Three step CYP1A2 Mediated Metabolism of the prodrug<unk>  to its active metabolite 6-MNA.<unk>  is a nonsteroidal anti-inflammatory drug (NSAID).<unk>  was developed by Beecham and first received regulatory approval in 1991. It is available under numerous brand names, such as Relafen, Relifex, and Gambaran.<unk>  is a nonacidic NSAID prodrug that is rapidly metabolized in the liver to the active metabolite, 6-methoxy-2-naphthyl acetic acid. As found with previous NSAIDs,<unk> 's active metabolite inhibits the cyclooxygenase enzyme and preferentially blocks COX-2 activity (which is indirectly responsible for the production of inflammation and pain during arthritis). The active metabolite of<unk>  is felt to be the compound primarily responsible for therapeutic effect. Comparatively, the parent drug is a poor inhibitor of COX-2 byproducts, particularly prostaglandins. It may be less nephrotoxic than indomethacin. There are two known polymorphs of the compound.<unk>  has little effect on renal prostaglandin secretion and less of an association with heart failure than other traditional drugs of the class. Effects of<unk>  on blood pressure control in hypertensive patients on ACE inhibitors is also good—equivalent to paracetamol.
Nabumetone
Enoximone
Bisoctrizole
Flupamesone
Ethisterone
Trafermin
Medifoxamine
Lapisteride