Study Completed

Clinical pharmacology

Bayer Identifier:

15817

ClinicalTrials.gov Identifier:

Not Available

EudraCT Number:

2013-005115-27

EU CT Number:

Not Available

BAY 1021189 Mass Balance Study

Trial purpose

The primary objectives of this study were:
• to measure the cumulative amount as well as the time course of drug-related, radiolabeled material excreted in urine and feces following a single oral dose of 5 mg [14C] vericiguat
• to characterize the metabolic pattern in plasma, urine and feces and to identify metabolites where possible
• to quantify total radioactivity in blood and plasma
• to quantify parent vericiguat and metabolites circulating in plasma (reported separately).

The secondary objective of this study was to assess the safety and tolerability of 5 mg vericiguat administered as an oral solution in healthy subjects.

Key Participants Requirements

Sex

Male

Age

45 - 65 Years

Inclusion Criteria

- Gender: male
- Ethnicity: White
- Age: 45 to 65 years (inclusive) at the first screening examination/visit
- Body mass index (BMI): above/equal 18.0 and below/equal 30.0 kg/m²
Exclusion Criteria
- Incompletely cured pre-existing diseases for which it could have been assumed that the absorption, distribution, metabolism, elimination and effects of the study drugs were not normal
- Known or suspected hypersensitivity to vericiguat or to excipients in the formulation
- Known severe allergies, non-allergic drug reactions or multiple drug allergies
- Relevant diseases within the last 4 weeks prior to the administration of study drug
- Past or present renal impairment, including but not limited to glomerulonephritis, glomerulosclerosis, diabetic nephropathy, as determined by an estimated (MDRD formula) glomerular filtration rate (eGFR) > 90 mL/min/1.73 m2 and urine tests within clinically normal ranges
- Subjects with Gilbert’s syndrome (associated with the UGT1A1 promoter genotype)
- Febrile illness within 1 week before the first study drug administration
- Subjects with a history of malignant disease during the last 5 years
Regular use of nitrates and/or other NO donors and phosphodiesterase-5 inhibitors

Trial summary

Enrollment Goal

Trial Dates

April 2014 - February 2015

Phase

Phase 1

Could I Receive a placebo

Products

Verquvo (Vericiguat, BAY1021189)

Accepts Healthy Volunteer

Yes

Where to participate

Status	Institution	Location
Completed		GRONINGEN, 9728 NZ, Netherlands

Primary Outcome

Area Under the Concentration Versus Time Curve From Zero to Infinity in Plasma (AUC) of Vericiguat
Time Frame:
0 hour (h) Pre-dose to 336 h post-dose
Maximum Observed Drug Concentration in Plasma (Cmax) of Vericiguat
Time Frame:
0 h Pre-dose to 336 h post-dose
Area Under the Concentration Versus Time Curve From Zero to Infinity Divided by Dose per Kilogram Body Weight (AUCnorm) of Vericiguat and its Metabolites
Time Frame:
0 h Pre-dose to 336 h post-dose
Maximum Observed Drug Concentration in Plasma Divided by Dose per Kilogram Body Weight (Cmax,norm) of Vericiguat and its Metabolites
Time Frame:
0 h Pre-dose to 336 h post-dose
Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC) of Radioactivity in Whole Blood and Plasma
Time Frame:
0 h Pre-dose to 336 h post-dose
Area Under the Concentration Versus Time Curve From Zero to Infinity Divided by Dose per Kilogram Body Weight (AUCnorm) of Radioactivity in Whole Blood and Plasma
Time Frame:
0 h Pre-dose to 336 h post-dose
Maximum Observed Drug Concentration (Cmax) of Radioactivity in Whole Blood and Plasma
Time Frame:
0 h Pre-dose to 336 h post-dose
Maximum Observed Radioactivity Concentration Divided by Dose per Kilogram Body Weight (Cmax,norm) of Radioactivity in Whole Blood and Plasma
Time Frame:
0 h Pre-dose to 336 h post-dose
Area Under the Concentration Versus Time Curve From Zero to the Last Data Point (AUC[0-tlast]) of Radioactivity in Whole Blood and Plasma
Time Frame:
0 h Pre-dose to 336 h post-dose
Metabolite Profile in Plasma
Time Frame:
0 h Pre-dose to 336 h post-dose
Metabolite Profile in Urine
Time Frame:
0 h Pre-dose to 336 h post-dose
Metabolite Profile in Feces
Time Frame:
0 h Pre-dose to 336 h post-dose
Cumulative Percentage of Amount of Radioactivity and Metabolites Excreted in Urine (%AE,ur)
Time Frame:
0 h Pre-dose to 288h post-dose
Cumulative Percentage of Amount of Radioactivity and Metabolites Excreted in Feces (%AE,fec)
Time Frame:
0 h Pre-dose to 288h post-dose
Area Under the Concentration Versus Time Curve From Zero to Infinity in Plasma (AUC) of Vericiguat Metabolite (M-1)
Time Frame:
0 h Pre-dose to 336 h post-dose
Maximum Observed Drug Concentration in Plasma (Cmax) of Vericiguat Metabolite (M-1)
Time Frame:
0 h Pre-dose to 336 h post-dose

Trial design

Single center, open-label, non-randomized, non-placebo-controlled study to investigate the pharmacokinetics, metabolic disposition and mass balance after single administration of 5 mg [14C]BAY 1021189 (oral solution) in healthy male subjects

Trial Type

Interventional

Intervention Type

Drug

Trial Purpose

Basic Science

Allocation

N/A

Blinding

Open Label

Assignment

Single Group Assignment

Trial Arms