Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug
Top Cited Papers
- 1 July 2002
- journal article
- review article
- Published by Springer Nature in Nature Reviews Drug Discovery
- Vol. 1 (7) , 493-502
- https://doi.org/10.1038/nrd839
Abstract
In the early 1980s, it became apparent that the work of pioneers such as Robert Weinberg, Mariano Barbacid and many others in identifying cancer-causing genes in humans was opening the door to a new era in anticancer research. Motivated by this, and by dissatisfaction with the limited efficacy and tolerability of available anticancer modalities, a drug discovery programme was initiated with the aim of rationally developing targeted anticancer therapies. Here, we describe how this programme led to the discovery and continuing development of Glivec (Gleevec in the United States), the first selective tyrosine-kinase inhibitor to be approved for the treatment of a cancer.Keywords
This publication has 59 references indexed in Scilit:
- Hematologic and Cytogenetic Responses to Imatinib Mesylate in Chronic Myelogenous LeukemiaNew England Journal of Medicine, 2002
- Roots of Clinical Resistance to STI-571 Cancer TherapyScience, 2001
- Clinical Resistance to STI-571 Cancer Therapy Caused by BCR-ABL Gene Mutation or AmplificationScience, 2001
- Activity of a Specific Inhibitor of the BCR-ABL Tyrosine Kinase in the Blast Crisis of Chronic Myeloid Leukemia and Acute Lymphoblastic Leukemia with the Philadelphia ChromosomeNew England Journal of Medicine, 2001
- Effect of the Tyrosine Kinase Inhibitor STI571 in a Patient with a Metastatic Gastrointestinal Stromal TumorNew England Journal of Medicine, 2001
- Structural Mechanism for STI-571 Inhibition of Abelson Tyrosine KinaseScience, 2000
- Blockade of the Bcr-Abl Kinase Activity Induces Apoptosis of Chronic Myelogenous Leukemia Cells by Suppressing Signal Transducer and Activator of Transcription 5–Dependent Expression of Bcl-XLThe Journal of Experimental Medicine, 2000
- KIT Extracellular and Kinase Domain Mutations in Gastrointestinal Stromal TumorsThe American Journal of Pathology, 2000
- The Design of Leadlike Combinatorial LibrariesAngewandte Chemie International Edition in English, 1999
- Gain-of-Function Mutations of c- kit in Human Gastrointestinal Stromal TumorsScience, 1998