Varespladibmethyl (A-002) (A-002; LY333013) 是 II 组分泌型磷脂酶 A2 (PLA2) 的选择性抑制剂。
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Varespladib methyl is a selective inhibitor of group II secretory phospholipase A2 (PLA2).
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.
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