Events | 33.3 percentage of participants |
| 10 mg/kg BI 655130 (Dose Group 10) | Percentage of Subjects With Drug Related Adverse Events | 0.0 percentage of participants |
| 0.050 mg/kg BI 655130 (Unplanned) | Percentage of Subjects With Drug Related Adverse Events | 33.3 percentage of participants |
| Placebo | Percentage of Subjects With Drug Related Adverse Events | 15.0 percentage of participants |
Secondary
Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞)
Area under the concentration-time curve of the BI 655130 in plasma over the time interval from 0 extrapolated to infinity (AUC0-∞) is presented. Reliable values of AUC0-∞ could not be calculated because concentrations were too high at the last PK sample collected 1680h after drug administration. AUC0-tz was utilized for the dose proportionality analyses instead of AUC0-∞.
Time frame: -2 hours (h) before and 0.5h, 1h, 2h, 3h, 4h, 8h, 12h, 24h, 48h, 72h, 96h, 168h, 336h, 504h, 672h, 840h, 1008h, 1344h, 1680h after drug administration
Population: Descriptive pharmacokinetic analysis set (PKSD): The descriptive analysis of PK (pharmacokinetic) concentrations and parameters was based on all treated subjects who provided at least 1 PK concentration (plasma or urine) that was judged as PK evaluable and not affected by protocol violations relevant to the evaluation of PK parameters.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 0.001 mg/kg BI 655130 (Dose Group 1) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) | NA micrograms*day/milliLitres (μg*day/mL) | — |
| 0.003 mg/kg BI 655130 (Dose Group 2) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) | NA micrograms*day/milliLitres (μg*day/mL) | — |
| 0.010 mg/kg BI 655130 (Dose Group 3) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) | 0.0234 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 125 |
| 0.030 mg/kg BI 655130 (Dose Group 4) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) | 2.35 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 23.9 |
| 0.100 mg/kg BI 655130 (Dose Group 5) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) | 27.7 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 16.6 |
| 0.300 mg/kg BI 655130 (Dose Group 6) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) | 127 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 6.05 |
| 1 mg/kg BI 655130 (Dose Group 7) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) | 563 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 26.2 |
| 3 mg/kg BI 655130 (Dose Group 8) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) | 1260 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 6.81 |
| 6 mg/kg BI 655130 (Dose Group 9) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) | 3380 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 15.6 |
| 10 mg/kg BI 655130 (Dose Group 10) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) | 5080 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 18.9 |
| 0.050 mg/kg BI 655130 (Unplanned) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) | 13.0 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 6.59 |
Secondary
Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 to the Last Measurable Plasma Concentration (AUC0-tz)
Area under the concentration-time curve of the BI 655130 in plasma over the time interval from 0 to the last measurable plasma concentration (AUC0-tz) is presented.
Time frame: -2 hours (h) before and 0.5h, 1h, 2h, 3h, 4h, 8h, 12h, 24h, 48h, 72h, 96h, 168h, 336h, 504h, 672h, 840h, 1008h, 1344h, 1680h after drug administration
Population: Descriptive pharmacokinetic analysis set (PKSD): The descriptive analysis of PK (pharmacokinetic) concentrations and parameters was based on all treated subjects who provided at least 1 PK concentration (plasma or urine) that was judged as PK evaluable and not affected by protocol violations relevant to the evaluation of PK parameters.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 0.001 mg/kg BI 655130 (Dose Group 1) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 to the Last Measurable Plasma Concentration (AUC0-tz) | NA micrograms*day/milliLitres (μg*day/mL) | — |
| 0.003 mg/kg BI 655130 (Dose Group 2) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 to the Last Measurable Plasma Concentration (AUC0-tz) | NA micrograms*day/milliLitres (μg*day/mL) | — |
| 0.010 mg/kg BI 655130 (Dose Group 3) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 to the Last Measurable Plasma Concentration (AUC0-tz) | 0.00652 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 121 |
| 0.030 mg/kg BI 655130 (Dose Group 4) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 to the Last Measurable Plasma Concentration (AUC0-tz) | 2.08 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 29 |
| 0.100 mg/kg BI 655130 (Dose Group 5) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 to the Last Measurable Plasma Concentration (AUC0-tz) | 25.1 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 15.5 |
| 0.300 mg/kg BI 655130 (Dose Group 6) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 to the Last Measurable Plasma Concentration (AUC0-tz) | 113 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 5.86 |
| 1 mg/kg BI 655130 (Dose Group 7) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 to the Last Measurable Plasma Concentration (AUC0-tz) | 420 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 13.3 |
| 3 mg/kg BI 655130 (Dose Group 8) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 to the Last Measurable Plasma Concentration (AUC0-tz) | 1050 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 7.26 |
| 6 mg/kg BI 655130 (Dose Group 9) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 to the Last Measurable Plasma Concentration (AUC0-tz) | 2610 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 11.7 |
| 10 mg/kg BI 655130 (Dose Group 10) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 to the Last Measurable Plasma Concentration (AUC0-tz) | 4130 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 12.1 |
| 0.050 mg/kg BI 655130 (Unplanned) | Area Under the Concentration-time Curve of the BI 655130 in Plasma Over the Time Interval From 0 to the Last Measurable Plasma Concentration (AUC0-tz) | 9.57 micrograms*day/milliLitres (μg*day/mL) | Geometric Coefficient of Variation 5.9 |
Comparison: Dose proportionality in plasma for AUC(0-tz) (log-transformed scale) was explored based on the linear regression model.95% CI: [2.1856, 3.2389]
Comparison: Dose proportionality in plasma for AUC(0-tz) (log-transformed scale) was explored based on the linear regression model.95% CI: [0.9482, 1.0525]
Secondary
Maximum Measured Concentration of BI 655130 in Plasma (Cmax)
Maximum measured concentration of BI 655130 in plasma (Cmax) is presented.
Time frame: -2 hours (h) before and 0.5h, 1h, 2h, 3h, 4h, 8h, 12h, 24h, 48h, 72h, 96h, 168h, 336h, 504h, 672h, 840h, 1008h, 1344h, 1680h after drug administration
Population: Descriptive pharmacokinetic analysis set (PKSD): The descriptive analysis of PK (pharmacokinetic) concentrations and parameters was based on all treated subjects who provided at least 1 PK concentration (plasma or urine) that was judged as PK evaluable and not affected by protocol violations relevant to the evaluation of PK parameters.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 0.001 mg/kg BI 655130 (Dose Group 1) | Maximum Measured Concentration of BI 655130 in Plasma (Cmax) | NA micrograms/milliLitres (μg/mL) | — |
| 0.003 mg/kg BI 655130 (Dose Group 2) | Maximum Measured Concentration of BI 655130 in Plasma (Cmax) | NA micrograms/milliLitres (μg/mL) | — |
| 0.010 mg/kg BI 655130 (Dose Group 3) | Maximum Measured Concentration of BI 655130 in Plasma (Cmax) | 0.0228 micrograms/milliLitres (μg/mL) | Geometric Coefficient of Variation 33.5 |
| 0.030 mg/kg BI 655130 (Dose Group 4) | Maximum Measured Concentration of BI 655130 in Plasma (Cmax) | 0.413 micrograms/milliLitres (μg/mL) | Geometric Coefficient of Variation 21.2 |
| 0.100 mg/kg BI 655130 (Dose Group 5) | Maximum Measured Concentration of BI 655130 in Plasma (Cmax) | 1.96 micrograms/milliLitres (μg/mL) | Geometric Coefficient of Variation 11.9 |
| 0.300 mg/kg BI 655130 (Dose Group 6) | Maximum Measured Concentration of BI 655130 in Plasma (Cmax) | 6.63 micrograms/milliLitres (μg/mL) | Geometric Coefficient of Variation 3.28 |
| 1 mg/kg BI 655130 (Dose Group 7) | Maximum Measured Concentration of BI 655130 in Plasma (Cmax) | 20.3 micrograms/milliLitres (μg/mL) | Geometric Coefficient of Variation 13.6 |
| 3 mg/kg BI 655130 (Dose Group 8) | Maximum Measured Concentration of BI 655130 in Plasma (Cmax) | 60.6 micrograms/milliLitres (μg/mL) | Geometric Coefficient of Variation 7.17 |
| 6 mg/kg BI 655130 (Dose Group 9) | Maximum Measured Concentration of BI 655130 in Plasma (Cmax) | 153 micrograms/milliLitres (μg/mL) | Geometric Coefficient of Variation 12.7 |
| 10 mg/kg BI 655130 (Dose Group 10) | Maximum Measured Concentration of BI 655130 in Plasma (Cmax) | 235 micrograms/milliLitres (μg/mL) | Geometric Coefficient of Variation 2.79 |
| 0.050 mg/kg BI 655130 (Unplanned) | Maximum Measured Concentration of BI 655130 in Plasma (Cmax) | 0.998 micrograms/milliLitres (μg/mL) | Geometric Coefficient of Variation 15.7 |
Comparison: Dose proportionality in plasma for Cmax (log-transformed scale) was explored based on the linear regression model.95% CI: [1.3784, 1.8151]
Comparison: Dose proportionality in plasma for Cmax (log-transformed scale) was explored based on the linear regression model.95% CI: [0.9668, 1.0747]