NLRP3 is a highly attractive drug target due to its implication in the pathogenesis of a number of diseases, including both monogenic NLRP3-driven disorders and more complex inflammatory disorders. Pharmacological inhibitors of NLRP3 would impact on IL-1β and IL-18 production and pyroptosis, potentially resulting in more effective antiinflammatory therapies than those targeting just IL-1. As our understanding of the molecular mechanisms underlying NLRP3 activation improves, so does our capability to design novel specific pharmacological inhibitors of the pathway. Several NLRP3 inhibitors have been reported to date and are at different stages of clinical development. This chapter will highlight the potential therapeutic opportunities targeting the different steps of NLRP3 activation, and will provide a framework for the development of future therapeutics targeting the inflammasome.
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