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Varespladib is a small molecule inhibitor of secretory phospholipase A2 (sPLA2), specifically targeting the IIA, V, and X isoforms. It acts as an anti-inflammatory agent by disrupting the first step of the arachidonic acid pathway, thereby reducing inflammation and modulating lipid levels. Varespladib has been investigated for several indications including acute coronary syndrome, sickle cell disease, vaso-occlusive crisis, and as a broad-spectrum antidote for snakebite envenoming due to its ability to inhibit sPLA2 present in most snake venoms. The drug is not currently approved but has reached Phase 2 clinical trials for these indications. Its prodrug form, varespladib methyl (LY333013), is orally bioavailable and rapidly converted to active varespladib after absorption[1][3][5][6][8].
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