Trifluridine Tipiracil: Mechanism of action

The combination medicine Trifluridine Tipiracil is used in treating patients with metastatic colorectal cancer and metastatic gastric or gastroesophageal junction adenocarcinoma. This medicine comes in tablets in 15 mg Trifluridine/6.14 mg Tipiracil and 20 mg Trifluridine/8.19 mg to administer orally via the mouth. Trifluridine tipiracil 15 mg/6.14 mg tablets consist of a thymidine-based nucleoside analog, trifluridine, and the thymidine phosphorylase inhibitor, tipiracil. The inclusion of tipiracil increases trifluridine exposure by inhibiting its metabolism by thymidine phosphorylase. Following uptake into cancer cells, trifluridine is incorporated into DNA, interferes with DNA synthesis and inhibits cell proliferation.