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| Clinical data | |
|---|---|
| Other names | GTx027 |
| Routes of administration | Oral [1] |
| Drug class | Selective androgen receptor modulator [1] |
| Identifiers | |
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| PubChem CID | |
| 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]
Selective androgen receptor modulators (SARMs) are a class of drugs that selectively activate the androgen receptor in specific tissues, promoting muscle and bone growth while having less effect on male reproductive tissues like the prostate gland.
BMS-564,929 is an investigational selective androgen receptor modulator (SARM) which is being developed by Bristol-Myers Squibb for treatment of the symptoms of age-related decline in androgen levels in men ("andropause"). These symptoms may include depression, loss of muscle mass and strength, reduction in libido and osteoporosis. Treatment with exogenous testosterone is effective in counteracting these symptoms but is associated with a range of side effects, the most serious of which is enlargement of the prostate gland, which can lead to benign prostatic hyperplasia and even prostate cancer. This means there is a clinical need for selective androgen receptor modulators, which produce anabolic effects in some tissues such as muscle and bone, but without stimulating androgen receptors in the prostate.
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Andarine is a selective androgen receptor modulator (SARM) which was developed by GTX, Inc for the treatment of conditions such as muscle wasting, osteoporosis, and benign prostatic hyperplasia (BPH), using the nonsteroidal antiandrogen bicalutamide as a lead compound. Development of andarine for all indications has been discontinued, in favor of the structurally related and improved compound enobosarm.
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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.