Proxalutamide
Proxalutamide (developmental code name GT-0918) is a nonsteroidal antiandrogen (NSAA) – specifically, a selective high-affinity silent antagonist of the androgen receptor (AR) – which is under development by Suzhou Kintor Pharmaceuticals for the treatment of prostate cancer.[1][2][3] It inhibits AR-mediated gene transcription more potently than bicalutamide (by ~5- to 10-fold) and enzalutamide (by 2- to 5-fold) and maintains silent antagonism in castration-resistant prostate cancer (CRPC) cells.[2] It has also been found to downregulate the AR, which could further confer it greater efficacy against CRPC compared to existing NSAAs.[2] Unlike enzalutamide, the drug showed low central nervous system distribution and no induction of seizures in animals.[2][3] As of 2017, it is in phase II clinical trials for prostate cancer.[1] It is also in preclinical investigation for the treatment of AR-positive breast cancer.[1][2][3]
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| Other names | GT-0918 |
| Routes of administration | By mouth |
| Drug class | Nonsteroidal antiandrogen |
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| Formula | C24H19F4N5O2S |
| Molar mass | 517.503 g/mol g·mol−1 |
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References
- http://adisinsight.springer.com/drugs/800046361
- Tong, Youzhi; Chen, Chunyun; Wu, Juan; Yang, Jiangtao; Zhang, Huihui; Wu, Xiaojun; Duan, Yanmei; Gao, Wei; Qian, Weidong; Niu, Xiaoxia; Mi, Lili; Guo, Chuangxing (2014). "Abstract 614: Proxalutamide (GT0918), a potent androgen receptor pathway inhibitor". Cancer Research. 74 (19 Supplement): 614–614. doi:10.1158/1538-7445.AM2014-614. ISSN 0008-5472.
- Tong, Youzhi; Chen, Chunyun; Wu, Juan; Zhang, Huihui; Wu, Xiaojun; Duan, Yanmei; Gao, Wei; Niu, Xiaoxia; Ma, Linglan; Guo, Chuangxing (2014). "Abstract 2460: Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer". Cancer Research. 73 (8 Supplement): 2460–2460. doi:10.1158/1538-7445.AM2013-2460. ISSN 0008-5472.