Abstract
This single-blind, placebo-controlled study evaluated the tolerability and pharmacodynamic (PD) response of the first dose of the oral GPllb/llla receptor antagonist, SC-54684A (ethyl 3S-[[4-[[4(amino-iminomethyl)phenyl]amino]-l,4-dioxobutyl]amino]-4-pentynoate, monohydrochloride). SC-54684A (SC) is the pro-drug of the active compound, SC-54701A. Six healthy male subjects received 50 mg of SC (free base) and 2 received placebo (PBO). Results of the inhibition to AOD (20 μM) induced platelet aggregation are shown below: Bleeding time increased a mean of 5.6 fold at 4 hrs post-dose and returned to within normal limits at 8 hrs after dosing. No significant changes in lab values or bleeding complications occurred. Peak serum concentrations coincided with peak PD effects of inhibition of platelet aggregation. SC-54684A has a rapid onset of potent inhibition of platelet aggregation that is sustained for up to 10 hours after dosing
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