Phospholipases A2 (PLA2) are enzymes of high medical scientific interest due to their involvement in a large number of human inflammatory diseases. PLA2 constitute a diverse family of enzymes which catalyses the hydrolysis of the sn-2 ester bond in glycerophospholipids and exhibit a wide range of physiological and pathological effects. The ubiquitous nature of PLA2 highlights the important role they play in many biological processes, as cell signaling and cell growth, including the generation of proinflammatory lipid mediators such as prostaglandin and leukotrienes, regulation of lipid mediators. The activity and expression of several PLA2 isoforms are increased in several human cancers, suggesting that these enzymes have a central role in both tumor development and progression and can be targets for anti-cancer drugs. On the other hand, some PLA2 isolated from Viperidae venoms are capable to induce antitumoral activity. In summary PLA2 from snake venoms can be a new class of anticancer agents and provide new molecular and biological insights of cancer development.