Apricoxib (CS-706), a small-molecule, orally active, selective COX-2 inhibitor, is under development by Tragara Pharmaceuticals Inc as an analgesic and anti-inflammatory agent, and also for its anticancer potential. The compound has desirable pharmacokinetic parameters, and has demonstrated good gastrointestinal tolerability and safety in preclinical studies and clinical trials. Phase IIa trial data indicated that apricoxib was a potent analgesic in the treatment of pain in postoperative dental surgery. At the time of publication, phase II trials assessing apricoxib in combination with anticancer drugs in patients with breast, lung and pancreatic cancer were ongoing. Evidence for the anticancer activity of oral apricoxib appears to be highly promising. However, the market success of apricoxib will depend mainly on long-term safety trials, which are needed to establish the cardiovascular safety of the drug when administered alone or in combination with other agents in cancer chemotherapy.