TAK-024 is an inhibitor of platelet(IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively).

Platelet (human):31 nM , Platelet (monkey):79 nM , Platelet (Pig):51 nM

TAK-024 is a inhibitor of platelet(IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively).The IC50 value of TAK-024 in the heparinized blood sample is 230 nM, 4.5-fold less potent than that in the citrated physiological blood sample. The ID50 value of TAK-024 on ex vivo ADP-induced platelet aggregation in guinea pigs is 0.18 μg/kg/min, the dissociation ratio of TAK-024 is found to be 32.

TAK-024(Intravenous infusion; 1.6 μg/mL/min) completely prevents arterial thrombus formation induced by endothelial injury in guinea pigs. Results demonstrate the inhibitory effects of TAK-024 on the carotid thrombosis induced by balloon injury in guinea pigs and the ID50 value is 0.73 μg/kg/min. TAK-024 at (single dose;100 μg/kg iv) produces almost complete inhibition for 120 min, and about 40% inhibition is observed after 240 min. Dose-dependent inhibition of platelet aggregation is achieved with a single iv dose of 30 to 100 μg/kg of TAK-024.