Disease prevention is one area that both public and governmental agencies strongly support owing to its potential for an improved lifestyle and a reduction in health care costs. In this review, we focus on the clinical development of one target for cancer prevention, the COX-2 enzyme. This provides an excellent example of how basic research in biochemistry and pharmacology can lead to translational studies and eventually to approval of a drug by the FDA for use as a chemopreventive agent in humans. It is hoped that, as the genome sequence is understood more clearly, other targets will emerge that will provide even more effective drugs for future cancer prevention.