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Selective androgen receptor modulator
Class of pharmaceutical drugs

Selective androgen receptor modulators (SARMs) are drugs that selectively activate the androgen receptor in specific tissues, promoting muscle and bone growth with fewer effects on male reproductive tissues like the prostate gland. Unlike non-selective steroidal anabolic androgenic steroids, SARMs offer potent benefits for conditions such as osteoporosis and cachexia. Though unapproved by the FDA or EMA, they have mild but notable side effects like elevated liver enzymes and HPG axis suppression. Since 2008, SARMs have been banned in sports by the World Anti-Doping Agency but remain available on gray markets.

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History

Steroidal androgens

Anabolic androgenic steroids (AAS) are used to treat a variety of medical conditions, but their side effects have fueled a search for a new class of drugs, with a better separation between desirable anabolic and undesirable androgenic effects. The first clinically used AAS was testosterone which was discovered in 1935 and first approved for medical use in 1939.1 AAS including those produced endogenously such as testosterone and dihydrotestosterone (DHT), bind to and activate the androgen receptor (AR) to produce their effects. AAS effects can be separated into androgenic (the development and maintenance of male sexual characteristics) and anabolic (increasing bone density, muscle mass and strength). AAS also affect hematopoiesis, coagulation, metabolism, and cognition.23 For most medical applications, an AAS with potent anabolic and minimal androgenic and cardiovascular effects would be an advantage.

In the 1930s, 17α-alkylated anabolic steroids were discovered. These have increased metabolic stability and are orally active, but are not tissue selective.4 These alkylated anabolic steroids still have significant androgenic effects, and are also hepatotoxic.56 In 1950, nandrolone (19-nortestosterone) was first synthesized, which is sometimes considered a SARM due to greater tissue selectivity than testosterone.789 In addition, 7α-alkyl substitution of testosterone (for example trestolone) has also been reported to increase its anabolic effects.10 However, efforts to develop a steroid with anabolic but minimal androgenic effects were not successful.11

SERMs

Interest in nonsteroidal AR mixed agonists/antagonists increased after the therapeutic uses of selective estrogen receptor modulators (SERMs) became evident.12 The first SERM, tamoxifen, was originally developed as an anti-estrogen contraceptive. However, it was discovered it promoted ovulation in humans by acting as an agonist in ovaries. The drug was then successfully repurposed as a treatment for breast cancer where it was found to act as a full antagonist in breast tissue.13 Somewhat unexpectedly, it was also discovered that tamoxifen preserves bone density14 by acting as an agonist in bone resorbing osteoclasts.15 The clinical success of SERMs stimulated interest in analogous tissue selective drugs that target the AR.16

Non-steroidal AR antagonists

The chemical starting point for AR mixed agonist/antagonists were nonsteroidal AR antiandrogens such as flutamide, nilutamide, bicalutamide. These antagonists work by binding to the AR to prevent androgenic action; this class of chemicals dates to the 1970s.1718 The discovery of arylpropionamides, which share structural similarity with bicalutamide and hydroxyflutamide, suggested a way to make compounds that bind to the AR and produce both anabolic and antiandrogenic effects.19 Selective androgen receptor modulators (SARMs) were developed out of a desire to maintain the anabolic effects of androgens on muscle and bone, while avoiding side effects on other tissues such as the prostate and cardiovascular system.20

Non-steroidal SARMs

The first non-steroidal SARMs were developed in 1998 independently by two research groups, one at the University of Tennessee that created an arylpropionamide SARM and Ligand Pharmaceuticals that made a SARM with a quinolone core structure. The name was adopted by analogy with SERMs.21 Other SARMs include tetrahydroquinolines, tricyclics, bridged tricyclics, aniline, diaryl aniline, bicylclic hydantoins, benzimidazole, imidazolopyrazole, indole, and pyrazoline derivatives.22 SARMs can be agonists, antagonists, or partial agonists of the AR depending on the tissue, which can enable targeting specific medical conditions while minimizing side effects.23 Those that have advanced to human trials show stronger effects in bone and muscle tissue and weaker effects in the prostate.24

Unlike most current forms of testosterone replacement, SARMs are orally bioavailable25 and largely eliminated via hepatic metabolism and metabolized through amide hydrolysis in the case of arylpropionamides and A-ring nitro reduction of andarine.26

Proposed treatment of hypogonadism

Because of the potentially better side effect profile of SARMs compared to testosterone, SARMs have been proposed for use in the treatment of hypogonadism and for androgen replacement therapy.272829 Phase I and II trials have provided preliminary evidence that the SARMs enobosarm and GSK-2881078 (in elderly men and postmenopausal women), and OPL-88004 (prostate cancer survivors with low levels of testosterone) increase lean body mass and muscle size with little effect on the prostate, supporting the potential of SARMs for use in hormone replacement therapy.30 However, it has been argued that SARMs are not ideal for use in androgen replacement therapy and could not replace testosterone in this context as they do not reproduce testosterone's full spectrum of effects, including androgenic potentiation via 5α-reduction and aromatization into estrogen.3132 Estrogenic signaling in particular is essential for normal male physiology and health, including for instance maintenance of bone strength.3334

Mechanism

The mechanism of action of SARMs' tissue-specific effects continues to be debated as of 2020.3536 A number of hypotheses have been advanced. These include the non-activation of SARMs by 5α-reductase, tissue selective expression of androgen receptor coregulators, non-genomic signaling, and tissue selective uptake of SARMs.3738

5α-Reductase

Testosterone is active in non-reproductive tissue without activation. In contrast, tissue selective activation by 5α-reductase to the more active form DHT is required for significant activity in reproductive tissue. The net result is that testosterone and its metabolite together are not tissue selective.39 SARMs are not substrates of 5α-reductase, hence they are not selectively activated like testosterone in tissues such as prostate.40 This lack of activation effectively imparts a degree of tissue selectivity to SARMs.41

Androgen receptor coregulators

Tissue selective transcription coregulator expression is another possible contributor to the selectivity of SARMs.4243 Like other type I nuclear receptors, the unliganded androgen receptor (AR) resides in the cytosol complexed with heat shock proteins (HSP). Upon ligand binding, the AR freed from HSPs and translocated into the nucleus where it binds to androgen response elements on DNA to regulate gene expression.44 AR agonists such as testosterone recruit coactivator proteins to AR that facilitate upregulation of gene expression while antagonists recruit corepressors which down regulate gene expression. Furthermore, the ratio of coactivators to corepressors is known to vary depending on tissue type.4546 Structurally, pure AR agonists stabilize the position of helix-12 (H12) in the ligand binding domain of AR near H3 and H4 to produce a surface cleft that binds to a FxxLF motif contained in coactivators.47 Conversely, antagonists destabilize the agonist conformation of H12 blocking the binding of the FXXLF coactivator motif while facilitating the binding of the corepressor LXX(I/H)IXXX(I/L) motif found in NCOR1 and SMRT corepressors.48

In analogy to SERMs, SARMs are mixed agonists/antagonists displaying agonist androgen receptor activity in bone and muscle and partial agonist or antagonist activity in other tissues such as prostate.4950 Non-selective agonists such as testosterone are able to recruit coactivators when bound to AR but not corepressors and hence are agonists in all tissues. In contrast, SARMs can recruit both coactivators and corepressors by partially destabilizing the agonist conformation of H12. In tissues where coactivators are in excess (as in bone and muscle), SARMs act as agonists. Conversely, in tissues where corepressors are in excess (such as prostate), SARMs act as partial agonists or antagonists.51

In vitro testing of the SARMs enobosarm (ostarine) and YK-11 showed that they bound to the AR, but unlike full AR agonists, they blocked interaction between the N-terminus and C-terminus of AR which resulted in a mixed agonist/antagonist mode of action.5253

Non-genomic signaling

In addition to the regulation of gene expression by nuclear AR, membrane associated AR is known to have rapid non-genomic effects on cells through signal transduction cascades. Non-genomic effects appear to significantly contribute to the anabolic effects of androgens whereas genomic effects are primarily responsible for the development of male sexual organs. Furthermore, each steroidal androgen or non-steroidal SARM uniquely influences distinct pathways depending on cell type.54

Tissue distribution

Tissue selective uptake into anabolic tissues presents another potential mechanism for SARM tissue selectivity. However autoradiography studies with radiolabeled SARMs show no preferential distribution to anabolic tissues.55

Drug candidates

SARM drug candidates5657
NameClassDeveloperInvestigated forHighest development stage reachedStructure
Andarine (S-4, GTx-007)ArylpropionamideGTx, Oncternal Therapeutics58Cachexia59Phase I (discontinued)60
Arcarine (ORM-11984)61Unknown62Orion Corporation63Benign prostatic hyperplasia, hypogonadism, osteoporosis64Phase I (discontinued)6566Structure undisclosed67
BMS-564,929 (PS-178990)Pyrroloimidazole68Bristol-Myers Squibb, Ligand Pharmaceuticals69Andropause, cachexia7071Phase I (discontinued)72737475
DT-200 (GLPG-0492)Imidazolidine-2,4-dioneProSkelia, Akashi Therapeutics, Galapagos NV76Muscular dystrophy, cachexia77Phase I787980
Enobosarm (ostarine, GTx-024, MK-2866, S-22)ArylpropionamideGTx, Veru Healthcare81Breast cancer, cachexia, muscular dystrophy, stress urinary incontinence82Phase III8384
GSK-971086Indole85GlaxoSmithKline86Sarcopenia87Phase I (discontinued)888990
GSK-2849466N-arylhydroxyalkyl 91GlaxoSmithKline92Cachexia, heart failure93Phase I (discontinued)949596
GSK-2881078IndoleGlaxoSmithKline97Cachexia9899Phase II100101
GTx-027ArylpropionamideGTx102103Breast cancer, stress urinary incontinence104105Phase I (discontinued)106107 or preclinical108
LGD-2941 (LGD-122941)QuinolinoneLigand Pharmaceuticals109Cachexia, sexual dysfunction, hypogonadism, menopause, osteoporosis110Phase I (discontinued)111
LGD-4033 (VK5211, ligandrol)PyrrolidinebenzonitrileLigand Pharmaceuticals112Muscle wasting due to hip fracture, cachexia, hypogonadism, osteoporosis113114Phase II115116
LY305N-arylhydroxyalkylEli Lilly117Osteoporosis118Phase I119
MK-0773 (PF-05314882)SteroidGTx, Merck120Sarcopenia, osteoporosis121122Phase II (discontinued)123124125126
MK-3984BenzylpropionamideMerckSarcopenia127Phase I128
OPK-88004 (LY-2452473, TT-701)IndoleEli Lilly, OPKO129Benign prostatic hyperplasia, quality of life in prostate cancer, erectile dysfunction130131Phase II132133
PF-06260414IsoquinolinePfizer134135Cachexia136Phase I (discontinued)137
Vosilasarm (RAD140, EP0062, testolone)PhenyloxadiazoleEllipsis138Breast cancer, osteoporosis, sarcopenia139Phase I/II140141
YK-11SteroidToho UniversityMuscle wasting142Preclinical

Certain anabolic steroids, like trestolone, dimethandrolone undecanoate, and 11β-methyl-19-nortestosterone dodecylcarbonate, have also sometimes been classified as SARMs.143

Possible therapeutic applications

Due to their tissue selectivity, SARMs have the potential to treat a wide variety of conditions, including debilitating diseases. They have been investigated in human studies for the treatment of osteoporosis, cachexia, benign prostatic hyperplasia, stress urinary incontinence, prostate cancer, and breast cancer and have also been considered for the treatment of Alzheimer's disease, Duchenne muscular dystrophy, hypogonadism and as a male contraceptive.144145 As of 2023, there are no SARMs which have been approved for therapeutic use by the United States Food and Drug Administration or the European Medicines Agency.146

Most SARMs have been tested in vitro or on rodents, while limited clinical trials in humans have been carried out.147148 Initial research focused on muscle wasting.149 Enobosarm (ostarine) is the most well-studied SARM; according to its manufacturer, GTx Incorporated, 25 studies have been carried out on more than 1,700 humans as of 2020 involving doses from 1 to 18 mg each day.150151 As of 2020, there is little research distinguishing different SARMs from each other.152 Much of the research on SARMs has been conducted by corporations and has not been made publicly available.153

Benign prostatic hyperplasia

In rat models of benign prostatic hyperplasia (BPH), a condition where the prostate is enlarged in the absence of prostate cancer, SARMs reduced the weight of the prostate.154 OPK-88004 advanced to a phase II trial in humans, but it was terminated due to difficulty in measuring prostate size, the trial's primary endpoint.155

Cancer

SARMs may help treat AR and estrogen receptor (ER) positive breast cancer, which comprise the majority of breast cancers.156157 AAS were historically used successfully to treat AR positive breast cancer, but were phased out after the development of antiestrogen therapies, due to androgenic side effects and concerns about aromatization to estrogen (which does not occur with SARMs).158159 Although a trial on AR positive triple negative breast cancer (which is ER-) was ended early due to lack of efficacy, enobosarm showed benefits in some patients with ER+, AR+ breast cancer in a phase II study. In patients with more than 40 percent AR positivity as determined by immunohistochemistry, the clinical benefit rate (CBR) was 80 percent and the objective response rate (ORR) was 48 percent—which was considered promising given that the patients had advanced disease and had been heavily pretreated.160161 In 2022, the FDA granted fast track designation to enobosarm for AR+, ER+, HER2- metastatic breast cancer.162 Other SARMs such as vosilasarm have reached clinical trials in breast cancer patients.163

Bone and muscle wasting

As of 2020, there are no drugs approved to treat muscle wasting in people with chronic diseases, and there is therefore an unmet need for anabolic drugs with few side effects. One aspect hindering drug approval for treatments for cachexia and sarcopenia (two types of muscle wasting) is disagreement in what outcomes would demonstrate the efficacy of a drug. Several clinical trials have found that SARMs improve lean mass in humans, but it is not clear whether strength and physical function are also improved. After promising results in a phase II trial, a phase III trial of enobosarm was proven to increase lean body mass but did not show significant improvement in function. It and other drugs have been refused regulatory approval due to a lack of evidence that they increased physical performance; preventing decline in functionality was not considered an acceptable endpoint by the Food and Drug Administration. It is not known how SARMs interact with dietary protein intake and resistance training in people with muscle wasting.164165

Phase II trials of enobosarm for stress urinary incontinence—considered promising, given that the levator ani muscle in the pelvic floor has a high androgen receptor density—did not meet their endpoint and were abandoned.166167

Unlike other treatments for osteoporosis, which work by decreasing bone loss, SARMs have shown potential to promote growth in bone tissue. LY305 showed promising results in a phase I trial in humans.168

Side effects

In contrast to AAS and testosterone replacement, which have many side effects that have curtailed their medical use, SARMs are well tolerated and have mild and infrequent adverse events in randomized controlled trials.169 SARMs are sometimes claimed to be non-virilizing (non-masculinizing).170171 However, SARMs are largely uncharacterized clinically in terms of potential virilizing effects.172 In addition, SARMs cannot be aromatized to estrogen, thus causing no estrogenic side effects, for instance gynecomastia.173174175

SARM use can cause elevated liver enzymes and reduction in HDL cholesterol.176177 Transdermal administration via a skin patch may reduce these effects.178179 Several case reports have associated SARMs with hepatocellular drug-induced liver injury when used recreationally,180 it is not known if the risk is significant for medical use.181182 Whether SARMs increase the risk of cardiovascular events is unknown.183184 SARMs have less effect on blood lipid profiles than testosterone replacement; it is not known whether androgen-induced HDL reductions increase cardiovascular risk; and SARMs increase insulin sensitivity and lower triglycerides.185186

Although they cause less suppression of the hypothalamic–pituitary–gonadal axis (HPG axis) than testosterone, studies have found that gonadotropins, free and total testosterone, and SHBG can be reduced in a compound- and dose-dependent fashion in men from SARM usage.187188 Typically, SHBG is reduced along with total testosterone and total cholesterol, while hematocrit is increased. Most studies have found that follicle-stimulating hormone (FSH), luteinizing hormone (LH), prostate-specific antigen, estradiol, and DHT levels are not altered.189 Of SARMs that have been investigated, enobosarm is one of the least suppressive of gonadotropins, even in doses much higher than used in clinical trials. How the HPG axis is affected in women using SARMs is unknown.190191 SARMs' effect in suppressing the gonadotropins FSH and LH is what makes SARMs potentially useful as a male contraceptive.192

Non-medical use

See also: List of doping cases in sport by substance § Selective androgen receptor modulators

Outside of pharmaceutical research, SARMs are a gray market substance produced by small laboratories and often marketed as a research chemical supposedly not for human consumption.193194195 Marketing SARMs for human consumption is illegal in some jurisdictions and has led to criminal convictions in the United States196 and the largest-ever fine levied under Australia's Therapeutic Goods Act 1989.197 Although SARMs are readily available for purchase on the internet, one study found that a majority of products advertised as SARMs online were mislabeled. Anecdotes and guides on usage can also be found online and on social media.198199200 Some compounds are commonly marketed for recreational use as SARMs despite having a different mechanism of action. These substances include ibutamoren (MK-677), which increases secretion of growth hormone; GW501516 (cardarine), an exercise mimetic that works as an agonist of the PPARβ/δ; and SR9009 (Stenabolic), an agonist of the Rev-Erb, which plays a role in circadian rhythm.201202

SARMs are used by bodybuilders and competitive athletes due to their anabolic and lack of androgenic effects,203 particularly in the United States, Europe, and other western countries.204 Some individuals using SARMs recreationally combine multiple SARMs or take a SARM along with other compounds, although there is no research on combining SARMs. The doses used often exceed those from clinical trials; nevertheless, the fat-free mass gained from SARMs is generally lower than what is obtained with moderate doses of testosterone derivatives.205 According to one study of SARM users, more than 90 percent were satisfied with their usage and 64 percent would take SARMs again even though a majority experienced adverse effects.206

SARMs were banned by the World Anti-Doping Agency (WADA) in 2008.207 SARMs can be detected in urine and hair after consumption.208 WADA reported its first adverse analytical finding for SARMs in 2010 and the number of positive tests has increased since then; the most commonly detected SARMs are enobosarm (ostarine) and LGD-4033 (ligandrol).209210 Athletes competing in the NFL, NBA, UFC, NCAA, and the Olympics have tested positive.211 There is limited evidence on how SARMs affect athletic performance.212

Terminology

SARMs are sometimes also referred to as "nonsteroidal androgens",213214 although not all SARMs are nonsteroidal in structure and steroidal SARMs also exist.215 In 1999, the term "selective androgen receptor modulator" or "SARM" was introduced, as the mixed agonist–antagonist and tissue-selective activity of these nonsteroidal androgen receptor agonists had similarities with selective estrogen receptor modulators (SERMs).216 Despite its widespread use, the term "selective androgen receptor modulator" has been criticized by some authors, like David Handelsman, who argue that it is a misleading pharmaceutical marketing term rather than an accurate pharmacological description.217 He has also critiqued notions that SARMs isolate anabolic effects from androgenic or virilizing effects, as has been previously claimed in the case of anabolic steroids.218219220221

References

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  2. Machek SB, Cardaci TD, Wilburn DT, Willoughby DS (2020). "Considerations, possible contraindications, and potential mechanisms for deleterious effect in recreational and athletic use of selective androgen receptor modulators (SARMs) in lieu of anabolic androgenic steroids: A narrative review". Steroids. 164: 108753. doi:10.1016/j.steroids.2020.108753. ISSN 0039-128X. PMID 33148520. S2CID 225049089. Archived from the original on 2023-08-30. Retrieved 2023-08-30. Sex-specific SARM effects on humans also remain considerably nebulous. SARMs may represent a more tempting option for female recreational use given potential previous tendencies towards less androgenic AAS (i.e. oxandrolone) [103]. Regardless, as the latter still imposes risk for permanent masculinization and hepatotoxicity, SARMs are largely uncharacterized for female-specific impacts. https://www.sciencedirect.com/science/article/abs/pii/S0039128X20301793 ↩

  3. Solomon ZJ, Mirabal JR, Mazur DJ, Kohn TP, Lipshultz LI, Pastuszak AW (2019). "Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications". Sexual Medicine Reviews. 7 (1): 84–94. doi:10.1016/j.sxmr.2018.09.006. PMC 6326857. PMID 30503797. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6326857 ↩

  4. Jasuja R, Zacharov MN, Bhasin S (2012). "The state-of-the-art in the development of selective androgen receptor modulators". In Nieschlag E, Behre HM (eds.). Testosterone: Action, Deficiency, Substitution (4th ed.). Cambridge University Press. pp. 459–460. doi:10.1017/CBO9781139003353.022. ISBN 978-1-107-01290-5. 978-1-107-01290-5 ↩

  5. Bhasin S, Krishnan V, Storer TW, Steiner M, Dobs AS (2023). "Androgens and Selective Androgen Receptor Modulators to Treat Functional Limitations Associated With Aging and Chronic Disease". The Journals of Gerontology: Series A. 78 (Supplement_1): 25–31. doi:10.1093/gerona/glad027. PMC 10272983. PMID 37325955. Archived from the original on September 1, 2023. Retrieved September 1, 2023. https://academic.oup.com/biomedgerontology/article/78/Supplement_1/25/7199272#408664293 ↩

  6. Bhasin S, Jasuja R (2009). "Selective Androgen Receptor Modulators (SARMs) as Function Promoting Therapies". Current Opinion in Clinical Nutrition and Metabolic Care. 12 (3): 232–240. doi:10.1097/MCO.0b013e32832a3d79. ISSN 1363-1950. PMC 2907129. PMID 19357508. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2907129 ↩

  7. Jasuja R, Zacharov MN, Bhasin S (2012). "The state-of-the-art in the development of selective androgen receptor modulators". In Nieschlag E, Behre HM (eds.). Testosterone: Action, Deficiency, Substitution (4th ed.). Cambridge University Press. pp. 459–460. doi:10.1017/CBO9781139003353.022. ISBN 978-1-107-01290-5. 978-1-107-01290-5 ↩

  8. Bhasin S, Jasuja R (2009). "Selective Androgen Receptor Modulators (SARMs) as Function Promoting Therapies". Current Opinion in Clinical Nutrition and Metabolic Care. 12 (3): 232–240. doi:10.1097/MCO.0b013e32832a3d79. ISSN 1363-1950. PMC 2907129. PMID 19357508. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2907129 ↩

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  10. Jasuja R, Zacharov MN, Bhasin S (2012). "The state-of-the-art in the development of selective androgen receptor modulators". In Nieschlag E, Behre HM (eds.). Testosterone: Action, Deficiency, Substitution (4th ed.). Cambridge University Press. pp. 459–460. doi:10.1017/CBO9781139003353.022. ISBN 978-1-107-01290-5. 978-1-107-01290-5 ↩

  11. Katzung BG (2017). Basic and Clinical Pharmacology (14th ed.). McGraw Hill Professional. p. 741. ISBN 978-1-259-64116-9. 978-1-259-64116-9 ↩

  12. Temerdashev AZ, Dmitrieva EV (2020). "Methods for the Determination of Selective Androgen Receptor Modulators". Journal of Analytical Chemistry. 75 (7): 835–850. doi:10.1134/S1061934820070187. S2CID 220398030. /wiki/Doi_(identifier) ↩

  13. Quirke VM (2017). "Tamoxifen from Failed Contraceptive Pill to Best-Selling Breast Cancer Medicine: A Case-Study in Pharmaceutical Innovation". Frontiers in Pharmacology. 8: 620. doi:10.3389/fphar.2017.00620. PMC 5600945. PMID 28955226. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5600945 ↩

  14. Jordan VC (November 2021). "Turning scientific serendipity into discoveries in breast cancer research and treatment: a tale of PhD students and a 50-year roaming tamoxifen team". Breast Cancer Research and Treatment. 190 (1): 19–38. doi:10.1007/s10549-021-06356-8. PMC 8557169. PMID 34398352. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8557169 ↩

  15. Komm BS, Cheskis B, Bodine PV (November 2007). "Regulation of Bone Cell Function by Estrogens". In Marcus R (ed.). Osteoporosis. Elsevier Science. pp. 383–412 (409). ISBN 978-0-08-055347-4. Archived from the original on 2024-03-08. Retrieved 2024-02-04. 978-0-08-055347-4 ↩

  16. Solomon ZJ, Mirabal JR, Mazur DJ, Kohn TP, Lipshultz LI, Pastuszak AW (2019). "Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications". Sexual Medicine Reviews. 7 (1): 84–94. doi:10.1016/j.sxmr.2018.09.006. PMC 6326857. PMID 30503797. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6326857 ↩

  17. Machek SB, Cardaci TD, Wilburn DT, Willoughby DS (2020). "Considerations, possible contraindications, and potential mechanisms for deleterious effect in recreational and athletic use of selective androgen receptor modulators (SARMs) in lieu of anabolic androgenic steroids: A narrative review". Steroids. 164: 108753. doi:10.1016/j.steroids.2020.108753. ISSN 0039-128X. PMID 33148520. S2CID 225049089. Archived from the original on 2023-08-30. Retrieved 2023-08-30. Sex-specific SARM effects on humans also remain considerably nebulous. SARMs may represent a more tempting option for female recreational use given potential previous tendencies towards less androgenic AAS (i.e. oxandrolone) [103]. Regardless, as the latter still imposes risk for permanent masculinization and hepatotoxicity, SARMs are largely uncharacterized for female-specific impacts. https://www.sciencedirect.com/science/article/abs/pii/S0039128X20301793 ↩

  18. Temerdashev AZ, Dmitrieva EV (2020). "Methods for the Determination of Selective Androgen Receptor Modulators". Journal of Analytical Chemistry. 75 (7): 835–850. doi:10.1134/S1061934820070187. S2CID 220398030. /wiki/Doi_(identifier) ↩

  19. Machek SB, Cardaci TD, Wilburn DT, Willoughby DS (2020). "Considerations, possible contraindications, and potential mechanisms for deleterious effect in recreational and athletic use of selective androgen receptor modulators (SARMs) in lieu of anabolic androgenic steroids: A narrative review". Steroids. 164: 108753. doi:10.1016/j.steroids.2020.108753. ISSN 0039-128X. PMID 33148520. S2CID 225049089. Archived from the original on 2023-08-30. Retrieved 2023-08-30. Sex-specific SARM effects on humans also remain considerably nebulous. SARMs may represent a more tempting option for female recreational use given potential previous tendencies towards less androgenic AAS (i.e. oxandrolone) [103]. Regardless, as the latter still imposes risk for permanent masculinization and hepatotoxicity, SARMs are largely uncharacterized for female-specific impacts. https://www.sciencedirect.com/science/article/abs/pii/S0039128X20301793 ↩

  20. Bhasin S, Krishnan V, Storer TW, Steiner M, Dobs AS (2023). "Androgens and Selective Androgen Receptor Modulators to Treat Functional Limitations Associated With Aging and Chronic Disease". The Journals of Gerontology: Series A. 78 (Supplement_1): 25–31. doi:10.1093/gerona/glad027. PMC 10272983. PMID 37325955. Archived from the original on September 1, 2023. Retrieved September 1, 2023. https://academic.oup.com/biomedgerontology/article/78/Supplement_1/25/7199272#408664293 ↩

  21. Temerdashev AZ, Dmitrieva EV (2020). "Methods for the Determination of Selective Androgen Receptor Modulators". Journal of Analytical Chemistry. 75 (7): 835–850. doi:10.1134/S1061934820070187. S2CID 220398030. /wiki/Doi_(identifier) ↩

  22. Machek SB, Cardaci TD, Wilburn DT, Willoughby DS (2020). "Considerations, possible contraindications, and potential mechanisms for deleterious effect in recreational and athletic use of selective androgen receptor modulators (SARMs) in lieu of anabolic androgenic steroids: A narrative review". Steroids. 164: 108753. doi:10.1016/j.steroids.2020.108753. ISSN 0039-128X. PMID 33148520. S2CID 225049089. Archived from the original on 2023-08-30. Retrieved 2023-08-30. Sex-specific SARM effects on humans also remain considerably nebulous. SARMs may represent a more tempting option for female recreational use given potential previous tendencies towards less androgenic AAS (i.e. oxandrolone) [103]. Regardless, as the latter still imposes risk for permanent masculinization and hepatotoxicity, SARMs are largely uncharacterized for female-specific impacts. https://www.sciencedirect.com/science/article/abs/pii/S0039128X20301793 ↩

  23. Solomon ZJ, Mirabal JR, Mazur DJ, Kohn TP, Lipshultz LI, Pastuszak AW (2019). "Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications". Sexual Medicine Reviews. 7 (1): 84–94. doi:10.1016/j.sxmr.2018.09.006. PMC 6326857. PMID 30503797. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6326857 ↩

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  51. Narayanan R, Coss CC, Dalton JT (April 2018). "Development of selective androgen receptor modulators (SARMs)". Molecular and Cellular Endocrinology. 465: 134–142. doi:10.1016/j.mce.2017.06.013. PMC 5896569. PMID 28624515. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5896569 ↩

  52. Machek SB, Cardaci TD, Wilburn DT, Willoughby DS (2020). "Considerations, possible contraindications, and potential mechanisms for deleterious effect in recreational and athletic use of selective androgen receptor modulators (SARMs) in lieu of anabolic androgenic steroids: A narrative review". Steroids. 164: 108753. doi:10.1016/j.steroids.2020.108753. ISSN 0039-128X. PMID 33148520. S2CID 225049089. Archived from the original on 2023-08-30. Retrieved 2023-08-30. Sex-specific SARM effects on humans also remain considerably nebulous. SARMs may represent a more tempting option for female recreational use given potential previous tendencies towards less androgenic AAS (i.e. oxandrolone) [103]. Regardless, as the latter still imposes risk for permanent masculinization and hepatotoxicity, SARMs are largely uncharacterized for female-specific impacts. https://www.sciencedirect.com/science/article/abs/pii/S0039128X20301793 ↩

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  201. Machek SB, Cardaci TD, Wilburn DT, Willoughby DS (2020). "Considerations, possible contraindications, and potential mechanisms for deleterious effect in recreational and athletic use of selective androgen receptor modulators (SARMs) in lieu of anabolic androgenic steroids: A narrative review". Steroids. 164: 108753. doi:10.1016/j.steroids.2020.108753. ISSN 0039-128X. PMID 33148520. S2CID 225049089. Archived from the original on 2023-08-30. Retrieved 2023-08-30. Sex-specific SARM effects on humans also remain considerably nebulous. SARMs may represent a more tempting option for female recreational use given potential previous tendencies towards less androgenic AAS (i.e. oxandrolone) [103]. Regardless, as the latter still imposes risk for permanent masculinization and hepatotoxicity, SARMs are largely uncharacterized for female-specific impacts. https://www.sciencedirect.com/science/article/abs/pii/S0039128X20301793 ↩

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  205. Machek SB, Cardaci TD, Wilburn DT, Willoughby DS (2020). "Considerations, possible contraindications, and potential mechanisms for deleterious effect in recreational and athletic use of selective androgen receptor modulators (SARMs) in lieu of anabolic androgenic steroids: A narrative review". Steroids. 164: 108753. doi:10.1016/j.steroids.2020.108753. ISSN 0039-128X. PMID 33148520. S2CID 225049089. Archived from the original on 2023-08-30. Retrieved 2023-08-30. Sex-specific SARM effects on humans also remain considerably nebulous. SARMs may represent a more tempting option for female recreational use given potential previous tendencies towards less androgenic AAS (i.e. oxandrolone) [103]. Regardless, as the latter still imposes risk for permanent masculinization and hepatotoxicity, SARMs are largely uncharacterized for female-specific impacts. https://www.sciencedirect.com/science/article/abs/pii/S0039128X20301793 ↩

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  216. Negro-Vilar A (October 1999). "Selective androgen receptor modulators (SARMs): a novel approach to androgen therapy for the new millennium". The Journal of Clinical Endocrinology and Metabolism. 84 (10): 3459–3462. doi:10.1210/jcem.84.10.6122. PMID 10522980. We have chosen the term selective androgen receptor modulators (SARMs) after the terminology currently used for similar molecules targeting the estrogen receptor. ... Desired profile of activity of new SARMs: male applications: Selected indications may include glucocorticoid-induced osteoporosis, androgen replacement in elderly men, HIV-wasting, cancer cachexia, certain anemias, muscular dystrophies, and male contraception. /wiki/Doi_(identifier) ↩

  217. Handelsman DJ (July 2022). "History of androgens and androgen action". Best Practice & Research. Clinical Endocrinology & Metabolism. 36 (4): 101629. doi:10.1016/j.beem.2022.101629. PMID 35277356. The next invention was that of the first non-steroidal androgen by Dalton et al. [111] in 1998, six decades after the first non-steroidal estrogen [112]. This creates a new class of non-steroidal synthetic androgen, often termed Specific Androgen Receptor Modulators (SARM), a misleading marketing term rather than an accurate pharmacological description [113,114], usurping a speculative but unsound analogy with Specific Estrogen Receptor Modulators (SERM). [...] none of the non-steroidal androgens under development [116,117] are marketed by 2021. Yet hope springs eternal for this new attempt to separate anabolic from androgenic properties of androgens to facilitate marketing for muscle wasting and other selective effects of testosterone. /wiki/Doi_(identifier) ↩

  218. Handelsman DJ (July 2022). "History of androgens and androgen action". Best Practice & Research. Clinical Endocrinology & Metabolism. 36 (4): 101629. doi:10.1016/j.beem.2022.101629. PMID 35277356. The next invention was that of the first non-steroidal androgen by Dalton et al. [111] in 1998, six decades after the first non-steroidal estrogen [112]. This creates a new class of non-steroidal synthetic androgen, often termed Specific Androgen Receptor Modulators (SARM), a misleading marketing term rather than an accurate pharmacological description [113,114], usurping a speculative but unsound analogy with Specific Estrogen Receptor Modulators (SERM). [...] none of the non-steroidal androgens under development [116,117] are marketed by 2021. Yet hope springs eternal for this new attempt to separate anabolic from androgenic properties of androgens to facilitate marketing for muscle wasting and other selective effects of testosterone. /wiki/Doi_(identifier) ↩

  219. Handelsman DJ (May 2011). "Commentary: androgens and "anabolic steroids": the one-headed janus". Endocrinology. 152 (5): 1752–4. doi:10.1210/en.2010-1501. PMID 21511988. Although development of the first nonsteroidal androgens (17, 18) as candidate selective AR modulators (19) raises hope of resurrecting this defunct term (20), prereceptor activation mechanisms cannot apply to nonsteroidal androgens, and the singular AR lacks a dual drive mechanism of the other paired sex steroid receptors. Consequently, it is not surprising that available knowledge (21) provides only slender hope that this failed, and probably false, dichotomy will now succeed through a renewed search guided by the same in vivo bioassay. /wiki/Doi_(identifier) ↩

  220. Handelsman DJ (July 2021). "Androgen Misuse and Abuse". Endocr Rev. 42 (4): 457–501. doi:10.1210/endrev/bnab001. PMID 33484556. However, a third major quest, for the development of a nonvirilizing androgen ("anabolic steroid") suitable for use in women and children, based on dissociating the virilizing from the anabolic effects of androgens failed comprehensively (36). This failure is now understood as being due to the discovery of a singular androgen receptor (AR) together with the misinterpretation of nonspecific whole animal androgen bioassays employed to distinguish between anabolic and virilizing effects (37). The term "androgen" is used herein for both endogenous and synthetic androgens including references to chemicals named elsewhere as "anabolic steroids," "anabolic-androgenic steroids," or "specific AR modulators" (SARM), which continue to make an obsolete and oxymoronic distinction between virilizing and anabolic effects of androgens where there is no difference (36). /wiki/Doi_(identifier) ↩

  221. Handelsman DJ (2012-07-26). "Androgen therapy in non-gonadal disease". Testosterone. Cambridge University Press. pp. 372–407. doi:10.1017/cbo9781139003353.018. ISBN 978-1-139-00335-3. The development of nonsteroidal androgens, marketed as "selective androgen receptor modulators" (SARMs), offers new possibilities for adjuvant pharmacological androgen therapy. In contrast to the full spectrum of androgen effects of testosterone, such SARMs would be pure androgens not subject to tissue-specific activation by aromatization to a corresponding estrogen or to amplification of androgenic potency by 5α-reduction. In this context the endogenous pure androgens nandrolone and DHT can be considered prototype SARMs. SARMs are not the modern embodiment of so-called "anabolic steroids," an outdated term referring to hypothetical but nonexistent non-virilizing androgens targeted exclusively to muscle, a failed concept lacking biological proof of principle (Handelsman 2011). 978-1-139-00335-3 ↩