trifluridine + tipiracil (Taiho Pharmaceutical Co., Ltd.)

TAS-102 (trifluridine/tipiracil) is an orally administered combination chemotherapy agent. It consists of trifluridine, a thymidine-based nucleoside analog, and tipiracil hydrochloride, a thymidine phosphorylase inhibitor. Trifluridine's primary mechanism of action is its incorporation into DNA during synthesis, which leads to DNA damage and subsequent tumor cell death. Tipiracil hydrochloride functions to inhibit the enzyme thymidine phosphorylase, which otherwise rapidly degrades trifluridine, thereby maintaining effective systemic concentrations of the cytotoxic component. Developed by Taiho Pharmaceutical and marketed as Lonsurf, TAS-102 is approved for the treatment of metastatic colorectal cancer and metastatic gastric or gastroesophageal junction adenocarcinoma. In a specific clinical context at The First Affiliated Hospital of Zhengzhou University, TAS-102 is being investigated in a Phase 2 trial (NCT05364489) as part of a combination regimen with bevacizumab and oxaliplatin for the first-line treatment of advanced unresectable colorectal cancer.

Brand names

Lonsurf

Other names

trifluridine/tipiraciltrifluridine and tipiracil hydrochloride