Indisulam: an anticancer sulfonamide in clinical development

被引：140

作者：

Supuran, CT ^{[1
]}

机构：

[1] Univ Florence, Dipartimento Chim, Lab Chim Bioinorgan, I-50019 Sesto Fiorentino, Florence, Italy

来源：

EXPERT OPINION ON INVESTIGATIONAL DRUGS | 2003年 / 12卷 / 02期

关键词：

anticancer agent; carbonic anhydrase inhibitor; cell-cycle arrest; G1; phase; sulfonamide;

D O I：

10.1517/13543784.12.2.283

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Indisulam (N-(3-chloro-7-indolyl)-1,4-benzenedisulfonamide, E7070) is a novel sulfonamide anticancer agent in clinical development for the treatment of solid tumours. Its mechanism of action is multifactorial, as indisulam arrests cell cycle in the G1 phase, strongly inhibits carbonic anhydrase, a critical enzyme involved in many physiological processes and whose association with cancer became obvious in the last period, and markedly alters gene expression levels of at least 60 transcripts. Four Phase I clinical trials gave promising results, showing the compound to possess nonlinear pharmacokinetics. Presently this compound is in Phase II trials in Europe and USA for the treatment of solid tumours.

引用

页码：283 / 287

页数：5

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