Varespladib methyl is an oral secretory phospholipase A2 inhibitor that is being 
developed by Anthera Pharmaceuticals Inc for the potential treatment of coronary 
artery disease, acute coronary syndrome and inflammation. Varespladib methyl is 
a prodrug that is rapidly metabolized to varespladib, and both compounds are 
able to potently inhibit the enzymes of the human secretory phospholipase groups 
IIa, V and X, which play a pivotal role in atherosclerotic disease and 
inflammation. Phase II clinical trials of varespladib methyl in patients with 
coronary artery disease, rheumatoid arthritis, asthma and ulcerative colitis 
revealed that the drug was well tolerated. Varespladib methyl did not 
demonstrate a good efficacy profile in patients with rheumatoid arthritis, 
asthma and ulcerative colitis, whereas in patients with coronary artery disease, 
varespladib methyl consistently reduced LDL-cholesterol levels (elevated 
LDL-cholesterol levels are a marker of increased cardiovascular risk). At the 
time of publication, phase II trials were ongoing in patients with acute 
coronary syndrome and in patients undergoing elective percutaneous coronary 
intervention, and a phase III trial in patients with acute coronary syndrome was 
planned. Varespladib methyl could represent a novel therapy for the treatment of 
cardiovascular disease, although the efficacy, safety profile and advantages of 
this drug compared with existing therapeutic options would need to be 
established in upcoming phase III trials.