check_circleStudy Completed

Pharmacology, clinical

Bayer Identifier:

13790

ClinicalTrials.gov Identifier:

NCT00855660

EudraCT Number:

2008-005569-70

EU CT Number:

Not Available
Effect of Riociguat on bone metabolism

Trial purpose

Investigation of the effect of Riociguat, administered as 2.5 mg IR-tablets TID over 14 days, on bone metabolism.

Key Participants Requirements

Sex

Male

Age

18 - 45 Years
  • - Healthy male white subjects
    - 18 to 45 years of age
    - BMI between 18 and 28 kg/m2
    - Subjects who are able to understand and follow instructions and who are able to participate in the study for the entire period
  • - Relevant deviation from the normal range in the clinical examination; in clinical chemistry, hematology, or urinalysis
    - Resting heart rate in the awake subject below 45 BPM or above 90 BPM
    - Systolic blood pressure below 100 mmHg or above 145 mmHg
    - Diastolic blood pressure above 95 mmHg
    - Relevant pathological changes in the ECG such as a second or third-degree AV block, prolongation of the QRS complex over 120 msec or of the QT / QTc-interval over 450 msec for males
    - History of genetic muscle or bone disease of any kind
    - Completely sedentary or extremely fit subjects
    - Fractures in the preceding 12 months
    - Psychiatric diseases
    - History of peptic ulcers or relevant gastro-esophageal reflux disease
    - Subjects with hypersensitivity to the investigational drug riociguat or ranitidine, or to inactive constituents
    - Regular daily consumption of more than half a liter of usual beer or the equivalent
    quantity of approximately 20 g of alcohol in another form, more than 1 L of xanthine-containing beverages, recent smoking history
    - Use of medication within the 2 weeks preceding the study which could have
    interfered with the investigational drug riociguat or ranitidine
    - Subjects with a medical disorder, condition or history of such that would have
    impaired the subject's ability to participate or complete this study in the opinion of
    the investigator or the sponsor

Trial summary

Enrollment Goal
17
Trial Dates
March 2009 - July 2010
Phase
Phase 1
Could I Receive a placebo
Yes
Products
Adempas (Riociguat, BAY63-2521)
Accepts Healthy Volunteer
Yes

Where to participate

StatusInstitutionLocation
Completed
Deutsches Zentrum für Luft- und Raumfahrt e. V. (DLR)Köln, 51147, Germany

Primary Outcome

  • Urinary excretion (over 24 hours) of C-terminal cross-linking telopeptides of type I collagen (CTX)
    Marker of bone resorption
    date_rangeTime Frame:
    From Day -01 to 16
    enhanced_encryption
    Safety Issue:
    No
  • AUC(0-7)
    Area under the plasma concentration vs time curve (AUC) from zero to 7 hours after single (first) dose for riociguat and its metabolite M-1 (BAY60-4552)
    date_rangeTime Frame:
    Pre-dose and up to 7 hours post-dose on Day 0
    enhanced_encryption
    Safety Issue:
    No
  • AUC(0-7)ss
    AUC(0-7) at steady state
    date_rangeTime Frame:
    Pre-dose and up to 7 hours post-dose on Day 13
    enhanced_encryption
    Safety Issue:
    No
  • Cmax
    Maximum drug concentration in plasma after single dose administration for riociguat and its metabolite M-1 (BAY60-4552)
    date_rangeTime Frame:
    Pre-dose and up to 7 hours post-dose on Day 0
    enhanced_encryption
    Safety Issue:
    No
  • Cmax,ss
    Maximum drug concentration in plasma at steady state during a dosage interval for riociguat and its metabolite M-1 (BAY60-4552)
    date_rangeTime Frame:
    Pre-dose and up to 7 hours post-dose on Day 13
    enhanced_encryption
    Safety Issue:
    No

Secondary Outcome

  • Number of participants with adverse events
    date_rangeTime Frame:
    Approximately 12 weeks
    enhanced_encryption
    Safety Issue:
    yes
  • Ctrough
    Drug concentration in plasma at expected time of minimum (trough) concentration for riociguat and its metabolite M-1 (BAY60-4552)
    date_rangeTime Frame:
    On Days 03 and 08
    enhanced_encryption
    Safety Issue:
    No
  • AUC(0-7)norm
    AUC(0-7) divided by dose per kg body weight for riociguat and its metabolite M-1 (BAY60-4552)
    date_rangeTime Frame:
    Pre-dose and up to 7 hours post-dose on Day 0
    enhanced_encryption
    Safety Issue:
    No
  • AUC(0-7)ss,norm
    AUC(0-7)ss divided by dose per kg body weight for riociguat and its metabolite M-1 (BAY60-4552)
    date_rangeTime Frame:
    Pre-dose and up to 7 hours post-dose on Day 13
    enhanced_encryption
    Safety Issue:
    No
  • Cmax,norm
    Maximum drug concentration in plasma after (first) single dose administration divided by dose (mg) per kg body weight for riociguat and its metabolite M-1 (BAY60-4552)
    date_rangeTime Frame:
    Pre-dose and up to 7 hours post-dose on Day 0
    enhanced_encryption
    Safety Issue:
    No
  • Cmax,ss,norm
    Maximum drug concentration in plasma at steady state during a dosage interval divided by dose (mg) per kg body weight for riociguat and its metabolite M-1 (BAY60-4552)
    date_rangeTime Frame:
    Pre-dose and up to 7 hours post-dose on Day 13
    enhanced_encryption
    Safety Issue:
    No
  • tmax
    Time to reach maximum drug concentration in plasma after single (first) dose for riociguat and its metabolite M-1 (BAY60-4552)
    date_rangeTime Frame:
    Pre-dose and up to 7 hours post-dose on Day 0
    enhanced_encryption
    Safety Issue:
    No
  • tmax,ss
    tmax at steady state for riociguat and its metabolite M-1 (BAY60-4552)
    date_rangeTime Frame:
    Pre-dose and up to 7 hours post-dose on Day 13
    enhanced_encryption
    Safety Issue:
    No
  • Aeur(0-7)
    Amount of drug excreted via urine from zero to 7 hours after administration for riociguat and its metabolite M-1 (BAY60-4552)
    date_rangeTime Frame:
    Pre-dose and up to 7 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • %Aeur(0-7)
    Aeur(0-7) expressed as percent of dose administered for riociguat and its metabolite M-1 (BAY60-4552)
    date_rangeTime Frame:
    Pre-dose and up to 7 hours post-dose
    enhanced_encryption
    Safety Issue:
    No
  • Urinary excretion (over 24 hours) of N-terminal cross-linking telopeptides of type I collagen (NTX)
    Marker of bone resorption
    date_rangeTime Frame:
    From -01 to 16 Days
    enhanced_encryption
    Safety Issue:
    No
  • Serum CTX
    Marker of bone resorption
    date_rangeTime Frame:
    From -01 to 16 Days
    enhanced_encryption
    Safety Issue:
    No
  • Serum N-terminal propeptide of type I collagen (PINP)
    Marker of bone formation
    date_rangeTime Frame:
    From -01 to 16 Days
    enhanced_encryption
    Safety Issue:
    No
  • Serum bone-specific alkaline phosphatase (bAP)
    Marker of bone formation
    date_rangeTime Frame:
    From -01 to 16 Days
    enhanced_encryption
    Safety Issue:
    No
  • Serum albumin, protein
    Determination of albumin, protein in serum
    date_rangeTime Frame:
    From -01 to 16 Days
    enhanced_encryption
    Safety Issue:
    No
  • Cyclic guanosine monophosphate (cGMP)
    Determination of cGMP in plasma and urinary excretion (over 24 hours)
    date_rangeTime Frame:
    From -01 to 16 Days
    enhanced_encryption
    Safety Issue:
    No
  • Calcium, sodium, potassium
    Determination of calcium, sodium, potassium in serum and urinary excretion (over 24 hours)
    date_rangeTime Frame:
    From -01 to 16 Days
    enhanced_encryption
    Safety Issue:
    No
  • Urine volume
    Volume of urine excreted (over 24 hours)
    date_rangeTime Frame:
    From -01 to 16 Days
    enhanced_encryption
    Safety Issue:
    No
  • Renin
    Determination of plasma renin level
    date_rangeTime Frame:
    From -01 to 16 Days
    enhanced_encryption
    Safety Issue:
    No
  • Creatinine clearance
    For estimation of glomerular filtration rate
    date_rangeTime Frame:
    From -01 to 16 Days
    enhanced_encryption
    Safety Issue:
    No
  • Serum osteocalcin
    Determination of osteocalcin in serum
    date_rangeTime Frame:
    From -01 to 16 Days
    enhanced_encryption
    Safety Issue:
    No
  • Creatinine
    Determination of creatinine in serum and urinary excretion (over 24 hours)
    date_rangeTime Frame:
    From -01 to 16 Days
    enhanced_encryption
    Safety Issue:
    No
  • Phosphate
    Determination of phosphate in serum only
    date_rangeTime Frame:
    From -01 to 16 Days
    enhanced_encryption
    Safety Issue:
    No
  • Parathyroid hormone (PTH)
    Determination of PTH in serum only
    date_rangeTime Frame:
    From -01 to 16 Days
    enhanced_encryption
    Safety Issue:
    No

Trial design

Investigation of the effect of riociguat, administered as 2.5 mg IR-tablets TID over 14 days, on bone metabolism in a randomized, placebo-controlled, double-blind, 2-fold cross-over design in healthy male subjects
Trial Type
Interventional
Intervention Type
Drug
Trial Purpose
Treatment
Allocation
Randomized
Blinding
Double Blind
Assignment
Crossover Assignment
Trial Arms
2

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