The discovery and elucidation of prostaglandin (PG) pathways, particularly the molecular and clinical role of cyclooxygenase-2 (COX-2) function, has been found to have an important role in neoplasia. Current understanding of the role of COX-2 activity and therefore the potential clinical usefulness of COX-2-specific inhibitors in prostate cancer will be discussed herein. The discovery of PG pathways, the molecular and clinical roles of COX-2 function, and the corresponding application to neoplasia were reviewed in the scientific literature from 1960 through the present time. In addition, thorough review of recent abstract presentations at scientific meetings (American Urological Association and American Society of Clinical Oncology annual meetings from 1998 to the present) was undertaken regarding the potential role of COX-2 in urologic cancers. Reduced apoptosis, increased angiogenesis, and immunosuppression are just some of the known sequelae of COX-2 overexpression, and each effect could have an important role in tumor formation and progression. Preclinical research and pilot clinical studies in prostate cancer to date have been promising. We are just beginning to understand the molecular mechanisms and clinical effects of COX-2 function and its inhibition and the potential for COX-2-specific inhibitors to affect tumor biology and growth, and thereby serve as antitumor drugs in therapeutic and chemopreventive roles in prostate cancer. The absence of complete scientific understanding in these areas presents an exciting opportunity for innovative and important scientific study.