Document Detail


Enzastaurin hydrochloride for lymphoma: reassessing the results of clinical trials in light of recent advances in the biology of B-cell malignancies.
MedLine Citation:
PMID:  21639821     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
INTRODUCTION: The B-cell receptor (BCR) is critical for the development and persistence of B-cell non-Hodgkin lymphoma (B-NHL). Protein kinase C-beta (PKC-?) has been identified as one of the key signaling hubs downstream of the BCR and constitutes a valuable target in B-NHL. As a potent PKC-? inhibitor, enzastaurin is currently being tested in Phase II/III trials.
AREAS COVERED: This review summarizes the latest results and ongoing clinical trials with enzastaurin in light of basic scientific advances in the understanding of various lymphoid cancers, including diffuse large B-cell lymphoma (DLBCL), mantle cell lymphoma (MCL), follicular lymphoma (FL), chronic lymphocytic leukemia (CLL) and Waldenstr?m's macroglobulinemia (WM).
EXPERT OPINION: While its continued clinical development is uncertain, enzastaurin should be regarded as a stepping stone for the development of future therapies; indeed, the recent research has provided valuable insight into the possible molecular mechanisms that explain its limited clinical activity especially in the treatment of DLBCL and MCL. It should be noted that there is still some interest in enzastaurin, in combination, for the treatment of WM.
Authors:
Loic Ysebaert; Franck Morschhauser
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Review     Date:  2011-06-05
Journal Detail:
Title:  Expert opinion on investigational drugs     Volume:  20     ISSN:  1744-7658     ISO Abbreviation:  Expert Opin Investig Drugs     Publication Date:  2011 Aug 
Date Detail:
Created Date:  2011-07-13     Completed Date:  2011-12-20     Revised Date:  2014-07-30    
Medline Journal Info:
Nlm Unique ID:  9434197     Medline TA:  Expert Opin Investig Drugs     Country:  England    
Other Details:
Languages:  eng     Pagination:  1167-74     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Clinical Trials, Phase II as Topic
Clinical Trials, Phase III as Topic
Humans
Indoles / pharmacology*,  therapeutic use*
Lymphoma, B-Cell / drug therapy*,  enzymology,  metabolism*
Protein Kinase C / antagonists & inhibitors*,  metabolism
Protein Kinase C beta
Protein Kinase Inhibitors / pharmacology,  therapeutic use
Chemical
Reg. No./Substance:
0/Indoles; 0/Protein Kinase Inhibitors; EC 2.7.11.13/Protein Kinase C; EC 2.7.11.13/Protein Kinase C beta; UC96G28EQF/enzastaurin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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