Relative Bioavailability and Food Effect Study

NCT01489488 | Completed Phase 1

• 2 other identifiers: 149862011-001893-24
• Study Type: interventional
• Target: 32
• Locations: 1 country
• Sites: 1

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).

Conditions

Pharmacology, Clinical

Keywords

Relative bioavailability study

Outcome Measures

Primary Outcomes (4)

• 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.

  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.

  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.

  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.

  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 (8)

• 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

  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

  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

  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)

  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)

  0 hour (predose), 15, 30, 45 minutes; 1, 1.5, 2, 3, 4, 6, 8, 12, 15, 24, 36, 48, and 72 hours postdose

Study Arms (5)

Arm 1

EXPERIMENTAL

Drug: Riociguat (BAY63-2521)

Arm 2

EXPERIMENTAL

Drug: Riociguat (BAY63-2521)

Arm 3

EXPERIMENTAL

Drug: Riociguat (BAY63-2521)

Arm 4

EXPERIMENTAL

Drug: Riociguat (BAY63-2521)

Arm 5

EXPERIMENTAL

Drug: Riociguat (BAY63-2521)

Interventions

Riociguat (BAY63-2521) DRUG

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

Arm 1

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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

Sponsors & Collaborators

• Bayer: lead

Study Sites (1)

Unknown Facility

Cologne, North Rhine-Westphalia, 51063, Germany

Location

Related Links

• Click here to find information about studies related to Bayer Healthcare products conducted in Europe

MeSH Terms

Interventions

riociguat

Study Officials

• Bayer Study Director

  Bayer

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: December 8, 2011
• First Posted: December 9, 2011
• Study Start: January 1, 2012
• Primary Completion: April 1, 2012
• Study Completion: May 1, 2012
• Last Updated: July 1, 2015

Record last verified: 2015-06

Locations

DE (1)