GTx-027
Abandoned cancer drug
From Wikipedia, the free encyclopedia
GTx-027 is a selective androgen receptor modulator (SARM) which was under development for or of potential interest in the treatment of breast cancer and stress urinary incontinence (SUI) but was never marketed.[2][3][1][4][5] It is taken by mouth.[1]
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| Other names | GTx027 |
| Routes of administration | Oral[1] |
| Drug class | Selective androgen receptor modulator[1] |
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| Chemical and physical data | |
| Formula | C18H14ClN3O3 |
| Molar mass | 355.78 g·mol−1 |
| 3D model (JSmol) | |
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Description
The drug is a nonsteroidal androgen receptor (AR) modulator with mixed agonistic (androgenic) and antagonistic (antiandrogenic) effects.[1][5] It has been found to reduce the growth of androgen receptor-expressing MDA-MB-231 breast cancer cells in vitro.[6][7] In addition, it has been found to increase pelvic floor muscle weight in ovariectomized female rodents.[1][8][4] The drug has been found to increase body weight, lean body mass, and muscle strength in animals as well.[9][10] In terms of chemical structure, GTx-027 is a nonsteroidal arylpropionamide SARM and is an analogue of enobosarm (ostarine; GTx-024).[1][4]
GTx-027 was first described in the scientific literature by 2013.[5][11] It is said to have either not passed preclinical research[1] or to have reached phase 1 clinical trials prior to the discontinuation of its development.[3] The drug was developed by GTx.[2][3]