C tier · mixed
A small first-in-human phase 1 oncology study defined a maximum tolerated dose but reported abnormal liver tests in roughly half of participants, and there is no human data of any kind outside advanced breast cancer.
rad-140
RAD140, now developed under the name vosilasarm, has a completed first-in-human phase 1 study in 22 postmenopausal women with metastatic breast cancer and is in phase 1/2 development. The trial defined a maximum tolerated dose but reported a high frequency of hepatic laboratory abnormalities, and the compound is not approved for any use.
// we supply this one
available as a research reagent
≥ 98% HPLC · research solution · batch certificate published. Grade C above is our own and is not adjusted because we stock it.
the explanation
RAD140 has been tested in a small number of women with advanced breast cancer, not in healthy people or athletes. In that trial, abnormal liver blood tests showed up in roughly half of participants, which is a meaningful signal from a study of only 22 people.
regulatory status
Not approved by FDA or any regulator; WADA-prohibited; not a lawful dietary supplement ingredient
RAD140 was originated by Radius Health in 2010 and is now in phase 1/2 development as vosilasarm by Ellipses Pharma for AR-positive breast cancer; it is not approved for any indication anywhere. FDA classifies SARMs in bodybuilding products as unapproved drugs and has issued public safety notifications citing liver injury and acute liver failure, heart attack and stroke. RAD140 is prohibited at all times in sport under WADA class S1.2. The SARMs Control Act (S.2742, 2018; S.2895, 2019) sought Schedule III placement for SARMs but was never enacted, with no further action reported as of 2022.
how it works · proposed mechanism
RAD140 is a high-affinity non-steroidal androgen receptor agonist under clinical investigation as an anti-tumour agent in AR-positive breast cancer.
High-affinity AR binding
RAD140 binds the androgen receptor with reported Ki of approximately 7 nM, compared with roughly 29 nM for testosterone. This higher affinity underlies its potency in preclinical anabolic assays.
Anabolic tissue selectivity
In castrated male rats RAD140 stimulated levator ani muscle to 117% of the effect of testosterone propionate at 10 mg/kg/day, with a preclinical profile favouring muscle over prostate. These are rodent findings and have not been reproduced as human muscle endpoints.
AR agonism in breast tumour tissue
The clinical development rationale is that AR agonism is growth-inhibitory in AR-positive, ER-positive breast cancer, which is why the only human trials are oncology trials. This is a distinct therapeutic hypothesis from the muscle-building use for which the compound is sold non-medically.
what’s reported
evidence shape
8 sourcesThe composition of the cited literature by study type. This describes the shape of the evidence, not its quality — and it does not by itself set the grade.
⚠ the catch
RAD140's only human data comes from an oncology dose-escalation study in 22 women with metastatic disease, where elevated AST occurred in 59% and elevated ALT in 46% of participants. A hepatic abnormality rate approaching half of a small cohort, in a compound with a 45–60 hour half-life, is a substantial signal that the non-medical literature almost never reports.
key published findings
- Human trial (phase 1, first-in-human, October 2017–September 2020): 22 postmenopausal women with metastatic breast cancer received 50–150 mg/day; the maximum tolerated dose was identified as 100 mg/day.
- Human trial (phase 1, safety): treatment-emergent findings included decreased SHBG in 100% of participants, elevated PSA in 80%, elevated AST in 59%, elevated ALT in 46% and elevated bilirubin in 27%, alongside vomiting (27%), dehydration (27%) and decreased appetite with weight loss (27%).
- Human trial (phase 1/2, ASCO 2025): results of a phase 1 study of vosilasarm (EP0062) in advanced or metastatic AR+/ER+/HER2- breast cancer were presented, with an ongoing phase 1/2 trial designed to enrol up to 128 patients.
- Rodent: in castrated male rats, RAD140 stimulated levator ani muscle to 117% of the response to testosterone propionate at 10 mg/kg/day.
- Non-human primate: in cynomolgus monkeys, RAD140 suppressed circulating testosterone by approximately 50% across dose levels spanning 0.01–1.0 mg/kg.
limitations of the evidence
- All human data derives from a small oncology dose-escalation cohort of postmenopausal women with metastatic breast cancer, a population whose baseline hepatic and metabolic status differs fundamentally from healthy users.
- No randomised controlled trial of RAD140 exists in any population, and there is no human data in men.
- Hepatic laboratory abnormalities in the phase 1 study cannot be cleanly attributed to RAD140 because oncology patients receive concurrent therapies and have disease-related organ involvement.
documented safety signals
- Hepatic laboratory abnormalities in the phase 1 trial were frequent: AST elevated in 59%, ALT in 46% and bilirubin in 27% of 22 participants.
- Drug-induced liver injury: RAD140 (vosilasarm) is specifically named in the NIH LiverTox SARMs chapter; multiple case reports document liver toxicity with non-medical use, and the class likelihood score is B (likely cause of clinically apparent liver injury).
- The class hepatotoxicity phenotype is cholestatic jaundice with bilirubin often peaking above 30 mg/dL against only 2–5 × ULN ALT and near-normal alkaline phosphatase, latency typically 2–3 months, occasionally causing reversible renal dysfunction requiring temporary dialysis.
- A published case report documents acute myocarditis associated with RAD140 use.
- Complete SHBG suppression (100% of phase 1 participants) and approximately 50% testosterone suppression in non-human primates indicate potent HPG axis interference.
- Elevated PSA in 80% of phase 1 participants indicates significant androgenic prostate-axis activity despite the 'selective' designation.
- FDA public safety notification on SARM-containing bodybuilding products names heart attack, stroke, psychosis, sleep disturbance, sexual dysfunction, liver injury and acute liver failure, infertility, miscarriage and testicular shrinkage.
- The unusually long 45–60 hour half-life means accumulation on repeated exposure and slow washout if an adverse reaction develops.
identity
| full name | RAD140 (testolone, vosilasarm, EP0062) |
| category | Anabolic & Receptor |
| modality | small molecule |
| formula | C20H16ClN5O2 |
| molar mass | 393.8 g/mol |
| cas | 1182367-47-0 |
| half-life | 45–60 hours (elimination half-life) |
laboratory handling
| storage | Reference material: store as a solid, desiccated and protected from light, at -20 °C for long-term stability; stock solutions typically stored at -80 °C with freeze-thaw cycles minimised. |
| solubility | Lipophilic small molecule; soluble in DMSO and ethanol, poorly soluble in aqueous buffer. Lot-specific figures should be taken from the certificate of analysis. |
| co-studied with | Evidence caveat only: phase 1 hepatic and PSA abnormalities occurred in patients receiving concurrent oncology care, so co-exposure confounding must be weighed before attributing those rates to RAD140 alone. |
Handling information describes laboratory practice for a research reagent. It is not a preparation guide for use in humans.
the receipts
5 citedLiverTox: Clinical and Research Information on Drug-Induced Liver Injury, NIDDK/NIH · 2024 · official
U.S. Food and Drug Administration · 2025 · official
Business Wire (San Antonio Breast Cancer Symposium) · 2022 · official
Journal of Clinical Oncology (ASCO Annual Meeting Abstracts) · 2025 · observational
Wikipedia (secondary compilation of primary trial and preclinical sources) · 2025 · reviews
others in Anabolic & Receptor