RAD-140 (Testolone)

1. Overview and Critical Disclosure

RAD-140 (Testolone; development codes RAD140, EP0062; INN vosilasarm) is NOT a peptide. It is a non-steroidal small-molecule selective androgen receptor modulator (SARM) with a molecular weight of 393.83 Da and the formula C20H16ClN5O2. It contains a cyanophenyl-oxadiazole head group and a chloro-methyl-aryl-propanamide scaffold — chemistry wholly unrelated to amide-bond-linked amino-acid peptides. This profile is included on PeptideInsight solely because RAD-140 is prominent in the overlapping research-chemical, bodybuilding, and "peptide community" commerce channels where it is frequently sold alongside genuine peptides such as BPC-157, TB-500, or growth-hormone secretagogues. Readers seeking peptides should note this is a synthetic small molecule; its pharmacology, risks, and regulatory status are not analogous to any peptide hormone.

RAD-140 was first described in medicinal-chemistry terms by Miller and colleagues at Radius Health in a 2010 disclosure published in ACS Medicinal Chemistry Letters (collected 2011) [1]. It was designed as an orally bioavailable agonist of the androgen receptor (AR) with tissue-selective activity — potent anabolic action on skeletal muscle and bone, greatly reduced agonism on prostate, seminal vesicle, and sebaceous tissue — in the same mechanistic family as enobosarm (ostarine, MK-2866) and LGD-4033 (ligandrol). Preclinical profiling established a binding Ki of approximately 7 nM for human AR, dose-dependent stimulation of levator ani muscle beginning at 0.03 mg/kg in castrated rats, and a distinctive lack of prostate stimulation up to 30 mg/kg in intact males [1].

Subsequent mechanistic work extended RAD-140 beyond musculoskeletal indications. Jayaraman and colleagues (2014) demonstrated MAPK/ERK-dependent neuroprotection of cultured hippocampal neurons and in vivo protection against kainate-induced cell death in gonadectomized rats, positioning the compound as a candidate scaffold for Alzheimer disease research [2]. Yu and colleagues at Radius Health (2017) reported that RAD-140 inhibited the growth of AR+/ER+ breast cancer patient-derived xenografts more effectively than fulvestrant, with a novel mechanism centered on AR-mediated repression of the ESR1 gene [3]. This preclinical oncology data enabled a Phase 1 first-in-human trial in heavily pretreated postmenopausal women with ER+/HER2- metastatic breast cancer, reported by Dalton and colleagues in Clinical Breast Cancer in 2022 (NCT02692755) [4].

In October 2020, Radius Health divested the RAD-140 oncology program to Ellipses Pharma, where it was renamed EP0062 and later vosilasarm; Ellipses is continuing clinical development in AR+/ER+/HER2- advanced/metastatic breast cancer. Radius retained royalty rights. Radius Health itself was subsequently acquired by Gurnet Point Capital and Patient Square Capital in 2022 in a transaction unrelated to the SARM asset.

The clinical signal driving inclusion of RAD-140 on this reference is the expanding case-report literature of severe adverse events in recreational users — including cholestatic drug-induced liver injury (Flores 2020 [5]; Barbara 2020 [6]; Mohideen 2022 [9]; Alhumaidan 2023 [10]) and acute myocarditis or myopericarditis in young healthy males (Bedi 2022 [7]; Nasser 2024 [8]). These signals are concerning precisely because the user demographic driving RAD-140 consumption is young, previously healthy, and physically active. The compound is prohibited at all times under WADA Section S1.2 (Other Anabolic Agents) and has not been approved by any regulatory agency for any indication.

Drug Class

Non-steroidal selective androgen receptor modulator (SARM)

NOT a peptide

Small-molecule aryl-propanamide derivative; listed for research-chemical community crossover only

Chemical Name

2-chloro-4-{[(1R,2S)-1-[5-(4-cyanophenyl)-1,3,4-oxadiazol-2-yl]-2-hydroxypropyl]amino}-3-methylbenzonitrile

Molecular Formula

C20H16ClN5O2

Molecular Weight

393.83 Da

Route

Oral (bioavailable)

Target

Androgen receptor (AR) — tissue-selective agonist (muscle/bone) with reduced prostate stimulation

Plasma Half-life

Approximately 60 hours in humans (phase 1 data)

Developer

Radius Health (originator, 2010-2020); divested to Ellipses Pharma October 2020 as EP0062/vosilasarm

FDA Status

Not approved. Phase 1 completed in ER+/HER2- metastatic breast cancer; no Phase 3

WADA Status

Prohibited at all times (in- and out-of-competition) under S1.2 Other Anabolic Agents since 2008

Discovery

Miller et al., Radius Health, first described 2010/2011 (ACS Med Chem Lett)

2. Why RAD-140 Is Not a Peptide

The term "peptide" refers to short polymers of alpha-amino acids linked by amide (peptide) bonds, typically ranging from dipeptides to polypeptides of several dozen residues. Genuine peptides listed on this reference (oxytocin, BPC-157, semaglutide, thymosin beta-4, GHRP-6, etc.) consist of 2 to approximately 100 amino-acid residues, are typically synthesized by solid-phase peptide synthesis or recombinant expression, and act via receptors evolved to recognize peptide ligands (GPCRs, receptor tyrosine kinases, or intracellular peptide targets).

RAD-140 meets none of these criteria. Its scaffold is an aryl-propanamide containing:

• a cyanophenyl-oxadiazole head group
• a central chiral secondary amine
• a chloro-methyl-benzonitrile anilide
• a pendant hydroxypropyl linker

It is synthesized by conventional small-molecule medicinal chemistry. It binds the ligand-binding domain of the nuclear hormone androgen receptor in the same pocket that accommodates testosterone and dihydrotestosterone (DHT). Its pharmacology, metabolism (primarily hepatic CYP-mediated oxidation), tissue distribution (high volume of distribution, lipophilic partitioning into adipose and muscle), and oral bioavailability are typical of a non-steroidal small molecule, not a peptide. Recreational mis-classification of SARMs as "peptides" is a marketing artifact of the underground research-chemical economy — not a reflection of molecular reality.

This distinction has practical importance for readers. Peptides are typically degraded rapidly in the gastrointestinal tract (hence the prevalence of injectable peptide drugs), have short half-lives (minutes to hours), do not accumulate, and are cleared enzymatically to amino acids. RAD-140, in contrast, is orally active, has a half-life of approximately 60 hours, accumulates on daily dosing (steady state reached at 2-3 weeks), and is cleared by hepatic metabolism — properties that underlie both its convenience for users and its capacity for sustained androgen-receptor activation with associated hepatic and cardiovascular stress.

3. Pharmacology and Mechanism of Action

Androgen Receptor Binding

RAD-140 binds the human androgen receptor ligand-binding domain with a Ki of approximately 7 nM, comparable to DHT (Ki approximately 1-5 nM) and greater than testosterone (Ki approximately 10 nM) in competitive binding assays against tritiated R1881 (methyltrienolone) [1]. Binding induces the canonical AR conformational change, dissociation of heat-shock protein chaperones (HSP90), homodimerization, and nuclear translocation. In reporter-gene assays of AR transcriptional activation, RAD-140 behaved as a full agonist with EC50 values in the low nanomolar range [1].

Tissue Selectivity: Proposed Molecular Basis

The hallmark property of a SARM is tissue-selective AR agonism — anabolic on muscle and bone, neutral or partial-agonist/partial-antagonist on prostate, seminal vesicle, and skin. For RAD-140, this selectivity is evidenced by:

• Full agonism on levator ani weight in castrated rats at 0.03-0.3 mg/kg versus the positive control testosterone propionate 1 mg/kg [1]
• Failure of RAD-140 (up to 10 mg/kg) to match testosterone-propionate-induced prostate and seminal vesicle stimulation [1]
• At 10 mg/kg, partial antagonism of testosterone-propionate-induced seminal vesicle growth, suggesting competitive displacement by a weaker-agonist ligand [1]
• In intact male rats, no prostate stimulation above control until 30 mg/kg — a wide separation from the musculoskeletal effective dose [1]

The molecular basis is thought to involve differential co-activator recruitment: RAD-140, like other non-steroidal SARMs, stabilizes an AR conformation that recruits muscle-relevant transcriptional machinery more efficiently than prostate-relevant machinery. SRC family co-activators, p160 proteins, and tissue-specific chromatin landscapes all contribute [14][19]. The selectivity is relative, not absolute — at high doses or in genetically sensitive individuals, prostate, sebaceous, and hepatic AR-mediated effects re-emerge.

Non-Androgenic Activities

Beyond musculoskeletal AR agonism, RAD-140 has been characterized in:

• Central nervous system: MAPK/ERK-dependent neuroprotection in cultured hippocampal neurons and in rat kainate lesion models at 1 mg/kg oral [2]. The ERK-dependence was confirmed by inhibition with the MEK inhibitor U0126.
• Breast cancer: AR-mediated repression of ESR1 (estrogen receptor alpha) transcription in AR+/ER+ breast cancer cell lines and patient-derived xenografts, inhibiting tumor growth more potently than fulvestrant and synergizing with palbociclib and everolimus [3].
• Metabolic: Consistent with general SARM pharmacology, chronic RAD-140 dosing tends to suppress HDL cholesterol and endogenous testosterone via hypothalamic-pituitary-gonadal (HPG) axis feedback [14][20].

Pharmacokinetics in Humans

From the Phase 1 trial and doping-control micro-dose studies:

• Oral bioavailability: High (estimated greater than 50% based on plasma exposure at clinical doses)
• Tmax: 1-2 hours
• Plasma half-life: Approximately 60 hours — enabling once-daily dosing
• Accumulation: Steady state reached at approximately 2-3 weeks of daily dosing
• Metabolism: Primarily hepatic CYP-mediated oxidation; multiple phase I hydroxylated metabolites identified by Thevis group in human urine [13][16]
• Excretion: Predominantly urinary as conjugated metabolites; parent drug also detectable for doping-control purposes

The long half-life is clinically significant: adverse events emerging during use often take weeks to resolve after discontinuation, and hepatotoxicity cases in the literature typically show delayed onset (4-12 weeks into a cycle) followed by prolonged recovery (2-6 months to normalization of liver enzymes and bilirubin) [5][6][9][10][11].

4. Researched Applications

ER+/AR+ Metastatic Breast Cancer — the Only Real Clinical Program

Evidence level: Low (Phase 1 completed; no Phase 3)

The only sustained clinical program for RAD-140 has been in AR+/ER+/HER2- advanced or metastatic breast cancer. The preclinical rationale is based on Yu and colleagues' 2017 observation that RAD-140 activates AR in AR+/ER+ breast cancer models while simultaneously repressing ESR1 gene expression — simultaneously exploiting AR as an anti-estrogenic signaling node [3]. Preclinical xenograft efficacy exceeded fulvestrant and was enhanced by combination with palbociclib or everolimus.

The first-in-human Phase 1 trial (NCT02692755, sponsored by Radius Health) enrolled 22 heavily pretreated postmenopausal women (21 AR+) at oral doses of 50 mg, 100 mg, or 150 mg once daily [4]. Key findings reported by Dalton and colleagues:

• Safety: The most common treatment-emergent adverse events were elevated AST (59.1%), elevated ALT (45.5%), hyperbilirubinemia (27.3%), vomiting, dehydration, decreased appetite, and decreased weight (27.3% each). The 150 mg cohort showed dose-limiting hepatotoxicity.
• Recommended Phase 2 dose: 100 mg once daily.
• Evidence of activity: Target engagement (e.g., SHBG changes) and preliminary evidence of anti-tumor activity supported proof of concept, though formal Phase 2 efficacy readouts in the RAD-140 asset have been limited.

Following the October 2020 divestiture to Ellipses Pharma, the program was re-launched as EP0062/vosilasarm with revised dosing (10 mg BID was subsequently selected as an optimal dose in further phase 1/2 work presented at ASCO 2025). Ellipses Pharma has been developing vosilasarm in AR+/ER+/HER2- advanced breast cancer. As of early 2026, no Phase 3 trial has been completed, and the drug has not received regulatory approval for any indication.

Muscle Wasting and Cachexia

Evidence level: Preclinical only

Despite the original SARM rationale being centered on muscle-wasting indications (cancer cachexia, age-related sarcopenia, chronic kidney disease), RAD-140 has not been advanced in a registered clinical program for these indications. Preclinical muscle data are robust [1][19], but the SARM field as a whole has faced translational setbacks — enobosarm (the most advanced SARM, now under Veru) failed to meet primary endpoints in Phase 3 cancer cachexia trials. No RAD-140 muscle-wasting trial has reported.

Neuroprotection / Alzheimer Disease

Evidence level: Preclinical only

Jayaraman and colleagues' 2014 report of MAPK/ERK-dependent neuroprotection in hippocampal neurons and in vivo in rat kainate lesion models established a proof-of-concept for AR-mediated neuroprotection [2]. However, no clinical Alzheimer or neurodegenerative disease trial of RAD-140 has been initiated.

Bone / Osteoporosis

Evidence level: Preclinical only

SARMs generally preserve or increase bone mineral density via AR-mediated osteoblast activation and reduced RANKL-driven osteoclastogenesis. RAD-140 increased bone mineral density in castrated rat models at doses producing musculoskeletal anabolism [1][19]. No clinical osteoporosis trial of RAD-140 has been initiated.

5. Clinical Evidence Summary

6. Dosing

The following table summarizes doses used in preclinical studies, the completed Phase 1 oncology trial, and those commonly reported in recreational-use case reports. Recreational use of RAD-140 is unapproved, illegal in most jurisdictions for human consumption, prohibited by WADA, and has been associated with severe adverse events in published case reports.

7. Safety Signals — the Central Concern

The safety profile that emerges from the existing literature — Phase 1 trial adverse events plus a growing case-report series in recreational users — is the single most important reason this reference entry exists.

Hepatotoxicity (Drug-Induced Liver Injury)

A consistent signal of cholestatic drug-induced liver injury (DILI) has emerged in the peer-reviewed case-report literature:

• Flores et al. 2020 [5] reported two cases of DILI in young male bodybuilders using SARMs, one involving a RAD-140 plus LGD-4033 combination. The clinical phenotype was cholestatic jaundice developing several weeks into a cycle, with marked hyperbilirubinemia. Hepatology Communications, March 2020.
• Barbara et al. 2020 [6] reported a 52-year-old male who developed severe cholestatic DILI after using Alpha Bolic (RAD-140) and Alpha Elite (RAD-140 + LGD-4033). Drug-Induced Liver Injury Network (DILIN) causality score was 1 (probable); severity score was 3 (severe injury). Clinical course showed moderate transaminase elevation followed by profound hyperbilirubinemia. Described as the third RAD-140 DILI case in the published literature.
• Mohideen et al. 2022 [9] (Ochsner Journal) added another RAD-140-associated cholestatic DILI case.
• Alhumaidan et al. 2023 [10] reported a 24-year-old Asian male with 5-week RAD-140 exposure presenting with jaundice, pruritus, and biopsy-confirmed cholestatic injury.
• Vignera et al. 2023 [11] provided a further case plus systematic review concluding that RAD-140 and other SARMs produce a clinical DILI phenotype resembling 17-alpha-alkylated anabolic-androgenic steroid jaundice.
• Leciejewska et al. 2023 [12] pharmacovigilance analysis of SARM-related adverse events identified DILI as the dominant category, with RAD-140 and LGD-4033 most frequently implicated.

The clinical pattern is remarkably consistent: previously healthy males (ages typically 20-55), 4-12 weeks of oral RAD-140 (often 10-30 mg/day, sometimes stacked with LGD-4033), onset of jaundice, hyperbilirubinemia (peak total bilirubin often greater than 20 mg/dL), moderate transaminase elevation, and prolonged recovery taking 2-6 months. Liver biopsy when performed shows cholestatic injury with bile plugs and mild inflammation, occasionally progressing to ductopenia. Corticosteroid therapy has been used in several reports with variable response.

Acute Myocarditis and Cardiomyopathy

The cardiac safety signal is more recent but particularly concerning because of the young, healthy demographic:

• Bedi et al. 2022 [7] reported a 32-year-old male bodybuilder using RAD-140 for approximately 3 months who presented with exertional dyspnea. Laboratory values: troponin I 77.1 ng/mL, BNP 1288 pg/mL, ESR 75 mm/h, CRP 147.22 mg/L. After exclusion of infectious, ischemic, and autoimmune causes, and with consistent cardiac MRI findings, a presumptive diagnosis of RAD-140-induced acute myocarditis was made. Patient had no baseline cardiac disease (history notable only for type 1 diabetes).
• Nasser et al. 2024 [8] reported a 16-year-old male who developed myopericarditis within days of a single first dose of RAD-140. This is among the most striking signals in the literature — acute cardiac inflammation after a single dose, in an adolescent, from a recreational research-chemical source.

The mechanism is unclear but likely involves direct AR-mediated cardiomyocyte stress, off-target immune activation, or a combination. Anabolic-androgenic steroid use is a well-established cause of cardiomyopathy [17]; the SARM cardiac signal appears to be a qualitatively similar phenomenon despite the tissue-selective claims made for SARMs.

Hypothalamic-Pituitary-Gonadal (HPG) Axis Suppression

Like other exogenous AR agonists, RAD-140 suppresses endogenous testosterone production via hypothalamic-pituitary feedback — measured decreases in LH, FSH, and testosterone of 50-80% from baseline have been reported in recreational users on 10-20 mg/day cycles [14][15][20]. Recovery timelines after discontinuation range from weeks to months. Post-cycle therapy (PCT) protocols used in the bodybuilding community (e.g., tamoxifen, clomiphene) have no safety or efficacy data from controlled human trials in this context.

Lipid Effects

SARMs generally suppress HDL cholesterol via hepatic AR-mediated effects on ApoA1 and lipoprotein metabolism. In the Phase 1 breast cancer trial, lipid-panel changes were among the treatment-emergent changes noted [4]. Recreational users have reported 30-50% decreases in HDL during cycles, with recovery over weeks to months after discontinuation.

Other Adverse Effects Reported

• Testicular atrophy from HPG suppression
• Acne and hair loss (dose-dependent, off-target androgenic skin/scalp effects)
• Visual disturbances (occasionally reported, mechanism unclear, distinct from well-documented effects with andarine/S4)
• Headache, nausea, fatigue
• Mood changes, aggression (inconsistently reported)

Contamination and Mislabeling of Supplements

A 2020 analysis of SARM supplements found that fewer than 50% of products contained the labeled compound; approximately 39% contained other unapproved drugs (steroids, growth hormones). A separate analysis of 20 dietary supplements found only six matched their labeling [18]. Users purchasing "RAD-140" online may be consuming LGD-4033, anabolic steroids, or other compounds — adding variability to any attempt to interpret personal experience or to link case reports to a specific compound.

8. Why the Safety Signal Matters More Than Usual

Drug-safety signals are always context-dependent. For RAD-140, several factors compound the concern:

1. The user demographic is young and healthy. Unlike cancer or cachexia patients in regulated trials, recreational RAD-140 users are typically males aged 18-40 with no baseline disease. Adverse events of the magnitude reported (severe cholestatic DILI, acute myocarditis) in this demographic are qualitatively different from similar events in older, comorbid populations: the relative risk is driven entirely by the drug exposure.

2. The doses used recreationally are similar to or exceed the dose-limiting range in the Phase 1 trial. Dalton and colleagues found dose-limiting hepatotoxicity at 150 mg/day and selected 100 mg/day as the recommended Phase 2 dose in breast cancer patients [4]. Recreational users typically take 10-30 mg/day, which is lower in absolute milligram terms but comparable in exposure given body-composition considerations and lack of concurrent oncologic illness. Cases of severe DILI and myocarditis in recreational users are occurring at exposures below the Phase 1 MTD.

3. The long half-life (approximately 60 hours) means accumulation and prolonged washout. Once an adverse event develops, resolution requires weeks of tapering drug exposure plus months of hepatic or cardiac recovery.

4. The supply chain is unregulated. Products sold as RAD-140 online may be mislabeled, contaminated with other SARMs, anabolic-androgenic steroids, or unknown compounds. Any "personal experience" of RAD-140 safety in recreational contexts is inferential at best.

5. No human clinical program exists outside breast cancer. There is no Phase 3 safety database. The peer-reviewed safety evidence consists of a Phase 1 trial in 22 heavily-pretreated cancer patients plus an expanding series of adverse-event case reports in recreational users. This is an extremely thin safety profile.

6. The cardiac signal is particularly concerning. Myocarditis and cardiomyopathy in young healthy males carry significant mortality risk and can result in permanent systolic dysfunction. The Nasser 2024 case of myopericarditis after a single dose in a 16-year-old [8] is the kind of idiosyncratic signal that — if reproducible — would be disqualifying for any therapeutic development program.

9. Regulatory and WADA Status

• FDA: RAD-140 is not approved. It is not a legal dietary-supplement ingredient under DSHEA; the FDA has issued warnings against the use of SARMs including RAD-140 in bodybuilding products.
• EMA: Not approved.
• WADA: Prohibited at all times (in- and out-of-competition) under Section S1.2 (Other Anabolic Agents) since 2008. RAD-140 is the second most commonly detected SARM in doping-control samples after LGD-4033 [16]. Urinary detection by LC-HRMS/MS using parent drug and hydroxylated metabolites has been extensively characterized [13].
• UK: SARMs including RAD-140 are unlicensed medicines; sale for human consumption is prohibited under the Human Medicines Regulations. Sale and possession have been restricted.
• Australia: RAD-140 is Schedule 4 (prescription-only); importation without a prescription is illegal.
• Contamination risk to athletes: Even small amounts of RAD-140 contamination in legitimate supplements can produce positive doping-control tests. Athletes are strongly cautioned against supplements not independently certified.

10. Development History and Corporate Context

• 2010 (December 2): Miller and colleagues at Radius Health disclose RAD140 in ACS Medicinal Chemistry Letters (collection date February 2011) [1].
• 2014: Jayaraman and colleagues publish the neuroprotection paper [2].
• 2017: Yu and colleagues publish the ER+/AR+ breast cancer PDX paper in Clinical Cancer Research [3]. Radius Health moves RAD140 into oncology development.
• 2019 (December): Phase 1 breast cancer results presented at San Antonio Breast Cancer Symposium (SABCS) as abstract P5-11-01.
• 2020 (October 1): Radius Health announces divestiture of the RAD-140 program to Ellipses Pharma, transferring development rights in exchange for milestone and royalty payments. The program is renamed EP0062.
• 2022: Dalton and colleagues publish the first-in-human Phase 1 trial in Clinical Breast Cancer [4].
• 2022: Radius Health is acquired by Gurnet Point Capital and Patient Square Capital (transaction unrelated to SARM program).
• 2023-2025: Ellipses Pharma advances vosilasarm (EP0062) in AR+/ER+/HER2- advanced breast cancer. Phase 1 follow-up data presented at ASCO 2025 describe 10 mg BID as a selected dose for further development.
• As of early 2026: No Phase 3 trial completed; no regulatory approval for any indication.

Note the important distinction: Ellipses Pharma's vosilasarm (EP0062) is RAD-140. This is NOT the same as Radius Health's RAD1901 (elacestrant), which is a selective estrogen receptor degrader (SERD) with a completely different chemical scaffold, mechanism, and development path. Elacestrant was approved by the FDA in January 2023 for ER+/HER2-, ESR1-mutated advanced breast cancer under the brand name Orserdu and is marketed by Menarini Stemline. These two compounds are sometimes confused in secondary literature because both carried "Radius" development codes.

11. Comparison with Related SARMs and Anabolic-Androgenic Steroids

RAD-140 vs. Ostarine (MK-2866, enobosarm)

• Development status: Enobosarm reached Phase 3 in cancer cachexia (POWER trials, failed primary endpoints) and is currently being developed by Veru in AR+/ER+/HER2- breast cancer (ARTEST Phase 3). RAD-140 is behind enobosarm in clinical stage.
• Selectivity: Enobosarm has been more extensively characterized in humans; both show tissue selectivity with musculoskeletal anabolism. RAD-140 may have a longer half-life and somewhat greater potency.
• Safety: Both have been implicated in DILI case reports. Enobosarm has a larger human safety database.

RAD-140 vs. LGD-4033 (ligandrol)

• Both are non-steroidal AR agonists, often stacked in recreational use.
• LGD-4033 has a somewhat shorter half-life (approximately 24-36 hours) and is also WADA-prohibited.
• The Barbara 2020 case [6] and Flores 2020 series [5] both involved combinations of RAD-140 plus LGD-4033, making single-compound attribution difficult — though both compounds independently have case-report DILI signals.

RAD-140 vs. Anabolic-Androgenic Steroids (testosterone, nandrolone, oxandrolone)

• AAS are steroidal AR agonists (modified from the testosterone backbone). RAD-140 is non-steroidal.
• AAS often undergo aromatization to estrogens (producing gynecomastia) or 5-alpha-reduction to DHT (producing prostate stimulation). RAD-140 is non-aromatizable and does not undergo 5-alpha reduction.
• Recreational marketing of SARMs has emphasized these mechanistic differences as evidence of improved safety. The emerging case-report literature does not clearly support a safer hepatic or cardiac profile in recreational-dose RAD-140 compared with 17-alpha-alkylated oral steroids [11][17].

12. Related Compounds

See also: Ostarine (MK-2866), LGD-4033 (Ligandrol), GW-501516 (Cardarine), SR9009 (Stenabolic)

13. References

1. [1] Miller CP, Shomali M, Lyttle CR, OʼDea LS, Herendeen H, Gallacher K, Paquin D, Compton DR, Sahoo B, Kerrigan SA, Burge MS, Nickels M, Green JL, Katzenellenbogen JA, Tchesnokov A, Hattersley G. (2011). Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140. ACS Medicinal Chemistry Letters. DOI PubMed
2. [2] Jayaraman A, Christensen A, Moser VA, Vest RS, Miller CP, Hattersley G, Pike CJ. (2014). Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats. Endocrinology. DOI PubMed
3. [3] Yu Z, He S, Wang D, Patel HK, Miller CP, Brown JL, Hattersley G, Saeh JC. (2017). Selective Androgen Receptor Modulator RAD140 Inhibits the Growth of Androgen/Estrogen Receptor-Positive Breast Cancer Models with a Distinct Mechanism of Action. Clinical Cancer Research. DOI PubMed
4. [4] Dalton JT, Taylor RP, Mohler ML, Steiner MS. (2022). A First-in-Human Phase 1 Study of a Novel Selective Androgen Receptor Modulator (SARM), RAD140, in ER+/HER2- Metastatic Breast Cancer. Clinical Breast Cancer. DOI PubMed
5. [5] Flores JE, Chitturi S, Walker S. (2020). Drug-Induced Liver Injury by Selective Androgenic Receptor Modulators. Hepatology Communications. DOI PubMed
6. [6] Barbara M, Dhingra S, Mindikoglu AL. (2020). Drug-Induced Liver Injury Associated With Alpha Bolic (RAD-140) and Alpha Elite (RAD-140 and LGD-4033). ACG Case Reports Journal. DOI PubMed
7. [7] Bedi H, Hammond C, Sanders D, Yang HM, Yoshida EM. (2022). Acute Myocarditis From the Use of Selective Androgen Receptor Modulator (SARM) RAD-140 (Testolone). Cureus. DOI PubMed
8. [8] Nasser N, Ahmed I, Lowe DL. (2024). Myopericarditis Following Use of Selective Androgen Receptor Modifier RAD-140. JACC Case Reports. DOI PubMed
9. [9] Mohideen H, Hussain H, Dahiya DS, Wehbe H. (2022). RAD-140 Drug-Induced Liver Injury. Ochsner Journal. DOI PubMed
10. [10] Alhumaidan N, Shamoon Y, Edem B, Saidi W, Castro-Sierra F. (2023). Idiosyncratic drug-induced liver injury related to use of novel selective androgen receptor modulator RAD140 (Testalone): a case report. Journal of Medical Case Reports. DOI PubMed
11. [11] Vignera S, Mazzoli S, Cannarella R, Iolascon G, Pellegrino R, Calogero AE. (2023). Selective Androgen Receptor Modulators (SARMs)-Induced Liver Injury: A Case Report and Review of Literature. Cureus. DOI PubMed
12. [12] Leciejewska N, Pruszynska-Oszmalek E, Nogowski L, Kolodziejski PA. (2023). Selective androgen receptor modulator use and related adverse events including drug-induced liver injury: Analysis of suspected cases. European Journal of Clinical Pharmacology. DOI PubMed
13. [13] Thevis M, Piper T, Dib J, Lagojda A, Kuehne D, Thomas A. (2022). Human In Vivo Metabolism and Elimination Behavior of Micro-Dosed Selective Androgen Receptor Modulator RAD140 for Doping Control Purposes. Metabolites. DOI PubMed
14. [14] 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. DOI PubMed
15. [15] Christiansen AR, Lipshultz LI, Hotaling JM, Pastuszak AW. (2020). Selective androgen receptor modulators: the future of androgen therapy?. Translational Andrology and Urology. DOI PubMed
16. [16] Thevis M, Schanzer W. (2018). Detection of SARMs in doping control analysis. Molecular and Cellular Endocrinology. DOI PubMed
17. [17] Bond P, Smit DL, de Ronde W. (2022). Anabolic-androgenic steroids: How do they work and what are the risks?. Frontiers in Endocrinology. DOI PubMed
18. [18] Hilkens L, Cruyff M, Woertman L, Benjamins J, Evers C. (2021). Social Media, Body Image and Resistance Training: Creating the Perfect Me with Dietary Supplements, Anabolic Steroids and SARMs. Sports Medicine - Open. DOI PubMed
19. [19] Narayanan R, Coss CC, Dalton JT. (2018). Development of selective androgen receptor modulators (SARMs). Molecular and Cellular Endocrinology. DOI PubMed
20. [20] 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. DOI PubMed

14. Plain-Language Bottom Line

RAD-140 is not a peptide. It is a small-molecule non-steroidal SARM developed by Radius Health, currently owned by Ellipses Pharma as EP0062/vosilasarm, with a single completed Phase 1 trial in metastatic breast cancer and no regulatory approval. Its safety profile in the recreational-use population is characterized by a pattern of severe cholestatic drug-induced liver injury and acute myocarditis in young, previously healthy males. It is prohibited at all times by WADA and is an unapproved, illegal-to-sell-for-human-use substance in most jurisdictions. Researchers who see this compound sold alongside genuine peptides should understand that its pharmacology, regulatory status, and safety concerns are categorically different from those of peptide research chemicals. Clinically significant risks — hepatic failure, myocarditis, HPG axis suppression — have been documented at recreational doses below the Phase 1 dose-limiting range.