Boeri Luca, Capogrosso Paolo, Ventimiglia Eugenio, Serino Alessandro, La Croce Giovanni, Russo Andrea, Damiano Rocco, Montorsi Francesco, Salonia Andrea
a Division of Experimental Oncology/Unit of Urology , URI, IRCCS Ospedale San Raffaele , Milan , Italy.
b Università Vita-Salute San Raffaele & Division of Experimental Oncology/Unit of Urology, URI, IRCCS Ospedale San Raffaele , Milan , Italy.
Expert Rev Clin Pharmacol. 2016 Sep;9(9):1171-81. doi: 10.1080/17512433.2016.1195261. Epub 2016 Jun 13.
Phosphodiesterase type 5 inhibitors (PDE5Is) represent the first-line treatment for erectile dysfunction (ED). Almost one in two patients, however, show some level of treatment dissatisfaction and up to 30% fail to respond to any of the currently available PDE5Is. Recently, the second-generation PDE5I avanafil was launched for the treatment of ED.
Pivotal studies of clinical development along with placebo-controlled randomized clinical trials (RCTs) of avanafil in patients with ED were reviewed. Studies concerning the pharmacokinetics and pharmacodynamic of the drug were also analysed. A systematic literature search for English-language studies published up to May 2016 using the Medline database was performed. The search included the terms avanafil and ED. Expert commentary: Avanafil is a potent, highly selective PDE5I whose efficacy is comparable to that of currently available PDE5Is in both naïve and previous PDE5I users. Avanafil is effective within approximately 15 minutes of dosing, thus representing the only PDE5I approved for as-needed use, 15 to 30 minutes before sexual activity. Avanafil has high selectivity for the PDE5 isoenzyme, thus resulting in a lower incidence of drug-related side effects compared to other PDE5Is.
5型磷酸二酯酶抑制剂(PDE5Is)是勃起功能障碍(ED)的一线治疗药物。然而,几乎每两名患者中就有一人对治疗存在一定程度的不满,高达30%的患者对目前任何一种PDE5Is均无反应。最近,第二代PDE5I阿伐那非被批准用于治疗ED。
回顾了阿伐那非在ED患者中的关键临床开发研究以及安慰剂对照随机临床试验(RCTs)。还分析了有关该药物药代动力学和药效学的研究。使用Medline数据库对截至2016年5月发表的英文研究进行了系统的文献检索。检索词包括阿伐那非和ED。
阿伐那非是一种强效、高度选择性的PDE5I,其疗效在初治患者和既往使用过PDE5Is的患者中均与现有PDE5Is相当。阿伐那非在给药后约15分钟内起效,因此是唯一被批准在性活动前15至30分钟按需使用的PDE5I。阿伐那非对PDE5同工酶具有高度选择性,因此与其他PDE5Is相比,药物相关副作用的发生率较低。