Bioavailability, Healthy Subjects, Pharmacokinetics of Mirabegron
Conditions
Keywords
Pharmacokinetics, Mirabegron, Phase 1
Brief summary
A study to evaluate how much of the active compound of mirabegron comes into the blood circulation when given as a controlled-release pill as compared to given intravenously.
Detailed description
All participants will receive both oral and iv formulations, separated by a washout period. Treatment arm A will receive a lower dose of mirabegron; Treatment arm B will receive a higher dose of mirabegron.
Interventions
DRUGmirabegron OCAS
oral administration
DRUGmirabegron
iv administration
Sponsors
Astellas Pharma Inc
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Body weight between 60.0 and 100.0 kg and Body Mass Index between 18.0 and 30.0 kg/m2
Exclusion criteria
* Known or suspected hypersensitivity to β-adrenergic receptor agonists or constituents of the formulations used * Clinically significant elevation of serum creatinine or liver enzymes as evidenced by creatinine \>150 ųmol/L; ASAT, ALAT or LDH\> 2x ULN; ɣ-GT \> 3x ULN and/or abnormal serum bilirubin * Any clinically significant history of asthma, eczema, any other allergic condition or previous severe hypersensitivity to any drug * Subjects taking β blockers or β agonists (eye drops allowed) * Any clinically significant history of upper gastrointestinal symptoms (such as nausea, vomiting, abdominal discomfort or upset, or heartburn) in the 4 weeks prior to the first admission to the Research Unit * Any clinically significant history of any other disease or disorder - gastrointestinal, cardiovascular, respiratory, ophthalmologic, 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 * QTcB interval of \> 430 (mean QTcB of two measurements \> 430msec) * Abnormal pulse rate measurement (\<40 or \>90 bpm) at the pre-study visit after subject has been resting in supine position for 5 min. * Abnormal blood pressure measurements taken at the pre-study visit after subject has been resting in supine position for 5 min as follows: * Systolic blood pressure \<95 or \>160 mmHg * Diastolic blood pressure \<40 or \>90 mmHg * Positive orthostatic test at screening i.e. any symptoms of dizziness, light-headedness etc. and a fall of \> 20 mmHg in systolic blood pressure after 2 min standing and an increase in pulse rate of ≥ 20 bpm * Regular use of any prescribed or OTC drugs except paracetamol up to 3 g/day, in the 4 weeks prior to admission to the Research Unit OR any use of such drugs in the 2 weeks prior to first admission to the Research Unit
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Assessment of pharmacokinetics of mirabegron assessed by plasma concentration | Pre-dose until 72 hours after dosing |
Secondary
| Measure | Time frame |
|---|---|
| Monitoring of safety and tolerability through assessment of vital signs, Electrocardiogram (ECG), clinical safety laboratory and adverse events | Baseline until 72 hours after dosing |
Countries
Netherlands
Outcome results
None listed