Ro 44-3888, the active component of sibrafiban, achieves predictable plasma concentrations when administered orally in its prodrug form, Ro 48-3657. Upon reaching a steady state after the second dose, Ro 44-3888 exhibits concentration-dependent inhibition of platelet aggregation and prolongs bleeding time. These findings suggest that Ro 44-3888 merits further evaluation, especially in patients at high risk of arterial thrombosis and those with acute coronary syndrome, due to its reliable absorption.