A compendium of extracellular vesicle biogenesis inhibitors: From bench to bedside

Abstract Extracellular vesicles (EVs) are cell‐derived particles delimited by a lipid bilayer and containing a wide variety of cargos that cannot replicate independently. Their key role as mediators of intercellular communication implicates them in a broad spectrum of physiological and pathological processes. In recent years, EVs have gained increasing attention as potential biomarkers, therapeutic targets and drugs delivery vehicles. However, the successful translation of EV‐based strategies from bench to bedside requires a deeper understanding of EV composition and the biogenesis mechanisms. A particularly promising and actively investigated avenue in EV research is the targeted inhibition of EV biogenesis. Modulating these processes not only provides valuable tools for dissecting EV functions in vitro and in vivo, but also opens new therapeutic possibilities, especially in diseases where EVs contribute to pathogenesis, such as cancer, neurodegeneration, inflammation and infectious diseases. Identifying and characterizing compounds that interfere with EV biogenesis is therefore of high relevance, both for fundamental research and clinical applications. This review aims to contribute to the field by offering a comprehensive overview of the most studied EV inhibitors, highlighting their mechanisms of action, experimental utility, and potential for therapeutic exploitation. Particular attention is given to their advantages and limitations as modulators of EV biogenesis, with the goal of guiding future research toward more effective and selective strategies.