varespladib methyl

11/01/2021 - "Inhibitors of secreted PLA2, varespladib and varespladib methyl, are under investigation for repositioning in snakebite envenoming. "
01/01/2018 - "The orally bioavailable, heat-stable, secretory phospholipase A₂ (sPLA₂) inhibitor, LY333013, demonstrates antidotal characteristics for severe snakebite envenoming in both field and hospital use. "
11/01/2020 - "The phospholipase A2 (PLA2) inhibitors varespladib (LY315920) and its orally available derivative methyl-varespladib (LY333013) have been proposed as potential therapies for the treatment of snakebite envenomings in which toxicity depends on the action of PLA2s. "
12/28/2022 - "BRAVO (Broad-spectrum Rapid Antidote: Varespladib Oral for snakebite) is a multicenter, randomized, double-blind, placebo-controlled, phase 2 study to evaluate the safety, tolerability, and efficacy of oral varespladib-methyl plus standard of care (SoC) vs. SoC plus placebo in patients presenting with acute SBE by any venomous snake species. "
01/01/2023 - "Varespladib (intravenous, IV) and varespladib-methyl (oral) have been shown to potently inhibit sPLA2s from snake venoms in murine and porcine models, thus supporting their further study as potential treatments for snakebite envenoming. "

02/01/2012 - "The VISTA-16 study will determine whether varespladib methyl has a beneficial impact on cardiovascular events in patients with an acute coronary syndrome."
12/01/2011 - "Anti-inflammatory effects of varespladib methyl in diabetic patients with acute coronary syndrome."
10/01/2010 - "The experimental basis for sPLA(2) inhibition with varespladib methyl as a potential candidate for lowering recurrent cardiovascular events particularly in acute coronary syndrome patients is discussed. "
09/28/2010 - "Effects of varespladib methyl on biomarkers and major cardiovascular events in acute coronary syndrome patients."
02/01/2012 - "Up to 6,500 patients with acute coronary syndrome will be randomized to receive treatment with varespladib methyl 500 mg daily or placebo for 16 weeks, in addition to background treatment with atorvastatin and other evidence-based therapies. "

01/01/2011 - "In order to achieve the widespread use of varespladib methyl in ACS patients, completion of a prospective, randomized placebo-controlled trial in ACS patients and stable coronary artery disease patients with increased sPLA(2) activity will be required."
03/01/2013 - "The results may provide an explanation for the recently reported inefficacy of A-002 (varespladib) to treat patients with coronary artery disease. "
09/01/2009 - "Varespladib methyl, an oral phospholipase A2 inhibitor for the potential treatment of coronary artery disease."
09/01/2009 - "Phase II clinical trials of varespladib methyl in patients with coronary artery disease, rheumatoid arthritis, asthma and ulcerative colitis revealed that the drug was well tolerated. "
09/01/2009 - "Varespladib methyl is an oral secretory phospholipase A2 inhibitor that is being developed by Anthera Pharmaceuticals Inc for the potential treatment of coronary artery disease, acute coronary syndrome and inflammation. "

02/17/2009 - "The use of A-002 may have a beneficial effect in preventing diet-induced atherosclerosis in guinea pigs."
01/01/2009 - "(1) In a high-fat diet model, A-002 (30 and 90 mg/kg twice a day for 16 weeks) reduced aortic atherosclerosis by 50% (P < 0.05). "
02/17/2009 - "Thus, A-002 (varespladib), an inhibitor of sPLA2enzymes, is proposed to modulate the development of atherosclerosis. "
01/01/2009 - "In addition, the effects of A-002 on atherosclerosis in 2 ApoE mouse models were evaluated using en face analysis. "
01/01/2009 - "(2) In an accelerated atherosclerosis model, with angiotensin II-induced aortic lesions and aneurysms, A-002 (30 mg/kg twice a day) reduced aortic atherosclerosis by approximately 40% (P < 0.05) and attenuated aneurysm formation (P = 0.0096). "

03/01/2005 - "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."
09/01/2009 - "Phase II clinical trials of varespladib methyl in patients with coronary artery disease, rheumatoid arthritis, asthma and ulcerative colitis revealed that the drug was well tolerated. "
03/01/2005 - "To evaluate the efficacy and safety of a selective inhibitor of secretory phospholipase (sPLA2), LY333013, in the treatment of rheumatoid arthritis (RA). "
09/01/2009 - "Varespladib methyl did not demonstrate a good efficacy profile in patients with rheumatoid arthritis, asthma and ulcerative colitis, whereas in patients with coronary artery disease, varespladib methyl consistently reduced LDL-cholesterol levels (elevated LDL-cholesterol levels are a marker of increased cardiovascular risk). "
11/11/2022 - "The development of varespladib and its oral dosage form, varespladib-methyl, has been accelerated by previous clinical development campaigns to treat non-envenoming conditions related to ulcerative colitis, rheumatoid arthritis, asthma, sepsis, and acute coronary syndrome. "