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Increasing evidence suggests that upregulation of cyclooxygenase-2 (COX-2) gene expression is implicated in colorectal carcinogenesis. Large epidemiologic studies as well as
clinical studies consistently show that long-term use of aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs) reduces the relative risk of colorectal cancer. The effect of NSAIDs on chemoprevention and tumor regression has also been demonstrated in a range of
experimental models in animals. Recently, specific COX-2 inhibitors such as celecoxib, rofecoxib, and valdecoxib have been developed and marketed. These compounds have been
shown in several clinical trials to produce fewer gastrointestinal adverse effects than classical
COX inhibitors. To date, celecoxib is the first specific COX-2 inhibitor approved by the United States Food and Drug Administration (US FDA) for the prophylaxis and treatment of
familial adenomatous polyposis (FAP), a benign colorectal tumor that would eventually progress to malignancy.
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