Comprehensive Monograph on Sarpogrelate (DB12163)

Executive Summary

Sarpogrelate is a selective serotonin 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist with a unique pharmacological profile characterized by a dual mechanism of action involving both the inhibition of platelet aggregation and the suppression of vasoconstriction. Developed primarily in Japan and South Korea, it has established a significant clinical role in the management of ischemic symptoms associated with chronic arterial occlusive diseases. This monograph provides a comprehensive analysis of Sarpogrelate, synthesizing available data on its chemical properties, pharmacology, clinical efficacy, safety, and comparative positioning against other antiplatelet agents.

Key findings from extensive clinical investigation reveal Sarpogrelate's efficacy in improving hemodynamic parameters and symptoms in patients with peripheral arterial disease (PAD). Furthermore, it has demonstrated vasculoprotective effects in coronary artery disease (CAD), particularly in populations with comorbid diabetes mellitus, where it improves not only vascular function but also underlying metabolic and inflammatory markers. A pivotal aspect of Sarpogrelate's clinical profile is its safety, most notably a significantly lower risk of bleeding complications compared to aspirin, as demonstrated in the large-scale S-ACCESS trial for secondary stroke prevention. While it did not prove non-inferior to aspirin in preventing recurrent infarction in the overall population, its favorable safety profile and a signal of potential benefit in diabetic patients highlight its importance as a strategic therapeutic alternative.