选择性雄激素受体调节剂治疗骨质疏松症的研究

Research progress of selective androgen receptor modulators for treatment of osteoporosis

骨质疏松症(osteoporosis,OP)是常见的临床疾病,对于该疾病的治疗仍以药物治疗为主。选择性雄激素受体调节剂(selective androgen receptor modulators,SARMs)是一种具有组织选择性的激动剂,可以对骨组织的雄激素受体(androgen receptor,AR)产生强大合成代谢作用,同时又降低了传统雄激素治疗带来的副作用,因此被认为是有前途的OP雄激素药物治疗的替代品。目前,多项OP相关的临床前研究表明SARMs具有治疗效果,其中有些进入了临床试验阶段。本综述通过阐述雄激素与骨组织AR之间的关系,解释SARMs治疗OP的可能机制,并就SARMs的研究进展进行总结。

Osteoporosis(OP)is a common clinical disease,and the treatment of this disease is still mainly drug therapy.Selective androgen receptor modulators(SARMs)are agonists with tissue selectivity,which have potent anabolic effect on androgen receptor(AR)of bone tissue and minimize the side effects of traditional androgen replacement therapy(ART),therefore,SARMs are considered as promising alternatives to androgen drug therapy.At present,multiple preclinical studies related to osteoporosis suggested that SARMs may have therapeutic effect,and some of them have entered clinical trials.By elaborating relationship between androgen and AR of bone tissue,his review proposes possible mechanisms to explain therapeutic effect of SARMs for OP and then summarizes the progress of SARMs researches.