Primary objective: To determine oral bioavailability of the liquid formulation intended for pediatric use and potential food effects in healthy adults. Secondary objective: To evaluate safety and tolerability measured by physical examination findings, vital signs, electrocardiogram (ECG), laboratory parameters, and adverse events (AEs).
Clinical pharmacology
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Masking
NONE
Enrollment
32
Single oral dose of 2.4 milligram (mg) riociguat (BAY63-2521) as pediatric high-concentration suspension (0.15 mg per milliliter \[mg/mL\], i.e. 16 mL) under fasting conditions
Single oral dose of 2.4 mg riociguat as pediatric high-concentration suspension (0.15 mg/mL, i.e. 16 mL) under fed conditions
Single oral dose of 0.3 mg riociguat as pediatric high-concentration suspension (0.15 mg/mL, i.e. 2 mL) under fasting conditions
Unnamed facility
Cologne, North Rhine-Westphalia, Germany
Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC) of Riociguat and its Analyte M1 (BAY60-4552)
AUC is a measure of systemic drug exposure, which is obtained by collecting a series of blood samples and measuring the concentrations of drug in each sample. AUC is defined as area under concentration versus time curve from time 0 (predose) to extrapolated infinite time. Geometric mean and percentage geometric coefficient of variation (%CV) were reported.
Time frame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
Maximum Observed Drug Concentration (Cmax) of Riociguat and its Analyte M1 (BAY60-4552) After a Single Dose
Cmax refers to the highest measured drug concentration which is obtained by collecting a series of plasma samples and measuring the concentrations of drug in each sample. Geometric mean and percentage geometric coefficient of variation (%CV) were reported.
Time frame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
Area Under the Concentration Versus Time Curve From Zero to Infinity Divided by Dose (AUC/D) of Riociguat and its Analyte M1 (BAY60-4552) After a Single Dose
Geometric mean and percentage geometric coefficient of variation (%CV) were reported.
Time frame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
Maximum Observed Drug Concentration Adjusted by Dose (Cmax/D) of Riociguat and its Analyte M1 (BAY60-4552) After a Single Dose
Geometric mean and percentage geometric coefficient of variation (%CV) were reported.
Time frame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
Area Under the Concentration Versus Time Curve From Zero to Infinity Divided by Dose per Kilogram Body Weight (AUC,norm) of Riociguat and its Analyte M1 (BAY60-4552) After a Single Dose
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Single oral dose of 0.15 mg riociguat as pediatric low-concentration suspension (0.03 mg/mL, i.e. 5 mL) under fasting conditions
Single oral dose of riociguat immediate release (IR) tablet 1 mg under fasting conditions
AUC is a measure of the plasma concentration of the drug over time. It is used to characterize drug absorption. AUCnorm is defined as AUC divided by dose per kg body weight.
Time frame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
Maximum Observed Plasma Concentration Divided by Dose per Kilogram Body Weight (Cmax,norm) of Riociguat and its Analyte M1 (BAY60-4552) After a Single Dose
Cmax refers to the highest measured drug concentration which is obtained by collecting a series of blood samples and measuring the concentrations of drug in each sample. Cmax,norm is defined as Cmax divided by dose per kg body weight.
Time frame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
Time to Reach Maximum Drug Concentration in Plasma (tmax) of Riociguat and its Analyte M1 (BAY60-4552) After a Single Dose
tmax refers to the time after dosing when a drug attains its highest measurable concentration (Cmax). It is obtained by collecting a series of blood samples at various times after dosing, and measuring them for drug content.
Time frame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
Terminal Half Life (t1/2) of Riociguat and its Analyte M1 (BAY60-4552)
Half life associated with terminal slope refers to the elimination of the drug. It is the time taken for the blood plasma concentration to reach half the concentration in the terminal phase of elimination. It is expressed in hours and derived from the terminal slope of the concentration versus time curve. Geometric mean and percentage geometric coefficient of variation (%CV) were reported.
Time frame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
Mean Residence Time (MRT) of Riociguat and its Analyte M1 (BAY604552)
MRT is an average duration of the drug in the body, and is expressed in hours.
Time frame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
Area Under the Concentration Versus Time Curve From Zero to Last Quantifiable Concentration (AUC[0-tlast]) of Riociguat and its Analyte M1 (BAY60-4552) After a Single Dose
AUC is a measure of systemic drug exposure, which is obtained by collecting a series of blood samples and measuring the concentrations of drug in each sample. AUC(0-tlast) is defined as AUC from time zero to the last data point above the lower limit of quantification. Geometric mean and percentage geometric coefficient of variation (%CV) were reported.
Time frame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
Area Under the Concentration Versus Time Curve From Zero to Last Quantifiable Concentration Divided by Dose per Kilogram Body Weight (AUC[0-tlast]norm) of Riociguat and its Analyte M1 (BAY60-4552) After a Single Dose
AUC is a measure of systemic drug exposure, which is obtained by collecting a series of blood samples and measuring the concentrations of drug in each sample. AUC(0-tlast), norm is defined as AUC from time zero to the last data point above the lower limit of quantification divided by dose per kg body weight. Geometric mean and percentage geometric coefficient of variation (%CV) were reported.
Time frame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
Area Under the Concentration Versus Time Curve From Zero to Last Quantifiable Concentration Divided by Dose (AUC[0-tlast]/D) of Riociguat and its Analyte M1 (BAY60-4552) After a Single Dose
AUC is a measure of systemic drug exposure, which is obtained by collecting a series of blood samples and measuring the concentrations of drug in each sample. AUC(0-tlast)/D is defined as AUC from time zero to the last data point above the lower limit of quantification divided by dose. Geometric mean and percentage geometric coefficient of variation (%CV) were reported.
Time frame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose