A Study to Find Out How YM150 is Absorbed Into and Eliminated From the Body in Healthy Male Subjects

NCT01657981 | Completed Phase 1

• 2 other identifiers: 150-CL-0152006-001968-22
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

The study aims to observe how YM150 was absorbed, distributed and excreted after dosing with a radio labeled drinking solution.

Conditions

Pharmacokinetics; Healthy Male Subjects

Keywords

Pharmacokinetics; Phase 1; 14C-labeled

Outcome Measures

Primary Outcomes (2)

• Pharmacokinetics of 14C-labeled YM150 assessed by whole blood, plasma, urine, feces and expired air concentrations

  AUCinf (Amount excreted in urine extrapolated until infinity), AUClast (Amount excreted in urine until last sample), Cmax (Maximum concentration), tmax (Time to attain maximum concentration), tlag (Absorption lag time) and t1/2 (Apparent terminal elimination half-life). Excretion rate and cumulative excretion of radioactivity in urine, feces and expired air.

  Day 1 - Day 6

• Pharmacokinetics of YM150 and metabolites assessed by plasma and urine concentrations

  \- AUCinf, AUClast, Cmax, tmax, tlag and t1/2. In urine - amount excreted in urine, CLR (Renal clearance) and % of dose excreted.

  Day 1 - Day 6

Secondary Outcomes (2)

• Identification of the metabolic profile of YM150 in human plasma, urine and feces

  0 - 2 hours Day 1

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

  Day 1 - 14

Study Arms (1)

Treatment arm 1

EXPERIMENTAL

Drug: YM150

Interventions

YM150 DRUG

14C-labeled YM150, oral solution

Also known as: darexaban

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 weight between 60 and 100 kg and Body Mass Index between 18 and 30 kg/m2

You may not qualify if:

• Known or suspected hypersensitivity to YM150 or any of the constituents of the formulations used
• History of and/or any sign or symptom indicating current abnormal hemostasis or blood dyscrasia, including but not limited to neutropenia, thrombocytopenia, thrombocytopathy, thromboasthenia, hemophilia, Von Willebrand's disease, and vascular purpura, bleeding gums or frequent nose bleeding
• Family history of congenital vascular malformation (e.g. Marfan's Syndrome) and/or bleeding disorder (e.g. hemophilia, Von Willebrand's disease, Christmas disease)
• History of peptic ulcer or of any other organic lesion susceptible to bleeding
• Prothrombin time (PT) or Activated partial thromboplastin time (aPTT) at the screening visit outside the normal range
• Any surgical intervention (including tooth extraction) or trauma within the last 3 months preceding the start of the study
• Any clinically significant history of asthma, eczema, any other clinically significant allergic condition or previous severe hypersensitivity to any other drug
• Any clinically significant upper gastro-intestinal symptoms likely to interfere with the absorption of the drug
• History or presence of any cardiovascular disease or disorder
• History of a clinically significant ECG abnormality
• Any clinically relevant history of other disease or disorder - gastrointestinal, respiratory, renal, hepatic, neurological, dermatological, psychiatric or metabolic
• Any clinically significant abnormality following the Investigator's review of the pre-study physical examination, ECG, and clinical laboratory tests
• Abnormal heart rate and blood pressure measurements at the screening visit as follows: heart rate \<40 or \>90 bpm; mean systolic blood pressure \<95 or \>160 mmHg; mean diastolic blood pressure \<40 or \>95 mmHg (blood pressure measurements taken in triplicate after subject has been resting in supine position for 5 min)
• Regular use of any prescribed or OTC drugs (including vitamins and herbal remedies) in the 4 weeks prior to admission to the clinical unit OR any use of such drugs in the 2 weeks prior to admission to the clinical unit
• History of drug abuse at any time, OR any use of drugs of abuse within 3 months prior to admission to the clinical unit

Sponsors & Collaborators

• Astellas Pharma Europe B.V.: lead

Study Sites (1)

PRA International EDS NL

Zuidlaren, 9471 GP, Netherlands

Location

MeSH Terms

Interventions

darexaban

Study Officials

• Clinical Study Manager

  Astellas Pharma Europe B.V.

  STUDY CHAIR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 10, 2012
• First Posted: August 6, 2012
• Study Start: February 1, 2007
• Primary Completion: March 1, 2007
• Study Completion: March 1, 2007
• Last Updated: June 26, 2013

Record last verified: 2012-08

Locations

NL (1)