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PMID: 19860730 Published · ppublish English Journal Article Review

Update on Hsp90 inhibitors in clinical trial.

Current topics in medicinal chemistry ·Vol. 9 ·No. 15 ·2009-00-00 ·Pages 1479-92

Kim YS, Alarcon SV, Lee S, Lee MJ, Giaccone G, Neckers L, Trepel JB

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.

MeSH Terms
Antineoplastic Agents/chemistry,pharmacology,therapeutic use Clinical Trials as Topic HSP90 Heat-Shock Proteins/antagonists & inhibitors Humans Neoplasms/drug therapy
Chemicals
Antineoplastic Agents HSP90 Heat-Shock Proteins
Authors & Affiliations
7 authors, click to expand affiliations / ORCID
Kim Y S
Medical Oncology Branch, NCI, NIH, Bethesda, MD 20892, USA.
Alarcon S V
Lee S
Lee M-J
Giaccone G
Neckers L
Trepel J B
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Article Info
Journal
Current topics in medicinal chemistry
Abbr.
Curr Top Med Chem
ISSN
1873-4294
DOI
10.2174/156802609789895728
Published
2009-00-00
Pages
1479-92
Language
English
Region
United Arab Emirates
NLM ID
101119673
PMCID
PMC7241864
Subset
IM
Grants
Intramural NIH HHS · Z01 BC010854 · United States
Intramural NIH HHS · Z01 SC010074 · United States
External Links
PubMed source DOI: 10.2174/156802609789895728 PMC Full Text View journal details
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