Earl Joshua A, Kim Edward D
a Department of Urology , University of Tennessee, Graduate School of Medicine , Knoxville , TN , USA.
Expert Rev Endocrinol Metab. 2019 May;14(3):157-165. doi: 10.1080/17446651.2019.1612239. Epub 2019 May 7.
Hypogonadism is an important issue among the male population. Treatments such as exogenous testosterone have become very popular. One of the adverse effects of testosterone is its suppression of fertility. This has lead to the use of alternative therapies such as selective estrogen receptor modulators (SERMs) that aim to correct hypogonadism without reducing fertility. Areas covered: The SERM, clomiphene citrate, which is approved by the FDA for the treatment of ovarian dysfunction, has been shown to have beneficial effects on male hypogonadism. Clomiphene citrate exists as a mixture of both the cis-isomer (zuclomiphene) and the trans-isomer (enclomiphene). The literature has suggested that most of the beneficial effects of clomiphene are due to the trans-isomer enclomiphene. Zuclomiphene contributes little to the intended outcomes. The purpose of this drug profile is to examine the available literature on the trans-isomer enclomiphene. Expert opinion: Enclomiphene has been shown to increase testosterone levels while stimulating FSH and LH production. Initial studies demonstrated that enclomiphene maintains the androgenic benefit of clomiphene citrate without the undesirable effects attributable to zuclomiphene. This article reviews the difficulties associated with the FDA approval of a new molecular entity related to the treatment of hypogonadism.
性腺功能减退在男性群体中是一个重要问题。外源性睾酮等治疗方法已变得非常普遍。睾酮的不良反应之一是抑制生育能力。这导致了诸如选择性雌激素受体调节剂(SERM)等替代疗法的使用,这些疗法旨在纠正性腺功能减退而不降低生育能力。涵盖领域:已获美国食品药品监督管理局(FDA)批准用于治疗卵巢功能障碍的SERM枸橼酸氯米芬,已被证明对男性性腺功能减退有有益作用。枸橼酸氯米芬以顺式异构体(左氯米芬)和反式异构体(恩氯米芬)的混合物形式存在。文献表明,氯米芬的大部分有益作用归因于反式异构体恩氯米芬。左氯米芬对预期结果贡献不大。本药物简介的目的是研究关于反式异构体恩氯米芬的现有文献。专家意见:已证明恩氯米芬可提高睾酮水平,同时刺激促卵泡生成素(FSH)和促黄体生成素(LH)的产生。初步研究表明,恩氯米芬保留了枸橼酸氯米芬的雄激素益处,而没有左氯米芬带来的不良影响。本文综述了与FDA批准一种与性腺功能减退治疗相关的新分子实体有关的困难。