Abstract:
INTRODUCTION:Heat shock protein 90 (HSP90) serves as a critical facilitator for oncogene addiction. There has been augmenting enthusiasm in pursuing HSP90 as an anticancer strategy. In fact, since the initial serendipitous discovery that geldanamycin (GM) inhibits HSP90, the field has rapidly moved from proof-of-concept clinical studies with GM derivatives to novel second-generation inhibitors. AREAS COVERED:The authors highlight the current status of the second-generation HSP90 inhibitors in clinical development. Herein, the authors note the lessons learned from the completed clinical trials of first- and second-generation inhibitors and describe various assays attempting to serve for a more rational implementation of these agents to cancer treatment. Finally, the authors discuss the future perspectives for this promising class of agents. EXPERT OPINION:The knowledge gained thus far provides perhaps only a glimpse at the potential of HSP90 for which there is still much work to be done. Lessons from the clinical trials suggest that HSP90 therapy would advance at a faster pace if patient selection and tumor pharmacokinetics of these drugs were better understood and applied to their clinical development. It is also evident that combining HSP90 inhibitors with other potent anticancer therapies holds great promise not only due to synergistic antitumor activity but also due to the potential of prolonging or preventing the development of drug resistance.
journal_name
Expert Opin Investig Drugsjournal_title
Expert opinion on investigational drugsauthors
Jhaveri K,Ochiana SO,Dunphy MP,Gerecitano JF,Corben AD,Peter RI,Janjigian YY,Gomes-DaGama EM,Koren J 3rd,Modi S,Chiosis Gdoi
10.1517/13543784.2014.902442subject
Has Abstractpub_date
2014-05-01 00:00:00pages
611-28issue
5eissn
1354-3784issn
1744-7658journal_volume
23pub_type
杂志文章,评审abstract:INTRODUCTION:Psychostimulants are first-line treatments for attention-deficit/hyperactivity disorder (ADHD), but their tolerability profiles and individual response variability fuel a continuing search for alternative medications. The observation that nicotinic agents improve cognition has led pharmaceutical companies ...
journal_title:Expert opinion on investigational drugs
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doi:10.1517/13543784.2014.934806
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abstract:INTRODUCTION:Rheumatoid arthritis (RA) is a chronic inflammatory auto-immune disease that can lead to permanent disability and deformity. Despite current treatment modalities, many patients are still unable to reach remission. Interleukin-1 receptor-associated kinase 4 (IRAK-4) inhibitors are novel agents designed to s...
journal_title:Expert opinion on investigational drugs
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journal_title:Expert opinion on investigational drugs
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journal_title:Expert opinion on investigational drugs
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journal_title:Expert opinion on investigational drugs
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journal_title:Expert opinion on investigational drugs
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journal_title:Expert opinion on investigational drugs
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journal_title:Expert opinion on investigational drugs
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.7.12.1977
更新日期:1998-12-01 00:00:00
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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更新日期:2014-12-01 00:00:00
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2012.642368
更新日期:2012-01-01 00:00:00
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abstract:INTRODUCTION:Medical treatment of brain metastases (BM) is still a controversial issue in cancer therapy being mainly limited by the existence of the BBB. Temozolomide (TMZ) can cross BBB and several clinical trials have been performed attempting to demonstrate the activity of TMZ in combination with whole brain radiot...
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journal_title:Expert opinion on investigational drugs
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journal_title:Expert opinion on investigational drugs
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更新日期:2000-11-01 00:00:00
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