Skip to content
StackItSmart
CCase reports / series
High riskHepatotoxic signalHepatotoxicCardiotoxic

RAD-140

Testolone

RAD-140 (Testolone) is an orally active, non-steroidal selective androgen receptor modulator (SARM) originally developed by Radius Health as an experimental drug for breast cancer and muscle wasting. It is not an approved medicine and is banned in sport by WADA. People use it recreationally to try to build muscle, but the human safety record is dominated by harm signals: multiple published cases of severe cholestatic drug-induced liver injury (jaundice, bilirubin >30 mg/dL) in otherwise healthy young men, plus a case of acute myocarditis/heart failure. The only formal human trial was a small Phase 1 cancer study that found frequent liver-enzyme elevations. The main risks are serious, sometimes weeks-to-months-delayed liver injury; suppression of the body's own testosterone/HPTA axis; and cardiovascular strain. Products sold as RAD-140 are unregulated and frequently mislabeled or contaminated, compounding the risk. This compound has caused real liver failure risk in young users and should not be taken without medical supervision and bloodwork.

Clinical readoutSARM · sarm
Hepatic strainHigh
CardiovascularModerate
HPTA suppressionHigh
Half-life
44.7 h
Route
Oral
Evidence
C
Active
Long-acting
44.7 h3.7 d5.6 d7.5 d9.3 d
Illustrative single-compartment washout · each mark = one half-life · t½ ≈ Approximately 44.7 hours (terminal half-life) as measured in the first-in-human Phase 1 study, supporting once-daily dosing.
Pharmacology

Mechanism of action

RAD-140 is a non-steroidal SARM that binds the androgen receptor (AR) with high affinity and selectivity and acts as a tissue-selective AR agonist. In preclinical models it activates AR signaling in muscle and bone (anabolic) while producing comparatively less activity in classic androgenic tissues such as the prostate; in AR+/ER+ breast cancer models it acts as an AR agonist that represses estrogen-receptor signaling. As an AR agonist it also engages the hypothalamic-pituitary axis, lowering sex hormone-binding globulin (SHBG) and, by feedback, is expected to suppress endogenous gonadotropin and testosterone production. Its mechanism of hepatotoxicity is not fully defined and appears idiosyncratic/cholestatic.
Kinetics

Pharmacokinetics

Half-life

Approximately 44.7 hours (terminal half-life) as measured in the first-in-human Phase 1 study, supporting once-daily dosing.

Active duration

Long-acting; the ~45-hour half-life implies multi-day accumulation and a washout of roughly 1-2 weeks (about 5 half-lives) for near-complete clearance. Reported here for clinician discussion, monitoring, and washout reasoning only.

Route

Oral (oral tablet/capsule; the drug is orally bioavailable).

Metabolism & clearance

Hepatically metabolized with formation of multiple phase I/II metabolites; parent drug and metabolites are excreted in urine (characterized in a controlled human micro-dose excretion study). Hepatic involvement is consistent with the observed liver injury signal.

For monitoring and washout planning, not drug-test evasion.

Reported effects

Physiological & performance effects

  • Investigational anabolic effect on skeletal muscle: AR activation increased muscle fiber cross-sectional area in rats (preclinical).
  • Preclinical AR agonism in bone with potential to support bone mineral density (animal data; not demonstrated in humans).
  • Antitumor activity in AR+/ER+/HER2- metastatic breast cancer as an AR-targeted agent, with preliminary target engagement in a Phase 1 trial (partial response in 1 of 22 heavily pretreated patients; clinical benefit rate ~18% at 24 weeks).
  • Biochemical AR-engagement markers in humans: decreased serum SHBG in all treated patients and increased PSA in most, in the Phase 1 study.
  • Commonly used recreationally in an attempt to increase muscle mass and athletic performance; efficacy for this purpose in healthy people is not established in controlled human trials.
Safety

Adverse effects by system

Cardiovascular

A published case report describes acute myocarditis with heart failure and pulmonary edema in a young man self-medicating RAD-140 for bodybuilding. As an AR agonist it is also expected to adversely affect lipids (as androgens generally do), though RAD-140-specific human lipid data are lacking. Overall cardiovascular safety in humans is poorly characterized.

Hepatic

Most prominent documented harm. Multiple case reports describe severe cholestatic/mixed drug-induced liver injury (marked jaundice, pruritus, peak total bilirubin up to ~38 mg/dL) in young men after weeks to months of use, with liver biopsy showing canalicular/intracytoplasmic cholestasis. The Phase 1 trial found frequent treatment-emergent AST (59%), ALT (46%), and bilirubin (27%) elevations. Injury generally reversed after discontinuation but recovery can take months.

Endocrine / HPTA

As an AR agonist, RAD-140 lowers SHBG in humans (Phase 1) and is expected to suppress the hypothalamic-pituitary-gonadal axis and endogenous testosterone production, a known class effect of SARMs. Dedicated human studies of testosterone/LH/FSH suppression specific to RAD-140 are lacking; this is inferred and should be considered likely. No adequate human RAD-140 data quantify the degree of suppression.

Reproductive

Via expected HPTA suppression, reduced endogenous testosterone and potential impairment of spermatogenesis/fertility are plausible class effects; no adequate human RAD-140-specific reproductive outcome data exist. Contraindicated in pregnancy given androgenic mechanism.

Neuropsychiatric

No well-documented RAD-140-specific psychiatric adverse effects in the primary literature. Mood and behavioral changes are a general concern with androgenic compounds, but no adequate human RAD-140 data exist to confirm this.

Renal

No specific renal toxicity has been established for RAD-140 in humans; dehydration and decreased appetite/weight were reported as treatment-emergent events in the Phase 1 trial. No adequate data to characterize direct nephrotoxicity.

Hematologic

No RAD-140-specific human hematologic data (e.g., on hematocrit/polycythemia). Androgens can raise hematocrit as a class, but this has not been characterized for RAD-140; no adequate data.

Dermatologic

No robust RAD-140-specific dermatologic data. Androgenic skin effects (e.g., acne, hair changes) are theoretically possible given AR agonism but are not documented in the primary RAD-140 literature.

Recovery

HPTA suppression & recovery

Suppression: Expected moderate-to-significant suppression (class effect; not quantified for RAD-140 in humans)

RAD-140 is an AR agonist and reduced SHBG in all Phase 1 patients, consistent with meaningful axis engagement; suppression of endogenous testosterone is a recognized SARM class effect and should be assumed likely. The magnitude and time course of HPTA suppression and recovery specific to RAD-140 have not been studied in humans. Recovery is individual and variable. Any recovery approach must be directed by an endocrinologist; only single-SERM approaches are within scope of harm-reduction discussion, and dual-SERM protocols are explicitly out of scope. Do not self-manage recovery.

Bloodwork & vitals

Monitoring

Recommended labs & checks
Liver function panel (AST, ALT, ALP, total and direct bilirubin, GGT)Total and free testosterone, LH, FSH, SHBGFasting lipid panel (LDL, HDL, triglycerides)Complete blood count including hematocritPSA in men where clinically appropriateRenal function (creatinine, eGFR) and hydration status

Cadence: Baseline before any use; liver enzymes and bilirubin within the first 2-4 weeks and repeated periodically, given that injury has appeared anywhere from 5 weeks to 4 months in. Any symptoms warrant immediate testing rather than waiting for a scheduled interval. Ongoing care should be directed by a clinician.

Warning signs — seek care
  • Yellowing of the skin or eyes (jaundice), scleral icterus
  • Dark urine, pale/clay-colored stools
  • Itching (pruritus), right-upper-quadrant or diffuse abdominal pain
  • Nausea, vomiting, unusual fatigue, poor appetite
  • Chest pain, shortness of breath, leg swelling, or exercise intolerance (possible cardiac involvement)
Do not use if

Contraindications

  • Pre-existing liver disease or any condition with elevated liver enzymes/hyperbilirubinemia.
  • Concurrent use of other hepatotoxic drugs, supplements, or alcohol.
  • Known or suspected hormone-sensitive cancer, or use outside a supervised oncology trial.
  • Pregnancy and breastfeeding (androgenic mechanism; fetal risk).
  • Pre-existing cardiovascular disease, cardiomyopathy, or dyslipidemia.
  • Adolescents/individuals under 21 and anyone seeking non-medical performance enhancement.
  • Use of unregulated, non-prescription products of unknown identity/purity.
Combinations

Interaction profile

  • ModerateWith a thermogenic stimulant: Additive cardiovascular strain
  • MajorWith a 17α-alkylated oral: Additive liver strain
  • ModerateWith another liver-signal SARM: Additive liver strain
  • ModerateWith an anabolic steroid: Hormonal
  • ContraindicatedWith DNP: Additive cardiovascular strain

Check a specific combination in the interaction checker.

Harm reduction

Reducing harm & when to stop

  • RAD-140 is not an approved medicine and has caused serious, biopsy-confirmed liver injury in previously healthy young men; there is no established safe recreational dose.
  • Stop immediately and seek urgent medical care for any jaundice (yellow skin/eyes), dark urine, pale stools, itching, right-upper-quadrant pain, persistent nausea/vomiting, or unusual fatigue - these can signal liver injury that may progress to liver failure.
  • Seek emergency care for chest pain, breathlessness, or leg swelling, given a documented case of myocarditis/heart failure.
  • Get baseline bloodwork (liver panel, hormones, lipids, CBC) and follow-up testing under a clinician; liver injury has appeared from 5 weeks up to 4 months in, so a normal early test does not guarantee safety.
  • Avoid combining with alcohol, other hepatotoxic drugs, or additional hormonal/anabolic compounds, which compound liver and cardiovascular risk.
  • Products marketed as RAD-140 are unregulated and frequently mislabeled or contaminated; contents and dose cannot be assumed accurate.
  • HPTA suppression is expected; do not attempt to self-manage hormonal recovery - consult an endocrinologist. Dual-SERM protocols are out of scope.
  • This information is educational, not medical advice, and does not create a doctor-patient relationship; consult a qualified physician. 21+ only.
Evidence

Citations (12)

Every clinical claim above is tied to a primary source. Overall evidence grade C — graded to the best available evidence for its core claims.

  1. 01

    RAD-140 is an orally active non-steroidal SARM developed as an AR-targeted agent; first-in-human Phase 1 trial in ER+/HER2- metastatic breast cancer characterized safety, PK, and target engagement.

    RCTA First-in-Human Phase 1 Study of a Novel Selective Androgen Receptor Modulator (SARM), RAD140, in ER+/HER2- Metastatic Breast Cancer.PMID 34565686 ↗

  2. 02

    Terminal half-life is approximately 44.7 hours, supporting once-daily oral dosing; SHBG decreased in all treated patients and PSA increased in most (AR engagement).

    RCTA First-in-Human Phase 1 Study of a Novel Selective Androgen Receptor Modulator (SARM), RAD140, in ER+/HER2- Metastatic Breast Cancer.PMID 34565686 ↗

  3. 03

    In the Phase 1 trial, the most frequent treatment-emergent adverse events were elevated AST (59.1%), ALT (45.5%), and total bilirubin (27.3%), with Grade 3/4 transaminase elevations and hypophosphatemia.

    RCTA First-in-Human Phase 1 Study of a Novel Selective Androgen Receptor Modulator (SARM), RAD140, in ER+/HER2- Metastatic Breast Cancer.PMID 34565686 ↗

  4. 04

    RAD-140 caused severe cholestatic drug-induced liver injury in a 24-year-old man after 5 weeks of use, with peak total bilirubin 38.5 mg/dL and biopsy-confirmed canalicular cholestasis, resolving after cessation.

    Case reportRAD-140 Drug-Induced Liver Injury.PMID 36561105 ↗

  5. 05

    RAD-140 use was associated with jaundice, elevated liver enzymes and hepatic steatosis in a 29-year-old man after three months, resolving after discontinuation.

    Case reportSelective Androgen Receptor Modulators Leading to Liver Injury: A Case Report.PMID 39328701 ↗

  6. 06

    Severe liver injury followed RAD-140 use for body building (case report).

    Case reportSevere liver injury following use of RAD-140, a selective androgen receptor modulatorPMID 38444893 ↗

  7. 07

    A 22-year-old man developed cholestatic DILI after 16 weeks of RAD-140 with total bilirubin peaking ~530 umol/L; liver enzymes normalized 3-12 months after discontinuation.

    Case reportSelective Androgen Receptor Modulators (SARMs)-Induced Liver Injury: A Case Report and Review of LiteraturePMID 36945289 ↗

  8. 08

    RAD-140 was associated with idiosyncratic drug-induced liver injury in a 26-year-old man, with normalization at 2-month follow-up after stopping.

    Case reportIdiosyncratic drug-induced liver injury related to use of novel selective androgen receptor modulator RAD140 (Testalone): a case report.PMID 36978171 ↗

  9. 09

    Acute myocarditis with heart failure and pulmonary edema occurred in a young man self-medicating with RAD-140 for bodybuilding.

    Case reportAcute Myocarditis From the Use of Selective Androgen Receptor Modulator (SARM) RAD-140 (Testolone).PMID 35233331 ↗

  10. 10

    RAD-140 undergoes hepatic metabolism to multiple metabolites excreted in urine, characterized in a controlled human micro-dose excretion study; it is prohibited in sport at all times by WADA.

    CohortHuman In Vivo Metabolism and Elimination Behavior of Micro-Dosed Selective Androgen Receptor Modulator RAD140 for Doping Control Purposes.PMID 35888790 ↗

  11. 11

    RAD-140 binds the androgen receptor with high affinity/specificity and acts as a tissue-selective AR agonist, activating AR in breast cancer/muscle while repressing ER signaling (preclinical mechanism).

    PreclinicalSelective Androgen Receptor Modulator RAD140 Inhibits the Growth of Androgen/Estrogen Receptor-Positive Breast Cancer Models with a Distinct Mechanism of Action.PMID 28974548 ↗

  12. 12

    RAD-140 increased skeletal muscle fiber cross-sectional area in rats, supporting an anabolic effect (preclinical).

    PreclinicalPreclinical assessment of the selective androgen receptor modulator RAD140 to increase muscle mass and bone mineral density.PMID 40680216 ↗

Last reviewed 2026-07-06 · Verified against PubMed · Educational, not medical advice