SARMs Meaning: What Selective Androgen Receptor Modulators Are and Why the Term Is Used
SARMs stands for "selective androgen receptor modulators," a class of synthetic, nonsteroidal compounds designed to bind androgen receptors with tissue-selective effects on muscle and bone, none of which is approved by the FDA for human use.
Key takeaways
What SARM Stands For
SARM is an acronym for selective androgen receptor modulator. The NCBI Bookshelf LiverTox database describes SARMs as a group of orally available, synthetic, nonsteroidal drugs that bind androgen receptors with tissue-selective activity that preserves anabolic actions on muscle and bone, but with fewer and milder androgenic effects on organs such as the prostate, skin, hair, liver, and heart. The same source notes that several such agents were developed and evaluated as therapy for cancer cachexia, osteoporosis, and age-related bone and muscle wasting, but that none has been approved for human use.
The term distinguishes these molecules from anabolic-androgenic steroids, which share the same steroid ring structure as testosterone. Because SARMs are nonsteroidal, they are structurally different from testosterone and its derivatives even though they are designed to act on the same androgen receptor.
Ostarine, LGD-4033, RAD140: Are All SARMs the Same?
Several distinct molecules are grouped under the SARM label, and they are not interchangeable in terms of chemical structure, evidence base, or degree of study. Enobosarm (ostarine, GTx-024, MK-2866) has one of the longest clinical development histories of any SARM, having been studied in phase 1 and phase 2 trials and then in the pivotal phase 3 POWER 1 and POWER 2 trials, two identically designed randomized, double-blind, placebo-controlled trials that assessed enobosarm's effect on lean body mass and physical function in patients with non-small-cell lung cancer starting chemotherapy. Both POWER trials failed to meet their co-primary endpoints of improvement in lean body mass and physical function, despite earlier phase 2 signals of benefit. Enobosarm has more recently been studied in a placebo-controlled phase 2b trial in combination with a GLP-1 receptor agonist for body composition in older adults with obesity; the developer has reported meeting the trial's primary endpoint in a topline company announcement, but independent peer-reviewed publication of these results was not identified in this review.
LGD-4033 (ligandrol) has undergone early-phase human study but has substantially less late-stage clinical trial data than enobosarm. It is also one of the SARMs most frequently implicated in published cases of drug-induced liver injury, including reports of severe cholestatic hepatitis confirmed by liver biopsy in a previously healthy man who had taken the compound for about two weeks, and a separate case of jaundice and elevated liver enzymes after three months of use.
RAD140 (testolone) is described in case-report literature as a novel SARM with very limited data available on its adverse-effect profile, despite being readily accessible on the consumer market. Multiple case reports describe cholestatic drug-induced liver injury in people who used RAD140 as an over-the-counter bodybuilding product, including cases with markedly elevated bilirubin that resolved after the product was stopped. One case-report author group concluded that RAD140 and other SARMs should be used with caution and under close clinical supervision until further hepatic safety data become available, given their potential hepatotoxicity and ready availability on the consumer market.
Andarine (S-4) is another nonsteroidal compound marketed as a SARM. It appears among the compounds analyzed in a 2017 JAMA study of SARM products purchased online, which found that only 23 of 44 products (52%) contained a labeled SARM ingredient such as ostarine, ligandrol, or andarine, often not in the amount stated on the label, while other products contained different unapproved drugs or, in a few cases, no active ingredient at all.
None of these compounds is FDA-approved, and the depth of human safety data differs considerably between them. Enobosarm has the most extensive trial record of any SARM, having progressed through phase 3 testing, whereas RAD140, LGD-4033, and other compounds sold under "research chemical" labeling have comparatively little controlled human data and rely mainly on case reports and small early-phase studies for their safety picture.
Frequently asked
References
- Selective Androgen Receptor Modulators - LiverTox
- Bodybuilding Products: SARMs Cause Harm
- Study Design and Rationale for the Phase 3 Clinical Development Program of Enobosarm... (POWER Trials)
- Enobosarm - an overview
- Ligandrol (LGD-4033)-Induced Liver Injury
- LGD-4033 and a Case of Drug-Induced Liver Injury
- RAD-140 Drug-Induced Liver Injury
- Idiosyncratic drug-induced liver injury related to use of novel selective androgen receptor modulator RAD140 (Testalone): a case report
- Severe liver injury following use of RAD-140, a selective androgen receptor modulator, for body building
- Selective Androgen Receptor Modulators Leading to Liver Injury: A Case Report
- SARMs sold online often contain unapproved drugs, study says
- The Prohibited List
- Selective Androgen Receptor Modulators (SARMs)
- Verus enobosarm meets primary endpoint in Phase 2b weight reduction trial
- Selective Androgen Receptor Modulators (SARMs)
This page is for education and does not provide medical or legal advice. No SARM is approved for human use.