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
Current Topics in Medicinal Chemistry
Title: Update on Hsp90 Inhibitors in Clinical Trial
Volume: 9 Issue: 15
Author(s): Y. S. Kim, S. V. Alarcon, S. Lee, M.-J. Lee, G. Giaccone, L. Neckers and J. B. Trepel
Affiliation:
Keywords: Hsp90 inhibitors, targeted therapy, clinical trial
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.
Export Options
About this article
Cite this article as:
Kim S. Y., Alarcon V. S., Lee S., Lee M.-J., Giaccone G., Neckers L. and Trepel B. J., Update on Hsp90 Inhibitors in Clinical Trial, Current Topics in Medicinal Chemistry 2009; 9 (15) . https://dx.doi.org/10.2174/156802609789895728
DOI https://dx.doi.org/10.2174/156802609789895728 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Therapeutic Rationale for mTOR Inhibition in Advanced Renal Cell Carcinoma
Current Clinical Pharmacology Clinical Utility of Combined 18F-Fluoro-2-deoxyglucose Positron Emission Tomography – Computed Tomography in the Evaluation of Gastrointestinal Malignancies
Current Medical Imaging Cellular Physiology of Mismatch Repair
Current Pharmaceutical Design The Neuroendocrine Component in Bladder Tumors
Current Medicinal Chemistry Anticancer Agents Derived from Natural Products
Mini-Reviews in Medicinal Chemistry Cancer Prevention with Promising Natural Products: Mechanisms of Action and Molecular Targets
Anti-Cancer Agents in Medicinal Chemistry Meet Our Editorial Board Member:
Anti-Cancer Agents in Medicinal Chemistry Neurokinin-1 Receptor (NK-1R) Antagonists: Potential Targets in the Treatment of Glioblastoma Multiforme
Current Medicinal Chemistry Amplified Crosstalk Between Estrogen Binding and GFR Signaling Mediated Pathways of ER Activation Drives Responses in Tumors Treated with Endocrine Disruptors
Recent Patents on Anti-Cancer Drug Discovery Dimethyl Sulfoxide as an Excitatory Modulator and its Possible Role in Cancer Pain Management
Inflammation & Allergy - Drug Targets (Discontinued) Redistribution of CD95 into the Lipid Rafts to Treat Cancer Cells?
Recent Patents on Anti-Cancer Drug Discovery Transcatheter Aortic Valve Implantation Infective Endocarditis: Current Data and Implications on Prophylaxis and Management
Current Pharmaceutical Design Hydrogen Sulphide and Pain
Inflammation & Allergy - Drug Targets (Discontinued) An Overview of Emerging Immunotargets of Genitourinary Tumors
Current Drug Targets VEGF Inhibitors and Prostate Cancer Therapy
Current Molecular Pharmacology Combining Gene Therapy and Radiation Against Cancer
Current Gene Therapy Dissecting the Therapeutic Potency of Antimicrobial Peptides Against Microbial Biofilms
Current Protein & Peptide Science Geriatric Evaluation of Oncological Elderly Patients
Anti-Cancer Agents in Medicinal Chemistry Dry Age-Related Macular Degeneration: Recent Progress of Therapeutic approaches
Current Molecular Pharmacology Influence of Aldo-keto Reductase 1C3 in Prostate Cancer - A Mini Review
Current Cancer Drug Targets