Clinical Pharmacology Clinical Trial
Official title:
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
Verified date | April 2020 |
Source | Bayer |
Contact | n/a |
Is FDA regulated | No |
Health authority | |
Study type | Interventional |
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
Status | Completed |
Enrollment | 40 |
Est. completion date | September 20, 2011 |
Est. primary completion date | March 17, 2011 |
Accepts healthy volunteers | Accepts Healthy Volunteers |
Gender | All |
Age group | 18 Years to 79 Years |
Eligibility |
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 |
Country | Name | City | State |
---|---|---|---|
n/a |
Lead Sponsor | Collaborator |
---|---|
Bayer |
Germany,
Type | Measure | Description | Time frame | Safety issue |
---|---|---|---|---|
Primary | 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 | |
Primary | 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 | |
Primary | t½ | Half-life associated with the terminal slope for BAY 63-2521 and its metabolite M1 | Pre-dose up to 72 hours post-dose | |
Primary | fu | Fraction unbound for BAY 63-2521 and its metabolite M1 | From 2 hours post-dose up to 24 hours post-dose | |
Primary | AUCu | AUC for unbound drug for BAY 63-2521 and its metabolite M1 | From 2 hours post-dose up to 24 hours post-dose | |
Primary | 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 | AUC/D | AUC divided by dose for BAY 63-2521 and its metabolite M1 | Pre-dose up to 72 hours post-dose | |
Secondary | AUCnorm | AUC divided by dose per kg body weight for BAY 63-2521 and its metabolite M1 | Pre-dose up to 72 hours post-dose | |
Secondary | AUCu,norm | AUCnorm for unbound drug for BAY 63-2521 and its metabolite M1 | From 2 hours post-dose up to 24 hours post-dose | |
Secondary | AUC(0-tlast) | 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 | |
Secondary | Cmax/D | Cmax divided by dose for BAY 63-2521 and its metabolite M1 | Pre-dose up to 72 hours post-dose | |
Secondary | Cmax,norm | Cmax divided by dose per kg body weight for BAY 63-2521 and its metabolite M1 | Pre-dose up to 72 hours post-dose | |
Secondary | Cmax,u,norm | Cmax,norm for unbound drug for BAY 63-2521 and its metabolite M1 | From 2 hours post-dose up to 24 hours post-dose | |
Secondary | 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 | Pre-dose up to 72 hours post-dose | |
Secondary | MRT | Mean residence time for BAY 63-2521 and its metabolite M1 | Pre-dose up to 72 hours post-dose | |
Secondary | CL/F | Total body clearance of drug calculated after extravascular administration (eg apparent oral clearance) for BAY 63-2521 and its metabolite M1 | Pre-dose up to 72 hours post-dose | |
Secondary | CLu/F | CL/F for unbound drug for BAY 63-2521 and its metabolite M1 | From 2 hours post-dose up to 24 hours post-dose | |
Secondary | Vz/F | Apparent volume of distribution during terminal phase after extravascular administration for BAY 63-2521 and its metabolite M1 | Pre-dose up to 72 hours post-dose | |
Secondary | AE,ur | Amount of (total) drug excreted in urine for BAY 63-2521 and its metabolite M1 | From 24 hours prior to drug administration up to 72 hours post-dose | |
Secondary | CLR | Renal body clearance of drug for BAY 63-2521 and its metabolite M1 | From 24 hours prior to drug administration up to 72 hours post-dose | |
Secondary | Number of participants with adverse events | Approximately 5 weeks |
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