University of Genoa, Institute for Cancer Research, San Martino Hospital, Department of Obstetrics and Gynecology, Genoa, Italy.
Expert Opin Pharmacother. 2013 Jul;14(10):1383-97. doi: 10.1517/14656566.2013.796930. Epub 2013 May 6.
Imidafenacin (KRP-197/ONO-8025) is the latest antimuscarinic (AM) developed for the treatment of overactive bladder syndrome (OAB) and, at the moment, it is marketed only in Japan. This compound has been developed to improve the tolerability of AM therapy by binding specifically the M3 receptor subtype, thus limiting undesirable adverse events (AEs).
This systematic review offers a brief explanation of the mechanism of action and of the pharmacokinetics of imidafenacin and helps readers to understand the clinical efficacy, tolerability, and safety of the compound in the setting of OAB therapy.
Imidafenacin is an AM drug with excellent efficacy, tolerability, and safety. It is indicated for patients with nocturia, nocturnal polyuria, and benign prostatic hyperplasia. This compound, due to its pharmacokinetic properties, gives the opportunity to be easily adjusted in its dosages. Further studies should assess the pharmacokinetics, clinical efficacy, safety, and tolerability of imidafenacin in Caucasian and African populations because this AM agent, at the moment, has been evaluated just in Asian populations. More studies should evaluate and compare efficacy, safety, and tolerability of imidafenacin also with other largely utilized AMs, such as oxybutynin, tolterodine, and fesoterodine, or with the other M3 selective compound, darifenacin.
依美斯汀（KRP-197/ONO-8025）是最新研发的抗毒蕈碱药物（AM），用于治疗膀胱过度活动症（OAB），目前仅在日本上市。该化合物旨在通过特异性结合 M3 受体亚型来提高 AM 治疗的耐受性，从而限制不良事件（AE）的发生。
本系统评价简要阐述了依美斯汀的作用机制和药代动力学，有助于读者了解其在 OAB 治疗中的临床疗效、耐受性和安全性。
依美斯汀是一种疗效、耐受性和安全性良好的 AM 药物。适用于夜尿症、夜间多尿症和良性前列腺增生症患者。鉴于其药代动力学特性，该化合物在剂量调整方面具有优势。进一步的研究应评估依美斯汀在白种人和非洲人群中的药代动力学、临床疗效、安全性和耐受性，因为该 AM 药物目前仅在亚洲人群中进行了评估。更多的研究还应评估并比较依美斯汀与其他广泛应用的 AM 药物（如奥昔布宁、托特罗定和非索罗定）或与其他 M3 选择性化合物达非那新的疗效、安全性和耐受性。
