Clinical trial NCT01657981: A Study to Find Out How YM150 is Absorbed Into and Eliminated From the Body in Healthy Male Subjects
Official title: An Open Label Study to Evaluate the Pharmacokinetics of YM150 After a Single Oral Dose of C14-labeled YM150 in Healthy Male Subjects
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Pharmacokinetics
Healthy Male Subjects
Keywords: Pharmacokinetics
Phase 1
14C-labeled
Lead sponsor: Astellas Pharma Inc
Sponsor class: INDUSTRY
First posted: 2012-08-06
Enrollment: 6
Sex: MALE
Minimum age (years): 18
Maximum age (years): 55
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: NON_RANDOMIZED
Intervention model: SINGLE_GROUP
Primary purpose: BASIC_SCIENCE

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.

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
* 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
* 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
* History of drinking more than 21 units of alcohol per week (1 unit = 270 ml of beer or 40 ml of spirits or 125 ml of wine) within 3 months prior to admission to the clinical unit
* History of smoking more than 10 cigarettes (or equivalent amount of tobacco) per day within 3 months prior to admission to the clinical unit
* Subject, who is anti-HAV (IgM), anti-HCV, HBsAg or HIV-1 or -2 positive
* Donation of blood (\>400 ml) or blood products within 3 months prior to admission to the clinical unit or plasmapheresis within 4 weeks prior to admission to the clinical unit
* Exposure to radiation for diagnostic reasons (except dental X-rays and plain X-rays of thorax and bony skeleton (excluding spinal column)), during work or during participation in a clinical study in the previous year

Primary outcomes:
measure: Pharmacokinetics of 14C-labeled YM150 assessed by whole blood, plasma, urine, feces and expired air concentrations
timeFrame: Day 1 - Day 6
measure: Pharmacokinetics of YM150 and metabolites assessed by plasma and urine concentrations
timeFrame: Day 1 - Day 6
Secondary outcomes:
measure: Identification of the metabolic profile of YM150 in human plasma, urine and feces
timeFrame: 0 - 2 hours Day 1
measure: Monitoring of safety and tolerability through assessment of vital signs, Electrocardiogram (ECG), clinical safety laboratory and adverse events
timeFrame: Day 1 - 14
Other outcomes:
Locations:
city: Zuidlaren
country: Netherlands
facility: PRA International EDS NL
Study officials:
affiliation: Astellas Pharma Europe B.V.
name: Clinical Study Manager
role: STUDY_CHAIR
References: