COMPOUND

Compounds / SARMs

RAD-140

Vosilasarm (formerly Testolone, RAD140)

SARMs Oral Not FDA approved

Nonsteroidal selective androgen receptor modulator (SARM) originally developed by Radius Health (now Ellipses Pharma) as an investigational therapy for AR+/ER+/HER2- metastatic breast cancer. Long elimination half-life (~45-60h) supports once-daily oral dosing. Highly suppressive of endogenous testosterone production at any meaningful dose. Multiple peer-reviewed case reports of severe cholestatic drug-induced liver injury (DILI) at biohacker doses (10-30 mg/day), with one report documenting peak total bilirubin of 708 µmol/L (~35x ULN).

At a glance

Half-life
~50 h Clinical phase 1 (Hamilton 2021) reported t½ ~44.7h supporting QD dosing. Secondary sources cite a 45-60h range; 50h midpoint is a reasonable default.
Routes
Oral
Evidence base
3 studies 3 human

Mechanism

Tissue-selective AR agonist. Strong anabolic effect in muscle and bone via AR transactivation, with reduced androgenic activity in prostate and seminal vesicles compared to testosterone. Cannot aromatize to estradiol or 5α-reduce to DHT, but strongly suppresses LH and FSH via hypothalamic-pituitary feedback, shutting down endogenous testosterone production. Phase 1 in metastatic breast cancer: t½ 44.7h; AST elevation 59.1%, ALT 45.5%, bilirubin 27.3% at therapeutic doses. Hepatic metabolism is mixed (CYP3A4 dominant); the cholestatic DILI pattern resembles 17α-alkylated anabolic steroids despite RAD-140 being non-steroidal.

Dosing

Any amounts shown here are reported from published studies only. 3 of 3 catalogued studies involved human subjects. COMPOUND does not publish its own dosing guidance.

Where a study reports an amount, it appears in that study's entry below, attributed to the source.

Published evidence

  1. Human RCT 2022

    A First-in-Human Phase 1 Study of a Novel SARM (RAD140) in ER+/HER2- Metastatic Breast Cancer

    Hamilton EP, Wang JS, Pluard T, et al. Clinical Breast Cancer

    n=22 postmenopausal women, doses 50/100/150 mg/day. MTD = 100 mg/day. t½ = 44.7h supports QD dosing. AST↑ 59.1%, ALT↑ 45.5%, bilirubin↑ 27.3%. Clinical benefit rate 18.2% at 24 weeks.

    PMID 34565686

  2. Human case report 2024

    Severe liver injury following use of RAD-140, a SARM, for body building

    Perananthan V, George J Australian Prescriber

    43-y/o male, 2 months RAD-140. Peak total bilirubin 708 µmol/L (~35x ULN), ALT 158, INR 1.5. Cholestatic hepatitis on biopsy. Naranjo score 8 (probable). Full biochemical recovery 5 months post-discontinuation.

    PMID 38444893

  3. Human case report 2022

    RAD-140 Drug-Induced Liver Injury

    Leung K, Yaramada P, Goyal P, Cai CX, Thung I, Hammami MB Ochsner Journal

    24-y/o male, 5 weeks RAD-140 use. Presented with jaundice, pruritus. Peak total bilirubin 38.5 mg/dL. Liver biopsy: intracytoplasmic and canalicular cholestasis. Resolved after cessation.

    PMID 36561105

Reported side effects

HPTA suppression (testosterone, LH, FSH)
Very common Serious · Dose-related and severe at any meaningful biohacker dose. Recovery 4-12 weeks; longer cycles and higher doses prolong recovery.
Cholestatic drug-induced liver injury
Rare Serious · Multiple peer-reviewed case reports of severe cholestatic hepatitis at typical biohacker doses (5-30 mg/day for 4-8 weeks). Pattern: jaundice, scleral icterus, pruritus, total bilirubin 5-35x ULN. Recovery 3-6 months after discontinuation. PMID 36561105 (Leung 2022, peak bilirubin 38.5 mg/dL); PMID 38444893 (Perananthan 2024, peak bilirubin 708 µmol/L).
HDL cholesterol reduction
Very common Moderate · Class-wide effect of all SARMs. Reductions of 30-50% reported in clinical trials. Reverses on discontinuation.
AST/ALT/bilirubin elevation
Common Moderate · In oncology phase 1 (Hamilton 2021): AST elevation 59.1%, ALT 45.5%, bilirubin 27.3%. Generally reversible on dose reduction or discontinuation.
Aggression / mood changes
Occasional Mild · Community-reported. Likely AR-mediated CNS effect. Not formally studied.
Hair loss / acne
Occasional Mild · Androgenic side-effects from AR agonism in skin. Genetic-susceptibility-dependent.

Interactions

  • Anastrozole Redundant

    RAD-140 cannot aromatize to estradiol; AI is mechanistically unnecessary unless co-running aromatizable compounds (testosterone esters). May worsen lipid changes (HDL further reduced).

  • Test Cypionate Synergy

    Both AR agonists. Stacked use compounds suppression and cardiovascular/hepatic risk: additive HDL suppression, hematocrit elevation, HPTA shutdown.

  • MK-677 Synergy

    Common bulking stack. Insulin resistance from MK-677 + AR-mediated muscle growth amplifies anabolic signal but may worsen blood glucose control.

Storage

Capsules: room temperature, dry, dark. Liquid (PEG/ethanol vehicle): refrigerate after opening; protect from light. Underground source mislabeling is significant (Van Wagoner 2017: 39% of products mislabeled). Third-party COA recommended.