Clinical Pharmacology
Conditions
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
Interventions
0.5 mg riociguat as an immediate-release (IR) tablet
Sponsors
Bayer
Study design
Allocation
NON_RANDOMIZED
Intervention model
PARALLEL
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 79 Years
Healthy volunteers
Yes
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
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| AUC | 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) |
| Cmax | Pre-dose up to 72 hours post-dose | Maximum total (bound and unbound) drug concentration in plasma after single dose administration for BAY 63-2521 and its metabolite M1 |
| t½ | Pre-dose up to 72 hours post-dose | Half-life associated with the terminal slope for BAY 63-2521 and its metabolite M1 |
| fu | From 2 hours post-dose up to 24 hours post-dose | Fraction unbound for BAY 63-2521 and its metabolite M1 |
| AUCu | From 2 hours post-dose up to 24 hours post-dose | AUC for unbound drug for BAY 63-2521 and its metabolite M1 |
| Cmax,u | From 2 hours post-dose up to 24 hours post-dose | Cmax for unbound drug for BAY 63-2521 and its metabolite M1 |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Cmax,u,norm | From 2 hours post-dose up to 24 hours post-dose | Cmax,norm for unbound drug for BAY 63-2521 and its metabolite M1 |
| tmax | 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 |
| MRT | Pre-dose up to 72 hours post-dose | Mean residence time for BAY 63-2521 and its metabolite M1 |
| CL/F | Pre-dose up to 72 hours post-dose | Total body clearance of drug calculated after extravascular administration (eg apparent oral clearance) for BAY 63-2521 and its metabolite M1 |
| AUC/D | Pre-dose up to 72 hours post-dose | AUC divided by dose for BAY 63-2521 and its metabolite M1 |
| Vz/F | Pre-dose up to 72 hours post-dose | Apparent volume of distribution during terminal phase after extravascular administration for BAY 63-2521 and its metabolite M1 |
| AE,ur | From 24 hours prior to drug administration up to 72 hours post-dose | Amount of (total) drug excreted in urine for BAY 63-2521 and its metabolite M1 |
| CLR | 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 |
| Number of participants with adverse events | Approximately 5 weeks | — |
| CLu/F | From 2 hours post-dose up to 24 hours post-dose | CL/F for unbound drug for BAY 63-2521 and its metabolite M1 |
| AUCnorm | Pre-dose up to 72 hours post-dose | AUC divided by dose per kg body weight for BAY 63-2521 and its metabolite M1 |
| AUCu,norm | From 2 hours post-dose up to 24 hours post-dose | AUCnorm for unbound drug for BAY 63-2521 and its metabolite M1 |
| AUC(0-tlast) | 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 |
| Cmax/D | Pre-dose up to 72 hours post-dose | Cmax divided by dose for BAY 63-2521 and its metabolite M1 |
| Cmax,norm | Pre-dose up to 72 hours post-dose | Cmax divided by dose per kg body weight for BAY 63-2521 and its metabolite M1 |
Countries
Germany
Outcome results
None listed