Lessons learned from the development of imatinib.

It is now 5 years since clinical trials with imatinib (Gleevec, Glivec, previously STI571 or CGP 57148B) began. In January 2000, we published a perspective entitled “Lessons learned from the development of an Abl tyrosine kinase inhibitor for chronic myelogenous leukemia” [1]. This perspective looked at the transition of imatinib from preclinical to clinical development and discussed issues that would have to be addressed for the success of protein kinase inhibitors in the clinic. In this article, we update our thinking on the development of kinase inhibitors as anti-cancer agents in the context of the volumes of new data on both the preclinical and clinical activity of imatinib. A number of recent reviews have been published on the preclinical and clinical profile of imatinib [2–4]. Other articles in this special issue of Leukemia Research review specific aspects regarding imatinib. Additional details can be found in the following sources: (1) original publications on the discovery of imatinib [5–8]; (2) pivotal, early clinical trials in CML [9,10]; and (3) registration and phase III trials in CML [11–14].