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Current Topics in Medicinal Chemistry
ISSN (Print): 1568-0266
ISSN (Online): 1873-5294
VOLUME: 9
ISSUE: 15
DOI: 10.2174/156802609789895728      Price:  $58









Update on Hsp90 Inhibitors in Clinical Trial

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Author(s): Y. S. Kim, S. V. Alarcon, S. Lee, M.-J. Lee, G. Giaccone, L. Neckers and J. B. Trepel
Pages 1479-1492 (14)
Abstract:
Twenty-five years ago the first small molecule inhibitors of Hsp90 were identified. In the intervening years there has been dramatic progress in basic scientific understanding of the Hsp90 chaperone machinery and in the role of Hsp90 in malignancy. The first-in-class Hsp90 inhibitor 17-AAG entered into Phase I clinical trials in 1999. There are now 13 Hsp90 inhibitors in clinical trial, representing multiple drug classes, and hundreds of patients have been treated in adult oncology and pediatric oncology trials. This review will provide an overview of the clinical trial results thus far. In addition, pivotal issues in further development of Hsp90 inhibitors as anticancer drugs will be discussed.
Keywords:
Hsp90 inhibitors, targeted therapy, clinical trial
Affiliation:
Medical Oncology Branch, NCI, Bldg 10, Rm 12N230, NIH, 10 Center Drive, Bethesda, MD 20892, USA.