Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications
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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.
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SARMs are orally administered and relatively well-tolerated with few adverse events, though concern exists as to whether these lead to hepatotoxicity and decreased levels of HDL cholesterol.
“These compounds are currently being investigated as treatment options for hypogonadism, as they are orally administered and are relatively well-tolerated with few adverse events, though some concern exists as to whether these lead to hepatotoxicity and decreased levels of HLD cholesterol (81).”
From Non-testosterone management of male hypogonadism: an examination of the existing literature (2020) · cites this paper as [81]
Excessive synaptic strengthening, prolonged translational disinhibition, or poorly calibrated excitability modulation could promote maladaptive plasticity, excitotoxic stress, epileptiform activity, or aberrant stabilization of pathological circuit states.
“Excessive synaptic strengthening, prolonged translational disinhibition, or poorly calibrated excitability modulation could promote maladaptive plasticity, excitotoxic stress, epileptiform activity, or aberrant stabilization of pathological circuit states.”
From Synaptic Plasticity—Intrinsic Excitability and Antidepressant Discovery (2026) · cites this paper as [435]
The Alzheimer’s disease section discusses testosterone, cognition, and amyloid, while the cachexia section discusses muscle protein synthesis and growth signaling. Neither addresses the claimed risks of excessive synaptic strengthening, translational disinhibition, or excitability modulation. Searches for maladaptive plasticity, excitotoxic stress, epileptiform activity, and pathological circuit states found no supporting passage in our copy. (LLM, conf=0.76)
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- Authors
- Solomon, Z. J., Mirabal, J. R., Mazur, D. J., Kohn, T. P., Lipshultz, L. I., & Pastuszak, A. W.
- Affiliations
- Baylor College of Medicine (US)
- Urology Associates (US)
- Johns Hopkins University (US)
- Corresponding author
- Pastuszak, Alexander W.
- Venue
- Sexual Medicine Reviews
- Publisher
- Oxford University Press (OUP)
- Published
- 2019-01
- Volume
- 7
- Issue
- 1
- Pages
- 84-94
- ISSN
- 2050-0513 (ISSN-L)
- 2050-0521
- PMC
- PMC6326857
- OpenAlex
- W2903095656
- Cited by
- 174
- References
- 61
- Citations by year
- 2026: 18 · 2025: 19 · 2024: 30 · 2023: 28 · 2022: 36 · 2021: 20 · 2020: 16 · 2019: 7
- FWCI
- 1.65
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Sexual Medicine Reviews (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Institute of Diabetes and Digestive and Kidney Diseases
- Urology Care Foundation
- Topics
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Hormonal and reproductive studies
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Prostate Cancer Treatment and Research
- Life Sciences › Agricultural and Biological Sciences › Animal Science and Zoology › Pharmacological Effects and Assays
- Keywords
- selective androgen receptor modulators, androgen receptor, anabolic steroids, cancer cachexia, benign prostatic hyperplasia, hypogonadism, breast cancer, prostate cancer, sexual desire, lean muscle mass, pharmacokinetics, pharmacodynamics
- MeSH terms
- Androgens, Breast Neoplasms, Cachexia, Clinical Trials as Topic, Female, Humans, Hypogonadism, Male, Prostatic Neoplasms, Receptors, Androgen, Androgen Receptor Antagonists
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