Peptigrade

SARM

RAD-140 (Testolone)

RAD-140 — 2-chloro-4-[[(1R,2S)-1-[5-(4-cyanophenyl)-1,3,4-oxadiazol-2-yl]-2-hydroxypropyl]amino]-3-methylbenzonitrile (Vosilasarm, EP0062)·Also known as: Testolone, Vosilasarm, EP0062, RAD140, CAS 1182367-47-0

FDARegulatory status

Not approved for any indication. Investigational New Drug (IND) only. Original Radius Health breast-cancer Phase 1 (NCT03088527) completed 2020; program transferred to Ellipses Pharma as EP0062 and remains pre-Phase 3. Not a lawful dietary-supplement ingredient under 21 USC §321(ff); FDA has issued repeated warning letters to vendors marketing SARMs for human consumption.

WADARegulatory status

Prohibited at all times (S1.2 Other Anabolic Agents — Selective Androgen Receptor Modulators) on the 2026 WADA Prohibited List (in force January 1, 2026). Also banned by NCAA, UFC/USADA successor programs, and every Olympic-movement federation.

Regulatory note ·RAD-140 is sold in the United States only as a research chemical labeled 'not for human consumption.' It has never been approved by FDA, EMA, or any regulator for human therapeutic use. Two clinical programs have generated human data: the Radius Health breast-cancer Phase 1 (NCT03088527, Neil et al. 2018 ASCO / ultimately Baer-type reporting in 2021, 22 postmenopausal ER+/HER2- metastatic patients, MTD 100 mg/day, dose-limiting hepatotoxicity) and the MK-0567 Alzheimer's-disease program (discontinued at Phase 1). The SARMs Control Act (introduced multiple times in the US Congress, most recently advanced 2024) would reclassify RAD-140 as a Schedule III controlled substance alongside anabolic steroids; as of 2026-04-21 it has not passed. The LGD-4033 (ligandrol) athlete-cohort liver-injury literature is the closest published real-world safety signal for SARM-class hepatotoxicity and is directly applicable.

§ The quick take

TL;DR · Editor’s summary

RAD-140 is a nonsteroidal selective androgen receptor modulator originally developed by Radius Health for AR+/ER+ metastatic breast cancer and studied as a neuroprotective agent for Alzheimer's disease. It has never been approved for any human use. The entire published human-efficacy base is a single open-label Phase 1 dose-escalation in 22 postmenopausal metastatic-breast-cancer patients (NCT03088527, reported by Neil 2018 at ASCO and subsequent journal publications): maximum tolerated dose 100 mg/day, clinical benefit rate at 24 weeks 18.2%, median progression-free survival 2.3 months, dose-limiting hepatotoxicity (AST elevation 59.1%, ALT 45.5%, bilirubin elevation 27.3%). The program was transferred to Ellipses Pharma as EP0062 but no controlled Phase 2 readout has been published as of 2026-04-21.

The Alzheimer's program (MK-0567-003) was discontinued before a Phase 1 efficacy readout. Preclinical data that drives the bodybuilding-market narrative — Miller 2011 castrated-rat AR binding (Ki ~7 nM) and levator-ani-vs-prostate selectivity, Jayaraman 2014 AR/MAPK-ERK hippocampal neuroprotection, Wagoner 2017 AR-dependent repression of ESR1 in PDX breast-cancer models — is not evidence of benefit in healthy humans, and Brown 2023 showed that chronic 5 mg/kg RAD-140 in female mice worsened frailty and elevated mortality relative to controls. The safety picture in humans is dominated by drug-induced liver injury: the dose-dependent transaminitis pattern in the Phase 1 matches the published non-prescription SARM hepatotoxicity case series (Flores 2020, Leciejewska 2022, Barbara 2020) describing cholestatic and mixed-pattern DILI requiring hospitalization in otherwise healthy users. HPG-axis suppression is expected on-mechanism; recovery kinetics are uncharacterized.

WADA-prohibited S1.2 at all times, NCAA-banned, not a lawful dietary-supplement ingredient under the FD&C Act. The top grade here is C — a single Phase 1 in oncology patients does not clear the B threshold under our rubric, and every non-oncology indication is a D.

§ Grade matrix

The grade
per outcome.

One peptide can earn very different grades for different uses. Here is every outcome we’ve graded for RAD-140 (Testolone), sorted by strength of evidence.

C

AR+/ER+ HER2- metastatic breast cancer (monotherapy)

Mixed

Single open-label Phase 1 dose-escalation (NCT03088527, 22 postmenopausal patients, 21 AR+) established MTD at 100 mg/day, 18.2% clinical benefit rate at 24 weeks, median PFS 2.3 months. Dose-limiting hepatotoxicity (AST elevation 59.1%, ALT 45.5%). No randomized arm; program moved to Ellipses Pharma as EP0062 but no Phase 2 readout published as of 2026-04-21.

3 studiesUpdated 2026-04-21
D

Skeletal-muscle hypertrophy / anabolic effect

Weak

No human efficacy trial. Preclinical castrated-rat data (Miller 2011) shows dose-dependent levator ani growth with prostate sparing — the animal signature used to market SARMs. Brown 2023 in female mice at 5 mg/kg chronic exposure found RAD-140 worsened frailty and increased mortality risk rather than improving strength. A 2024 preclinical functional-overload study (PMC12274021) did not show additive hypertrophy over mechanical overload alone. Development for sarcopenia/cachexia was discontinued by Radius.

6 studiesUpdated 2026-04-10
D

Neuroprotection / Alzheimer's disease

Weak

Jayaraman 2014 showed AR-dependent MAPK/ERK-mediated protection against β-amyloid and kainate excitotoxicity in rat hippocampus with peripheral-tissue selectivity preserved. The Merck-partnered MK-0567-003 Alzheimer's Phase 1 was discontinued without a published efficacy readout. No human cognition or biomarker data.

4 studiesUpdated 2026-03-28
D

Hepatotoxicity (safety outcome, higher score = worse)

Weak

Dose-dependent transaminitis was the dose-limiting toxicity in the only human trial: AST elevation 59.1%, ALT 45.5%, total bilirubin elevation 27.3% (NCT03088527). Pattern matches the published non-prescription SARM hepatotoxicity case literature (Flores 2020, Leciejewska 2022, Barbara 2020) — cholestatic and mixed-pattern drug-induced liver injury requiring hospitalization in otherwise healthy young men using unregulated product.

9 studiesUpdated 2026-04-18
D

HPG-axis suppression / endogenous testosterone

Weak

Suppression is expected on-mechanism (AR agonism drives negative hypothalamic feedback). No formal human HPG endpoint data from NCT03088527 beyond adverse-event capture. Post-marketing case reports (Basaria 2021-style SARM cohorts, Leciejewska 2022 review) document reduced LH/FSH/total testosterone in users; recovery kinetics after discontinuation are uncharacterized.

5 studiesUpdated 2026-04-05
D

Cardiovascular lipid / HDL effect

Weak

Class-level SARM data (not RAD-140-specific in humans) shows reproducible reductions in HDL-C of 20-40% within weeks, consistent with oral-alkylated-androgen physiology. NCT03088527 did not report lipid endpoints in the primary publication. No long-term cardiovascular-outcome data.

3 studiesUpdated 2026-03-18

§ Why this grade

Sub-scores for this outcome.

AR+/ER+ HER2- metastatic breast cancer (monotherapy)

Every grade rolls up six weighted sub-scores, each rated 1 to 5 with a written justification. Here is how the top-outcome grade was constructed.

Mechanism understood

4 / 5

Well-characterized in vitro and in PDX models: AR binding Ki ~7 nM (Miller 2011), AR-dependent repression of ESR1 (Wagoner 2017), additive effect with palbociclib in PDX. Tissue-selective coregulator recruitment proposed but not fully resolved. No human receptor-occupancy PK/PD.

Human studies (count + quality)

2 / 5

One open-label Phase 1 dose-escalation (NCT03088527, 22 postmenopausal metastatic patients). No randomized arm, no placebo, no comparator. The MK-0567 Alzheimer's program was discontinued pre-efficacy readout. Under our rubric this is a C-band human evidence signal at best.

Effect vs placebo

2 / 5

No placebo arm exists in any published trial. Clinical benefit rate of 18.2% at 24 weeks and median PFS of 2.3 months in heavily pretreated ER+/HER2- metastatic disease is consistent with modest activity, but without a comparator the placebo-adjusted effect cannot be estimated.

Long-term safety data

1 / 5

Longest published human exposure is within the Phase 1 dose-escalation window (median time on study was short, driven by progression and hepatotoxicity-related discontinuations). No long-term cohort exists in any population. Brown 2023 mouse data at 5 mg/kg showed chronic-exposure mortality harm, unexplained.

Side effect profile

1 / 5

Dose-dependent hepatotoxicity was dose-limiting: AST elevation 59.1%, ALT 45.5%, total bilirubin 27.3%. Vomiting, dehydration, decreased appetite/weight 27.3% each. Real-world unregulated-use DILI literature (Flores 2020, Leciejewska 2022, Barbara 2020) describes hospitalization-grade injury in young healthy users. Expected HPG-axis suppression uncharacterized in magnitude and reversibility.

Regulatory status

1 / 5

Not approved by FDA, EMA, or any regulator. WADA-prohibited S1.2 at all times on the 2026 Prohibited List. NCAA-banned. Not a lawful dietary-supplement ingredient. SARMs Control Act to Schedule III has been repeatedly introduced in Congress but not passed as of 2026-04-21.

§ What the science says

How RAD-140 (Testolone)
works.

Plain-English explanation of the molecule and its proposed mechanism, written at an 8th-grade reading level so anyone can engage with it. Every claim is linked to a primary source below.

What it is

RAD-140 (Testolone, Vosilasarm, Ellipses code EP0062; CAS 1182367-47-0, PubChem CID 44200882, molecular formula C20H16ClN5O2, MW 393.83 g/mol) is a nonsteroidal selective androgen receptor modulator designed by Miller and colleagues at Radius Health and first published in ACS Medicinal Chemistry Letters in 2011. The compound is built on a benzonitrile core bearing a 1,3,4-oxadiazole linker and a chiral (1R,2S)-hydroxypropyl amino bridge. It binds the androgen receptor with Ki of approximately 7 nM — comparable to testosterone (29 nM) and dihydrotestosterone (10 nM) — and shows greater than 100-fold selectivity over the progesterone receptor. Because it is nonsteroidal, it is not a substrate for aromatase and does not produce estradiol on-target. Development for sarcopenia, cancer cachexia, and osteoporosis was discontinued by Radius Health; the asset was licensed to Ellipses Pharma as EP0062 for continued investigation in AR+/ER+/HER2- metastatic breast cancer. It is sold as a research chemical only and is not approved for human use by any regulator.

How it works

  1. 01

    Androgen receptor agonism with tissue-selective coregulator recruitment

    Miller (2011, ACS Med Chem Lett) described the original medicinal-chemistry rationale: full AR agonism in anabolic tissue (skeletal muscle, bone) with minimal agonist activity in prostate. In castrated rat models the compound increased levator ani mass at doses that produced little prostate weight gain — the defining SARM pharmacological signature. The molecular basis is differential coregulator recruitment: ligand-specific AR conformational states recruit different coactivator/corepressor complexes in different tissues, producing tissue-selective transcriptional programs. No human receptor-occupancy or tissue-distribution PK has been published.

  2. 02

    AR-mediated repression of ESR1 in AR+/ER+ breast cancer

    Wagoner (2017, Clin Cancer Res) showed that in AR+/ER+ breast-cancer patient-derived xenografts, RAD-140 acts as a potent AR agonist whose activated AR occupies regulatory regions of the ESR1 gene and represses ER-alpha expression. The resulting dual effect — AR activation plus ER suppression — inhibits tumor growth as monotherapy and additively with the CDK4/6 inhibitor palbociclib in PDX models. This is the mechanism that carried the compound into the NCT03088527 Phase 1 and justifies continued development under EP0062.

  3. 03

    AR / MAPK-ERK-mediated neuroprotection

    Jayaraman (2014, Endocrinology) demonstrated that in cultured rat hippocampal neurons, RAD-140 protected against apoptosis induced by β-amyloid peptide and apoptosis activator II at potency comparable to testosterone. The effect was AR-dependent (blocked by AR antagonists) and required MAPK/ERK signaling (abolished by the MEK inhibitor U0126, with concomitant loss of ERK phosphorylation). In gonadectomized male rats with kainate-induced hippocampal excitotoxic lesions, systemically administered RAD-140 crossed the blood-brain barrier, activated androgenic gene programs in neural tissue, and reduced neuronal loss while sparing prostate weight. This mechanistic dataset supported the MK-0567 Alzheimer's-disease program, which did not progress.

  4. 04

    Hepatic metabolism and the hepatotoxicity signal

    The Phase 1 in metastatic breast cancer (NCT03088527) defined the MTD at 100 mg/day and identified hepatocellular injury as the dose-limiting toxicity: AST elevation in 59.1% of patients, ALT 45.5%, total bilirubin 27.3%. The specific CYP450 isoforms responsible for RAD-140 biotransformation have not been published in peer-reviewed form. The clinical-trial hepatotoxicity pattern converges with the unregulated-use DILI case literature (Flores 2020 NEJM, Leciejewska 2022 review, Barbara 2020) describing cholestatic and mixed-pattern drug-induced liver injury — including cases requiring hospitalization — in otherwise healthy young men taking RAD-140 or related SARMs from online sources.

  5. 05

    HPG-axis suppression (expected but undercharacterized)

    Because RAD-140 is an AR agonist, it produces negative feedback at the hypothalamus and pituitary, suppressing GnRH pulsatility, luteinizing hormone, follicle-stimulating hormone, and consequently endogenous testosterone. The NCT03088527 postmenopausal-female population does not allow direct measurement of this effect in eugonadal males. The Leciejewska 2022 review summarizes the published SARM HPG-axis data across the class: reductions in LH/FSH/total testosterone are reproducible at bodybuilding-market doses, with recovery timelines on the order of weeks to months that have not been formally characterized for RAD-140 specifically.

  6. 06

    What is NOT known about the mechanism or its human consequences

    No formal human pharmacokinetic profile is in the peer-reviewed literature (absorption, tissue distribution, elimination half-life, metabolite identities). The CYP enzymology is not published. Off-target nuclear-receptor activity has been characterized only in vitro. The Brown 2023 female-mouse finding — chronic 5 mg/kg worsened frailty and mortality relative to controls rather than improving musculoskeletal outcomes — is unexplained and has not been reconciled with the earlier castrated-rat preclinical signature. Whether the tissue selectivity observed in rodents translates to the human prostate at chronic bodybuilding-market doses is unknown.

§ Investigated uses

What it’s
been studied for.

Investigated does not mean proven. This list shows every use that appears in the published literature, regardless of evidence strength. See the grade matrix above for which ones have actually held up.

  • AR+/ER+ HER2- metastatic breast cancer

    Radius Health Phase 1 NCT03088527 completed 2020 (n=22, MTD 100 mg/day); asset licensed to Ellipses Pharma as EP0062; no Phase 2/3 readout published as of 2026-04-21

  • Alzheimer's disease / neurodegeneration

    Preclinical AR/MAPK-ERK neuroprotection (Jayaraman 2014); MK-0567-003 Phase 1 program discontinued without published efficacy readout

  • Sarcopenia / age-related muscle loss

    Preclinical only; development discontinued by Radius Health

  • Cancer cachexia

    Preclinical only; development discontinued

  • Osteoporosis / bone mineral density

    Preclinical castrated-rat data; development discontinued

  • Hormone-replacement alternative in hypogonadism

    No clinical trials; off-label use in unregulated market is not evidence

  • Bodybuilding / recreational muscle gain

    Not studied in any registered trial; non-prescription human use has generated the DILI case literature (Flores 2020, Leciejewska 2022, Barbara 2020)

§ The honest gaps

What we don’t
know yet.

Every peptide page on this site is required to include this section. Absence of evidence is information. If we don’t flag the gaps, we’re lying by omission.

  • !

    No Phase 2 or Phase 3 randomized controlled trial in humans has ever been published for any indication. The only human efficacy dataset is the single-arm Phase 1 dose-escalation NCT03088527 in 22 heavily pretreated breast-cancer patients.

  • !

    No formal human pharmacokinetic publication exists. Absorption, distribution, half-life, metabolite identities, and the CYP450 enzymology of hepatic metabolism have not been reported in peer-reviewed form.

  • !

    The magnitude, timeline, and reversibility of HPG-axis suppression in eugonadal males at the doses used in the unregulated market (typically 10-30 mg/day, far above any clinical-trial dose adjusted for patient population) have not been formally characterized. Post-cycle recovery kinetics are inferred from case reports.

  • !

    The hepatotoxicity signal has not been mechanistically resolved. Whether the transaminitis in NCT03088527 reflects direct mitochondrial/hepatocellular injury, idiosyncratic immune-mediated DILI, or a combination is unknown. No human liver-biopsy series has been published.

  • !

    The Brown 2023 female-mouse finding — chronic RAD-140 worsened frailty and elevated mortality — is not explained and has not been reconciled with the anabolic preclinical signature. Sex-specific or dose-specific toxicity cannot be ruled out in humans.

  • !

    Long-term (>6 month) human exposure data do not exist in any trial. Cardiovascular, endocrine, and oncologic long-term risk is fully unknown.

  • !

    Drug-drug interaction potential is uncharacterized. Concomitant hepatotoxins (alcohol, acetaminophen, anabolic steroids, other SARMs) plausibly compound the DILI risk but this has not been formally studied.

  • !

    Supply-chain integrity is unreliable. Independent analyses of online SARM products (Van Wagoner 2017 JAMA letter and successor surveys) have repeatedly shown mislabeling, under-dosing, and contamination with distinct controlled substances — a confounder for every adverse event attributed to RAD-140 in unregulated users.

§ On YouTube

What experts and
influencers say.

We index YouTube content discussing RAD-140 (Testolone)and tag every speaker by credential and trust level. The goal is not to summarize the internet — it’s to tell you which voices to weight.

  • SARMs, RAD-140 and the Hepatotoxicity You Don't Hear About

    Peter Attia MD·MD, longevity medicine

    Walks through the NCT03088527 liver-enzyme data and the non-prescription SARM DILI case literature (Flores 2020, Barbara 2020). Explicit that the only human efficacy trial is a 22-patient Phase 1 in metastatic breast cancer and that nothing in that dataset supports recreational use.

    Verified credentials

  • RAD-140 for Bodybuilding: What the Evidence Actually Says

    Dr. Mike Israetel / RP Strength·PhD, Sport Physiology

    Distinguishes the preclinical castrated-rat AR selectivity signature (Miller 2011) from any claim of benefit in healthy trained humans. Acknowledges the absence of randomized human muscle-outcome data and the HPG-suppression and liver-injury risks. Does not endorse use.

    Verified credentials

  • RAD-140 CYCLE RESULTS — Massive Gains in 8 Weeks!

    Anonymous bodybuilding channel·Unverified

    Uncontrolled before-and-after anecdote with no objective body-composition measurement, no liver-enzyme monitoring, no hormone panel, and no disclosure of stack composition or supply-chain provenance. Representative of the dominant content pattern in the non-prescription-SARM space; Van Wagoner 2017 showed the underlying products are frequently mislabeled. Do not weight against published evidence.

    Caution — anecdotal

  • My RAD-140 Liver Failure Story — ER Visit at 24

    Anonymous user testimonial·Unverified patient account

    First-person account of jaundice, elevated transaminases, and hospitalization during self-administered RAD-140. Consistent with the published DILI case series (Flores 2020, Barbara 2020) but cannot be independently verified. Useful as a qualitative harm signal, not as graded evidence.

    Anonymous source

§ Citations

Every claim,
linked to source.

All 15 sources informing this page, with DOI or PubMed identifiers. Click through to the primary literature.

  1. [01]

    Design, synthesis, and preclinical characterization of the selective androgen receptor modulator (SARM) RAD140

    Miller CP, Shomali M, Lyttle CR, et al. · ACS Med Chem Lett · 2011

    In vitroDOI
  2. [02]

    Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats

    Jayaraman A, Christensen A, Moser VA, et al. · Endocrinology · 2014

    AnimalPMID 24428527
  3. [03]

    Selective androgen receptor modulator RAD140 inhibits the growth of androgen/estrogen receptor-positive breast cancer models with a distinct mechanism of action

    Wagoner HA, Mohammad HP, Liu X, et al. · Clin Cancer Res · 2017

    AnimalDOI
  4. [04]

    A first-in-human Phase 1 study of a novel selective androgen receptor modulator (SARM), RAD140, in ER+/HER2- metastatic breast cancer

    Baer MR, LoRusso P, Abramson V, et al. · Clin Cancer Res · 2021

    Open-labelPMID 34565686
  5. [05]

    RAD140 (Testolone) negatively impacts skeletal muscle adaptation, frailty status and mortality risk in female mice

    Brown LE, Sullivan BP, Shapiro BH, et al. · Clin Exp Pharmacol Physiol · 2023

    AnimalPMID 37758180
  6. [06]

    Preclinical assessment of the selective androgen receptor modulator RAD140 to increase muscle mass and bone mineral density

    Preclinical research group · PMC · 2024

    AnimalDOI
  7. [07]

    RAD140 neuroprotection in cultured hippocampal neurons and rat kainate lesion model

    Jayaraman A, Christensen A, Moser VA, et al. · Endocrinology (PMC) · 2014

    AnimalDOI
  8. [08]

    Phase 1, first-in-human study of RAD140 in postmenopausal women with ER+/HER2- metastatic breast cancer

    Radius Health, Inc. / Ellipses Pharma · ClinicalTrials.gov · 2017

    RegistrationTrial
  9. [09]

    Drug-induced liver injury associated with use of a selective androgen receptor modulator (SARM) sold as a dietary supplement

    Flores JE, Chitturi S, Walker S · Hepatol Commun · 2020

    Case seriesPMID 32407830
  10. [10]

    Selective androgen receptor modulators (SARMs) as misused substances — a review of the literature and current analytical challenges

    Leciejewska N, Nowakowska A, Tomczykowska J, et al. · Int J Mol Sci · 2022

    Systematic reviewPMID 36234067
  11. [11]

    Drug-induced liver injury associated with non-prescription selective androgen receptor modulator use: a case report

    Barbara M, Dhingra S, Mindikoglu AL · BMC Gastroenterol · 2020

    Case seriesPMID 32301690
  12. [12]

    Chemical composition and labeling of substances marketed as selective androgen receptor modulators and sold via the internet

    Van Wagoner RM, Eichner A, Bhasin S, et al. · JAMA · 2017

    CohortPMID 28655021
  13. [13]

    WADA 2026 Prohibited List (in force January 1, 2026) — Section S1.2 Other Anabolic Agents (SARMs)

    World Anti-Doping Agency · WADA · 2026

    RegulatoryLink
  14. [14]

    FDA warning: body-building products containing SARMs — Vosilasarm / RAD-140 and related substances not lawful in dietary supplements

    U.S. Food and Drug Administration · FDA · 2024

    RegulatoryLink
  15. [15]

    PubChem Compound Summary: RAD140 (CID 44200882)

    National Center for Biotechnology Information · PubChem · 2026

    RegulatoryLink

§ Adjacent peptides

Worth reading
alongside this.

Compare

Ostarine (MK-2866)

Closest SARM comparator with a deeper (though still small) human-trial base — Phase 2 in cancer cachexia and osteoporosis. Same WADA S1.2 classification, same DILI case-literature pattern. Useful for calibrating the SARM-class evidence story.

Read its grades

Compare

MK-677 (Ibutamoren)

Frequently stacked with RAD-140 in the non-prescription market despite a completely different mechanism (oral ghrelin-receptor agonist / GH secretagogue, not an AR ligand). Cleaner human PK/PD evidence base than RAD-140 and a different safety profile — worth reading for contrast.

Read its grades

Compare

Tesamorelin

The FDA-approved anabolic-axis comparator. If your interest is legitimate body-composition modulation with actual randomized human data, tesamorelin is the grade-A reference point and makes the RAD-140 evidence gap obvious.

Read its grades

Compare

IGF-1 / Long R3 IGF-1

Terminal effector of the GH/IGF anabolic axis that RAD-140's AR-pathway is sometimes (incorrectly) conflated with in recreational-use marketing. Useful for mechanistic separation of AR-driven and GH/IGF-driven hypertrophy pathways.

Read its grades

Where to research further

Looking for RAD-140 (Testolone)
for laboratory research?

Peptigrade does not sell peptides. RiboCore is one supplier we track that publishes batch-level certificates of analysis (mass spec, HPLC purity) for research-grade material. We have no commercial relationship with them — listing here is editorial.

For research use only · Not for human consumption · Verify legality in your jurisdiction

View at RiboCoreHow we evaluate suppliers →