Phase 1 study in 22 women with ER+/HER2- metastatic breast cancer: RAD140 (50-150 mg/day) demonstrated AR engagement; at the 100 mg/day MTD one patient with an ESR1 mutation had a partial response, with clinical benefit rate 18.2% at 24 weeks and median PFS 2.3 months. AST/ALT elevations occurred in 59%/45%.
RAD-140

WADA PROHIBITED - Not permitted in competitive sports
Overview
Last reviewed: 2026-08-18
Identity & Aliases
Also known as
Full composition (formula, molecular weight, sequence) in Quick Facts →
Research Areas
Available Evidence
A first-in-human phase 1 dose-escalation study (3+3 design) enrolled 22 postmenopausal women with heavily pretreated ER+/HER2- metastatic breast cancer. RAD140 (50-150 mg/day oral) showed AR engagement (decreased SHBG, increased PSA); at the 100 mg/day MTD, one patient with an ESR1 mutation had a partial response; clinical benefit rate at 24 weeks was 18.2% and median PFS was 2.3 months. Frequent adverse events were elevated AST (59.1%) and ALT (45.5%).
Preclinical studies show RAD140 increases lean mass and muscle strength in animal models and has antitumor activity in AR-positive breast cancer models.
RAD140 is a nonsteroidal SARM with tissue-selective AR agonism designed to spare reproductive tissues; AR binding/activity was characterized in cell assays.
Claims of anabolic effects in healthy users, post-cycle therapy needs, and long-term safety are not clinically validated; the compound is not approved and is banned by WADA. Liver enzyme elevations were common in the phase 1 trial.
Key Studies & Findings
Preclinical studies demonstrated RAD140 increases lean muscle mass and strength in animals and shows antitumor activity in androgen-receptor-positive breast cancer models.
Benefits & Effects
Side Effects & Safety
Severe side effect
Onset: 3-8 weeks
Management: DISCONTINUE; supportive care; corticosteroids
Dose-dependent
Moderate side effect
Onset: During use
Management: Post-cycle therapy; monitoring
Dose-dependent
Limitations & Open Questions
Pharmacology
Reported Research Dosing
Reported values from research literature and community protocols. Educational reference only — not a dosing recommendation or medical advice.
dosage not established
Frequently Asked Questions
Is RAD-140 a peptide?
No. RAD-140 (testolone) is a nonsteroidal selective androgen receptor modulator (SARM) — a small-molecule drug class, not a peptide.
Has RAD-140 been tested in humans?
Yes — in a small first-in-human phase 1 oncology trial in postmenopausal women with ER+/HER2- metastatic breast cancer; no trials support its use for muscle building.
What are the safety concerns with RAD-140?
The phase 1 trial reported frequent elevated liver enzymes (AST/ALT) and other toxicities; unregulated use also suppresses natural testosterone, and WADA bans it.
Research Citations
Leung K, Yaramada P, Goyal P, Cai CX, Thung I, Hammami MB (2022)
Schwartzman KH, Kohli U, Chaudhuri NR, Hoda M (2024)
Barbara M, Dhingra S, Mindikoglu AL (2020)
Zierau O, Kolodziejczyk A, Vollmer G, Machalz D, Wolber G, Thieme D, Keiler AM (2019)
+ 33 more citations
Related Resources
Quick Facts
Formula
C20H16ClN5O2
Molecular Weight
393.8
Sequence
MLSRLMSGSSRSLEREYSCTVRLLDDSEYTCTIQRDAKGQYLFDLLCHHLNLLEKDYFGIRFVDPDKQRHWLEFTKSVVKQLRSQPPFTMCFRVKFYPADPAALKEEITRYLVFLQIKRDLYHGRLLCKTSDAALLAAYILQAEIGDYDSGKHPEGYSSKFQFFPKHSEKLERKIAEIHKTELSGQTPATSELNFLRKAQTLETYGVDPHPCKDVSGNAAFLAFTPFGFVVLQGNKRVHFIKWNEVTKLKFEGKTFYLYVSQKEEKKIILTYFAPTPEACKHLWKCGIENQAFYKLEKSSQVRTVSSSNLFFKGSRFRYSGRVAKEVMESSAKIKREPPEIHRAGMVPSRSCPSITHGPRLSSVPRTRRRAVHISIMEGLESLRDSAHSTPVRSTSHGDTFLPHVRSSRTDSNERVAVIADEAYSPADSVLPTPVAEHSLELMLLSRQINGATCSIEEEKESEASTPTATEVEALGGELRALCQGHSGPEEEQVNKFVLSVLRLLLVTMGLLFVLLLLLIILTESDLDIAFFRDIRQTPEFEQFHYQYFCPLRRWFACKIRSVVSLLIDT
Mechanism
Selective Androgen Receptor Modulator (SARM) - NOT A PEPTIDE
Safety Information
SERIOUS SAFETY CONCERNS - NOT APPROVED. Multiple case reports of HEPATOTOXICITY (drug-induced liver injury). WADA BANNED. NO SAFE PROTOCOL. Sold illegally but carries significant health risks.
Citations
38Leung K, Yaramada P, Goyal P, Cai CX, Thung I, Hammami MB (2022)
Schwartzman KH, Kohli U, Chaudhuri NR, Hoda M (2024)
Barbara M, Dhingra S, Mindikoglu AL (2020)
Zierau O, Kolodziejczyk A, Vollmer G, Machalz D, Wolber G, Thieme D, Keiler AM (2019)
+ 33 more citations