Varespladib (LY315920) and Methyl Varespladib (LY333013) Abrogate or Delay Lethality Induced by Presynaptically Acting Neurotoxic Snake Venoms [PDF]
Toxins, 2020 The phospholipase A2 (PLA2) inhibitor Varespladib (LY315920) and its orally bioavailable prodrug, methyl-Varespladib (LY333013) inhibit PLA2 activity of a wide variety of snake venoms.
José María Gutiérrez +3 more
doaj +9 more sources
Delayed Oral LY333013 Rescues Mice from Highly Neurotoxic, Lethal Doses of Papuan Taipan (Oxyuranus scutellatus) Venom [PDF]
Toxins, 2018 There is an unmet need for economical snakebite therapies with long shelf lives that are effective even with delays in treatment. The orally bioavailable, heat-stable, secretory phospholipase A2 (sPLA2) inhibitor, LY333013, demonstrates antidotal ...
Matthew R. Lewin +8 more
doaj +10 more sources
Delayed LY333013 (Oral) and LY315920 (Intravenous) Reverse Severe Neurotoxicity and Rescue Juvenile Pigs from Lethal Doses of Micrurus fulvius (Eastern Coral Snake) Venom [PDF]
Toxins, 2018 There is a clear, unmet need for effective, lightweight, shelf-stable and economical snakebite envenoming therapies that can be given rapidly after the time of a snake’s bite and as adjuncts to antivenom therapies in the hospital setting. The sPLA2
Matthew R. Lewin +6 more
doaj +6 more sources
Varespladib in the Treatment of Snakebite Envenoming: Development History and Preclinical Evidence Supporting Advancement to Clinical Trials in Patients Bitten by Venomous Snakes [PDF]
Toxins, 2022 The availability of effective, reliably accessible, and affordable treatments for snakebite envenoming is a critical and long unmet medical need. Recently, small, synthetic toxin-specific inhibitors with oral bioavailability used in conjunction with ...
Matthew R. Lewin +6 more
doaj +2 more sources
Varespladib (LY315920) Appears to Be a Potent, Broad-Spectrum, Inhibitor of Snake Venom Phospholipase A2 and a Possible Pre-Referral Treatment for Envenomation [PDF]
Toxins, 2016 Snakebite remains a neglected medical problem of the developing world with up to 125,000 deaths each year despite more than a century of calls to improve snakebite prevention and care.
Matthew Lewin +3 more
doaj +2 more sources
Developing Small Molecule Therapeutics for the Initial and Adjunctive Treatment of Snakebite. [PDF]
J Trop Med, 2018 The World Health Organization (WHO) recently added snakebite envenoming to the priority list of Neglected Tropical Diseases (NTD). It is thought that ~75% of mortality following snakebite occurs outside the hospital setting, making the temporal gap between a bite and antivenom administration a major therapeutic challenge.
Bulfone TC +3 more
europepmc +2 more sources
Snake Venom PLA2, a Promising Target for Broad-Spectrum Antivenom Drug Development. [PDF]
Biomed Res Int, 2017 Snakebite envenomation is a neglected global health problem, causing substantial mortality, disability, and psychological morbidity, especially in rural tropical and subtropical zones. Antivenin is currently the only specific medicine for envenomation. However, it is restricted by cold storage, snakebite diagnosis, and high price.
Xiao H, Pan H, Liao K, Yang M, Huang C.
europepmc +2 more sources
Modulation of immunity by the secreted phospholipase A2 family
Immunological Reviews, Volume 317, Issue 1, Page 42-70, August 2023., 2023 Summary Among the phospholipase A2 (PLA2) superfamily, which typically catalyzes the sn‐2 hydrolysis of phospholipids to yield fatty acids and lysophospholipids, the secreted PLA2 (sPLA2) family contains 11 isoforms in mammals. Individual sPLA2s have unique enzymatic specificity toward fatty acids and polar heads of phospholipid substrates and display ...
Makoto Murakami +2 more
wiley +1 more source
Chemical Biology &Drug Design, Volume 103, Issue 2, February 2024.Due to their roles in inflammation, the sPLA2 enzymes are of much medicinal interest. sPLA2 inhibitors have been developed for the treatment of inflammatory and other conditions such as cardiovascular disease, arteriosclerosis and rheumatoid arthritis.
Chantalle Crous +2 more
wiley +1 more source
318 LY333013: A Candidate First-in-Class, Broad Spectrum, Oral Field Antidote to Snakebite With Curative Potential [PDF]
Annals of Emergency Medicine, 2018 M.R. Lewin +3 more
openaire +1 more source