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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.
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.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Treatment Arm A | Experimental | low dose of mirabegron |
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| Treatment Arm B | Experimental | high dose of mirabegron |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| mirabegron OCAS | Drug | oral administration |
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| Measure | Description | Time Frame |
|---|---|---|
| Assessment of pharmacokinetics of mirabegron assessed by plasma concentration | Pre-dose until 72 hours after dosing |
| Measure | Description | 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 |
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Inclusion Criteria:
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:
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
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| Name | Affiliation | Role |
|---|---|---|
| Clinical Study Manager | Astellas Pharma Europe B.V. | Study Chair |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Pharma Bio Research | Zuidlaren | 9470 AE | Netherlands |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 22943933 | Background | Eltink C, Lee J, Schaddelee M, Zhang W, Kerbusch V, Meijer J, van Marle S, Grunenberg N, Kowalski D, Drogendijk T, Moy S, Iitsuka H, van Gelderen M, Matsushima H, Sawamoto T. Single dose pharmacokinetics and absolute bioavailability of mirabegron, a beta(3)-adrenoceptor agonist for treatment of overactive bladder. Int J Clin Pharmacol Ther. 2012 Nov;50(11):838-50. doi: 10.5414/CP201782. |
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| ID | Term |
|---|---|
| C520025 | mirabegron |
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| mirabegron | Drug | iv administration |
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