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. Author manuscript; available in PMC: 2016 Nov 1.
Published in final edited form as: Cancer Treat Rev. 2015 Jun 6;41(9):777–783. doi: 10.1016/j.ctrv.2015.06.001

Table 1.

Overview of TAS-102 and 5-FU-based chemotherapy agents. [2]

Agent Route of Administration Active Metabolites and Their Functions
5-FU-based agents

5-FU IV FdUMP: Irreversible inhibitor of TS
FUTP: Incorporated into RNA
FdUTP: Incorporated into DNA
Capecitabine Oral
Tegafur-uracil Oral
S-1 Oral

FTD-based agents

TAS-102 (FTD + TPI) Oral F3dTMP: Reversible inhibitor of TS
F3dTTP: Incorporated into DNA
TPI: TP inhibition

5-FU: 5-fluorouracil; F3dTMP: trifluoromethyl deoxyuridine 5′-monophosphate; F3dTTP: trifluoromethyl deoxyuridine 5′-triphosphate; FdUMP: fluorodeoxyuridine monophosphate; FdUTP: fluorodeoxyuridine triphosphate; FTD: α,α,α-trifluorothymidine (trifluridine); FUTP: fluorouridine triphosphate; IV: intravenous; TP: thymidine phosphorylase; TPI: tipiracil hydrochloride; TS: thymidylate synthase.