- ICH GCP
- US Clinical Trials Registry
- Clinical Trial NCT04364464
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
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
Study Overview
Status
Conditions
Intervention / Treatment
Study Type
Enrollment (Actual)
Phase
- Phase 1
Contacts and Locations
Study Locations
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Schleswig-Holstein
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Kiel, Schleswig-Holstein, Germany, 24105
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-
Participation Criteria
Eligibility Criteria
Ages Eligible for Study
Accepts Healthy Volunteers
Genders Eligible for Study
Description
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
Study Plan
How is the study designed?
Design Details
- Primary Purpose: Basic Science
- Allocation: Non-Randomized
- Interventional Model: Parallel Assignment
- Masking: None (Open Label)
Arms and Interventions
Participant Group / Arm |
Intervention / Treatment |
---|---|
Experimental: Riociguat, healthy participants
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
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0.5 mg riociguat as an immediate-release (IR) tablet
|
Experimental: Riociguat, mild renal impairment
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
|
0.5 mg riociguat as an immediate-release (IR) tablet
|
Experimental: Riociguat, moderate renal impairment
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
|
0.5 mg riociguat as an immediate-release (IR) tablet
|
Experimental: Riociguat, severe renal impairment
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
|
0.5 mg riociguat as an immediate-release (IR) tablet
|
What is the study measuring?
Primary Outcome Measures
Outcome Measure |
Measure Description |
Time Frame |
---|---|---|
fu
Time Frame: From 2 hours post-dose up to 24 hours post-dose
|
Fraction unbound for BAY 63-2521 and its metabolite M1
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From 2 hours post-dose up to 24 hours post-dose
|
AUCu
Time Frame: From 2 hours post-dose up to 24 hours post-dose
|
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
Time Frame: From 2 hours post-dose up to 24 hours post-dose
|
Cmax for unbound drug for BAY 63-2521 and its metabolite M1
|
From 2 hours post-dose up to 24 hours post-dose
|
AUC
Time Frame: Pre-dose up to 72 hours post-dose
|
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
Time Frame: Pre-dose up to 72 hours post-dose
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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
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t½
Time Frame: Pre-dose up to 72 hours post-dose
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Half-life associated with the terminal slope for BAY 63-2521 and its metabolite M1
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Pre-dose up to 72 hours post-dose
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Secondary Outcome Measures
Outcome Measure |
Measure Description |
Time Frame |
---|---|---|
Number of participants with adverse events
Time Frame: Approximately 5 weeks
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Approximately 5 weeks
|
|
AUCu,norm
Time Frame: From 2 hours post-dose up to 24 hours post-dose
|
AUCnorm for unbound drug for BAY 63-2521 and its metabolite M1
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From 2 hours post-dose up to 24 hours post-dose
|
Cmax,u,norm
Time Frame: From 2 hours post-dose up to 24 hours post-dose
|
Cmax,norm for unbound drug for BAY 63-2521 and its metabolite M1
|
From 2 hours post-dose up to 24 hours post-dose
|
CLu/F
Time Frame: From 2 hours post-dose up to 24 hours post-dose
|
CL/F for unbound drug for BAY 63-2521 and its metabolite M1
|
From 2 hours post-dose up to 24 hours post-dose
|
AUC/D
Time Frame: Pre-dose up to 72 hours post-dose
|
AUC divided by dose for BAY 63-2521 and its metabolite M1
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Pre-dose up to 72 hours post-dose
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AUCnorm
Time Frame: Pre-dose up to 72 hours post-dose
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AUC divided by dose per kg body weight for BAY 63-2521 and its metabolite M1
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Pre-dose up to 72 hours post-dose
|
AUC(0-tlast)
Time Frame: Pre-dose up to 72 hours post-dose
|
AUC from time 0 to the last data point for BAY 63-2521 and its metabolite M1
|
Pre-dose up to 72 hours post-dose
|
Cmax/D
Time Frame: Pre-dose up to 72 hours post-dose
|
Cmax divided by dose for BAY 63-2521 and its metabolite M1
|
Pre-dose up to 72 hours post-dose
|
Cmax,norm
Time Frame: Pre-dose up to 72 hours post-dose
|
Cmax divided by dose per kg body weight for BAY 63-2521 and its metabolite M1
|
Pre-dose up to 72 hours post-dose
|
tmax
Time Frame: Pre-dose up to 72 hours post-dose
|
Time to reach Cmax (in case of two identical Cmax values, the first tmax was used) for BAY 63-2521 and its metabolite M1
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Pre-dose up to 72 hours post-dose
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MRT
Time Frame: Pre-dose up to 72 hours post-dose
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Mean residence time for BAY 63-2521 and its metabolite M1
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Pre-dose up to 72 hours post-dose
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CL/F
Time Frame: Pre-dose up to 72 hours post-dose
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Total body clearance of drug calculated after extravascular administration (eg apparent oral clearance) for BAY 63-2521 and its metabolite M1
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Pre-dose up to 72 hours post-dose
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Vz/F
Time Frame: Pre-dose up to 72 hours post-dose
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Apparent volume of distribution during terminal phase after extravascular administration for BAY 63-2521 and its metabolite M1
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Pre-dose up to 72 hours post-dose
|
AE,ur
Time Frame: From 24 hours prior to drug administration up to 72 hours post-dose
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Amount of (total) drug excreted in urine for BAY 63-2521 and its metabolite M1
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From 24 hours prior to drug administration up to 72 hours post-dose
|
CLR
Time Frame: From 24 hours prior to drug administration up to 72 hours post-dose
|
Renal body clearance of drug for BAY 63-2521 and its metabolite M1
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From 24 hours prior to drug administration up to 72 hours post-dose
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Collaborators and Investigators
Sponsor
Publications and helpful links
Study record dates
Study Major Dates
Study Start (Actual)
Primary Completion (Actual)
Study Completion (Actual)
Study Registration Dates
First Submitted
First Submitted That Met QC Criteria
First Posted (Actual)
Study Record Updates
Last Update Posted (Actual)
Last Update Submitted That Met QC Criteria
Last Verified
More Information
Terms related to this study
Additional Relevant MeSH Terms
Other Study ID Numbers
- 15000
- 2009-017685-23 (EudraCT Number)
Plan for Individual participant data (IPD)
Plan to Share Individual Participant Data (IPD)?
IPD Plan Description
Drug and device information, study documents
Studies a U.S. FDA-regulated drug product
Studies a U.S. FDA-regulated device product
This information was retrieved directly from the website clinicaltrials.gov without any changes. If you have any requests to change, remove or update your study details, please contact register@clinicaltrials.gov. As soon as a change is implemented on clinicaltrials.gov, this will be updated automatically on our website as well.
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