Varespladib has been used as a secretory phospholipase A (sPLA2) inhibitor: to test its effect on the human astrocytes subjected to psychosine-induced toxicityto test its neutralization functionality on the black snake species P. collettivenom in combination with snake venom metalloproteinases (SVMP)-inhibitor, marimastat to test its protective functionality on envenoming by vipers
Biochem/physiol Actions
Varespladib is effective against viper and elapid venoms and is used in snakebite therapy. It is reported to interact with the hydrophobic channel of the PLA2-like toxin in in vitro structural studies. It blocks inflammatory cascades related to the sPLA2.
Varespladib is a potent and selective inhibitor of secretory phospholipase A2 (sPLA2). The compound Varespladib inhibits both human and mouse sPLA2 group IIA, V, and X enzymes at low nM concentrations.