Prasugrel (DB06209): A Comprehensive Monograph on its Pharmacology, Clinical Efficacy, and Safety Profile

Section 1: Introduction and Drug Profile

1.1. Overview and Classification

Prasugrel is a potent, orally administered antiplatelet agent belonging to the third generation of the thienopyridine class of drugs.[1] Classified as a small molecule, it functions as a platelet activation and aggregation inhibitor.[3] Its therapeutic effect is achieved through the irreversible antagonism of the P2Y purinoceptor 12 (P2Y12), a key receptor in the process of thrombosis.[3]

Structurally and pharmacologically, prasugrel is related to its thienopyridine predecessors, ticlopidine and clopidogrel.[3] However, it was specifically developed to address certain limitations of these earlier agents, most notably the delayed onset of action and considerable interpatient variability in response observed with clopidogrel.[1] Like clopidogrel, prasugrel is a prodrug, meaning it is biologically inactive upon administration and requires metabolic conversion to exert its pharmacological effect.[3] This biotransformation, however, is more efficient and consistent than that of clopidogrel, leading to a more predictable and potent antiplatelet response.[1]

1.2. Historical Context and Regulatory Approval

Prasugrel was developed by the Japanese pharmaceutical company Daiichi Sankyo Co..[1] For marketing and distribution in North America, Daiichi Sankyo partnered with Eli Lilly and Company.[1] The drug's development pathway culminated in regulatory approvals in major markets, reflecting the clinical need for more effective antiplatelet therapies in high-risk cardiovascular patients.