Tipiralacil, also known as TPI, is a thymidine phosphorylase inhibitor (TPI). Tipiracil is one of the active components in TAS-102, which is an anticancer drug candidate currently in clinical trials. TAS-102 consists of the cytotoxin Trifluridine and the thymidine phosphorylase inhibitor (TPI) tipiracil. Trifluridine is incorporated into DNA during DNA synthesis and inhibits tumor cell growth. Tipiracil protects trifluridine from being broken down when taken orally. TAS-102 was approved in Japan in 2015.
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Wang, Shujuan; Xu, Hao; Kang, Wei Assignee Sinopharm A-Think Pharmaceutical Co., Ltd., Peop. Rep. China. Synthesis method of tipiracil hydrochloride as antitumor drug and its intermediate 6-chloromethyl uracil. CN 106892902. (2017).
Sun, Ping; Li, Sai; Du, Zuyin; Zhao, Junjun; Li, Xiaobi. Process for the preparation of 5-chloro-6-[(2-imino-1-pyrrolidinyl)methyl]-2,4(1H,3H)-pyrimidinedione hydrochloride. Assignee Jiangsu Hansoh Pharmaceutical Co., Ltd., Peop. Rep. China; Jiangsu Hansoh Pharmaceutical Group, Lianyungang Grand Champ Medicine Co., Ltd. CN 104945384 A (2015)
