An Open Label Study to Evaluate the Pharmacokinetics of YM150 After a Single Oral Dose of C14-labeled YM150 in Healthy Male Subjects
Overview
- Phase
- Phase 1
- Intervention
- YM150
- Conditions
- Pharmacokinetics
- Sponsor
- Astellas Pharma Europe B.V.
- Enrollment
- 6
- Locations
- 1
- Primary Endpoint
- Pharmacokinetics of 14C-labeled YM150 assessed by whole blood, plasma, urine, feces and expired air concentrations
- Status
- Completed
- Last Updated
- 12 years ago
Overview
Brief Summary
The study aims to observe how YM150 was absorbed, distributed and excreted after dosing with a radio labeled drinking solution.
Detailed Description
Healthy male subjects are admitted on Day 0. Subjects receive a single oral dose of 14C-labeled YM150 in the morning of Day 1 and remain in the unit for 7 days (6 nights). Blood, plasma, urine and feces samples are collected until 120 hrs after dosing for analysis of 14C-labeled radioactivity, YM150, YM-222714 and other metabolites. Expired air is collected as well for assessment of 14C-radioactivity.
Investigators
Eligibility Criteria
Inclusion Criteria
- •Body weight between 60 and 100 kg and Body Mass Index between 18 and 30 kg/m2
Exclusion Criteria
- •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
Arms & Interventions
Treatment arm 1
Intervention: YM150
Outcomes
Primary Outcomes
Pharmacokinetics of 14C-labeled YM150 assessed by whole blood, plasma, urine, feces and expired air concentrations
Time Frame: Day 1 - Day 6
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.
Pharmacokinetics of YM150 and metabolites assessed by plasma and urine concentrations
Time Frame: Day 1 - Day 6
- AUCinf, AUClast, Cmax, tmax, tlag and t1/2. In urine - amount excreted in urine, CLR (Renal clearance) and % of dose excreted.
Secondary Outcomes
- 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)