Literature DB >> 30503797

Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications.

Zachary J Solomon1, Jorge Rivera Mirabal2, Daniel J Mazur3, Taylor P Kohn4, Larry I Lipshultz5, Alexander W Pastuszak6.   

Abstract

INTRODUCTION: Selective androgen receptor modulators (SARMs) differentially bind to androgen receptors depending on each SARM's chemical structure. As a result, SARMs result in anabolic cellular activity while avoiding many of the side effects of currently available anabolic steroids. SARMs have been studied in the treatment of breast cancer and cachexia and have also been used as performance-enhancing agents. Here, we evaluate and summarize the current literature on SARMs. AIM: To present the background, mechanisms, current and potential clinical applications, as well as risks and benefits of SARMs.
METHODS: A literature review was performed in MEDLINE using the terms selective androgen receptor modulator, hypogonadism, cachexia, breast cancer, benign prostatic hyperplasia, libido, and lean muscle mass. Both basic research and clinical studies were included. MAIN OUTCOME MEASURE: To complete a review of peer-reviewed literature.
RESULTS: Although there are currently no U.S. Food and Drug Agency-approved indications for SARMs, investigators are exploring the potential uses for these compounds. Basic research has focused on the pharmacokinetics and pharmacodynamics of these agents, demonstrating good availability with a paucity of drug interactions. Early clinical studies have demonstrated potential uses for SARMs in the treatment of cancer-related cachexia, benign prostatic hyperplasia (BPH), hypogonadism, and breast cancer, with positive results.
CONCLUSION: SARMs have numerous possible clinical applications, with promise for the safe use in the treatment of cachexia, BPH, hypogonadism, breast cancer, and prostate cancer. Solomon ZJ, Mirabal JR, Mazur DJ, et al. Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications. Sex Med Rev 2019;7:84-94.
Copyright © 2018 International Society for Sexual Medicine. Published by Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Androgens; Drug-Related Side Effects and Adverse Reactions; Hypogonadism; Selective Androgen Receptor Modulators

Mesh:

Substances:

Year:  2018        PMID: 30503797      PMCID: PMC6326857          DOI: 10.1016/j.sxmr.2018.09.006

Source DB:  PubMed          Journal:  Sex Med Rev        ISSN: 2050-0521


  54 in total

Review 1.  Selective estrogen receptor modulation: a personal perspective.

Authors:  V C Jordan
Journal:  Cancer Res       Date:  2001-08-01       Impact factor: 12.701

2.  Testosterone protects from metabolic syndrome-associated prostate inflammation: an experimental study in rabbit.

Authors:  Linda Vignozzi; Annamaria Morelli; Erica Sarchielli; Paolo Comeglio; Sandra Filippi; Ilaria Cellai; Elena Maneschi; Sergio Serni; Mauro Gacci; Marco Carini; Marie-Pierre Piccinni; Farid Saad; Luciano Adorini; Gabriella B Vannelli; Mario Maggi
Journal:  J Endocrinol       Date:  2011-10-18       Impact factor: 4.286

3.  Safety, pharmacokinetics and pharmacological effects of the selective androgen receptor modulator, GSK2881078, in healthy men and postmenopausal women.

Authors:  Richard V Clark; Ann C Walker; Susan Andrews; Philip Turnbull; Jeffrey A Wald; Mindy H Magee
Journal:  Br J Clin Pharmacol       Date:  2017-06-10       Impact factor: 4.335

4.  Longitudinal assessment of serum free testosterone concentration predicts memory performance and cognitive status in elderly men.

Authors:  Scott D Moffat; Alan B Zonderman; E Jeffrey Metter; Marc R Blackman; S Mitchell Harman; Susan M Resnick
Journal:  J Clin Endocrinol Metab       Date:  2002-11       Impact factor: 5.958

5.  BA321, a novel carborane analog that binds to androgen and estrogen receptors, acts as a new selective androgen receptor modulator of bone in male mice.

Authors:  Kenta Watanabe; Michiko Hirata; Tsukasa Tominari; Chiho Matsumoto; Yasuyuki Endo; Gillian Murphy; Hideaki Nagase; Masaki Inada; Chisato Miyaura
Journal:  Biochem Biophys Res Commun       Date:  2016-07-09       Impact factor: 3.575

6.  Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140.

Authors:  Chris P Miller; Maysoun Shomali; C Richard Lyttle; Louis St L O'Dea; Hillary Herendeen; Kyla Gallacher; Dottie Paquin; Dennis R Compton; Bishwabhusan Sahoo; Sean A Kerrigan; Matthew S Burge; Michael Nickels; Jennifer L Green; John A Katzenellenbogen; Alexei Tchesnokov; Gary Hattersley
Journal:  ACS Med Chem Lett       Date:  2010-12-02       Impact factor: 4.345

7.  Androgenic/Anabolic steroid-induced toxic hepatitis.

Authors:  Davor Stimac; Sandra Milić; Renata Dobrila Dintinjana; Drazen Kovac; Smiljana Ristić
Journal:  J Clin Gastroenterol       Date:  2002-10       Impact factor: 3.062

8.  Preclinical characterization of a (S)-N-(4-cyano-3-trifluoromethyl-phenyl)-3-(3-fluoro, 4-chlorophenoxy)-2-hydroxy-2-methyl-propanamide: a selective androgen receptor modulator for hormonal male contraception.

Authors:  Amanda Jones; Jiyun Chen; Dong Jin Hwang; Duane D Miller; James T Dalton
Journal:  Endocrinology       Date:  2008-09-04       Impact factor: 4.736

9.  Optimizing Ligand Efficiency of Selective Androgen Receptor Modulators (SARMs).

Authors:  Anthony L Handlon; Lee T Schaller; Lisa M Leesnitzer; Raymond V Merrihew; Chuck Poole; John C Ulrich; Joseph W Wilson; Rodolfo Cadilla; Philip Turnbull
Journal:  ACS Med Chem Lett       Date:  2015-11-19       Impact factor: 4.345

10.  Antiinflammatory effect of androgen receptor activation in human benign prostatic hyperplasia cells.

Authors:  Linda Vignozzi; Ilaria Cellai; Raffaella Santi; Letizia Lombardelli; Annamaria Morelli; Paolo Comeglio; Sandra Filippi; Federica Logiodice; Marco Carini; Gabriella Nesi; Mauro Gacci; Marie-Pierre Piccinni; Luciano Adorini; Mario Maggi
Journal:  J Endocrinol       Date:  2012-05-04       Impact factor: 4.286

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  23 in total

Review 1.  The importance of androgen receptors in breast cancer.

Authors:  Irina Niţă; Cornelia Niţipir; Ştefania Andreea Toma; Alexandra Maria Limbău; Edvina Pîrvu; Ioana Anca Bădărău
Journal:  Med Pharm Rep       Date:  2021-07-29

Review 2.  Testosterone Replacement Therapy in Hypogonadal Men.

Authors:  Christina Wang; Ronald S Swerdloff
Journal:  Endocrinol Metab Clin North Am       Date:  2022-02-08       Impact factor: 4.741

3.  The Liver X Receptor Is Selectively Modulated to Differentially Alter Female Mammary Metastasis-associated Myeloid Cells.

Authors:  Liqian Ma; Hashni Epa Vidana Gamage; Srishti Tiwari; Chaeyeon Han; Madeline A Henn; Natalia Krawczynska; Payam Dibaeinia; Graeme J Koelwyn; Anasuya Das Gupta; Rafael Ovidio Bautista Rivas; Chris L Wright; Fangxiu Xu; Kathryn J Moore; Saurabh Sinha; Erik R Nelson
Journal:  Endocrinology       Date:  2022-07-01       Impact factor: 5.051

Review 4.  Understanding and managing the suppression of spermatogenesis caused by testosterone replacement therapy (TRT) and anabolic-androgenic steroids (AAS).

Authors:  Ankit Desai; Musaab Yassin; Axel Cayetano; Tharu Tharakan; Channa N Jayasena; Suks Minhas
Journal:  Ther Adv Urol       Date:  2022-06-26

5.  Role for androgens in determination of ovarian fate in the common snapping turtle, Chelydra serpentina.

Authors:  Anthony Schroeder; Turk Rhen
Journal:  Gen Comp Endocrinol       Date:  2019-05-03       Impact factor: 2.822

Review 6.  The role of the androgen receptor in the pathogenesis of obesity and its utility as a target for obesity treatments.

Authors:  Varun S Venkatesh; Mathis Grossmann; Jeffrey D Zajac; Rachel A Davey
Journal:  Obes Rev       Date:  2022-01-27       Impact factor: 10.867

Review 7.  Selective androgen receptor modulators: the future of androgen therapy?

Authors:  Andrew R Christiansen; Larry I Lipshultz; James M Hotaling; Alexander W Pastuszak
Journal:  Transl Androl Urol       Date:  2020-03

Review 8.  Androgen Treatment in Adolescent Males With Hypogonadism.

Authors:  Rodolfo A Rey; Romina P Grinspon
Journal:  Am J Mens Health       Date:  2020 May-Jun

9.  Crucial role of androgen receptor in resistance and endurance trainings-induced muscle hypertrophy through IGF-1/IGF-1R- PI3K/Akt- mTOR pathway.

Authors:  Lijun Yin; Lin Lu; Xiaojing Lin; Xiaohui Wang
Journal:  Nutr Metab (Lond)       Date:  2020-03-30       Impact factor: 4.169

10.  Liver injury associated with the use of selective androgen receptor modulators and post-cycle therapy: Two case reports and literature review.

Authors:  Tomas Koller; Petra Vrbova; Iveta Meciarova; Pavol Molcan; Michal Smitka; Svetlana Adamcova Selcanova; Lubomir Skladany
Journal:  World J Clin Cases       Date:  2021-06-06       Impact factor: 1.337

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