Upon oral administration at 60 mg/kg, T-98475 was able to suppress suppression of plasma LH concentrations in castrated male cynomolgus monkeys.

Labeled leuprorelin (0.15 nM) and the membrane fractions (0.2 mg/mL) of CHO cells expressing the human LHRH receptor were incubated at 25 °C for 60 min in 0.2 mL of assay buffer in the presence of various concentrations of test compound. The reaction was terminated by the addition of 2 mL of ice-cold assay buffer, and bound and free ligands were separated by filtration through a poly(ethylenimine)-coated glass microfiber filter. The filter was washed twice with 2 mL of assay buffer, and radioactivity was measured using a gamma-ray counter. Specific binding was determined by subtraction of the non-specific binding, which was measured in the presence of 1 uM unlabeled leuprorelin. T-98475 displaced leuprorelin with IC50 of 0.2 nM.