Advances in the Therapeutic Application of Small-Molecule Inhibitors and Repurposed Drugs against Snakebite,Journal of Medicinal Chemistry

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Advances in the Therapeutic Application of Small-Molecule Inhibitors and Repurposed Drugs against Snakebite
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2021-09-26 , DOI: 10.1021/acs.jmedchem.1c00266
Upasana Puzari ₁ , Pedro Alexandrino Fernandes ₂ , Ashis K Mukherjee _{1,

3}

Affiliation

The World Health Organization has declared snakebite as a neglected tropical disease. Antivenom administration is the sole therapy against venomous snakebite; however, several limitations of this therapy reinforce the dire need for an alternative and/or additional treatment against envenomation. Inhibitors against snake venoms have been explored from natural resources and are synthesized in the laboratory; however, repurposing of small-molecule therapeutics (SMTs) against the principal toxins of snake venoms to inhibit their lethality and/or obnoxious effect of envenomation has been garnering greater attention owing to their established pharmacokinetic properties, low-risk attributes, cost-effectiveness, ease of administration, and storage stability. Nevertheless, SMTs are yet to be approved and commercialized for snakebite treatment. Therefore, we have systematically reviewed and critically analyzed the scenario of small synthetic inhibitors and repurposed drugs against snake envenomation from 2005 to date and proposed novel approaches and commercialization strategies for the development of efficacious therapies against snake envenomation.

中文翻译：

小分子抑制剂和再利用药物抗蛇咬伤的治疗应用进展

世界卫生组织已宣布蛇咬伤为一种被忽视的热带疾病。抗蛇毒血清是对抗毒蛇咬伤的唯一疗法；然而，这种疗法的一些局限性加强了对替代和/或额外治疗方法的迫切需求。蛇毒抑制剂已从自然资源中探索出来，并在实验室合成；然而，重新利用小分子疗法 (SMT) 来抑制蛇毒的主要毒素以抑制其致命性和/或毒液的有害影响，由于其既定的药代动力学特性、低风险属性、成本效益、易于给药和储存稳定性。尽管如此，SMT 尚未获得批准和商业化用于治疗蛇咬伤。所以，

更新日期：2021-10-14

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