Safety, Tolerability, and Pharmacokinetics of Single Rising Oral Doses of BI 425809 in Healthy Male Subjects (Partially Randomised, Single-blind, Placebo-controlled) and Investigation of Relative Bioavailability and Food Effect of BI 425809 (Open-label, Randomised, Three-way Crossover)
Trial Snapshot
- Phase
- Phase 1
- Status
- Completed
- Sponsor
- Boehringer Ingelheim
- Enrollment
- 83
- Locations
- 1
- Primary Endpoint
- frequency [N(%)] of subjects with drug related adverse events (AEs)
Study Overview
Brief Summary
To investigate safety, tolerability, and pharmacokinetics of BI 425809 following single rising doses of BI 425809 in healthy male volunteers; To explore dose proportionality of BI 425809 as oral drinking solution; To investigate relative bioavailability of BI 425809 oral drinking solution fasted compared to BI 425809 tablet fasted and tablet fed
Study Design
- Study Type
- Interventional
- Allocation
- Randomized
- Intervention Model
- Crossover
- Primary Purpose
- Treatment
- Masking
- None
Masking Description
In Part 1 of this study, single-blind conditions regarding the subjects' treatment were maintained within each dose group, but the current dose level was known to subjects and investigators. Part 2 of this study did not have masking and treatments were open-label.
Eligibility Criteria
- Ages
- 18 Years to 45 Years (Adult)
- Sex
- Male
- Accepts Healthy Volunteers
- Yes
Inclusion Criteria
- •Healthy male subjects
- •Age 18 to 45 years (incl.)
- •Body mass index (BMI) 18.5 to 29.9 kg/m2 (incl.)
- •Subject must be able to understand and comply with study requirements
Exclusion Criteria
- •Any finding in the medical examination (including blood pressure (BP), pulse rate (PR) or electrocardiogram (ECG)) deviating from normal and judged clinically relevant by the investigator
- •Repeated measurement of systolic blood pressure <90 or >140 mmHg, or diastolic blood pressure <50 or >90 mmHg, or pulse rate <50 or >90
- •Any laboratory value outside the reference range that the investigator considers to be of clinical relevance
- •Any evidence of a concomitant disease judged clinically relevant by the investigator
- •Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
- •Surgery of the gastrointestinal tract that could interfere with kinetics of the study drug(s)
- •Diseases of the central nervous system (such as epilepsy), other neurological disorders or psychiatric disorders
Arms & Interventions
SRD Part: 0.5 mg BI 425809
Participants received a single dose of oral solution containing 0.5 milligrams (mg) of BI 425809. SRD = Single Rising Dose.
Intervention: BI 425809 PfOS (Drug)
SRD Part: 1 mg BI 425809
Participants received a single dose of oral solution containing 1 milligram (mg) of BI 425809. SRD = Single Rising Dose.
Intervention: BI 425809 PfOS (Drug)
SRD Part: Placebo
Participants received a single dose of oral solution of placebo matching BI 425809. SRD = Single Rising Dose.
Intervention: Placebo PfOS (Drug)
SRD Part: 2 mg BI 425809
Participants received a single dose of oral solution containing 2 milligrams (mg) of BI 425809. SRD = Single Rising Dose.
Intervention: BI 425809 PfOS (Drug)
SRD Part: 5 mg BI 425809
Participants received a single dose of oral solution containing 5 milligrams (mg) of BI 425809. SRD = Single Rising Dose.
Intervention: BI 425809 PfOS (Drug)
SRD Part: 10 mg BI425809
Participants received a single dose of oral solution containing 10 milligrams (mg) of BI 425809. SRD = Single Rising Dose.
Intervention: BI 425809 PfOS (Drug)
SRD Part: 25 mg BI 425809
Participants received a single dose of oral solution containing 25 milligrams (mg) of BI 425809. SRD = Single Rising Dose.
Intervention: BI 425809 PfOS (Drug)
SRD Part: 50 mg BI 425809
Participants received a single dose of oral solution containing 50 milligrams (mg) of BI 425809. SRD = Single Rising Dose.
Intervention: BI 425809 PfOS (Drug)
SRD Part: 100 mg BI 425809
Participants received a single dose of oral solution containing 100 milligrams (mg) of BI 425809. SRD = Single Rising Dose.
Intervention: BI 425809 PfOS (Drug)
SRD Part: 150 mg BI 425809
Participants received a single dose of oral solution containing 150 milligrams (mg) of BI 425809. SRD = Single Rising Dose.
Intervention: BI 425809 PfOS (Drug)
BA/FE Part: 25 mg BI 425809, R/T1/T2
Participants were administered 25 mg of BI 425809 as a tablet without food (reference treatment R), 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1), and 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.
Intervention: BI 425809 PfOS (Drug)
BA/FE Part: 25 mg BI 425809, R/T1/T2
Participants were administered 25 mg of BI 425809 as a tablet without food (reference treatment R), 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1), and 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.
Intervention: BI 425809 tablet (Drug)
BA/FE Part: 25 mg BI 425809, R/T2/T1
Participants were administered 25 mg of BI 425809 as a tablet without food (reference treatment R), 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2), and 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.
Intervention: BI 425809 PfOS (Drug)
BA/FE Part: 25 mg BI 425809, R/T2/T1
Participants were administered 25 mg of BI 425809 as a tablet without food (reference treatment R), 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2), and 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.
Intervention: BI 425809 tablet (Drug)
BA/FE Part: 25 mg BI 425809, T1/T2/R
Participants were administered 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1), 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2), and 25 mg of BI 425809 as a tablet without food (reference treatment R). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.
Intervention: BI 425809 PfOS (Drug)
BA/FE Part: 25 mg BI 425809, T1/T2/R
Participants were administered 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1), 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2), and 25 mg of BI 425809 as a tablet without food (reference treatment R). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.
Intervention: BI 425809 tablet (Drug)
BA/FE Part: 25 mg BI 425809, T1/R/T2
Participants were administered 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1), 25 mg of BI 425809 as a tablet without food (reference treatment R), and 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.
Intervention: BI 425809 PfOS (Drug)
BA/FE Part: 25 mg BI 425809, T1/R/T2
Participants were administered 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1), 25 mg of BI 425809 as a tablet without food (reference treatment R), and 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.
Intervention: BI 425809 tablet (Drug)
BA/FE Part: 25 mg BI 425809, T2/T1/R
Participants were administered 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2), 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1), and 25 mg of BI 425809 as a tablet without food (reference treatment R). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.
Intervention: BI 425809 PfOS (Drug)
BA/FE Part: 25 mg BI 425809, T2/T1/R
Participants were administered 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2), 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1), and 25 mg of BI 425809 as a tablet without food (reference treatment R). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.
Intervention: BI 425809 tablet (Drug)
BA/FE Part: 25 mg BI 425809, T2/R/T1
Participants were administered 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2), 25 mg of BI 425809 as a tablet without food (reference treatment R), and 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.
Intervention: BI 425809 PfOS (Drug)
BA/FE Part: 25 mg BI 425809, T2/R/T1
Participants were administered 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2), 25 mg of BI 425809 as a tablet without food (reference treatment R), and 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.
Intervention: BI 425809 tablet (Drug)
Outcomes
Primary Outcomes
frequency [N(%)] of subjects with drug related adverse events (AEs)
Time Frame: up to 18 days
Secondary Outcomes
- Cmax (maximum measured concentration of the analyte in plasma)(up to 192 hours)
- AUC0-infinity (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)(up to 192 hours)