|Drug class||Nonsteroidal antiandrogen|
|Chemical and physical data|
|Molar mass||517.503 g/mol|
|3D model (JSmol)|
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. 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. It has also been found to downregulate the AR, which could further confer it greater efficacy against CRPC compared to existing NSAAs. Unlike enzalutamide, the drug showed low central nervous system distribution and no induction of seizures in animals. As of 2017, it is in phase II clinical trials for prostate cancer. It is also in preclinical investigation for the treatment of AR-positive breast cancer.
- 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.
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