Lipoprotein-associated phospholipase A2: A new therapeutic target

Lipoprotein-associated phospholipase A2 is an enzyme produced by inflammatory cells, which binds to apolipoprotein B-containing lipoproteins and degrades oxidatively modified phospholipids in low-density lipoprotein cholesterol particles, leading to formation of proinflammatory and cytotoxic products. Experimental studies suggest a role for lipoprotein-associated phospholipase A2 in the formation of advanced rupture-prone atherosclerotic lesions, and epidemiological investigations have linked it to increased cardiovascular risk. Ongoing trials are evaluating the role of novel pharmacological inhibitors of this enzyme, such as darapladib, in the management of high-risk coronary artery disease patients.