The relationship between trifluridine, tipiracil (Lancever) and tas-102

Trifluridine, tipiracil (Lonsurf) and tas-102 are the same drug, just with different names. This drug is an oral chemotherapy drug commonly used to treat certain digestive system tumors, especially colorectal cancer, gastric cancer, etc. Trifluridine and tipiracil are composed of two active ingredients, trifluridine and tipiracil. The combination of these two ingredients allows the drug to effectively inhibit tumor growth and extend patient survival.

Tipiracil is a thymidine phosphorylase inhibitor that is combined with trifluridine at a ratio of 1:0.5 to form TAS-102, trifluridine-tipiracil. The main function of tipiracil is to increase the bioavailability of trifluridine by inhibiting its catabolism. Trifluridine is indicated for the treatment of metastatic colorectal cancer that has been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy or anti-VEGF or anti-EGFR therapy.

In early clinical studies, a twice-daily regimen (5 days on, 2 days off) every 4 weeks for 2 weeks produced significant disease control rates in a variety of malignancies. This schedule showed consistent activity in two randomized trials in patients with fluoropyrimidine-refractory colorectal cancer, reflected in a 2- to 3-month improvement in overall survival in the trifluridine-tipiracil group compared with placebo. In clinical studies of trifluridine tipiracil (70mg/m^2/day) and bevacizumab, the center-assessed disease control rate (DCR) was 64%, the median overall survival (OS) was 11 months, there were no drug interactions, and the toxicity was acceptable.