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Published on: January 22, 2018
A novel antimetabolite: TAS-102 for metastatic colorectal cancer
Yuji Miyamoto1,2, Heinz-Josef Lenz2, Hideo Baba1
1a Department of Gastroenterological Surgery, Graduate School of Medical Sciences , Kumamoto University , Kumamoto , Japan.
Abstract:
TAS-102 is a new oral anti-tumor drug, composed of a thymidine-based nucleoside analog (trifluridine: FTD) and a thymidine phosphorylase inhibitor (tipiracil hydrochloride: TPI). TAS-102 has been shown to significantly improve overall survival and progression-free survival in patients with refractory metastatic colorectal cancer (mCRC) in placebo-controlled randomized phase II and III trials. The current review summarizes mechanisms of action, pharmacokinetics/dynamics and preclinical and clinical data of TAS-102 in colorectal cancer. TAS-102 is a new salvage-line treatment option for patients with mCRC. TAS-102 is well tolerated and has great potential in future clinical drug combination therapies.

