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

This study has been completed.
Information provided by (Responsible Party):
Astellas Pharma Inc Identifier:
First received: July 28, 2011
Last updated: April 9, 2013
Last verified: March 2013
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.

Condition Intervention Phase
Pharmacokinetics of Darexaban and Metabolites
Healthy Subjects
Drug: darexaban
Drug: Rifampicin
Phase 1

Study Type: Interventional
Study Design: Intervention Model: Single Group Assignment
Masking: Open Label
Official Title: An Open-label, One-sequence Study to Evaluate the Effect of Multiple Doses of Rifampicin on the Pharmacokinetics of YM150 (Darexaban) and Metabolites in Young Healthy Male Subjects

Resource links provided by NLM:

Further study details as provided by Astellas Pharma Inc:

Primary Outcome Measures:
  • Pharmacokinetics of darexaban and its metabolites assessed by plasma concentration [ Time Frame: Plasma samples are taken until 72 hours after darexaban dosing ]

Secondary Outcome Measures:
  • Monitoring of safety and tolerability through assessment of vital signs, ECG, clinical safety laboratory and adverse events [ Time Frame: 15 days ]

Enrollment: 26
Study Start Date: January 2010
Study Completion Date: March 2010
Primary Completion Date: March 2010 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: Treatment arm 1
darexaban, wash-out, rifampicin + darexaban
Drug: darexaban
Other Name: YM150
Drug: Rifampicin
Other Name: Rifadin

Detailed Description:

This is an open-label, 1-sequence study in young healthy male subjects to evaluate the effect of multiple daily doses of rifampicin on the PK of darexaban and metabolites after a single dose of darexaban. In addition, safety and tolerability of darexaban administered alone and in combination with rifampicin is evaluated. Eligible subjects are admitted to the clinical unit in the morning of Day -1.

Subjects receive a single dose of darexaban on Day 1. Subjects then receive rifampicin once daily (qd) on Days 4-14.On Day 11, the second single dose of darexaban is given in combination with rifampicin.


Ages Eligible for Study:   18 Years to 55 Years   (Adult)
Sexes Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes

Inclusion Criteria:

  • 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

Exclusion Criteria:

  • 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
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Please refer to this study by its identifier: NCT01406002

SGS Aster
Paris, France, 75015
Sponsors and Collaborators
Astellas Pharma Inc
Study Chair: Clinical Study Manager Astellas Pharma Europe B.V.
Principal Investigator: Prinicpal Investigator SGS Aster, Paris, France
  More Information

Additional Information:
Responsible Party: Astellas Pharma Inc Identifier: NCT01406002     History of Changes
Other Study ID Numbers: 150-CL-045
2009-015763-13 ( EudraCT Number )
Study First Received: July 28, 2011
Last Updated: April 9, 2013

Keywords provided by Astellas Pharma Inc:
Phase 1

Additional relevant MeSH terms:
Factor Xa Inhibitors
Serine Proteinase Inhibitors
Protease Inhibitors
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action
Antibiotics, Antitubercular
Antitubercular Agents
Anti-Bacterial Agents
Anti-Infective Agents
Leprostatic Agents
Nucleic Acid Synthesis Inhibitors
Cytochrome P-450 CYP2B6 Inducers
Cytochrome P-450 Enzyme Inducers
Cytochrome P-450 CYP2C8 Inducers
Cytochrome P-450 CYP2C19 Inducers
Cytochrome P-450 CYP2C9 Inducers
Cytochrome P-450 CYP3A Inducers processed this record on March 27, 2017