Biological Availability
Conditions
Keywords
Endometriosis, Refractory chronic cough
Brief summary
The main purpose of this study is to investigate how quickly and to what extent BAY1817080 is absorbed (taken up), distributed, metabolized (broken down) and eliminated from the body (this is called pharmacokinetics). The pharmacokinetics of BAY1817080 administered as tablets will be compared to the pharmacokinetics of BAY1817080 administered as intravenous (iv; in the vein) infusion (this is called absolute bioavailability). Furthermore, 2 different types of tablets with BAY1817080 (Formulation A and Formulation B) will be compared with regard to pharmacokinetics (this is called relative bioavailability). The effect of a meal on the pharmacokinetics of BAY1817080 administered as tablets will be investigated as well. Finally, it will also be investigated how safe BAY1817080 is and how well BAY1817080 is tolerated.
Interventions
DRUGBAY1817080 - Formulation A
Formulation A
DRUGBAY1817080 - Formulation B
Formulation B
DRUG[13C715N]-BAY 181708 stable isotope label (SIL)
0.1 mg \[13C715N\]-BAY181708, 15 minutes i.v. infusion at the estimated tmax after administration of Formulation B
Sponsors
Bayer
Study design
Allocation
RANDOMIZED
Intervention model
PARALLEL
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy male subject * Age: 18 to 55 years (inclusive) at the time of informed consent and first dose of study medication * Body mass index (BMI) above/equal to 18 and below/equal to 30 kg/m\^2 at Screening * Body weight of at least 45 kg at Screening
Exclusion criteria
* Presence or history of clinically relevant cardiovascular, central nervous system (CNS), hepatic, hematopoietic disease, renal dysfunction, metabolic or endocrine dysfunction, serious allergy, asthma hypoxemia, hypertension, seizures, or allergic skin rash * Known hypersensitivity to the study drugs * Known severe allergies or significant non-allergic drug reactions * Febrile illness within 1 week before study drug administration * Current or recent (within 6 months) gastrointestinal disease that would be expected to influence the absorption of drugs * Subject has a history of cancer, except basal cell carcinoma which has been in remission for at least 5 years prior to Screening * Poor peripheral venous access * Regular use of medicines within 6 months prior to screening * Clinically relevant findings in the electrocardiogram (ECG), physical examination or laboratory examination
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Absolute oral bioavailability (F) of BAY1817080 | Up to 10 days |
| Relative bioavailability (frel) of Formulation A versus Formulation B given under different diets | Up to 10 days |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Dose proportionality in BAY1817080 PK after a single oral dose of Formulation B across three doses in fasted state evaluated by Cmax/D | Up to 10 days | To investigate dose-proportionality, Cmax divided by dose (Cmax/D) derived from the 3 oral doses of Formulation B in fasted state will be analyzed. |
| Effect of a high-fat, high-calorie meal (HF,HC) on the PK of BAY1817080 after a single oral dose of Formulation B at two doses in comparison to the fasted state evaluated by Cmax | Up to 10 days | Maximum observed drug concentration in plasma after single dose administration (Cmax) of BAY1817080 will be analyzed assuming log-normally distributed data. |
| Frequency and severity of treatment emergent adverse events (TEAEs) | Up to 42 days | — |
| Dose proportionality in BAY1817080 PK after a single oral dose of Formulation B across three doses in fasted state evaluated by AUC/D | Up to 10 days | To investigate dose-proportionality, AUC divided by dose (AUC/D) derived from the 3 oral doses of Formulation B in fasted state will be analyzed. AUC(0-tlast)/D will be used if AUC/D cannot be calculated reliably in all subjects. |
| Effect of a high-fat, high-calorie meal (HF,HC) on the PK of BAY1817080 after a single oral dose of Formulation B at two doses in comparison to the fasted state evaluated by AUC | Up to 10 days | Area under the concentration versus time curve from zero to infinity after single dose administration (AUC) of BAY1817080 will be analyzed assuming log-normally distributed data. AUC from time 0 to the last data point greater than lower limit of quantification (AUC\[0-tlast\]) will be used if AUC cannot be calculated reliably in all subjects. |
Countries
Netherlands
Outcome results
None listed