RAD-140 (Testolone): The Complete Guide

RAD-140 has more peer-reviewed published human harm evidence than published human benefit evidence. This is rare and load-bearing for any decision to use it.

Peer-reviewed human harm signals:

• Phase 1 trial (LoRusso 2022, PMID 34565686) in 22 metastatic breast-cancer patients: AST elevations 59.1%, ALT elevations 45.5%, hyperbilirubinemia 27.3%. MTD 100 mg/day. Half-life 44.7 hr. One partial response.
• Four peer-reviewed DILI case reports from gray-market bodybuilding use:
  • Leung 2022 (PMID 36561105) — cholestatic injury
  • Mohamed 2023 (PMID 36945289) — cholestatic injury
  • Perananthan 2024 (PMID 38444893) — mixed-pattern injury
  • Demangone 2024 (PMID 39328701) — cholestatic injury
• Acute myocarditis — Padappayil 2022 (PMID 35233331).
• Gynecomastia / HPTA suppression — Chong 2024 (PMID 39145153) from a SARM-containing supplement.
• Dedicated NIH LiverTox monograph for SARMs (NBK619971).

Lead with this. If you decide to use RAD-140 anyway, do so with the harm asymmetry fully visible.

RAD-140 (testolone, clinical name vosilasarm) is a non-steroidal small-molecule selective androgen receptor modulator (SARM). It is not a peptide — it’s a small molecule, despite living in peptide-adjacent vendor catalogs.

Origin and pharma history:

• Discovered and characterized at Radius Health, Inc. (Cambridge, MA). Original characterization: Miller CP, Shomali M, Lyttle CR, et al. ACS Med Chem Lett 2010. PMID 24900290.
• Clinical program ultimately licensed to Ellipses Pharma (London) under the development name vosilasarm.
• First-in-human trial: NCT03088527 (postmenopausal women with ER+/HER2− metastatic breast cancer; sponsor Stemline Therapeutics during a transitional phase). Completed 2020. Results published as LoRusso 2022, PMID 34565686.

Provenance is well-documented in the primary literature — this is not a "Chinese research chemical with no IP trail" compound. The published trial just doesn’t support most of what gray-market vendors claim.

Regulatory status:

• FDA (US): not approved for any indication. FDA has issued public warnings about SARMs broadly (consumer warning, multiple enforcement letters). Sold gray-market with "research chemical" labeling.
• WADA 2026: prohibited at all times under S1.2 Other Anabolic Agents (SARMs). RAD-140 is named explicitly. Detection windows are extended; metabolite-ratio analysis can fingerprint dosing pattern (Wagener 2022, PMID 35888790).
• NIH LiverTox has a dedicated SARM monograph (NBK619971).

1. AR binding. RAD-140 binds the androgen receptor with high affinity (sub-nanomolar to low-nanomolar Ki in vitro; Miller 2010 PMID 24900290; Yu 2017 PMID 28974548).
2. Tissue selectivity (the “SARM” claim). In rat preclinical work, RAD-140 produced anabolic effects on levator ani muscle and bone with markedly weaker stimulation of prostate and seminal vesicle weight vs testosterone — the canonical anabolic-vs-androgenic dissociation. Critically, this selectivity does not extend to liver: SARMs as a class produce hepatic injury at gray-market human doses despite their muscle-vs-prostate selectivity.
3. Breast-cancer mechanism. In AR+/ER+ breast-cancer cells, RAD-140 occupancy of AR suppresses ESR1 (estrogen receptor) expression and downstream estrogen-driven proliferation — a fundamentally different mechanism from antiestrogens or aromatase inhibitors. Wei 2023 Cancer Res (PMID 36469363).
4. Neuroprotection. RAD-140 reduced neuronal cell death from apoptotic insults in cultured hippocampal neurons (matching testosterone in potency) and protected hippocampal neurons against systemic kainate excitotoxicity in male rats; protection was dependent on MAPK/ERK signaling. Jayaraman 2014 (PMID 24428527).

The one Phase 1 trial:

LoRusso P, et al. “A First-in-Human Phase 1 Study of a Novel Selective Androgen Receptor Modulator (SARM), RAD140, in ER+/HER2− Metastatic Breast Cancer.” Clin Breast Cancer 2022. PMID 34565686.

• 22 postmenopausal women with hormone-receptor-positive metastatic breast cancer.
• Dose-escalation; MTD 100 mg/day; dose-limiting toxicity at 150 mg.
• Half-life: 44.7 hr (the verified human number; the “16–20 hr” figure that circulates on vendor pages is unanchored).
• One partial response. One.
• Hepatic AEs dominant: AST 59.1%, ALT 45.5%, hyperbilirubinemia 27.3%.

The case-report literature (the harm pattern):

Severe cholestatic and mixed-pattern drug-induced liver injury reports are now in the mainstream hepatology literature. Onset typically 4–12 weeks into use. Bilirubin peaks in the 10–30 mg/dL range. Recovery can take months; some cases require liver biopsy and prolonged corticosteroid therapy.

Preclinical reproducibility:

Anabolic muscle/bone effects with relative prostate sparing are robust across the preclinical record (Miller 2010, Puskas 2025 PMID 40680216). Neuroprotection is reproducible (Jayaraman 2014). Negative effects on female-mouse muscle adaptation, frailty status, and mortality have been reported (Brown 2023 PMID 37758180) — the “anabolic” framing is not symmetric across sex or age.

StackTrax does not endorse RAD-140 use. The dosing below is community / forum convention. The hepatotoxicity case reports involve gray-market users at typical “cycle” doses; they are not high-dose outliers.

Parameter	Community-cited Range
Dose	5–30 mg/day oral
Cycle length	4–8 weeks (community); the Phase 1 oncology trial dosed continuously up to 100 mg/day
Route	Oral (capsule or liquid)
Half-life	44.7 hr (verified human, LoRusso 2022) — supports once-daily dosing

If used:

• Get baseline liver panel (AST, ALT, ALP, bilirubin, GGT) before starting.
• Repeat liver panel at 2 weeks, 4 weeks, monthly thereafter.
• Stop immediately if any liver enzyme exceeds 3× ULN OR if any symptom of jaundice / dark urine / scleral icterus appears.
• Get baseline lipid panel; SARMs class lower HDL.
• Get baseline testosterone, LH, FSH; class effect of HPTA suppression.
• Have a hepatologist’s number ready, not a peptide-clinic Telegram contact.

Hepatotoxicity (dominant):

Cholestatic and mixed-pattern drug-induced liver injury. AST/ALT elevations in >50% of trial patients at 100 mg/day. Multiple peer-reviewed case reports of severe DILI from gray-market doses (5–30 mg/day range). Onset typically 4–12 weeks. Recovery weeks-to-months. Some cases require corticosteroids.

HPTA suppression (class effect):

SARMs as a class suppress LH/FSH and endogenous testosterone. Chong 2024 (PMID 39145153) demonstrates reversible gynecomastia and hypogonadism. Recovery time varies. PCT regimens used by gray-market users are not validated in trials.

Cardiac signal:

Padappayil 2022 (PMID 35233331) reports acute myocarditis. The FDA SARM warning explicitly cites heart attack and stroke risk. Brown 2023 (PMID 37758180) reported negative impacts on skeletal muscle adaptation, frailty status, and mortality risk in female mice — the anabolic framing isn’t symmetric across sex or age.

Lipid changes:

Class effect — SARMs lower HDL. Specific RAD-140 lipid signature not characterized in published human work beyond the Phase 1 record.

Other reported:

• Sleep disruption / insomnia (community).
• Mood changes (irritability, aggression).
• Headaches.

• Any history of liver disease (active hepatitis, NAFLD, cirrhosis, prior DILI, Gilbert’s syndrome) — absolute.
• Any concurrent hepatotoxic drug (acetaminophen at-risk doses, isoniazid, methotrexate, etc.) — absolute.
• Pregnancy / breastfeeding / planning pregnancy — absolute (androgen exposure to fetus / infant).
• Active or prior prostate cancer in male users — relative caution despite the “tissue selectivity” framing; specialist sign-off.
• Cardiovascular disease — case-report myocarditis signal; lipid concerns.
• Eating disorder — SARMs amplify body-image-driven use patterns; harm potential is high.
• Athletes subject to anti-doping testing — do not use. WADA S1.2 names RAD-140 explicitly; metabolites detectable for extended windows.
• Anyone unwilling to monitor liver function — the case-report DILI literature exists because users went weeks without checking enzymes.

• Anabolic-androgenic steroids (AAS). Different chemistry (small-molecule SARM vs steroid scaffold). Both are AR agonists; both produce HPTA suppression. SARMs were marketed as “safer” alternatives but the published case-report record does not support that framing for RAD-140.
• Other SARMs: LGD-4033 (ligandrol), MK-2866 (ostarine), S-23, RAD-150 (TLB-150). Each has its own preclinical and (mostly limited) clinical record. The DILI signal is a class concern.
• Testosterone replacement therapy (TRT). TRT is a regulated medical therapy with established monitoring protocols. RAD-140 is a research chemical without medical supervision.
• Vosilasarm. The clinical-development name for RAD-140 under Ellipses Pharma. Same molecule.