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.