Darolutamide CAS# 1297538-32-9 达若鲁胺
ODM-201, also known as Darolutamide, is a new-generation, potent and selective androgen receptor (AR) inhibitor which is potential useful for treatment of castration-resistant prostate cancer (CRPC). ODM-201 is a full and high-affinity AR antagonist that, similar to second-generation antiandrogens enzalutamide and ARN-509, inhibits testosterone-induced nuclear translocation of AR. Importantly, ODM-201 also blocks the activity of the tested mutant ARs arising in response to antiandrogen therapies, including the F876L mutation that confers resistance to enzalutamide and ARN-509. In addition, ODM-201 reduces the growth of AR-overexpressing VCaP prostate cancer cells both in vitro and in a castration-resistant VCaP xenograft model. ODM-201 overcomes resistance to AR-targeted therapies by antagonizing both overexpressed and mutated ARs. ODM-201 is currently in a phase 3 trial in CRPC.
📌 参考资料/链接：
Reference: Pan, Tingting; Xia, Chunguang; Yang, Yulei; Zhang, Aiming. Process and intermediates for preparation of androgen receptor antagonist. Assignee Lianyungang Runzhong Pharmaceutical Co., Ltd., Peop. Rep. China; Shanghai Institute of Pharmaceutical Industry. CN 108218908. (2018).
Reference: Pan, Tingting; Xia, Chunguang; Yang, Yulei; Zhang, Aiming. Process and intermediates for preparation of androgen receptor antagonist. Assignee Lianyungang Runzhong Pharmaceutical Co., Ltd., Peop. Rep. China; Shanghai Institute of Pharmaceutical Industry. CN 108218908. (2018).
📄 详细内容
CAS No. 1297538-32-9 达若鲁胺Darolutamide synthetic routes
Pan, Tingting; Xia, Chunguang; Yang, Yulei; Zhang, Aiming. Process and intermediates for preparation of androgen receptor antagonist. Assignee Lianyungang Runzhong Pharmaceutical Co., Ltd., Peop. Rep. China; Shanghai Institute of Pharmaceutical Industry. CN 108218908. (2018).
产品链接: CAS No. 1297538-32-9 ››
Pan, Tingting; Xia, Chunguang; Yang, Yulei; Zhang, Aiming. Process and intermediates for preparation of androgen receptor antagonist. Assignee Lianyungang Runzhong Pharmaceutical Co., Ltd., Peop. Rep. China; Shanghai Institute of Pharmaceutical Industry. CN 108218908. (2018).
产品链接: CAS No. 1297538-32-9 ››