Varespladib sodium

Varespladib Sodium is a pharmaceutical drug that was developed for the treatment of acute coronary syndrome and acute pancreatitis. It is a potent and selective inhibitor of secretory phospholipase A2 (sPLA2), an enzyme that has been associated with inflammatory diseases such as atherosclerosis and acute pancreatitis.

History

Varespladib Sodium was initially developed by Anthera Pharmaceuticals, a biopharmaceutical company based in the United States. The drug entered Phase III clinical trials in 2010, but the development was discontinued in 2012 after it failed to meet the primary endpoint in the VISTA-16 trial.

Mechanism of Action

Varespladib Sodium works by inhibiting the activity of sPLA2, an enzyme that catalyzes the hydrolysis of phospholipids, leading to the production of arachidonic acid and other pro-inflammatory mediators. By blocking the activity of sPLA2, Varespladib Sodium can potentially reduce inflammation and the associated tissue damage.

Clinical Trials

The efficacy of Varespladib Sodium was evaluated in several clinical trials. The most notable of these was the VISTA-16 trial, a randomized, double-blind, placebo-controlled study that enrolled over 6,500 patients with acute coronary syndrome. However, the trial was stopped prematurely after an interim analysis showed that Varespladib Sodium did not reduce the risk of cardiovascular events compared to placebo.

Side Effects

Like all drugs, Varespladib Sodium can cause side effects. The most common side effects reported in clinical trials included nausea, vomiting, and diarrhea. Serious side effects, such as liver damage, were also reported.

Current Status

As of 2022, Varespladib Sodium is not approved for use in any country. The development of the drug was discontinued after the failure of the VISTA-16 trial.