Table 1.
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.