check_circleStudy Completed

Pharmacology, Clinical

Bayer Identifier:

14986

ClinicalTrials.gov Identifier:

NCT01489488

EudraCT Number:

2011-001893-24

EU CT Number:

Not Available
Relative bioavailability and food effect study

Trial purpose

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).

Key Participants Requirements

Sex

Both

Age

18 - 45 Years
  • - Healthy male or female volunteers
    - Age 18-45 years
    - Body mass index (BMI) 18.0-29.9 kg/m²
    - Systolic blood pressure (SBP) 110-145 mmHg
    - No drugs 2 weeks before treatment
    - Nonsmokers for at least 12 weeks
  • - Incompletely cured pre-existing diseases for which it can be assumed that the absorption, distribution, metabolism, elimination and effects of the study drugs will not be normal
    - Medical disorder that would impair the subject's ability to complete the study in the opinion of the Investigator
    - Known hypersensitivity to the study drugs (active substance or excipients of the preparations)
    - Known severe allergies, non-allergic drug reactions, or multiple drug allergies
    - Relevant diseases within the last 4 weeks prior to the first study drug administration
    - Regular use of medicines
    - Regular use of therapeutic or recreational drugs
    - Use of any medication within the 2 weeks preceding the study

Trial summary

Enrollment Goal
32
Trial Dates
January 2012 - May 2012
Phase
Phase 1
Could I Receive a placebo
No
Products
Adempas (Riociguat, BAY63-2521)
Accepts Healthy Volunteer
Yes

Where to participate

StatusInstitutionLocation
Completed
MEDA Manufacturing GmbH, ClinPharmCologneKöln, 51063, Germany

Primary Outcome

  • 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.
    date_rangeTime 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
    enhanced_encryption
    Safety Issue:
    No
  • 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.
    date_rangeTime 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
    enhanced_encryption
    Safety Issue:
    No
  • 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.
    date_rangeTime 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
    enhanced_encryption
    Safety Issue:
    No
  • 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.
    date_rangeTime 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
    enhanced_encryption
    Safety Issue:
    No

Secondary Outcome

  • 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
    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.
    date_rangeTime 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
    enhanced_encryption
    Safety Issue:
    No
  • 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.
    date_rangeTime 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
    enhanced_encryption
    Safety Issue:
    No
  • 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.
    date_rangeTime 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
    enhanced_encryption
    Safety Issue:
    No
  • 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.
    date_rangeTime 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
    enhanced_encryption
    Safety Issue:
    No
  • 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.
    date_rangeTime 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
    enhanced_encryption
    Safety Issue:
    No
  • 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.
    date_rangeTime 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
    enhanced_encryption
    Safety Issue:
    No
  • 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.
    date_rangeTime 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
    enhanced_encryption
    Safety Issue:
    No
  • 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.
    date_rangeTime 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
    enhanced_encryption
    Safety Issue:
    No

Trial design

Relative bioavailability and food effect study of two oral liquid formulations in comparison to a 1 mg tablet of riociguat to characterize its pharmacokinetic properties in healthy male and female adult subjects in a randomized, open label, 5-fold crossover design
Trial Type
Interventional
Intervention Type
Drug
Trial Purpose
Other
Allocation
Randomized
Blinding
Open Label
Assignment
Crossover Assignment
Trial Arms
5

Additional Information

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