check_circleStudy 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

  • - 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


  • - 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
6
Trial Dates
April 2014 - February 2015
Phase
Phase 1
Could I Receive a placebo
No
Products
Verquvo (Vericiguat, BAY1021189)
Accepts Healthy Volunteer
Yes

Where to participate

StatusInstitutionLocation
Completed
GRONINGEN, 9728 NZ, Netherlands

Primary Outcome

  • Area Under the Concentration Versus Time Curve From Zero to Infinity in Plasma (AUC) of Vericiguat
    date_rangeTime Frame:
    0 hour (h) Pre-dose to 336 h post-dose
  • Maximum Observed Drug Concentration in Plasma (Cmax) of Vericiguat
    date_rangeTime 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
    date_rangeTime 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
    date_rangeTime 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
    date_rangeTime 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
    date_rangeTime Frame:
    0 h Pre-dose to 336 h post-dose
  • Maximum Observed Drug Concentration (Cmax) of Radioactivity in Whole Blood and Plasma
    date_rangeTime 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
    date_rangeTime 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
    date_rangeTime Frame:
    0 h Pre-dose to 336 h post-dose
  • Metabolite Profile in Plasma
    date_rangeTime Frame:
    0 h Pre-dose to 336 h post-dose
  • Metabolite Profile in Urine
    date_rangeTime Frame:
    0 h Pre-dose to 336 h post-dose
  • Metabolite Profile in Feces
    date_rangeTime Frame:
    0 h Pre-dose to 336 h post-dose
  • Cumulative Percentage of Amount of Radioactivity and Metabolites Excreted in Urine (%AE,ur)
    date_rangeTime Frame:
    0 h Pre-dose to 288h post-dose
  • Cumulative Percentage of Amount of Radioactivity and Metabolites Excreted in Feces (%AE,fec)
    date_rangeTime 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)
    date_rangeTime Frame:
    0 h Pre-dose to 336 h post-dose
  • Maximum Observed Drug Concentration in Plasma (Cmax) of Vericiguat Metabolite (M-1)
    date_rangeTime 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
1