The synthetic varespladib molecule is a multi-functional inhibitor for PLA(2) and PLA(2)-like ophidic toxins

摘要

Background: The treatment for snakebites is early administration of antivenom, which can be highly effective in inhibiting the systemic effects of snake venoms, but is less effective in the treatment of extra-circulatory and local effects. To complement standard-of-care treatments such as antibody-based antivenoms, natural and synthetic small molecules have been proposed for the inhibition of key venom components such as phospholipase A(2) (PLA(2)) and PLA(2)-like toxins. Varespladib (compound LY315920) is a synthetic molecule developed and clinically tested aiming to block inflammatory cascades of several diseases associated with high PLA(2)s. Recent studies have demonstrated this molecule is able to potently inhibit snake venom catalytic PLA(2) and PLA(2)-like toxins.