RAD-140
Selective Androgen Receptor Modulator | Investigational SARM
RAD-140 (Testolone) is a nonsteroidal investigational selective androgen receptor modulator (SARM) originally developed by Radius Health, Inc. for the potential treatment of muscle wasting conditions and hormone receptor-positive breast cancer. It was designed to provide the anabolic benefits of testosterone, specifically increased lean muscle mass and bone density, while minimizing androgenic side effects in tissues such as the prostate and skin. RAD-140 has demonstrated a high degree of tissue selectivity in preclinical models, with an anabolic-to-androgenic ratio substantially greater than that of testosterone. It entered Phase 1 clinical trials for metastatic breast cancer (ER+/HER2-) and has shown preliminary safety and tolerability in that context. However, RAD-140 is not approved for any medical use by any regulatory agency. It remains a research compound, and its widespread use in performance and physique enhancement contexts is based almost entirely on preclinical data and anecdotal reports rather than completed clinical trials for those indications.
Moleküler Gösterim
M.W.: 393.83 Da
PubChem 2D yapı diyagramı
Referans Flakon
Referans illüstrasyonu — ürün listesi değildir
Etki Mekanizması
RAD-140 binds to the androgen receptor (AR) with high affinity and selectivity, functioning as a full agonist in muscle and bone tissue while exhibiting minimal agonist activity in the prostate and other androgen-sensitive tissues. This tissue selectivity is achieved through differential cofactor recruitment: upon binding to the AR, RAD-140 induces a conformational change that favors interaction with coactivators predominantly expressed in skeletal muscle and bone, rather than those prevalent in prostate or sebaceous glands. In preclinical studies, RAD-140 demonstrated potent anabolic effects on levator ani muscle mass comparable to testosterone, while showing significantly less stimulation of prostate weight. RAD-140 also crosses the blood-brain barrier and has demonstrated neuroprotective properties in in vitro models, reducing cell death caused by apoptotic insults in hippocampal neurons. At the molecular level, it activates AR-dependent gene transcription pathways involved in protein synthesis, nitrogen retention, and satellite cell proliferation in skeletal muscle. Importantly, RAD-140 does not undergo aromatization to estrogen and is not a substrate for 5-alpha reductase, meaning it does not produce estrogenic or DHT-mediated side effects. However, like all exogenous AR agonists, it suppresses endogenous testosterone production through negative feedback on the hypothalamic-pituitary-gonadal (HPG) axis.
RAD-140 (Testolone) is a nonsteroidal investigational selective androgen receptor modulator (SARM) originally developed by Radius Health, Inc. for the potential treatment of muscle wasting conditions and hormone receptor-positive breast cancer. It was designed to provide the anabolic benefits of testosterone, specifically increased lean muscle mass and bone density, while minimizing androgenic side effects in tissues such as the prostate and skin. RAD-140 has demonstrated a high degree of tissue selectivity in preclinical models, with an anabolic-to-androgenic ratio substantially greater than that of testosterone. It entered Phase 1 clinical trials for metastatic breast cancer (ER+/HER2-) and has shown preliminary safety and tolerability in that context. However, RAD-140 is not approved for any medical use by any regulatory agency. It remains a research compound, and its widespread use in performance and physique enhancement contexts is based almost entirely on preclinical data and anecdotal reports rather than completed clinical trials for those indications.
Moleküler Veri
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Doz Protokolleri
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| Hedef | Doz | Sıklık | Yol |
|---|---|---|---|
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| MYMEMORY WARNING: YOU USED ALL AVAILABLE FREE TRANSLATIONS FOR TODAY. NEXT AVAILABLE IN 10 HOURS 42 MINUTES 59 SECONDS VISIT HTTPS://MYMEMORY.TRANSLATED.NET/DOC/USAGELIMITS.PHP TO TRANSLATE MORE | 15-20 mg/day | MYMEMORY WARNING: YOU USED ALL AVAILABLE FREE TRANSLATIONS FOR TODAY. NEXT AVAILABLE IN 11 HOURS 04 MINUTES 45 SECONDS VISIT HTTPS://MYMEMORY.TRANSLATED.NET/DOC/USAGELIMITS.PHP TO TRANSLATE MORE | MYMEMORY WARNING: YOU USED ALL AVAILABLE FREE TRANSLATIONS FOR TODAY. NEXT AVAILABLE IN 10 HOURS 58 MINUTES 01 SECONDS VISIT HTTPS://MYMEMORY.TRANSLATED.NET/DOC/USAGELIMITS.PHP TO TRANSLATE MORE |
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Etkileşimler
Testosterone
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Enclomiphene
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MK-677
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Cardarine (GW-501516)
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Other SARMs (LGD-4033, S-23, etc.)
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Yan Etkiler & Güvenlik
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Durdurma Belirtileri
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Kaynaklar
- Selective Androgen Receptor Modulator RAD140 Is Neuroprotective in Cultured Neurons and Kainate-Lesioned Male Rats — Jayaraman, A., Christensen, A., Moser, V.A., et al.
- RAD140, a Nonsteroidal Selective Androgen Receptor Modulator (SARM) for Hormonal Male Contraception and Treatment of Muscle Wasting — Miller, C.P., Shomali, M., Lyttle, C.R., et al.
- Phase 1 Study of RAD140 in Postmenopausal Women with Hormone Receptor-Positive Breast Cancer — Hattersley, G., Tian, H., Bolen, A.L., et al.
- Drug-Induced Liver Injury Associated with the Use of Selective Androgen Receptor Modulators — Flores, J.E., Chitturi, S., Walker, N.I.
- Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications — Narayanan, R., Coss, C.C., Dalton, J.T.