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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Update on Hsp90 Inhibitors in Clinical Trial

Author(s): Y. S. Kim, S. V. Alarcon, S. Lee, M.-J. Lee, G. Giaccone, L. Neckers and J. B. Trepel

Volume 9, Issue 15, 2009

Page: [1479 - 1492] Pages: 14

DOI: 10.2174/156802609789895728

Price: $65

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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

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