exisulind

Exisulind is a small molecule antineoplastic agent and the sulfone derivative of the nonsteroidal anti-inflammatory drug (NSAID) sulindac. It belongs to a class of compounds known as selective apoptotic anti-neoplastic drugs (SAANDs). Exisulind acts primarily by inhibiting cyclic guanosine monophosphate phosphodiesterase (cGMP-PDE), particularly phosphodiesterase type 5. This inhibition leads to sustained elevation of cGMP levels and activation of protein kinase G (PKG), which induces apoptosis in precancerous and cancerous cells—especially colorectal cells that overexpress cGMP-PDE—with minimal effects on normal cells. The pro-apoptotic effect is independent of cyclooxygenase-1 or -2 inhibition, p53 status, Bcl-2 expression, or cell cycle arrest. Preclinical evidence also suggests an inhibitory effect on angiogenesis. Exisulind was developed for potential use in familial adenomatous polyposis (FAP), sporadic colonic polyps, cervical dysplasia, Barrett's esophagus disease, prostate cancer recurrence prevention after surgery or radiation therapy, breast cancer recurrence prevention after surgery or radiation therapy, lung cancer and other solid tumors[1][2][4][5].

Brand names

AptosynPrevatac

Other names

exisulindsulindac sulfone