Chemistry:RAD140
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| Formula | C20H16ClN5O2 |
| Molar mass | 393.83 g·mol−1 |
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RAD140 is an investigational selective androgen receptor modulator (SARM) that is developed by Radius Health, Inc. for use in androgen replacement therapy. It was licensed to Ellipses Pharmaceuticals in 2020.[1][2][3][4] Some of the potential benefits under investigation are for the treatment of conditions such as muscle wasting and bone loss.
Clinical trials
The first-in-human study was initiated in October of 2017 and completed in September 2020 in postmenopausal women with breast cancer.[5][6]
In early 2020 a single case report of drug-induced liver injury following use of RAD 140 was published.[7][8]
Animal studies
RAD 140 appears to be safer than testosterone replacement therapy (TRT) in rats.[9]
RAD 140 slightly increased lean muscle mass when used in primates, by targeting androgen receptors in skeletal tissue.[10]
See also
References
- ↑ "Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats". Endocrinology 155 (4): 1398–406. April 2014. doi:10.1210/en.2013-1725. PMID 24428527.
- ↑ "Androgens increase survival of adult-born neurons in the dentate gyrus by an androgen receptor-dependent mechanism in male rats". Endocrinology 154 (9): 3294–304. September 2013. doi:10.1210/en.2013-1129. PMID 23782943.
- ↑ "Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140". ACS Medicinal Chemistry Letters 2 (2): 124–9. February 2011. doi:10.1021/ml1002508. PMID 24900290.
- ↑ "Selective Androgen Receptor Modulator RAD140 Inhibits the Growth of Androgen/Estrogen Receptor-Positive Breast Cancer Models with a Distinct Mechanism of Action". Clinical Cancer Research 23 (24): 7608–7620. December 2017. doi:10.1158/1078-0432.CCR-17-0670. PMID 28974548.
- ↑ "Abstract P5-11-01 : Phase 1 dose escalation study of a novel selective androgen receptor modulator (SARM), RAD140, in estrogen receptor positive (ER ), human epidermal growth factor receptor 2 negative (HER2-), metastatic breast cancer". Cancer Research 80 (4 Supplement): P5–11–01. 2020-02-15. doi:10.1158/1538-7445.sabcs19-p5-11-01. https://cancerres.aacrjournals.org/content/80/4_Supplement/P5-11-01.
- ↑ Clinical trial number NCT03088527 for "Phase 1, First-in-Human Study of RAD140 in Postmenopausal Women With Breast Cancer" at ClinicalTrials.gov
- ↑ "Drug-Induced Liver Injury by Selective Androgenic Receptor Modulators". Hepatology Communications 4 (3): 450–452. March 2020. doi:10.1002/hep4.1456. PMID 32140660.
- ↑ RAD 140 Testolone
- ↑ "Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats". Endocrinology 155 (4): 1398–406. April 2014. doi:10.1210/en.2013-1725. PMID 24428527.
- ↑ "Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140". ACS Medicinal Chemistry Letters 2 (2): 124–9. February 2011. doi:10.1021/ml1002508. PMID 24900290.
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