Recently, the new oral cytotoxic antitumor drug trehaluridine thiopyrimidine tablets (TAS-102) developed by Japan Dapeng Pharmaceutical Industry Co., Ltd. was approved by the National Drug Administration (NMPA) and officially listed in China. Indications: for previous fluoropyrimidine, oxaliplatin and irinotecan-based chemotherapy, and previously received or not suitable for anti-vascular endothelial growth factor (VEGF) treatment, anti-epidermal growth factor receptor (EGFR) treatment (RAS wild type) in patients with metastatic colorectal cancer (mCRC).
Trifluraltidine iripyrimidine tablets (TAS-102) are oral combination preparations consisting of trifluorothymidine (FTD) and tepicidin hydrochloride (TPI) in a molar ratio of 1:0.5. The main mechanism of action is that trifluorothymidine (FTD) replaces thymine into DNA double strands during DNA replication, resulting in DNA dysfunction exerting anti-tumor effects; while ticlopidine hydrochloride (TPI) inhibits thymidine phosphorylase (TPase) activity prevents rapid degradation of FTD, thereby maintaining the active pharmaceutical ingredient in plasma at an effective level.
This product was approved by the US FDA on September 22, 2015, under the trade name Lonsurf. Has been approved in Japan, the United States, the United Kingdom, Canada, the European Union and other 21 countries and regions for the treatment of metastatic colorectal cancer (mCRC).
The joint development interest in Europe and some designated regions is in the hands of Servier.
Previously, on July 27, 2018, Japan Dapeng Pharmaceutical Industry Co., Ltd. submitted the TAS-102 Chinese generic name application to the Chinese National Pharmacopoeia Commission. On August 22, 2018, the National Pharmacopoeia Committee approved the name TAS-102, which is commonly known as trehalidine glucopyrimidine.
