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RAD-140 / Testolone

RAD-140 · Testolone · SARM

C
Animal replicated
Research chemicalSARMSelective Androgen Receptor ModulatorSmall Molecule
RouteOralGray-market only
C
Evidence grade: Animal replicated

Effect demonstrated in multiple animal studies; human data sparse or extrapolated. Grades summarize evidence quality, not whether a compound is appropriate, legal, or risk-free.

At a glance
What it is
Nonsteroidal selective androgen receptor modulator (SARM); orally active small-molecule androgen receptor ligand.
Why people use it
Used primarily for muscle and performance and hormonal support.
What the evidence supports
Ostarine (MK-2866, enobosarm) is the most studied SARM and the one with the most published human clinical trial data. Comparing RAD-140 and Ostarine illuminates the risk-benefit tradeoffs within the SARM class.
If you only read one thing

RAD-140 is marketed to the community as the most selective SARM — greater anabolic effect per androgenic side effect ratio than any other compound in the class. The reality from human data is more troubling. The only published Phase 1 clinical trial documented elevated liver enzymes (AST, ALT) and elevated bilirubin in the majority of participants. The case report literature has accumulated 6+ published cases of serious RAD-140-associated DILI — including cholestatic hepatitis with near-transplant severity. The HPTA suppression is as real and often as severe as testosterone. The prostate selectivity advantage, while supported by animal data, has not been validated in human trials at the doses community users employ. The compound that was supposed to be 'steroids without the side effects' has demonstrated a serious hepatotoxicity signal and suppresses the testosterone axis reliably. This chapter does not argue that community users should never use RAD-140 — it argues that the risk-benefit calculation requires honest accounting of the hepatotoxicity signal, and that the selectivity claim should not be accepted uncritically.

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Published literature
1human RCT0human studies0animal0in vitro
Evidence reality check
Human evidence
1 human study
1 randomized; 0 observational.
Preclinical base
0 lab signals
0 animal; 0 in-vitro/mechanistic.
Evidence snapshot
Ostarine (MK-2866, enobosarm) is the most studied SARM and the one with the most published human clinical trial data. Comparing RAD-140 and Ostarine illuminates the risk-benefit tradeoffs within the SARM class.
From the chapter quick-reference block.
Categories
Muscle & PerformanceHormonal & HPTA
Properties
Active malignancy: hard stopWADA S1✓ Human RCTHPTA: suppressiveNot injectable
Evidence
CAnimal replicated
The Selectivity Problem
The SARM selectivity hypothesis: different tissues express different AR coregulators, which alter the conformational response of the AR to ligand binding, enabling selective agonism or antagonism depending on tissue context. For RAD-140, muscle AR = agonist (anabolic); prostate AR = antagonist (anti-androgenic). This is pharmacologically plausible and demonstrated in rodent models. The Phase 1 human trial: elevated AST in 59.1% of participants, elevated ALT in 45.5%, elevated total bilirubin in 27.3%. Liver is not the target tissue for RAD-140's proposed anabolic effect — hepatotoxicity was an off-target adverse effect that the selectivity hypothesis did not predict and the preclinical data did not adequately signal.
The Hepatotoxicity Signal
Multiple independent published case reports (2020-2024) document RAD-140-associated drug-induced liver injury (DILI): cholestatic hepatitis; jaundice; markedly elevated bilirubin (peak values up to 708 μmol/L in one severe case); cholestatic pattern on liver biopsy; one Australian case that nearly required liver transplantation. One additional case of acute myopericarditis in a 16-year-old following a single RAD-140 dose. All cases improved or resolved after RAD-140 discontinuation, but recovery took weeks to months and some cases were severe enough to require hospitalization. The hepatotoxicity mechanism is not established — direct toxicity, reactive metabolites, or cholestatic effects are proposed.
HPTA Suppression — Predictable and Real
RAD-140 suppresses the hypothalamic-pituitary-testicular axis via negative feedback from exogenous androgen receptor stimulation. LH and FSH fall; endogenous testosterone production declines substantially. Community users consistently report testosterone suppression — often more profound than expected, with values falling into the hypogonadal range during cycles. Recovery after stopping RAD-140 typically occurs over 6-12 weeks but is variable. PCT (Post-Cycle Therapy) with a SERM (clomiphene, tamoxifen) or hCG is used by most community users to accelerate recovery. Suppression severity is dose and duration dependent.
Legal and Regulatory Status
Not FDA-approved for any human use. FDA has issued multiple public warnings about SARMs specifically mentioning RAD-140, noting risks of liver toxicity, heart attack, stroke, and life-threatening adverse effects. WADA Prohibited List S1.2 (Other Anabolic Agents) — absolute ban in competition and out-of-competition for athletes. Not a scheduled controlled substance in the US (legal to possess but illegal to sell for human consumption or to mislabel as a supplement). Major online marketplaces have banned SARM sales. Despite this, RAD-140 is widely available on bodybuilding supplement websites.
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Alternatives

Compare nearby options

Browse this classCompare 4 side by side →
Enclomiphene
C
Same class · Small Molecule

The Pure Active Isomer in Clomid. The Drug That Raised Testosterone as Well as TRT While Preserving Fertility — and Still Failed FDA Approval. The Zuclomiphene Problem: Why the Racemic Mixture Causes Side Effects Pure Enclomiphene Shouldn't. The NDA That Died in 2021. How It Differs from TRT, HCG, and Gonadorelin for Male Hypogonadism. The 2025 Meta-Analysis: +273 ng/dL Testosterone vs Placebo.

LGD-4033 / Ligandrol
C
Same class · SARM

The Most Phase-1-Tested SARM in History. The Problem: Phase 1 Used 0.1-1 mg. The Community Uses 5-20 mg. +1.21 kg Lean Mass at 1 mg in 21 Days. Phase 2 Hip Fracture Trial Positive. HPTA Suppression Dose-Dependent and Documented in Clinical Data. The Dose Gap Between Clinical Trials and Community Use Is the Central Risk Issue. Multiple Elite Athlete Doping Violations Including Canelo Álvarez. WADA S1.2.

Ostarine (MK-2866)
C
Same class · SARM

The Most Clinically Studied SARM. The Phase 3 Trials That Nearly Got It Approved. Why the FDA Said No — and Why It Matters. The Most Modest HPTA Suppression Profile in the SARM Class. The Lowest Hepatotoxicity Signal. The Closest Any SARM Has Come to an FDA Indication. Why Phase 3 Failure Doesn't Mean the Compound Doesn't Work. Jonas Brodin and the NHL Doping Case.

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