Tipiracil HCl is an inhibitor of thymidine phosphorylase (TPase) with IC50 of 35 nM. It has been used in the combination therapy of metastatic colorectal cancer.

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).

MT-DADMe-ImmA, a chemically stable analogue for the proposed transition state of human MTAP, is a novel MTAP inhibitor with potential for the treatment of human head and neck and prostate carcinoma.

Doxifluridine is a thymidine phosphorylase activator for PC9-DPE2 cells with IC50 of 0.62 μM.

Tipiracil is a thymidine phosphorylase (TPase) inhibitor.

CP-91149 is a selective glycogen phosphorylase (GP) inhibitor with IC50 of 0.13 μM in the presence of glucose, 5- to 10-fold less potent in the absence of glucose.

AVE5688 is an inhibitor of glycogen phosphorylase (GP), with IC50s of 430 nM and 915 nM and Kds of 170 nM and 530 nM for rabbit muscle glycogen phosphorylase (rmGPb and rmGPa, respectively); can be used for the research of type 2 diabetes.

CP 316819 is a selective glycogen phosphorylase inhibitor.

Ingliforib is a glycogen phosphorylase inhibitor, with IC50s of 52, 352 and 150 nM for liver, muscle and brain glycogen phosphorylase, and has cardioprotective activity.