Clinical trial NCT01489488: Relative Bioavailability and Food Effect Study
Official title: 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
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Pharmacology, Clinical
Keywords: Relative bioavailability study
Lead sponsor: Bayer
Sponsor class: INDUSTRY
First posted: 2011-12-09
Enrollment: 32
Sex: ALL
Minimum age (years): 18
Maximum age (years): 45
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: CROSSOVER

Brief summary: 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).

Detailed description: Clinical pharmacology

Eligibility criteria: Inclusion Criteria:

* 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

Exclusion Criteria:

* 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

Primary outcomes:
measure: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC) of Riociguat and its Analyte M1 (BAY60-4552)
timeFrame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
measure: Maximum Observed Drug Concentration (Cmax) of Riociguat and its Analyte M1 (BAY60-4552) After a Single Dose
timeFrame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
measure: 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
timeFrame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
measure: Maximum Observed Drug Concentration Adjusted by Dose (Cmax/D) of Riociguat and its Analyte M1 (BAY60-4552) After a Single Dose
timeFrame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
Secondary outcomes:
measure: 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
timeFrame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
measure: 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
timeFrame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
measure: Time to Reach Maximum Drug Concentration in Plasma (tmax) of Riociguat and its Analyte M1 (BAY60-4552) After a Single Dose
timeFrame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
measure: Terminal Half Life (t1/2) of Riociguat and its Analyte M1 (BAY60-4552)
timeFrame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
measure: Mean Residence Time (MRT) of Riociguat and its Analyte M1 (BAY604552)
timeFrame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
measure: 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
timeFrame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
measure: 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
timeFrame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
measure: 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
timeFrame: 0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose
Other outcomes:
Locations:
city: Köln
country: Germany
state: Nordrhein-Westfalen
Study officials:
affiliation: Bayer
name: Bayer Study Director
role: STUDY_DIRECTOR
References: