A Study in Healthy Volunteers Investigating How Quickly and to What Extent BAY1817080 is Taken up, Distributed, Broken Down and Eliminated From the Body, as Well as the Difference Between 2 Different Types of Tablets of BAY1817080 and the Difference Between Oral Dose and Dose in the Vein

NCT03773068 | Completed Phase 1 FDA Drug

• 2 other identifiers: 195192018-001814-13
• Study Type: interventional
• Target: 30
• Locations: 1 country
• Sites: 1

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.

Conditions

Biological Availability

Keywords

Endometriosis; Refractory chronic cough

Outcome Measures

Primary Outcomes (2)

• 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 Outcomes (5)

• 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

• 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

• 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

• 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

• Frequency and severity of treatment emergent adverse events (TEAEs)

  Up to 42 days

Study Arms (3)

Group 1 - BAY1817080 Dose 1

EXPERIMENTAL

Participants will receive one single oral dose of BAY1817080 - Formulation B at dose 1 under fasted condition

Drug: BAY1817080 - Formulation B

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

Drug: BAY1817080 - Formulation A; Drug: BAY1817080 - Formulation B; Drug: [13C715N]-BAY 181708 stable isotope label (SIL)

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

Drug: BAY1817080 - Formulation A; Drug: BAY1817080 - Formulation B

Interventions

BAY1817080 - Formulation A DRUG

Formulation A

Group 2 - BAY1817080 Dose 2; Group 3 - BAY1817080 Dose 3

BAY1817080 - Formulation B DRUG

Formulation B

Group 1 - BAY1817080 Dose 1; Group 2 - BAY1817080 Dose 2; Group 3 - BAY1817080 Dose 3

[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

Group 2 - BAY1817080 Dose 2

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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

Sponsors & Collaborators

• Bayer: lead

Study Sites (1)

PRAHealthSciences

Groningen, 9728 NZ, Netherlands

Location

Related Publications (1)

• 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.

  PMID: 36469250 DERIVED

MeSH Terms

Conditions

Endometriosis; Chronic Cough

Condition Hierarchy (Ancestors)

Genital Diseases, Female; Female Urogenital Diseases; Female Urogenital Diseases and Pregnancy Complications; Urogenital Diseases; Genital Diseases; Cough; Respiration Disorders; Respiratory Tract Diseases; Signs and Symptoms, Respiratory; Signs and Symptoms; Pathological Conditions, Signs and Symptoms

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: December 4, 2018
• First Posted: December 12, 2018
• Study Start: December 13, 2018
• Primary Completion: June 21, 2019
• Study Completion: August 12, 2019
• Last Updated: August 19, 2019

Record last verified: 2019-08

Locations

NL (1)