RAD-140

Muscle Growth & Body Composition

Also known as: Testolone, Vosilasarm, RAD140

Selective Androgen Receptor ModulatorsResearch phase: Phase 1Regulatory: Not FDA-approved. WADA prohibited. Available as research chemical. Under clinical investigation for breast cancer.

Mechanism

RAD-140 (Testolone) is a potent SARM known for strong anabolic effects comparable to low-dose testosterone, plus emerging neuroprotective properties. It has shown ability to protect brain cells from amyloid-beta toxicity in preclinical models. It entered Phase 1 trials for breast cancer (as an AR agonist to counter ER-driven tumors).

Technical detail

RAD-140 (vosilasarm/testolone) is a non-steroidal SARM demonstrating an anabolic:androgenic ratio exceeding 90:1 in preclinical models. It exhibits potent AR agonism in muscle and bone with significant selectivity over prostate. Notably, it demonstrates neuroprotective effects through AR-mediated upregulation of brain-derived neurotrophic factor (BDNF) and protection against amyloid-beta and kainate-induced neurotoxicity. Ellipses Pharmaceuticals conducted Phase 1 trials for AR-positive, ER-positive breast cancer.

Evidence

A First-in-Human Phase 1 Study of a Novel Selective Androgen Receptor Modulator (SARM), RAD140, in ER+/HER2- Metastatic Breast Cancer
LoRusso et al. (2022) — Clinical Breast Cancer — PMID: 34565686
Among 22 postmenopausal women with ER+/HER2- metastatic breast cancer, RAD140 had a half-life of about 44.7 hours, biomarker evidence of androgen receptor engagement, a 24-week clinical benefit rate of 18.2%, and frequent liver-enzyme elevations; the maximum tolerated dose was 100 mg/day.
emerging

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