Varespladib is primarily investigated for its potential therapeutic applications in treating inflammatory conditions and diseases. It functions as a phospholipase A2 (sPLA2) inhibitor, which plays a critical role in the inflammatory response. By inhibiting sPLA2, it may help reduce inflammation and tissue damage associated with various conditions, such as sepsis, acute lung injury, and cardiovascular diseases.

In clinical studies, Varespladib has shown promise in managing severe inflammatory states, particularly in sepsis and acute respiratory distress syndrome (ARDS), where uncontrolled inflammation can lead to organ failure. Additionally, it is being explored for its potential in treating snakebite envenomation, as sPLA2 enzymes are a key component of many snake venoms. By neutralizing these enzymes, Varespladib could mitigate the toxic effects of venom and improve patient outcomes.

Research is ongoing to further evaluate its efficacy and safety in these and other inflammatory and toxin-related conditions.