TAS-102 is an oral combination drug consisting of trifluridine (FTD), which is a thymidine-based nucleoside analog, and tipiracil HCl (TPI), which improves the bioavailability of FTD by inhibiting its catabolism by thymidine phosphorylase (TP).

Trifluorothymidine is a derivative of thymidine that can inhibit thymidylate synthase and lead to DNA damage and apoptosis. It could be used to treat colorectal cancer.

Raltitrexed is an inhibitor of thymidylate synthase with IC50 of 9 nM in L1210 cell.

Nolatrexed, also known as AG337, is a thymidylate synthase inhibitor with potential anticancer activity. A phase II study of nolatrexed in 2007 in advanced HCC patients demonstrated minimal activity and significant stomatitis. Hence, it does not warrant further study as a single agent for this disease.

L-CCG-IV is a potent agonist of the NMDA receptor.

Tipiracil is a thymidine phosphorylase (TPase) inhibitor.