Relative Bioavailability Study

Relative Bioavailability Study of Riociguat Given Orally as a Crushed 2.5 mg Tablet Suspended in Applesauce, Crushed 2.5 mg Tablet Suspended in Water, and Whole 2.5 mg Tablet After a Continental Breakfast in Comparison to a Whole 2.5 mg Tablet Given in the Fasted State to Characterize the Pharmacokinetic Properties in Healthy Male Adult Subjects in a 4-fold Crossover Design

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT02159313

Enrollment

Registered

2014-06-09

Start date

2014-06-30

Completion date

2015-01-31

Last updated

2016-02-18

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy Volunteers

Keywords

Biological Availability

Brief summary

To investigate relative bioavailability of crushed tablets suspended in apple sauce or water

Interventions

DRUGRiociguat(Adempas,BAY63-2521)

Single dose of a whole 2.5 mg riociguat tablet

Study design

Allocation

RANDOMIZED

Intervention model

CROSSOVER

Masking

NONE

Eligibility

Sex/Gender

MALE

Age

18 Years to 45 Years

Healthy volunteers

Yes

Inclusion criteria

* Healthy male subject * Age: 18 to 45 years (inclusive) at the first screening examination * Ethnicity: white * Body mass index (BMI): \>18 and \<29.9 kg/m2

Exclusion criteria

* Incompletely cured pre-existing diseases for which it can be assumed that the absorption, distribution, metabolism, elimination, or effects of the study drug will not be normal * History of coronary artery disease * Symptomatic postural hypotension (e.g. dizziness, lightheadedness) * History of bronchial asthma or any other airway disease * Smoking (former smokers who have stopped smoking at least 3 months before the first study drug administration may be included) * Clinically relevant findings in the ECG such as a second- or third-degree atrioventricular block, prolongation of the QRS complex over 120 ms or of the QTc interval (QT interval corrected for heart rate) over 450 ms * Systolic blood pressure below 100 or above 145 mmHg * Diastolic blood pressure below 50 or above 95 mmHg * Heart rate below 45 or above 95 beats per minute

Design outcomes

Primary

Measure	Time frame
Pharmacokinetics of riociguat in plasma by maximal concentration (Cmax)	Multiple time ponits up to day 3
Pharmacokinetics of riociguat in plasma by Area under the plasma concentration time curve (AUC)	Multiple time points up to day 3

Secondary

Measure	Time frame
Number of participants with adverse events as a measure of safety and tolerability	Up to 12 weeks

Countries

Germany

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026