The science--equivalent efficacy and diminished risk.
Nabumetone is an effective anti-inflammatory drug in models of inflammation and in man, comparable in potency to other compounds of this type. It differs from other compounds in several important respects. The parent molecule is non-acidic and virtually inactive but is transformed to an active metabolite (6MNA) by the liver. 6MNA is not excreted in bile and cannot therefore, by reflux from the small intestine, reach the stomach. Many other compounds can reach the stomach in this way even when given by routes other than oral, for example by suppository. Prostaglandin production by the stomach, a protective mechanism, is not markedly affected by 6MNA whereas it is suppressed by other NSAIDs. These studies suggest a favourable therapeutic ratio for nabumetone.
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SmithKline Beecham Pharmaceuticals, Harlow, Essex, U.K.
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D002074:Butanones / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D005753:Gastric Mucosa / Q000187:drug effects; D006801:Humans; D007249:Inflammation / Q000188:drug therapy*; D000077430:Nabumetone; D009280:Naphthaleneacetic Acids / Q000097:blood
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002074:Butanones; D009280:Naphthaleneacetic Acids; C044612:6-methoxy-2-naphthylacetic acid; D000077430:Nabumetone