Figure 1.
Metabolism of sulindac. Prodrug sulindac undergoes reversible reduction into the active sulfide form through the action of liver enzymes and colonic bacteria. Sulindac sulfide is a non-selective COX inhibitor and is responsible for the anti-inflammatory properties of sulindac. The sulfone metabolite is generated by irreversible oxidation of the sulfoxide in the liver, and does not have anti-inflammatory activity. Figure adapted from Gurpinar et al., Frontiers in Oncology, 2013 (106).
