Drug intelligence / Profile preview

varespladib + varespladib-methyl

Development stage
Discontinued
Lead developer
Ophirex
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination of **varespladib** (an intravenous or oral phospholipase A2 inhibitor) and its orally bioavailable prodrug, **varespladib-methyl**. Both molecules are **synthetic small molecule inhibitors** of secretory phospholipase A2 (sPLA2), targeting type IIA, V and X isoforms. The combination may deliver rapid and broad-spectrum inhibition of sPLA2, which is present in more than 95% of all snake venoms and implicated in various inflammatory human diseases. While varespladib was previously explored for inflammatory and cardiovascular conditions, both have more recently been studied for *snakebite envenomation*, where they demonstrate inhibition of venom sPLA2 toxins, reduced neurotoxicity, myotoxicity, and other venom-induced pathologies in preclinical and clinical studies. The combination seeks to leverage both immediate and oral dosing forms to optimize therapeutic utility in the field and hospital settings. Ophirex is currently leading clinical development for snakebite treatment indications[1][3][6].

Other names
varespladib + varespladib methyl
02

Targets

svPLA2 (Snake venom phospholipase A2)PLA2G10 (Phospholipase A2 group X)PLA2G2A (Secretory phospholipase A2 group IIA)PLA2G5 (Secretory Phospholipase A2 Group V)

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