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Clinical data | |
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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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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]
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]
After 2 weeks, the body weights of the GTx-026-treated mice were greater than those of the vehicle-treated mice, with this difference increasing in magnitude throughout the duration of the study (62% in GTx-026-treated mice vs 31% in vehicle-treated mice; P < 0.001) (Fig. 2B). GTx-026 treatment also increased lean mass (20% vs 60%; P < 0.001) compared with vehicle treatment. Consistent with the increase in lean mass, grip strength also increased in the GTx-026-treated animals (Fig. 2B). These results were reproduced with the other two SARMs, GTx-024 and GTx-027, indicating that these effects are SARM-dependent (Supplementary Material, Fig. S1B).
Other SARMs in the Company's portfolio, GTx-024 (enobosarm) and GTx-027, showed similar positive effects on muscle mass, function, and histological characteristics.