Mawdsley P
Eur J Rheumatol Inflamm. 1982;5(3):313-7.
While looking for new and safer non-steroidal anti-inflammatory drugs (NSAID's) chemists at Lederle Laboratories isolated three compounds, on the basis of animal tests for anti-inflammatory activity, for further screening. Two of these turned out to be metabolites of the third. The parent drug, fenbufen, was found to be inactive in in vitro tests and was thought to be a pro-drug requiring metabolism to produce activity in vivo. This hypothesis has been shown to be correct and further toxicity testing and clinical trials have confirmed the low incidence of gastro-intestinal effects and clinical efficacy of fenbufen in osteo and rheumatoid arthritis.
在寻找新型、更安全的非甾体抗炎药(NSAID)时,利德雷实验室的化学家们根据抗炎活性的动物试验分离出三种化合物,以便进一步筛选。结果发现其中两种是第三种的代谢产物。母体药物芬布芬在体外试验中无活性,被认为是一种前体药物,需要通过代谢在体内产生活性。这一假设已被证明是正确的,进一步的毒性测试和临床试验证实了芬布芬在骨关节炎和类风湿性关节炎中胃肠道副作用发生率低且临床疗效良好。