The inclusion of Lonsurf (trifluralin/tipiracil, TAS‑102) in the treatment of metastatic colorectal cancer

06/2017

MUDr. Eugen Kubala

Klinika onkologie a radioterapie, LF UK a FN Hradec Králové

SUMMARY

Fluoropyrimidines have represented the cornerstone of treatment of colorectal cancer for a long time. Lonsurf is an orally administered combination of a thymidine-based nucleic acid analogue - trifluridine and a thymidine phosphorylase inhibitor - tipiracil hydrochloride with trifluridine being the active cytotoxic component of this combination. Its triphosphate form is incorporated into DNA appearing to result in antitumor effects. Tipiracil hydrochloride is a strong inhibitor of the thymidine phosphorylase and, when combined with trifluridine prevents the rapid degradation of the trifluridine, allowing longer maintenance of adequate plasma concentration of the active drug. The results of the placebo-controlled, double-blind, phase 3 clinical trial RECOURSE confirmed the results of previous assessments of oral Lonsurf in patients with metastatic colorectal cancer, who had already undergone extensive treatment. Lonsurf was associated with a clinically relevant prolongation of overall survival in essentially all treatment subgroups. Combination of trifluridine and tipiracil is able to replace 5-fluorouracil in patients who have developed resistance to this treatment. It turns out that the combination with a biologic therapy or oxaliplatin and irinotecan has a great future in the treatment of not only metastatic colorectal cancer.

KEY WORDS

trifluridine, tipiracil hydrochloride, Lonsurf, metastatic colorectal cancer