Christiansen Andrew R, Lipshultz Larry I, Hotaling James M, Pastuszak Alexander W
University of Utah School of Medicine, Salt Lake City, UT, USA.
Scott Department of Urology.
Transl Androl Urol. 2020 Mar;9(Suppl 2):S135-S148. doi: 10.21037/tau.2019.11.02.
Selective androgen receptor modulators (SARMs) are small molecule drugs that function as either androgen receptor (AR) agonists or antagonists. Variability in AR regulatory proteins in target tissues permits SARMs to selectively elicit anabolic benefits while eschewing the pitfalls of traditional androgen therapy. SARMs have few side effects and excellent oral and transdermal bioavailability and may, therefore, represent viable alternatives to current androgen therapies. SARMs have been studied as possible therapies for many conditions, including osteoporosis, Alzheimer's disease, breast cancer, stress urinary incontinence (SUI), prostate cancer (PCa), benign prostatic hyperplasia (BPH), male contraception, hypogonadism, Duchenne muscular dystrophy (DMD), and sarcopenia/muscle wasting/cancer cachexia. While there are no indications for SARMs currently approved by the Food and Drug Administration (FDA), many potential applications are still being explored, and results are promising. In this review, we examine the literature assessing the use of SARMS for a number of indications.
选择性雄激素受体调节剂(SARMs)是一类小分子药物,可作为雄激素受体(AR)激动剂或拮抗剂发挥作用。靶组织中AR调节蛋白的变异性使SARMs能够选择性地产生合成代谢益处,同时避免传统雄激素疗法的弊端。SARMs副作用少,口服和经皮生物利用度极佳,因此可能成为当前雄激素疗法的可行替代方案。SARMs已被研究作为多种病症的可能治疗方法,包括骨质疏松症、阿尔茨海默病、乳腺癌、压力性尿失禁(SUI)、前列腺癌(PCa)、良性前列腺增生(BPH)、男性避孕、性腺功能减退、杜氏肌营养不良症(DMD)以及肌肉减少症/肌肉萎缩/癌症恶病质。虽然目前美国食品药品监督管理局(FDA)尚未批准任何关于SARMs的适应症,但许多潜在应用仍在探索中,且结果很有前景。在本综述中,我们研究了评估SARMs在多种适应症中使用情况的文献。