Mirabegron(YM178)是β3肾上腺素受体激动剂,EC50为22.4 nM。
Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Takasu T, et al. J Pharmacol Exp Ther, 2007, 321(2), 642-647.
[2] Krauwinkel W, van Dijk J, Schaddelee M et al. Pharmacokinetic Properties of Mirabegron, a β(3)-Adrenoceptor Agonist: Results From Two Phase I, Randomized, Multiple-Dose Studies in Healthy Young and Elderly Men and Women. Clin Ther. 2012 Oct;34(10):2144-60.
[3] Tyagi P, Tyagi V, Chancellor M. Mirabegron: a safety review. Expert Opin Drug Saf. 2011 Mar;10(2):287-94.
分子式 C21H24N4O2S |
分子量 396.51 |
CAS号 223673-61-8 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 82 mg/mL |
Water <1 mg/mL |
Ethanol 10 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00940121 | Healthy|Pharmacokinetics of Mirabegron | Drug: mirabegron|Drug: mirabegron | Astellas Pharma Inc | Phase 1 | 2009-04-01 | 2013-07-01 |
NCT00939757 | Healthy|Pharmacokinetics of Mirabegron | Drug: mirabegron | Astellas Pharma Inc | Phase 1 | 2009-05-01 | 2013-06-24 |
NCT00776516 | Pharmacokinetics of YM178 | Drug: mirabegron|Drug: rifampin | Astellas Pharma Inc | Phase 1 | 2008-10-01 | 2013-07-01 |
NCT01478568 | Pharmacokinetics of Mirabegron|Healthy Subjects | Drug: mirabegron|Drug: desipramine | Astellas Pharma Inc | Phase 1 | 2008-10-01 | 2014-04-08 |
NCT01747564 | Healthy Subjects|Plasma Concentration of Mirabegron | Drug: YM178 (mirabegron) | Astellas Pharma Inc | Phase 1 | 2012-08-01 | 2012-12-10 |
NCT02211846 | Pharmacokinetics of Mirabegron|Neurogenic Detrusor Overactivity|Overactive Bladder | Drug: Mirabegron | Astellas Pharma Inc|Astellas Pharma Europe B.V. | Phase 1 | 2014-07-01 | 2015-10-02 |
NCT01478529 | Pharmacokinetics of Mirabegron|Bioavailability|Healthy Subjects | Drug: mirabegron OCAS|Drug: mirabegron | Astellas Pharma Inc | Phase 1 | 2006-02-01 | 2013-06-25 |
NCT02495389 | Overactive Bladder | Drug: mirabegron | Loyola University|Astellas Pharma US, Inc. | Phase 4 | 2015-01-01 | 2017-03-09 |
NCT02916693 | Erectile Dysfunction|Overactive Bladder|Urinary Incontinence | Drug: Mirabegron | Johns Hopkins University|Astellas Pharma US, Inc. | Phase 1|Phase 2 | 2016-09-01 | 2016-09-23 |
NCT01285596 | Healthy Volunteers|Pharmacokinetics of Mirabegron | Drug: Mirabegron | Astellas Pharma Inc | Phase 1 | 2009-03-01 | 2013-07-01 |
NCT02981459 | Urinary Frequency/Urgency|Bladder Irritable|Bladder Pain Syndrome | Drug: Mirabegron | State University of New York at Buffalo|Astellas Pharma Inc | Phase 4 | 2017-01-01 | 2016-12-02 |
NCT01478490 | Pharmacokinetics of Mirabegron|Healthy Subjects | Drug: mirabegron|Drug: metoprolol | Astellas Pharma Inc | Phase 1 | 2002-09-01 | 2014-04-08 |
NCT01297192 | Healthy Volunteers|Pharmacokinetics of Mirabegron | Drug: solifenacin succinate|Drug: mirabegron | Astellas Pharma Inc | Phase 1 | 2009-03-01 | 2013-07-25 |
NCT02044510 | Urinary Bladder, Neurogenic | Drug: Mirabegron|Drug: Placebo | Lawson Health Research Institute | Phase 2|Phase 3 | 2014-07-01 | 2017-03-21 |
NCT01284868 | Healthy Volunteers|Pharmacodynamics of Mirabegron | Drug: mirabegron|Drug: Bisoprolol|Drug: propranolol|Drug: placebo | Astellas Pharma Inc | Phase 1 | 2009-07-01 | 2013-07-01 |
NCT02570035 | Overactive Bladder|Cardiovascular Disease | Drug: Mirabegron | Astellas Pharma Inc | 2012-12-01 | 2015-10-06 | |
NCT02751931 | Neurogenic Detrusor Overactivity | Drug: Mirabegron | Astellas Pharma Europe B.V.|Astellas Pharma Inc | Phase 3 | 2016-06-01 | 2016-12-27 |
NCT01334905 | Healthy Volunteer|Pharmacokinetics of YM178 | Drug: YM178 | Astellas Pharma Inc|Astellas Pharma Taiwan, Inc. | Phase 1 | 2011-03-01 | 2013-06-10 |
NCT00965926 | Healthy Volunteer|Pharmacokinetics of YM178 | Drug: YM178 | Astellas Pharma Inc | Phase 1 | 2009-07-01 | 2013-07-15 |
NCT01964183 | Pharmacokinetics of Mirabegron and Tolterodine|Healthy | Drug: tolterodine|Drug: mirabegron | Astellas Pharma Inc | Phase 4 | 2013-06-01 | 2013-10-15 |
NCT00912964 | Urinary Bladder, Overactive | Drug: Mirabegron|Drug: Placebo | Astellas Pharma Inc | Phase 3 | 2009-04-01 | 2015-06-05 |
NCT02536976 | Parkinson Disease|Overactive Bladder|Impaired Cognition | Drug: mirabegron|Drug: Placebo | HealthPartners Institute | Phase 4 | 2015-12-01 | 2016-10-25 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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