check_circleStudy Completed

Clinical pharmacology

Bayer Identifier:

15000

ClinicalTrials.gov Identifier:

NCT04364464

EudraCT Number:

2009-017685-23

EU CT Number:

Not Available
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

Trial purpose

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

Key Participants Requirements

Sex

All

Age

18 - 79 Years
  • Inclusion criteria for all subjects:
    - 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

    Inclusion criteria for subjects with renal failure:
    - 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

    Inclusion criteria for healthy subjects:
    - Mean age and body weight not allowed to vary by more than +/- 10 years and +/- 10 kg from the subjects with renal impairment, respectively

    Exclusion criteria for all subjects:
    - Febrile illness within 1 week before the start of the study
    - Hypersensitivity to riociguat and / or to inactive constituents
    - Smoking

    Exclusion criteria for subjects with renal failure:
    - 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


    Exclusion criteria for healthy subjects:
    - Conspicuous findings in medical history or pre-study examination
    - History of relevant diseases of vital organs, central nervous system, or other organs
    - SBP below 100 mmHg or above 145 mmHg and / or DBP above 95 mmHg
    - Regular daily consumption of more than 1 liter of usual beer or the equivalent quantity of approximately 40 g of alcohol in another form

Trial summary

Enrollment Goal
40
Trial Dates
February 2010 - September 2011
Phase
Phase 1
Could I Receive a placebo
No
Products
Adempas (Riociguat, BAY63-2521)
Accepts Healthy Volunteer
Yes

Where to participate

StatusInstitutionLocation
Completed
Kiel, 24105, Germany

Primary Outcome

  • 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)
    date_rangeTime Frame:
    Pre-dose up to 72 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • Cmax
    Maximum total (bound and unbound) drug concentration in plasma after single dose administration for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    Pre-dose up to 72 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • t½
    Half-life associated with the terminal slope for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    Pre-dose up to 72 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • fu
    Fraction unbound for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    From 2 hours post-dose up to 24 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • AUCu
    AUC for unbound drug for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    From 2 hours post-dose up to 24 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • Cmax,u
    Cmax for unbound drug for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    From 2 hours post-dose up to 24 hours post-dose
    enhanced_encryption
    Safety Issue:
    No

Secondary Outcome

  • AUC/D
    AUC divided by dose for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    Pre-dose up to 72 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • AUCnorm
    AUC divided by dose per kg body weight for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    Pre-dose up to 72 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • AUCu,norm
    AUCnorm for unbound drug for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    From 2 hours post-dose up to 24 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • AUC(0-tlast)
    AUC from time 0 to the last data point for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    Pre-dose up to 72 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • Cmax/D
    Cmax divided by dose for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    Pre-dose up to 72 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • Cmax,norm
    Cmax divided by dose per kg body weight for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    Pre-dose up to 72 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • Cmax,u,norm
    Cmax,norm for unbound drug for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    From 2 hours post-dose up to 24 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • tmax
    Time to reach Cmax (in case of two identical Cmax values, the first tmax was used) for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    Pre-dose up to 72 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • MRT
    Mean residence time for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    Pre-dose up to 72 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • CL/F
    Total body clearance of drug calculated after extravascular administration (eg apparent oral clearance) for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    Pre-dose up to 72 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • CLu/F
    CL/F for unbound drug for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    From 2 hours post-dose up to 24 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • Vz/F
    Apparent volume of distribution during terminal phase after extravascular administration for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    Pre-dose up to 72 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • AE,ur
    Amount of (total) drug excreted in urine for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    From 24 hours prior to drug administration up to 72 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • CLR
    Renal body clearance of drug for BAY 63-2521 and its metabolite M1
    date_rangeTime Frame:
    From 24 hours prior to drug administration up to 72 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • Number of participants with adverse events
    date_rangeTime Frame:
    Approximately 5 weeks
    enhanced_encryption
    Safety Issue:
    Yes

Trial design

Investigation of pharmacokinetics, safety, and tolerability of BAY 63-2521 in male and female subjects with renal impairment and in age- and weight- matched healthy subjects following a single oral dose of 1 mg BAY 63-2521 in a single-center, non-randomized, non-controlled, non-blinded, observational study with group stratification
Trial Type
Interventional
Intervention Type
Drug
Trial Purpose
Basic Science
Allocation
Non-randomized
Blinding
Open Label
Assignment
Parallel Assignment
Trial Arms
4

Additional Information

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