Dapsone (DB00250): A Comprehensive Monograph on its Pharmacology, Clinical Utility, and Evolving Therapeutic Landscape

I. Introduction and Executive Summary

Dapsone is a synthetic sulfone therapeutic agent with a remarkably rich and evolving history. First synthesized in 1908 as a product of pure chemical science ambition [1], its therapeutic potential was not realized for nearly three decades. Its discovery as an antimicrobial agent in 1937 [1] set the stage for its introduction in 1945 as a revolutionary treatment for leprosy (Hansen's disease), a role in which it remains a cornerstone of global public health to this day.[4] However, the clinical narrative of dapsone extends far beyond its identity as an antibiotic. Decades of clinical observation and subsequent scientific inquiry have revealed it to be a multifaceted drug possessing potent and distinct anti-inflammatory and immunomodulatory properties.

This report provides an exhaustive analysis of dapsone, synthesizing a vast body of evidence to construct a comprehensive monograph. The central thesis is that dapsone's enduring clinical relevance and its expanding therapeutic applications are a direct consequence of its unique dual mechanism of action. This duality, which combines bacteriostatic activity through folic acid synthesis inhibition with powerful anti-inflammatory effects via myeloperoxidase inhibition, is the key to its broad utility.[1] Concurrently, the drug's complex metabolic profile, particularly the generation of a reactive hydroxylamine metabolite, defines both its therapeutic efficacy in inflammatory conditions and its significant, dose-limiting safety considerations.