Venom‐Derived Bioactive Peptides: From Toxins to Therapeutics

Abstract

Venoms are complex biochemical mixtures composed of diverse bioactive components, including proteins, enzymes, small molecules, and peptides. Among these, venom‐derived peptides have been evolutionarily optimized to interact with biological targets with exceptional potency and selectivity. Although historically regarded solely as toxic substances, these peptides have increasingly been recognized as valuable templates for therapeutic development. This review examines the structural and biochemical properties of venom‐derived peptides, as well as their molecular targets, with particular emphasis on their applications in pain management and cardiovascular disorders. Key milestones in venom‐based drug discovery are highlighted, from the approval of captopril in 1981 to more recent peptide candidates such as Hi1a and leptucin. Despite notable successes, the clinical translation of venom peptides remains constrained by challenges related to their physicochemical properties, including stability, bioavailability, and delivery. Emerging strategies aimed at overcoming these limitations are also discussed, underscoring advances in peptide engineering and drug delivery technologies. Overall, this review highlights the significant therapeutic potential of venom‐derived peptides and their expanding role in the development of novel treatments for a wide range of pathological conditions.