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在一项抗体导向酶前体药物疗法(ADEPT)临床研究中对前体药物、活性药物及代谢产物的鉴定。

Identification of prodrug, active drug, and metabolites in an ADEPT clinical study.

作者信息

Springer C J, Poon G K, Sharma S K, Bagshawe K D

机构信息

Department of Medical Oncology, Charing Cross Hospital, London, England.

出版信息

Cell Biophys. 1993 Jan-Jun;22(1-3):9-26. doi: 10.1007/BF03033864.

Abstract

Antibody-directed enzyme prodrug therapy (ADEPT) involves two phases. The first is an antibody-enzyme conjugate that localizes to tumor. The second phase is a prodrug that is administered when the enzyme-conjugate has cleared from blood and other nontumor tissues. In the pilot-scale clinical trial, the prodrug has been measured--in the plasma of patients, by liquid chromatography (HPLC) and by liquid chromatography-mass spectrometry (LC-MS). Active drug has been detected and metabolites identified. An indirect measurement of enzyme-conjugate in the plasma of patients has also been developed.

摘要

抗体导向酶前药疗法(ADEPT)包括两个阶段。第一阶段是一种抗体 - 酶偶联物,它会定位于肿瘤部位。第二阶段是在前药,当酶偶联物已从血液和其他非肿瘤组织中清除后给予。在中试规模的临床试验中,通过液相色谱法(HPLC)和液相色谱 - 质谱法(LC - MS)在患者血浆中对前药进行了测定。已检测到活性药物并鉴定出代谢产物。还开发了一种对患者血浆中酶偶联物的间接测量方法。

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