Drug intelligence / Profile preview

sulindac sulfide

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Sulindac sulfide is the pharmacologically active metabolite of sulindac, a nonsteroidal anti-inflammatory drug (NSAID) of the arylalkanoic acid class. Sulindac itself is a prodrug; following oral administration, it is metabolized in the liver to sulindac sulfide, which mediates the majority of the therapeutic effects. Sulindac sulfide inhibits cyclooxygenase (COX)-1 and COX-2, reducing conversion of arachidonic acid to pro-inflammatory prostaglandins, resulting in anti-inflammatory, analgesic, and antipyretic effects. Sulindac sulfide has also demonstrated apoptosis-inducing and antineoplastic (anticancer) effects in vitro and in vivo, particularly in colorectal and breast cancer models[3][5][7]. Its enterohepatic circulation helps maintain stable blood levels and may reduce gastrointestinal side effects relative to some other NSAIDs[3][7].

Other names
49627-27-2Z-sulindac sulfidecis-sulindac sulfidesulindac sulfidesulindac sulfide (Z)-
02

Targets

AR (Adrenergic receptors)ALOX5 (Arachidonate 5-lipoxygenase)PGHS-1 (Prostaglandin G/H Synthase 1)PPARD (Peroxisome proliferator–activated receptor delta)PTGDR2 (Prostaglandin D2 receptor 2)MAPK3 (Mitogen-activated protein kinase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)FLAP (Arachidonate 5-lipoxygenase-activating protein)

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