Pelubiprofen, 2-[4-(Oxocyclohexylidene methyl)phenyl]propionic acid, is one of the 2-arylpropionic acid class of non-steroidal anti-inflammatory drugs (NSAIDs). It has wide variety of indications proposed: osteoarthritis, rheumatoid arthritis, musculoskeletal pain, post-operative trauma, backache, neck-shoulder syndrome and dental pain. Pelubiprofen is a prodrug of 2-arylpropionic acid with relatively selective effects on cyclooxygenase-2 activity. Antiinflammatory properties of pelubiprofen are due to its ability to both decrease prostaglandin synthesis by inhibiting the activities of cyclooxygenases (COXs) and IkB kinase-b (IKK-b). Pelubiprofen was found to have an anti-edema effect in the carrageenan-induced paw edema model in rats, one of the well-established acute inflammatory models in vivo. Pelubiprofen was well tolerated in single doses up to 120mg and at a dosage of 180 mg/day. No drug accumulation was evident, suggesting that it may be useful for long term treatment.