University of Pittsburgh, Pittsburgh, PA, USA.
Expert Opin Drug Metab Toxicol. 2013 May;9(5):617-27. doi: 10.1517/17425255.2013.786700. Epub 2013 Apr 4.
Mirabegron is a new once-daily, oral treatment for management of overactive bladder (OAB) that is approved in USA, EU and Japan. It activates β3 adrenoceptor to facilitate bladder filling and reduce mean micturition frequency with better safety profile than current treatment of antimuscarinic drugs.
The following article reviews the information available from published randomized trials on the metabolism and pharmacokinetics mirabegron. The reader will gain better insight into the variability in plasma exposure of mirabegron due to various causes. Propensity for drug interactions with mirabegron is low as its clearance involves multiple metabolic and excretory pathways. Mirabegron is generally well tolerated, but its pharmacokinetics is altered by dose and gender with implications for cardiovascular toxicity.
Mirabegron is a first-in-class of β3 adrenoceptor agonists that could offer an alternative to antimuscarinics for OAB patients. The marketed dose of 50 mg achieves primary efficacy endpoints but causes only modest improvement over placebo in terms of daily incontinence and voiding episodes. Involvement of saturable efflux transporters is indicated in oral bioavailability of mirabegron. It is well tolerated with hypertension, nasopharyngitis, urinary tract infection and headache being the most common side effects.
米拉贝隆是一种新型的每日一次口服药物，用于治疗膀胱过度活动症（OAB），已在美国、欧盟和日本获得批准。它通过激活β3 肾上腺素受体促进膀胱充盈，并减少平均排尿频率，安全性优于当前的抗毒蕈碱药物治疗。
本文综述了已发表的米拉贝隆代谢和药代动力学随机试验的相关信息。读者将更好地了解由于各种原因导致米拉贝隆的血浆暴露存在差异。由于其清除涉及多种代谢和排泄途径，因此药物相互作用的可能性较低。米拉贝隆通常具有良好的耐受性，但剂量和性别会改变其药代动力学，这可能会导致心血管毒性。
米拉贝隆是一种新型的β3 肾上腺素受体激动剂，可为 OAB 患者提供一种替代抗毒蕈碱药物的选择。目前市场上的 50mg 剂量可达到主要疗效终点，但与安慰剂相比，每日失禁和排尿次数仅略有改善。米拉贝隆的口服生物利用度表明存在可饱和的外排转运体。米拉贝隆具有良好的耐受性，最常见的副作用是高血压、鼻咽炎、尿路感染和头痛。
