nabumetone

Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the prodrug of the active metabolite 6MNA.
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Nabumetone is a methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthylacetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs. It has a role as a non-steroidal anti-inflammatory drug, a non-narcotic analgesic, a cyclooxygenase 2 inhibitor and a prodrug. It is a methoxynaphthalene and a methyl ketone.|Nabumetone was originally developed as a non-acidic non-steroidal anti-inflammatory drug (NSAID). It was thought to avoid trapping of the drug in the stomach by making it unable to dissociate into ions which was believed to reduce GI toxicity by limiting local action. While slightly reduced, possibly due to a degree of cyclooxygenase-2 selectivity (COX-2), nabumetone still produces significant adverse effects in the GI tract. The molecule itself is a pro-drug with its 6-methoxy-2-naphthylacetic acid (6-MNA) metabolite acting as a potent COX inhibitor similar in structure to [naproxen]. Nabumetone was developed by Smithkline Beecham under the trade name Relafen and first received FDA approval in December, 1991.|Nabumetone is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of nabumetone is as a Cyclooxygenase Inhibitor.|Nabumetone is a long acting nonsteroidal antiinflammatory drug (NSAID) that is available by prescription only and is used in therapy of chronic arthritis. Nabumetone has been linked to rare instances of clinically apparent, idiosyncratic drug induced liver disease.|Nabumetone is a naphthylalkanone and non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic and analgesic activities. Nabumetone is a prodrug that upon hepatic catalysis converts into the active moiety 6-methoxy-2-naphthylacetic acid (6MNA). 6MNA inhibits the activity of the enzymes cyclo-oxygenase I and II, resulting in decreased formation of precursors of prostaglandins and thromboxanes. The resulting decrease in prostaglandin synthesis is responsible for the therapeutic effects of nabumetone. The formation of thromboxane A2, by thromboxane synthase, is also decreased and results in an inhibition of platelet aggregation.|A butanone non-steroidal anti-inflammatory drug and cyclooxygenase-2 (COX2) inhibitor that is used in the management of pain associated with OSTEOARTHRITIS and RHEUMATOID ARTHRITIS.