Document Detail

Danusertib, an aurora kinase inhibitor.
MedLine Citation:
PMID:  22242557     Owner:  NLM     Status:  MEDLINE    
INTRODUCTION: Drugs that interfere with the normal progression of mitosis belong to the most successful cytotoxic agents currently used for anticancer treatment. Aurora kinases are serine/threonine kinases that function as key regulators of mitosis and are frequently overexpressed in human cancers. The use of several small molecule aurora kinase inhibitors as potential anticancer therapeutic is being investigated. Danusertib (formerly PHA-739358) is a small ATP competitive molecule that inhibits aurora A, B and C kinases. Interestingly, danusertib also inhibits several receptor tyrosine kinases such as Abl, Ret, FGFR-1 and TrkA. These tyrosine kinases are involved in the pathogenesis of a variety of malignancies and the observed multi-target inhibition may increase the antitumor activity resulting in extending the indication. Danusertib was one of the first aurora kinase inhibitors to enter the clinic and has been studied in Phase I and II trials.
AREAS COVERED: This review provides an updated summary of preclinical and clinical experience with danusertib up to July 2011.
EXPERT OPINION: Future studies with danusertib should focus on the possibility of combining this agent with other targeted anticancer agents, chemotherapy or radiotherapy. As a single agent, danusertib may show more promise in the treatment of leukemias than in solid tumors.
Hielke J Meulenbeld; Ron Hj Mathijssen; Jaap Verweij; Ronald de Wit; Maja Ja de Jonge
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Publication Detail:
Type:  Journal Article; Review     Date:  2012-01-13
Journal Detail:
Title:  Expert opinion on investigational drugs     Volume:  21     ISSN:  1744-7658     ISO Abbreviation:  Expert Opin Investig Drugs     Publication Date:  2012 Mar 
Date Detail:
Created Date:  2012-02-13     Completed Date:  2012-06-01     Revised Date:  2013-11-06    
Medline Journal Info:
Nlm Unique ID:  9434197     Medline TA:  Expert Opin Investig Drugs     Country:  England    
Other Details:
Languages:  eng     Pagination:  383-93     Citation Subset:  IM    
Erasmus University Medical Center, Daniel den Hoed Cancer Center, Department of Medical Oncology, Groene Hilledijk 301, Rotterdam, the Netherlands.
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MeSH Terms
Antineoplastic Agents / pharmacology*,  therapeutic use
Benzamides / pharmacology*,  therapeutic use
Clinical Trials, Phase I as Topic
Clinical Trials, Phase II as Topic
Drug Delivery Systems
Drug Design
Neoplasms / drug therapy,  enzymology,  pathology
Protein Kinase Inhibitors / pharmacology*,  therapeutic use
Protein-Serine-Threonine Kinases / antagonists & inhibitors*
Protein-Tyrosine Kinases / antagonists & inhibitors
Pyrazoles / pharmacology*,  therapeutic use
Reg. No./Substance:
0/Antineoplastic Agents; 0/Benzamides; 0/Protein Kinase Inhibitors; 0/Pyrazoles; EC Kinases; EC Kinases; EC kinase; M3X659D0FY/danusertib

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