Indisulam: an anticancer sulfonamide in clinical development.
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.
Supuran
Claudiu T
CT
Università degli Studi di Firenze, Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Via della Lastruccia, 3, Rm. 188, I-50019 Sesto Fiorentino, Florence, Italy. claudiu.supuran@unifi.it
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D002986:Clinical Trials as Topic / Q000706:statistics & numerical data; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D013678:Technology, Pharmaceutical / Q000379:methods
D000970:Antineoplastic Agents; C439829:N-(3-chloro-7-indolyl)-1,4-benzenedisulphonamide; D013449:Sulfonamides