Varespladib methyl

Varespladib methyl is a selective inhibitor of group II secretory phospholipase A2 (PLA2).

Signaling Pathways >> Metabolic Enzyme/Protease >> Phospholipase

Research Areas >> Inflammation/Immunology

phospholipase A2 (PLA2)[1]

Varespladib methyl (LY333013) is an orally-administered methyl ester pro-drug that is metabolized to LY315920[1]. Varespladib and its orally bioavailable prodrug, Varespladib methyl (methyl-Varespladib) shows high-level secretory PLA2 (sPLA2) inhibition at nanomolar and picomolar concentrations against 28 medically important snake venoms from six continents[2].

[1]. Bradley JD, et al. A randomized, double-blinded, placebo-controlled clinical trial of LY333013, a selective inhibitor of group II secretory phospholipase A2, in the treatment of rheumatoid arthritis. J Rheumatol. 2005 Mar;32(3):417-23.

[2]. Lewin M, et al. Varespladib (LY315920) Appears to Be a Potent, Broad-Spectrum, Inhibitor of Snake Venom Phospholipase A2 and a Possible Pre-Referral Treatment for Envenomation. Toxins (Basel). 2016 Aug 25;8(9). pii: E248.

U73122 | D609 | Darapladib | Quinacrine (dihydrochloride) | FIPI | Melittin | Varespladib | CAY10650 | AA26-9 | ML348 | Tanshinone I | Methyl Arachidonyl Fluorophosphonate | ML 349 | 1-Monolinolein | Lp-PLA2 -IN-1