Suppr超能文献

选择性雄激素受体调节剂:雄激素治疗的未来?

Selective androgen receptor modulators: the future of androgen therapy?

作者信息

Christiansen Andrew R, Lipshultz Larry I, Hotaling James M, Pastuszak Alexander W

机构信息

University of Utah School of Medicine, Salt Lake City, UT, USA.

Scott Department of Urology.

出版信息

Transl Androl Urol. 2020 Mar;9(Suppl 2):S135-S148. doi: 10.21037/tau.2019.11.02.

Abstract

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.

摘要

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。

相似文献

1
Selective androgen receptor modulators: the future of androgen therapy?
Transl Androl Urol. 2020 Mar;9(Suppl 2):S135-S148. doi: 10.21037/tau.2019.11.02.
2
Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications.
Sex Med Rev. 2019 Jan;7(1):84-94. doi: 10.1016/j.sxmr.2018.09.006. Epub 2018 Nov 30.
3
Development of selective androgen receptor modulators (SARMs).
Mol Cell Endocrinol. 2018 Apr 15;465:134-142. doi: 10.1016/j.mce.2017.06.013. Epub 2017 Jun 15.
5
Analysis of the growing public interest in selective androgen receptor modulators.
Andrologia. 2021 Dec;53(11):e14238. doi: 10.1111/and.14238. Epub 2021 Sep 12.
7
Identification of an anabolic selective androgen receptor modulator that actively induces death of androgen-independent prostate cancer cells.
J Steroid Biochem Mol Biol. 2014 Sep;143:29-39. doi: 10.1016/j.jsbmb.2014.02.005. Epub 2014 Feb 22.
10
Drug-Induced Liver Injury Secondary to Enobosarm: A Selective Androgen Receptor Modulator.
J Med Cases. 2022 May;13(5):244-248. doi: 10.14740/jmc3937. Epub 2022 May 7.

引用本文的文献

1
When Gains Go Wrong: A Case of Selective Androgen Receptor Modulator-Related Liver Injury.
Cureus. 2025 Jul 6;17(7):e87376. doi: 10.7759/cureus.87376. eCollection 2025 Jul.
2
Sarcopenic obesity in the Asia-Pacific region: Epidemiology, risk factors, and management.
Osteoporos Sarcopenia. 2025 Jun;11(2 Suppl):40-49. doi: 10.1016/j.afos.2025.05.001. Epub 2025 May 21.
4
A Computational and In Vitro Appraisal of Ostarine to Target Androgen Receptor in Glioma C6 Cells.
Cell Biochem Biophys. 2025 Jun 13. doi: 10.1007/s12013-025-01797-0.
5
Hallmarks of Cancer Cachexia: Sexual Dimorphism in Related Pathways.
Int J Mol Sci. 2025 Apr 22;26(9):3952. doi: 10.3390/ijms26093952.
6
Discovery and development of steroidal enzyme inhibitors as anti-cancer drugs: state-of-the-art and future perspectives.
J Enzyme Inhib Med Chem. 2025 Dec;40(1):2483818. doi: 10.1080/14756366.2025.2483818. Epub 2025 Apr 2.
7
Clinical research framework proposal for ketogenic metabolic therapy in glioblastoma.
BMC Med. 2024 Dec 5;22(1):578. doi: 10.1186/s12916-024-03775-4.
9
Reversible Gynecomastia and Hypogonadism Due to Usage of Commercial Performance-Enhancing Supplement Use.
JCEM Case Rep. 2024 Aug 14;2(8):luae148. doi: 10.1210/jcemcr/luae148. eCollection 2024 Aug.

本文引用的文献

1
Selective androgen receptor modulator, S42 has anabolic and anti-catabolic effects on cultured myotubes.
Biochem Biophys Rep. 2019 Jan 15;17:177-181. doi: 10.1016/j.bbrep.2019.01.006. eCollection 2019 Mar.
2
What are the criteria for response to cachexia treatment?
Ann Palliat Med. 2019 Jan;8(1):43-49. doi: 10.21037/apm.2018.12.08.
3
Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications.
Sex Med Rev. 2019 Jan;7(1):84-94. doi: 10.1016/j.sxmr.2018.09.006. Epub 2018 Nov 30.
6
Human in vivo metabolism study of LGD-4033.
Drug Test Anal. 2018 Nov;10(11-12):1635-1645. doi: 10.1002/dta.2512. Epub 2018 Nov 8.
7
The relationship between muscle mass and function in cancer cachexia: smoke and mirrors?
Curr Opin Support Palliat Care. 2018 Dec;12(4):439-444. doi: 10.1097/SPC.0000000000000381.
8
GSK2881078, a SARM, Produces Dose-Dependent Increases in Lean Mass in Healthy Older Men and Women.
J Clin Endocrinol Metab. 2018 Sep 1;103(9):3215-3224. doi: 10.1210/jc.2017-02644.
9
Novel Therapy for Male Hypogonadism.
Curr Urol Rep. 2018 Jun 9;19(8):63. doi: 10.1007/s11934-018-0816-x.
10
Evaluation of ostarine as a selective androgen receptor modulator in a rat model of postmenopausal osteoporosis.
J Bone Miner Metab. 2019 Mar;37(2):243-255. doi: 10.1007/s00774-018-0929-9. Epub 2018 May 21.

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验