SARM

RAD-140

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Overview

A potent SARM studied preclinically (incl. breast-cancer models); human evidence is limited and includes published cases of drug-induced liver injury.

How it works

RAD-140 (testolone) is a potent SARM — a non-steroidal molecule that strongly activates the androgen receptor with the aim of building muscle while sparing other tissues.

Through androgen-receptor signaling it drives muscle-building gene activity, and it's been of preclinical interest in muscle and even in androgen-receptor-positive breast cancer.

The honest picture in humans is concerning rather than reassuring: the limited human literature is dominated by published case reports of liver injury, alongside the expected suppression of natural testosterone. It is not approved and is banned in sport.

Mechanism · Detailed Analysis

Molecular targetA high-affinity nonsteroidal AR agonist.

Signaling & downstream effectsAR transcriptional activation; preclinical interest spans muscle and AR-positive breast cancer.

CaveatsHuman data are sparse and dominated by published hepatotoxicity case reports plus expected HPTA suppression. Not approved; banned in sport.

Published EvidenceFree · cited live from PubMed

Human Data 15

Review

Detection of SARMs in doping control analysis

Thevis M et al. · Molecular and cellular endocrinology · 2018 — PMID 28137616 ↗

Research Support, N.I.H., Extramural

Pharmacological Targeting of Androgen Receptor Elicits Context-Specific Effects in Estrogen Receptor-Positive Breast Cancer

Wei L et al. · Cancer research · 2023 — PMID 36469363 ↗

Comparative Study

Comparison of the three SARMs RAD-140, GLPG0492 and GSK-2881078 in two different in vitro bioassays, and in an in silico androgen receptor binding assay

Zierau O et al. · The Journal of steroid biochemistry and molecular biology · 2019 — PMID 30825507 ↗

Clinical Trial, Phase I

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

LoRusso P et al. · Clinical breast cancer · 2022 — PMID 34565686 ↗

Study

The forensic response after an adverse analytical finding (doping) involving a selective androgen receptor modulator (SARM) in human athlete

Kintz P · Journal of pharmaceutical and biomedical analysis · 2022 — PMID 34715583 ↗

Study

Detection of anabolic agents including selective androgen receptor modulators in samples outside of sport

Bohlin KP et al. · Drug testing and analysis · 2024 — PMID 37986708 ↗

Research Support, N.I.H., Extramural

Systematic identification of ACE2 expression modulators reveals cardiomyopathy as a risk factor for mortality in COVID-19 patients

Kaur N et al. · Genome biology · 2022 — PMID 35012625 ↗

Study

Simultaneous detection of different chemical classes of selective androgen receptor modulators in urine by liquid chromatography-mass spectrometry-based techniques

Stacchini C et al. · Journal of pharmaceutical and biomedical analysis · 2021 — PMID 33383501 ↗

Case Reports

Idiosyncratic drug-induced liver injury related to use of novel selective androgen receptor modulator RAD140 (Testalone): a case report

Ladna M et al. · Journal of medical case reports · 2023 — PMID 36978171 ↗

Case Reports

Selective androgen receptor modulator abuse-induced heart failure: catastrophic effects of RAD-140 (Testolone)

Skorupski WJ et al. · Polish archives of internal medicine · 2024 — PMID 38864168 ↗

Evaluation Study

Expanding sports drug testing assays: mass spectrometric characterization of the selective androgen receptor modulator drug candidates RAD140 and ACP-105

Thevis M et al. · Rapid communications in mass spectrometry : RCM · 2013 — PMID 23650030 ↗

Study

Exploring transdermal SARMs exposure: analysis of the elimination profiles and metabolism for doping control purposes

Korsmeier L et al. · Journal of analytical toxicology · 2025 — PMID 40632609 ↗

See all 15 on PubMed →

Animal 9

Study

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

Puskas J et al. · Physiological reports · 2025 — PMID 40680216 ↗

Study

Identification of equine in vitro metabolites of seven non-steroidal selective androgen receptor modulators for doping control purposes

Cutler C et al. · Drug testing and analysis · 2022 — PMID 34714606 ↗

Research Support, Non-U.S. Gov't

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

Brown AM et al. · Clinical and experimental pharmacology & physiology · 2023 — PMID 37758180 ↗

Study

Label-free proteomics for discovering biomarker candidates of RAD140 administration to castrated horses

Cheung HW et al. · Drug testing and analysis · 2021 — PMID 33277807 ↗

Study

Detection of nonsteroidal and steroidal selective androgen receptor modulators in equine hair after oral administrations

So YM et al. · Drug testing and analysis · 2025 — PMID 39001560 ↗

Research Support, Non-U.S. Gov't

The impact of a selective androgen receptor modulator (RAD140) on frailty and underlying mechanisms in older male and female C57Bl/6 mice

Heinze SS et al. · Mechanisms of ageing and development · 2025 — PMID 40158703 ↗

Research Support, N.I.H., Extramural

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

Jayaraman A et al. · Endocrinology · 2014 — PMID 24428527 ↗

Validation Study

Development of a multi-residue high-throughput UHPLC-MS/MS method for routine monitoring of SARM compounds in equine and bovine blood

In Vitro 0

No indexed in vitro studies found for this term. Try the live PubMed query below.

Search this category on PubMed →

Studies are surfaced live from the U.S. National Library of Medicine (PubMed). biohackr indexes and links the published record; it does not host or alter source articles.

Published EvidenceLoading cited studies from PubMed…

Human Data ···

Searching the published record…

Animal ···

Searching the published record…

In Vitro ···

Searching the published record…

Educational aggregation of public literature. Not medical advice and not a recommendation to use any compound. Many compounds here are not approved for human use. Consult a licensed clinician.

Published EvidenceFree · cited live from PubMed

Human Data 15

Review

Detection of SARMs in doping control analysis

Thevis M et al. · Molecular and cellular endocrinology · 2018 — PMID 28137616 ↗

Research Support, N.I.H., Extramural

Pharmacological Targeting of Androgen Receptor Elicits Context-Specific Effects in Estrogen Receptor-Positive Breast Cancer

Wei L et al. · Cancer research · 2023 — PMID 36469363 ↗

Comparative Study

Comparison of the three SARMs RAD-140, GLPG0492 and GSK-2881078 in two different in vitro bioassays, and in an in silico androgen receptor binding assay

Zierau O et al. · The Journal of steroid biochemistry and molecular biology · 2019 — PMID 30825507 ↗

Clinical Trial, Phase I

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

LoRusso P et al. · Clinical breast cancer · 2022 — PMID 34565686 ↗

Study

The forensic response after an adverse analytical finding (doping) involving a selective androgen receptor modulator (SARM) in human athlete

Kintz P · Journal of pharmaceutical and biomedical analysis · 2022 — PMID 34715583 ↗

Study

Detection of anabolic agents including selective androgen receptor modulators in samples outside of sport

Bohlin KP et al. · Drug testing and analysis · 2024 — PMID 37986708 ↗

Research Support, N.I.H., Extramural

Systematic identification of ACE2 expression modulators reveals cardiomyopathy as a risk factor for mortality in COVID-19 patients

Kaur N et al. · Genome biology · 2022 — PMID 35012625 ↗

Study

Simultaneous detection of different chemical classes of selective androgen receptor modulators in urine by liquid chromatography-mass spectrometry-based techniques

Stacchini C et al. · Journal of pharmaceutical and biomedical analysis · 2021 — PMID 33383501 ↗

Case Reports

Idiosyncratic drug-induced liver injury related to use of novel selective androgen receptor modulator RAD140 (Testalone): a case report

Ladna M et al. · Journal of medical case reports · 2023 — PMID 36978171 ↗

Case Reports

Selective androgen receptor modulator abuse-induced heart failure: catastrophic effects of RAD-140 (Testolone)

Skorupski WJ et al. · Polish archives of internal medicine · 2024 — PMID 38864168 ↗

Evaluation Study

Expanding sports drug testing assays: mass spectrometric characterization of the selective androgen receptor modulator drug candidates RAD140 and ACP-105

Thevis M et al. · Rapid communications in mass spectrometry : RCM · 2013 — PMID 23650030 ↗

Study

Exploring transdermal SARMs exposure: analysis of the elimination profiles and metabolism for doping control purposes

Korsmeier L et al. · Journal of analytical toxicology · 2025 — PMID 40632609 ↗

See all 15 on PubMed →

Animal 9

Study

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

Puskas J et al. · Physiological reports · 2025 — PMID 40680216 ↗

Study

Identification of equine in vitro metabolites of seven non-steroidal selective androgen receptor modulators for doping control purposes

Cutler C et al. · Drug testing and analysis · 2022 — PMID 34714606 ↗

Research Support, Non-U.S. Gov't

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

Brown AM et al. · Clinical and experimental pharmacology & physiology · 2023 — PMID 37758180 ↗

Study

Label-free proteomics for discovering biomarker candidates of RAD140 administration to castrated horses

Cheung HW et al. · Drug testing and analysis · 2021 — PMID 33277807 ↗

Study

Detection of nonsteroidal and steroidal selective androgen receptor modulators in equine hair after oral administrations

So YM et al. · Drug testing and analysis · 2025 — PMID 39001560 ↗

Research Support, Non-U.S. Gov't

The impact of a selective androgen receptor modulator (RAD140) on frailty and underlying mechanisms in older male and female C57Bl/6 mice

Heinze SS et al. · Mechanisms of ageing and development · 2025 — PMID 40158703 ↗

Research Support, N.I.H., Extramural

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

Jayaraman A et al. · Endocrinology · 2014 — PMID 24428527 ↗

Validation Study

Development of a multi-residue high-throughput UHPLC-MS/MS method for routine monitoring of SARM compounds in equine and bovine blood

In Vitro 0

No indexed in vitro studies found for this term. Try the live PubMed query below.

Search this category on PubMed →

Studies are surfaced live from the U.S. National Library of Medicine (PubMed). biohackr indexes and links the published record; it does not host or alter source articles.

RAD-140

Detection of SARMs in doping control analysis

Pharmacological Targeting of Androgen Receptor Elicits Context-Specific Effects in Estrogen Receptor-Positive Breast Cancer

Comparison of the three SARMs RAD-140, GLPG0492 and GSK-2881078 in two different in vitro bioassays, and in an in silico androgen receptor binding assay

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

The forensic response after an adverse analytical finding (doping) involving a selective androgen receptor modulator (SARM) in human athlete

Detection of anabolic agents including selective androgen receptor modulators in samples outside of sport

Systematic identification of ACE2 expression modulators reveals cardiomyopathy as a risk factor for mortality in COVID-19 patients

Simultaneous detection of different chemical classes of selective androgen receptor modulators in urine by liquid chromatography-mass spectrometry-based techniques

Idiosyncratic drug-induced liver injury related to use of novel selective androgen receptor modulator RAD140 (Testalone): a case report

Selective androgen receptor modulator abuse-induced heart failure: catastrophic effects of RAD-140 (Testolone)

Expanding sports drug testing assays: mass spectrometric characterization of the selective androgen receptor modulator drug candidates RAD140 and ACP-105

Exploring transdermal SARMs exposure: analysis of the elimination profiles and metabolism for doping control purposes

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

Identification of equine in vitro metabolites of seven non-steroidal selective androgen receptor modulators for doping control purposes

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

Label-free proteomics for discovering biomarker candidates of RAD140 administration to castrated horses

Detection of nonsteroidal and steroidal selective androgen receptor modulators in equine hair after oral administrations

The impact of a selective androgen receptor modulator (RAD140) on frailty and underlying mechanisms in older male and female C57Bl/6 mice

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

Development of a multi-residue high-throughput UHPLC-MS/MS method for routine monitoring of SARM compounds in equine and bovine blood

Detection of SARMs in doping control analysis

Pharmacological Targeting of Androgen Receptor Elicits Context-Specific Effects in Estrogen Receptor-Positive Breast Cancer

Comparison of the three SARMs RAD-140, GLPG0492 and GSK-2881078 in two different in vitro bioassays, and in an in silico androgen receptor binding assay

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

The forensic response after an adverse analytical finding (doping) involving a selective androgen receptor modulator (SARM) in human athlete

Detection of anabolic agents including selective androgen receptor modulators in samples outside of sport

Systematic identification of ACE2 expression modulators reveals cardiomyopathy as a risk factor for mortality in COVID-19 patients

Simultaneous detection of different chemical classes of selective androgen receptor modulators in urine by liquid chromatography-mass spectrometry-based techniques

Idiosyncratic drug-induced liver injury related to use of novel selective androgen receptor modulator RAD140 (Testalone): a case report

Selective androgen receptor modulator abuse-induced heart failure: catastrophic effects of RAD-140 (Testolone)

Expanding sports drug testing assays: mass spectrometric characterization of the selective androgen receptor modulator drug candidates RAD140 and ACP-105

Exploring transdermal SARMs exposure: analysis of the elimination profiles and metabolism for doping control purposes

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

Identification of equine in vitro metabolites of seven non-steroidal selective androgen receptor modulators for doping control purposes

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

Label-free proteomics for discovering biomarker candidates of RAD140 administration to castrated horses

Detection of nonsteroidal and steroidal selective androgen receptor modulators in equine hair after oral administrations

The impact of a selective androgen receptor modulator (RAD140) on frailty and underlying mechanisms in older male and female C57Bl/6 mice

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

Development of a multi-residue high-throughput UHPLC-MS/MS method for routine monitoring of SARM compounds in equine and bovine blood

Metabolic studies of selective androgen receptor modulators RAD140 and S-23 in horses