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    RAD-140 (Testolone) molecular structure

    RAD-140 (Testolone)

    PerformancePhase 1

    Also known as: Testolone, RAD140, RAD 140, Vosilasarm, Testalone

    RAD-140, sold as testolone and given the international nonproprietary name vosilasarm, is a nonsteroidal selective androgen receptor modulator developed at Radius Health, whose scientists reported the first-in-human trial (PMID: 34565686), and first described in the medicinal chemistry literature as a compound with an oxadiazole core designed for oral androgen receptor activity with tissue selectivity (PMID: 24900290). Radius took it into oncology rather than into muscle wasting, and the only registered human trial is a phase 1 study in postmenopausal women with hormone receptor positive metastatic breast cancer.

    Half-Life: Terminal half-life 44.7 hours in humans, measured in a first-in-human phase 1 study in postmenopausal women with metastatic breast cancer (PMID: 34565686)Route: OralMW: 393.83 g/molCAS: 1182367-47-0
    Last reviewed:
    Performance
    Category
    Phase 1
    Research Stage

    Overview

    Best Price Available

    Disguised Alpha logo

    Disguised Alpha

    $84.99

    60 capsules · capsule

    At A Glance

    Mechanism

    RAD-140 is a nonsteroidal agonist of the androgen receptor built on a 1,3,4-oxadiazole scaffold (PMID: 24900290). It binds the receptor and drives transcription of androgen-responsive genes, producing anabolic effects in muscle in rats (PMID: 40680216) and neuroprotective effects

    Half-Life
    Terminal half-life 44.7 hours in humans, measured in a first-in-human phase 1 study in postmenopausal women with metastatic breast cancer (PMID: 34565686)
    Routes
    Oral
    Potential Benefits
    Reduced apoptotic neuron death in cultured rat hippocampal neurons and protected hippocampal neurons in kainate-lesioned male rats (PMID: 24428527)Inhibited growth of androgen receptor positive and estrogen receptor positive breast cancer models, including in animal studies (PMID: 28974548)Increased muscle fiber cross-sectional area in young male Sprague-Dawley rats, without additional benefit on top of functional overload and without change in bone microarchitecture over 14 days (PMID: 40680216)Documented androgen receptor engagement in humans, with sex hormone binding globulin falling in all 18 evaluable patients in a phase 1 study (PMID: 34565686)One partial response and an 18.2 percent clinical benefit rate at 24 weeks in heavily pretreated metastatic breast cancer in that phase 1 study (PMID: 34565686)

    Overview

    RAD-140, sold as testolone and given the international nonproprietary name vosilasarm, is a nonsteroidal selective androgen receptor modulator developed at Radius Health, whose scientists reported the first-in-human trial (PMID: 34565686), and first described in the medicinal chemistry literature as a compound with an oxadiazole core designed for oral androgen receptor activity with tissue selectivity (PMID: 24900290). Radius took it into oncology rather than into muscle wasting, and the only registered human trial is a phase 1 study in postmenopausal women with hormone receptor positive metastatic breast cancer. It is not approved by any regulator. The molecule binds the androgen receptor and acts as an agonist, changing which androgen-responsive genes are transcribed. The human phase 1 study used sex hormone binding globulin and prostate-specific antigen as markers of that engagement and saw sex hormone binding globulin fall in all 18 evaluable patients and prostate-specific antigen rise in 16 of 20, with paired tumor biopsies confirming receptor engagement (PMID: 34565686). Preclinical work covers three separate claims. For neuroprotection, RAD-140 reduced apoptotic cell death in cultured rat hippocampal neurons and protected hippocampal neurons in kainate-lesioned male rats, with the effect depending on MAPK signaling (PMID: 24428527). For oncology, it inhibited growth of androgen receptor positive and estrogen receptor positive breast cancer models (PMID: 28974548). For muscle, a study in young male Sprague-Dawley rats found increased muscle fiber cross-sectional area in unloaded animals but no additional benefit when combined with functional overload, and no change in cortical or trabecular bone over 14 days (PMID: 40680216). Two mouse studies point the other way on health span: in female mice, ten weeks of RAD140 increased frailty and mortality risk and failed to improve strength (PMID: 37758180), and a later study in older male and female mice again reported an effect on frailty (PMID: 40158703). The human safety signal is the clearest reason this compound is not a casual purchase. In the phase 1 cancer study, the most frequent treatment-emergent adverse events were raised aspartate aminotransferase in 59.1 percent, raised alanine aminotransferase in 45.5 percent and raised total bilirubin in 27.3 percent, and grade 3 or 4 events occurred in 72.7 percent of the 22 patients (PMID: 34565686). Outside trials, biopsy-confirmed cholestatic drug-induced liver injury after RAD-140 has been reported repeatedly, with peak total bilirubin far above normal and recovery taking months (PMID: 36561105, PMID: 36945289, PMID: 39328701, PMID: 36978171, PMID: 38444893). There are also cardiac case reports: acute myocarditis (PMID: 35233331), myopericarditis in a 16-year-old boy after a first dose (PMID: 39157568) and heart failure (PMID: 38864168). RAD140 is named in FDA warning letters to firms selling SARM products as unapproved new drugs (FDA warning letter to Titan SARMs LLC, 12 December 2025), and it is prohibited in sport at all times under the World Anti-Doping Agency anabolic agents class (PMID: 28137616).

    Potential Research Fields

    OncologyNeuroprotectionMuscle and bone anabolismHepatotoxicity surveillance

    Chemical Information

    IUPAC Name

    Not yet available

    CAS Number

    1182367-47-0

    Molecular Formula

    C20H16ClN5O2

    Molecular Mass

    393.83 g/mol

    Dosing & Protocols

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    Research

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    Interactions

    Contraindications

    Mechanism-based: contraindicated in pregnancy, since androgen receptor agonists can virilize a female fetus, and in men with known or suspected prostate cancer. Pre-existing liver disease or raised transaminases is both mechanism-based and case-report-based, given how frequently transaminase and bilirubin rises appeared in the phase 1 trial and in published liver injury reports (PMID: 34565686, PMID: 36945289). Cardiac case reports, including one in a 16-year-old, are a reason to avoid it in anyone with known cardiac disease (PMID: 39157568, PMID: 38864168). Prohibited in tested sport at all times (PMID: 28137616).

    Research Disclaimer

    This interaction data is compiled from published research and community reports. It may not be exhaustive. Always consult a healthcare professional before combining compounds.

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    t½ Not established from a retrieved human report; in rats the mean elimination half-life of radiolabeled GTx-024 was 0.6 h in males and 16.4 h in females (PMID: 24074268). Human plasma pharmacokinetics were characterized in phase 1 drug-interaction studies (PMID: 27105861)
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    Protocols, calculator & safety for RAD-140 (Testolone)

    Best Price

    Disguised Alpha logo

    Disguised Alpha

    $84.99

    1 vendors · 1 listings

    Research Score

    30

    0 PubMed studies

    Quality Indicators

    Data Completeness

    63%
    Description
    Mechanism of Action
    Chemical Data
    Dosing Protocols
    Safety Profile
    PubMed Studies
    Interactions
    Vendor Listings

    Quick Facts

    Half-Life

    Terminal half-life 44.7 hours in humans, measured in a first-in-human phase 1 study in postmenopausal women with metastatic breast cancer (PMID: 34565686)

    Molecular Weight

    393.83 g/mol

    Administration

    Oral

    CAS Number

    1182367-47-0

    Trial Phase

    Phase 1

    0

    Research Disclaimer

    This information is for educational and research purposes only. Not intended as medical advice. Consult a healthcare professional before use.

    Frequently Asked Questions

    What is RAD-140 (Testolone) used for in research?

    RAD-140, sold as testolone and given the international nonproprietary name vosilasarm, is a nonsteroidal selective androgen receptor modulator developed at Radius Health, whose scientists reported the first-in-human trial (PMID: 34565686), and first described in the medicinal chemistry literature as a compound with an oxadiazole core designed for oral androgen receptor activity with tissue selectivity (PMID: 24900290). Radius took it into oncology rather than into muscle wasting, and the only registered human trial is a phase 1 study in postmenopausal women with hormone receptor positive metastatic breast cancer. It is not approved by any regulator.

    The molecule binds the androgen receptor and acts as an agonist, changing which androgen-responsive genes are transcribed. The human phase 1 study used sex hormone binding globulin and prostate-specific antigen as markers of that engagement and saw sex hormone binding globulin fall in all 18 evaluable patients and prostate-specific antigen rise in 16 of 20, with paired tumor biopsies confirming receptor engagement (PMID: 34565686).

    Preclinical work covers three separate claims. For neuroprotection, RAD-140 reduced apoptotic cell death in cultured rat hippocampal neurons and protected hippocampal neurons in kainate-lesioned male rats, with the effect depending on MAPK signaling (PMID: 24428527). For oncology, it inhibited growth of androgen receptor positive and estrogen receptor positive breast cancer models (PMID: 28974548). For muscle, a study in young male Sprague-Dawley rats found increased muscle fiber cross-sectional area in unloaded animals but no additional benefit when combined with functional overload, and no change in cortical or trabecular bone over 14 days (PMID: 40680216). Two mouse studies point the other way on health span: in female mice, ten weeks of RAD140 increased frailty and mortality risk and failed to improve strength (PMID: 37758180), and a later study in older male and female mice again reported an effect on frailty (PMID: 40158703).

    The human safety signal is the clearest reason this compound is not a casual purchase. In the phase 1 cancer study, the most frequent treatment-emergent adverse events were raised aspartate aminotransferase in 59.1 percent, raised alanine aminotransferase in 45.5 percent and raised total bilirubin in 27.3 percent, and grade 3 or 4 events occurred in 72.7 percent of the 22 patients (PMID: 34565686). Outside trials, biopsy-confirmed cholestatic drug-induced liver injury after RAD-140 has been reported repeatedly, with peak total bilirubin far above normal and recovery taking months (PMID: 36561105, PMID: 36945289, PMID: 39328701, PMID: 36978171, PMID: 38444893). There are also cardiac case reports: acute myocarditis (PMID: 35233331), myopericarditis in a 16-year-old boy after a first dose (PMID: 39157568) and heart failure (PMID: 38864168).

    RAD140 is named in FDA warning letters to firms selling SARM products as unapproved new drugs (FDA warning letter to Titan SARMs LLC, 12 December 2025), and it is prohibited in sport at all times under the World Anti-Doping Agency anabolic agents class (PMID: 28137616).

    What forms does RAD-140 (Testolone) come in?

    RAD-140 (Testolone) is available in capsule form.

    How much does RAD-140 (Testolone) cost?

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    Research Tools

    Related Compounds

    View All

    ITPP

    PerformancePreclinical

    ITPP (myo-inositol trispyrophosphate, sometimes written myo-inositol tripyrophosphate or OXY111A in NormOxys trial documents) is a small-molecule allosteric effector of hemoglobin designed to increase the amount of oxygen red blood cells release to tissues.

    Research compound — IV infusion in studies, no established oral doses
    36 studiesView Profile

    LGD-4033 (Ligandrol)

    PerformancePhase 2

    LGD-4033, usually sold as ligandrol, is a nonsteroidal selective androgen receptor modulator that Viking Therapeutics took into clinical development under the code VK5211 (NCT02578095).

    t½ Long elimination half-life in humans with dose-proportional accumulation over 21 days of daily dosing in healthy young men; the report describes the profile without giving a single value in its summary (PMID: 22459616)
    PreclinicalView Profile

    Ostarine (Enobosarm, MK-2866)

    PerformancePhase 3

    Ostarine is the market name for enobosarm, a nonsteroidal selective androgen receptor modulator first developed by GTx Inc under the codes GTx-024, MK-2866 and S-22.

    t½ Not established from a retrieved human report; in rats the mean elimination half-life of radiolabeled GTx-024 was 0.6 h in males and 16.4 h in females (PMID: 24074268). Human plasma pharmacokinetics were characterized in phase 1 drug-interaction studies (PMID: 27105861)
    PreclinicalView Profile

    PEG-MGF

    PerformancePreclinical

    PEG-MGF (Pegylated Mechano Growth Factor) is a synthetic, PEGylated form of Mechano Growth Factor (MGF) — an alternatively spliced variant of IGF-1 produced locally in muscle and other tissues in response to mechanical loading or damage.

    t½ Native MGF: very short (minutes) due to rapid proteolysis. PEG-MGF: PEGylation is intended to extend this substantially (community estimates up to roughly 1 day), but there are no published human pharmacokinetic data to confirm a specific value. 200
    PreclinicalView Profile

    SLU-PP-332

    PerformancePreclinical

    SLU-PP-332 is the first-generation synthetic pan-agonist of the estrogen-related receptors (ERRα, ERRβ, ERRγ) developed by the laboratory of Thomas Burris at Saint Louis University and reported in a landmark 2023 publication that established ERR pan-agonism as a pharmacologically tractable exercise-mimetic drug mechanism.

    Research compound — no established human doses. Animal studies: 10-50 mg/kg
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    YK-11 is a synthetic steroid, not a nonsteroidal SARM, despite being sold alongside them.

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