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| ID | Type | Description | Link |
|---|---|---|---|
| 2018-001814-13 | EudraCT Number |
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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.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Group 1 - BAY1817080 Dose 1 | Experimental | Participants will receive one single oral dose of BAY1817080 - Formulation B at dose 1 under fasted condition |
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| Group 2 - BAY1817080 Dose 2 | Experimental | Participants will receive a) one single oral dose of BAY1817080 - Formulation A at dose 2 with moderate-fat, moderate-calorie meal (MF, MC); b) one single oral dose of BAY1817080 - Formulation B at dose 2 along with one intravenous (i.v.) infusion of 0.1 mg [13C715N]-BAY1817080; and c) one single oral dose of BAY1817080 - Formulation B at dose 2 with high-fat, high-calorie meal (HF, HC). The 3 treatments will be administered with a randomized sequence |
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| Group 3 - BAY1817080 Dose 3 | Experimental | Participants will receive a) one single oral dose of BAY1817080 - Formulation B at dose 3 under fasted condition; followed by one single oral dose of BAY1817080 - Formulation A at dose 3 with MF, MC; and followed by one single oral dose of BAY1817080 - Formulation B at dose 3 with HF, HC. The 3 treatments will be administered with a fixed sequence |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| BAY1817080 - Formulation A | Drug | Formulation A |
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| Measure | Description | 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 |
| Measure | Description | Time Frame |
|---|---|---|
| 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 | Maximum observed drug concentration in plasma after single dose administration (Cmax) of BAY1817080 will be analyzed assuming log-normally distributed data. | Up to 10 days |
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Inclusion criteria:
Exclusion criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| PRAHealthSciences | Groningen | 9728 NZ | Netherlands |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 36469250 | Derived | Francke K, Chattopadhyay N, Klein S, Rottmann A, Krickau D, van de Wetering J, Friedrich C. Preclinical and Clinical Pharmacokinetics and Bioavailability in Healthy Volunteers of a Novel Formulation of the Selective P2X3 Receptor Antagonist Eliapixant. Eur J Drug Metab Pharmacokinet. 2023 Jan;48(1):75-87. doi: 10.1007/s13318-022-00805-5. Epub 2022 Dec 5. |
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| BAY1817080 - Formulation B | Drug | Formulation B |
|
| [13C715N]-BAY 181708 stable isotope label (SIL) | Drug | 0.1 mg [13C715N]-BAY181708, 15 minutes i.v. infusion at the estimated tmax after administration of Formulation B |
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| 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 | 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. | Up to 10 days |
| Dose proportionality in BAY1817080 PK after a single oral dose of Formulation B across three doses in fasted state evaluated by Cmax/D | 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. | Up to 10 days |
| Dose proportionality in BAY1817080 PK after a single oral dose of Formulation B across three doses in fasted state evaluated by AUC/D | 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. | Up to 10 days |
| Frequency and severity of treatment emergent adverse events (TEAEs) | Up to 42 days |
| ID | Term |
|---|---|
| D004715 | Endometriosis |
| D000096822 | Chronic Cough |
| ID | Term |
|---|---|
| D005831 | Genital Diseases, Female |
| D052776 | Female Urogenital Diseases |
| D005261 | Female Urogenital Diseases and Pregnancy Complications |
| D000091642 | Urogenital Diseases |
| D000091662 | Genital Diseases |
| D003371 | Cough |
| D012120 | Respiration Disorders |
| D012140 | Respiratory Tract Diseases |
| D012818 | Signs and Symptoms, Respiratory |
| D012816 | Signs and Symptoms |
| D013568 | Pathological Conditions, Signs and Symptoms |
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