Study on the Safety of BAY 63-2521, How it is Tolerated and the Way the Body Absorbs, Distributes and Gets Rid of the Study Drug Given as a Single Oral Dose of 1 mg Tablet in Participants With Renal Impairment and Healthy Participants Matched for Age-, Gender-, and Weight

NCT04364464 | Completed Phase 1

• 2 other identifiers: 150002009-017685-23
• Study Type: interventional
• Target: 40
• Locations: 1 country
• Sites: 1

Brief Summary

BAY 63-2521 is intended to be used for a disease that affects the blood flow through the lungs. Renal impairment is a common condition in patients with this disease. The goal of the study is to learn more about the safety of BAY 63-2521, how it is tolerated and the way the body absorbs, distributes and gets rid of the study dug given as a single oral dose of 1 mg tablet in participants with renal impairment and healthy participants matched for age-, gender-, and weight

Conditions

Clinical Pharmacology

Outcome Measures

Primary Outcomes (6)

• AUC

  Area under the plasma concentration vs time curve from zero to infinity for total (bound and unbound) drug after single dose for BAY 63-2521 and its metabolite M1 (BAY 60-4552)

  Pre-dose up to 72 hours post-dose

• Cmax

  Maximum total (bound and unbound) drug concentration in plasma after single dose administration for BAY 63-2521 and its metabolite M1

  Pre-dose up to 72 hours post-dose

• t½

  Half-life associated with the terminal slope for BAY 63-2521 and its metabolite M1

  Pre-dose up to 72 hours post-dose

• fu

  Fraction unbound for BAY 63-2521 and its metabolite M1

  From 2 hours post-dose up to 24 hours post-dose

• AUCu

  AUC for unbound drug for BAY 63-2521 and its metabolite M1

  From 2 hours post-dose up to 24 hours post-dose

• Cmax,u

  Cmax for unbound drug for BAY 63-2521 and its metabolite M1

  From 2 hours post-dose up to 24 hours post-dose

Secondary Outcomes (15)

• AUC/D

  Pre-dose up to 72 hours post-dose

• AUCnorm

  Pre-dose up to 72 hours post-dose

• AUCu,norm

  From 2 hours post-dose up to 24 hours post-dose

• AUC(0-tlast)

  Pre-dose up to 72 hours post-dose

• Cmax/D

  Pre-dose up to 72 hours post-dose

Study Arms (4)

Riociguat, healthy participants

EXPERIMENTAL

Participants with creatinine clearance (CLCR) \>80 mL/min received a single dose of 1 mg (2 x 0.5 mg IR tablet) of riociguat in the fasted state

Drug: Riociguat (Adempas, BAY 63-2521)

Riociguat, mild renal impairment

EXPERIMENTAL

Participants with CLCR 50-80 mL/min received a single dose of 1 mg (2 x 0.5 mg IR tablet) of riociguat in the fasted state

Drug: Riociguat (Adempas, BAY 63-2521)

Riociguat, moderate renal impairment

EXPERIMENTAL

Participants with CLCR 30-\<50 mL/min received a single dose of 1 mg (2 x 0.5 mg IR tablet) of riociguat in the fasted state

Drug: Riociguat (Adempas, BAY 63-2521)

Riociguat, severe renal impairment

EXPERIMENTAL

Participants with CLCR \<30 mL/min received a single dose of 1 mg (2 x 0.5 mg IR tablet) of riociguat in the fasted state

Drug: Riociguat (Adempas, BAY 63-2521)

Interventions

Riociguat (Adempas, BAY 63-2521) DRUG

0.5 mg riociguat as an immediate-release (IR) tablet

Riociguat, healthy participants; Riociguat, mild renal impairment; Riociguat, moderate renal impairment; Riociguat, severe renal impairment

Eligibility Criteria

• Age: 18 Years - 79 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Male and female white subjects with 18 to ≤79 years of age, BMI between 18 and 34 kg/m\^2
• Women without childbearing potential or with childbearing potential but only if the pregnancy test is negative and are under highly effective contraception
• \- Stable renal disease, ie. a serum creatinine value determined at least 3 - 6 months before the pre-study visit was not allowed to vary by more than 20% from the serum creatinine value determined at the pre-study visit
• \- Mean age and body weight not allowed to vary by more than +/- 10 years and +/- 10 kg from the subjects with renal impairment, respectively

You may not qualify if:

• Febrile illness within 1 week before the start of the study
• Hypersensitivity to riociguat and / or to inactive constituents
• Smoking
• Resting heart rate in the awake subject below 45 BPM or above 90 BPM
• Acute renal failure or nephritis
• Any organ transplant
• Diastolic blood pressure (DBP) \>100 mmHg and / or systolic blood pressure (SBP) \>180 mmHg
• Hemoglobin \<8 g/dL, Proteinuria \>8 g/24 hours, Serum albumin \<30 g/L, Platelet count \<100 x 109/L
• History of bleeding within the past 3 months
• Diabetes mellitus with a fasting blood glucose \>220 mg/dL or HbA1c \>10%
• Concomitant use of any medication except medications necessary for the treatment of the kidney disease or related complications
• Concomitant use of phosphodiesterase-5 inhibitors, endothelin receptor antagonists (ERAs, eg bosentan), intravenous or inhalative prostacyclins, or nitrates
• Concomitant use of potent CYP3A4 inhibitors
• Conspicuous findings in medical history or pre-study examination
• History of relevant diseases of vital organs, central nervous system, or other organs

Sponsors & Collaborators

• Bayer: lead

Study Sites (1)

Unknown Facility

Kiel, Schleswig-Holstein, 24105, Germany

Location

Related Links

• Click here to find results for studies related to Bayer products

MeSH Terms

Interventions

riociguat

Study Officials

• Bayer Study Director

  Bayer

  STUDY DIRECTOR

Study Design

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

Study Record Dates

• First Submitted: April 23, 2020
• First Posted: April 28, 2020
• Study Start: February 19, 2010
• Primary Completion: March 17, 2011
• Study Completion: September 20, 2011
• Last Updated: April 28, 2020

Record last verified: 2020-04

Locations

DE (1)