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RAD-140

RAD-140 molecular structure

WADA PROHIBITED - Not permitted in competitive sports

Overview

RAD-140 (Testolone) is a selective androgen receptor modulator (SARM), not a peptide, being investigated for potential therapeutic applications in muscle wasting and breast cancer. SARMs are designed to selectively activate androgen receptors in muscle and bone while minimizing effects on reproductive organs, potentially offering anabolic benefits with fewer side effects than traditional androgens. Preclinical research demonstrates RAD-140 increases lean muscle mass, enhances strength, and may have neuroprotective properties. The compound has shown anti-tumor activity in androgen receptor-positive breast cancer models. Phase 1 clinical trials have evaluated safety in postmenopausal women with breast cancer. Despite being investigational and not approved for any medical use, RAD-140 is widely available in the supplement market and used for physique enhancement. The compound suppresses natural testosterone production, requires post-cycle therapy, and carries unknown long-term risks. RAD-140 is banned by WADA and most sports organizations. Liver toxicity has been reported in some users, highlighting the risks of unregulated use.

Last reviewed: 2026-08-18

Identity & Aliases

Also known as

TestoloneRAD140SARMSelective androgen receptor modulator
CAS1182367-47-0
PubChem44200882

Full composition (formula, molecular weight, sequence) in Quick Facts →

Research Areas

Breast cancer (ER+/HER2-)Muscle wastingAndrogen receptor signalingSarcopenia

Available Evidence

Human

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%).

Animal

Preclinical studies show RAD140 increases lean mass and muscle strength in animal models and has antitumor activity in AR-positive breast cancer models.

In Vitro

RAD140 is a nonsteroidal SARM with tissue-selective AR agonism designed to spare reproductive tissues; AR binding/activity was characterized in cell assays.

Uncertain

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

2 studies
Clinical2022

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%.

Benefits & Effects

2 documented

Anabolic effects (claimed)

anecdotalMuscle

Tissue-selective (theoretical)

anecdotalMuscle

Side Effects & Safety

7 reported

HEPATOTOXICITY (DILI case reports)

SevereUncommon

Onset: weeks

Myocarditis

SevereRare

Onset: weeks

Liver enzyme elevation

ModerateCommon Reversible

Onset: weeks

Testosterone suppression

ModerateCommon Reversible

Onset: weeks

Increased mortality (mice)

SevereUnknown

Severe side effect

Severe15+ case reports Reversible

Onset: 3-8 weeks

Management: DISCONTINUE; supportive care; corticosteroids

Dose-dependent

Moderate side effect

ModerateExpected Reversible

Onset: During use

Management: Post-cycle therapy; monitoring

Dose-dependent

Limitations & Open Questions

The only human trial is a small phase 1 oncology study in a specific patient population; there is no evidence of safety or efficacy for muscle-building use in healthy people, and liver enzyme elevations were frequent. It is not FDA approved and is prohibited in sport.

Pharmacology

RAD-140 (testolone) is an oral, nonsteroidal selective androgen receptor modulator (SARM), not a peptide. In the phase 1 trial, doses of 50-150 mg once daily were evaluated; the half-life was ~44.7 hours, supporting once-daily dosing, and the MTD was 100 mg/day. AR engagement was confirmed via decreased SHBG and increased PSA. WADA banned.

Reported Research Dosing

Reported values from research literature and community protocols. Educational reference only — not a dosing recommendation or medical advice.

dosage not established

Route: Oral
Half-life: ~60 hours

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

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.

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