Fisherman J S, Cline E M, Plowman J, Quinn F R, Hawkins M J
Cancer Therapy Evaluation Program, National Cancer Institute, NIH, Bethesda MD.
Invest New Drugs. 1991 Nov;9(4):295-303. doi: 10.1007/BF00183569.
Terephthalamidine (NSC 57155) is one of 800 terephthalanilides and related compounds which were synthesized and tested preclinically in the late 1950's and early 1960's. Based upon their activity against murine leukemias, some of these agents were tested briefly in clinical trials at that time. Despite the observation of responses, the compounds were dropped because of severe and unusual neurotoxicity. More recently, terephthalamidine has been screened for antitumor activity and chosen for further clinical investigation by the NCI's Project for the Review of Old Drugs (P.R.O.D.) because of its novel structure and spectrum of preclinical activity. The current availability of a plasma assay for the drug permits further study of its clinical pharmacokinetics and pharmacodynamics and, perhaps, the development of improved scheduling strategies.
对苯二甲脒（NSC 57155）是20世纪50年代末和60年代初合成并进行临床前测试的800种对苯二甲酰苯胺及其相关化合物之一。基于它们对鼠白血病的活性，当时其中一些药物在临床试验中进行了简短测试。尽管观察到有反应，但由于严重且异常的神经毒性，这些化合物被放弃。最近，对苯二甲脒因其新颖的结构和临床前活性谱而被筛选用于抗肿瘤活性研究，并被美国国立癌症研究所的旧药审查项目（P.R.O.D.）选中进行进一步的临床研究。目前可用于该药物的血浆检测方法允许进一步研究其临床药代动力学和药效学，也许还能开发出改进的给药方案策略。
