Pharmacological Potential of Sulindac and Its Active Metabolite: A Comprehensive Review

In this review, we describe and discuss the pharmaceutical aspects, pharmacokinetic profile, and preclinical and clinical studies of sulindac and its active metabolite and emphasise their potential activity not only in anti-inflammation strategies but also as chemoprevention drug candidates. Though they are widely validated through in vitro and in vivo models, to date, no efforts have been made to compile in a single review on their pharmacologically potential, pharmacokinetics and toxicity profiles. Key databases such as PubMed, Science Direct, Scopus, and Google Scholar, among others, were probed for a systematic search using keywords to retrieve relevant publications. An exhaustive electronic survey of the related literature on the pharmacologically potential activity and the pharmacokinetic and toxicity profiles of sulindac resulted in around 200 articles (1975 and 2023) being included. The studies conducted on sulindac sulphide and sulindac sulfone metabolites reported a varied range of biological effects deployed in this review. The review concluded that there is scope for repurposing sulindac using computer-aided drug design and biological study to find out possible new targets for strengthening the potency and selectivity of the metabolites.