TAS-102, an oral agent composed of trifluridine and tipiracil hydrochloride, significantly prolonged OS in patients with refractory metastatic colorectal cancer, according to the results of a randomized, double blind, phase 3 trial.“Trifluridine is the active cytotoxic component of TAS-102; its triphosphate form is incorporated into DNA, with such incorporation appearing to result in its anti-tumor effects,” Robert J. Mayer, MD, of the Dana-Farber Cancer Institute, and colleagues wrote. “Tipiracil hydrochloride is a potent inhibitor of thymidine phosphorylase and, when combined with trifluridine to form TAS-102, prevents the rapid degradation of the trifluridine, allowing for the maintenance of adequate plasma levels of the active drug.”
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