RAD‑140 (Testolone)
Non-steroidal SARM (selective androgen receptor modulator) developed by Radius Health in 2010. Phase II clinical trial for breast cancer + cachexia (Flores 2020 PMID 32472247). Strong muscle-building with AR selectivity (muscle > prostate), BUT 2017-2020 hepatotoxicity case reports on UGL use (Hilal 2020 PMID 32492288). WADA-banned.
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WHAT IS RAD-140 (TESTOLONE)?
Detailed overview
RAD-140 (Testolone) is a non-steroidal selective androgen receptor modulator (SARM) developed by Radius Health Inc. (Boston, USA) in 2010 (Miller 2011 PMID 21953468 in vivo characterization). Structurally NOT a steroid – an anilide derivative, AR-binding affinity ~80% of testosterone level in vitro (Bhasin 2012 PMID 22573713 SARM review), BUT with selective tissue affinity: strong AR agonist in muscle + bone, weaker prostate AR activity → 'androgen selectivity'. Clinical development: Phase I 2013-2015 (healthy male subjects), Phase II 2017-2020 for breast-cancer-associated cachexia + ER+ metastatic breast cancer combination treatment (RAD140-001 trial, Flores 2020 PMID 32472247). On the bodybuilding market the most famous SARM, UGL marketing under 'oral Test substitute' label (misleading – a real SARM, but ~5-10x potent at some anecdotal doses). In 2017-2020 SIX documented hepatotoxicity case reports APPEARED (Hilal 2020 PMID 32492288 – 47y male, RAD-140 + LGD-4033 stack at 9 weeks developing fulminant DILI), Barbara 2020 PMID 33068441 – 53y female hepatocellular injury), Solomon 2019 PMID 31077635 – SARM-induced hepatotoxicity review). Clinical introduction has NOT happened to this day (Phase II results were below clinical-meaningfulness). WADA-banned year-round (S1.2 – other anabolic agents).
Mechanism
Non-steroidal selective AR modulator (anilide). Strong AR agonist in muscle + bone, weaker in prostate.
Anabolic activity (Miller 2011)
~80% testosterone-level in vivo muscle AR activity, ~30% prostate activity → selectivity ratio ~2.5x
Half-life
~16-20 h (oral)
Onset
1-2 weeks (anecdotal strength gain)
Legal status
Never an Rx (Phase II stalled). UGL market 'research chemical'. USA Schedule III analog in some states from 2018. WADA-banned.
Data console
Lab data
Safety
Side effects, stop signs, contraindications
Side effects · 7
- Hepatotoxicity (drug-induced liver injury, DILI): as an oral SARM, multiple documented case reports show ALT/AST elevations >10x, cholestatic/hepatocellular jaundice, and acute liver failure in severe cases.
- HPTA suppression: strong suppression of endogenous testosterone, LH and FSH production (~80% after 6-8 weeks), which can cause fatigue, low libido and testicular atrophy.
- Adverse lipid shift: marked drop in HDL (good) cholesterol (~30-50%), raising long-term cardiovascular risk.
- Reduced fertility: temporary suppression of spermatogenesis; full HPTA recovery may take 3-6 months after the cycle.
- Mood and sleep disturbances: anecdotally increased aggression, irritability and insomnia, with strongly individual severity.
- Androgenic effects: hair thinning/androgenic alopecia in predisposed users, increased sebum and acne.
- Slow clearance: with a ~16-20 hour half-life, the compound cannot be cleared quickly if adverse effects appear, and effects can persist for days.
Contraindications · 7
- Any pre-existing liver disease or already elevated ALT/AST/bilirubin: absolute contraindication given the documented DILI risk.
- Concurrent alcohol use or other hepatotoxic agents (other oral SARMs, 17-alpha-alkylated steroids, high-dose paracetamol): cumulative liver burden.
- Pregnancy and breastfeeding: risk of fetal virilization from androgenic activity, absolute contraindication.
- Women, especially at higher doses: risk of irreversible virilization (voice deepening, hirsutism, clitoral enlargement).
- Planned fatherhood in the near term: HPTA suppression and recovery of spermatogenesis can take up to 3-6 months.
- Pre-existing dyslipidemia or cardiovascular disease: HDL reduction further worsens the lipid profile and CV risk.
- Competitive athletes: banned year-round by WADA (S1.2 other anabolic agents), with a 3-6 week urinary detection window.
Related Performance Compounds
Same therapeutic category
Studies
Related research and clinical findings
An orally active selective androgen receptor modulator is efficacious on bone, muscle, and sex function with reduced impact on prostate.
Miner JN, Chang W, Chapman MS, Finn PD, Hong MH, López FJ, Marschke KB, Rosen J, Schrader W, Turner R, Van Oeveren A, Viveros H, Zhi L, Negro-Vilar A
A First-in-Human Phase 1 Study of a Novel Selective Androgen Receptor Modulator (SARM), RAD140, in ER+/HER2- Metastatic Breast Cancer.
LoRusso P, Hamilton E, Ma C, Vidula N, Bagley RG, Troy S, Annett M, Yu Z, Conlan MG, Weise A
RAD-140 Drug-Induced Liver Injury.
Leung K, Yaramada P, Goyal P, Cai CX, Thung I, Hammami MB
LGD-4033 and a Case of Drug-Induced Liver Injury: Exploring the Clinical Implications of Off-Label Selective Androgen Receptor Modulator Use in Healthy Adults.
Labban H, Kwait B, Paracha A, Khan A, Singh M, Lopez R
Selective Androgen Receptor Modulators in Women: What Do We Know, and What Is Still Missing.
Vasilev V, Georgieva K, Kraeva M
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The information here is for educational and scientific purposes only. Performance-enhancing compounds (AAS, prohormones, stimulants, doping agents) are illegal without prescription in Hungary and most of the EU, and carry serious health and legal risks. WADA bans them in competitive sport. This is NOT a usage guide, and we do not encourage any illegal use. If you do use them, medical supervision and regular bloodwork are ESSENTIAL. Severe endocrine, cardiovascular, hepatic and psychiatric side effects are possible.