To Evaluate if Multiple Doses of Rifampicin Change the Blood Concentration of YM150 (Darexaban)

NCT01406002 | Completed Phase 1

• 2 other identifiers: 150-CL-0452009-015763-13
• Study Type: interventional
• Target: 26
• Locations: 1 country
• Sites: 1

Brief Summary

The primary objective of this study is to determine the effect of rifampicin on the way the body handles darexaban and its metabolites (drug degradation products). The secondary objective of the study is to evaluate the safety and tolerability of a single dose of darexaban alone and when administered together with rifampicin.

Conditions

Pharmacokinetics of Darexaban and Metabolites; Healthy Subjects

Keywords

Pharmacokinetics; darexaban; YM150; rifampicin; Phase 1

Outcome Measures

Primary Outcomes (1)

• Pharmacokinetics of darexaban and its metabolites assessed by plasma concentration

  Plasma samples are taken until 72 hours after darexaban dosing

Secondary Outcomes (1)

• Monitoring of safety and tolerability through assessment of vital signs, ECG, clinical safety laboratory and adverse events

  15 days

Study Arms (1)

Treatment arm 1

EXPERIMENTAL

darexaban, wash-out, rifampicin + darexaban

Drug: darexaban; Drug: Rifampicin

Interventions

darexaban DRUG

oral

Also known as: YM150

Treatment arm 1

Rifampicin DRUG

oral

Also known as: Rifadin

Treatment arm 1

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Body Mass Index (BMI) between 18.5-30.0 kg/m2
• Male subjects must be non-fertile, i.e. surgically sterilized or must practice an adequate contraceptive method to prevent pregnancies

You may not qualify if:

• Known or suspected hypersensitivity to darexaban or rifampicin or any components of the formulation used
• Any of the liver function tests (i.e. ALT and AST) above the upper limit of normal at repeated measures
• Any clinically significant history of any other disease or disorder - gastrointestinal, cardiovascular, respiratory, renal, hepatic, neurological, dermatological, psychiatric or metabolic as judged by the medical investigator
• Any clinically significant abnormality following the investigator's review of the pre-study physical examination, ECG and clinical laboratory tests
• Use of any prescribed or OTC drugs (including vitamins, natural and herbal remedies, e.g. St. John's wort) in the 2 weeks prior to admission to the Clinical Unit, except for occasional use of paracetamol (up to 3 g/day)
• Regular use of any inducer of liver metabolism (e.g. barbiturates, rifampicin) in the 3 months prior to admission to the Clinical Unit
• Any use of drugs of abuse, or smoking of more than 10 cigarettes (or equivalent) or more than 21 units (210 g) of alcohol per week within the 3 months prior to study Donation of blood or blood products within 3 months prior to admission to the Clinical Unit
• Participation in any clinical study within 3 months or participation in more than 3 clinical studies within 12 months, prior to the expected date of enrolment into the study, provided that the clinical study did not entail a biological compound with a long terminal half life

Sponsors & Collaborators

• Astellas Pharma Inc: lead

Study Sites (1)

SGS Aster

Paris, 75015, France

Location

Related Publications (1)

• Groenendaal D, Strabach G, Garcia-Hernandez A, Kadokura T, Heeringa M, Mol R, Eltink C, Onkels H. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4. Br J Clin Pharmacol. 2013 Feb;75(2):440-9. doi: 10.1111/j.1365-2125.2012.04346.x.

  PMID: 22642721 BACKGROUND

MeSH Terms

Interventions

darexaban; Rifampin

Intervention Hierarchy (Ancestors)

Rifamycins; Heterocyclic Compounds, 4 or More Rings; Heterocyclic Compounds, Fused-Ring; Heterocyclic Compounds; Lactams, Macrocyclic; Macrocyclic Compounds; Polycyclic Compounds

Study Officials

• Clinical Study Manager

  Astellas Pharma Europe B.V.

  STUDY CHAIR

• Prinicpal Investigator

  SGS Aster, Paris, France

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 28, 2011
• First Posted: July 29, 2011
• Study Start: January 1, 2010
• Primary Completion: March 1, 2010
• Study Completion: March 1, 2010
• Last Updated: April 11, 2013

Record last verified: 2013-03

Locations

FR (1)