Therapeutic potential of endothelin receptor modulators: lessons from human clinical trials.

Details

Serval ID
serval:BIB_7B4155B02DF6
Type
Article: article from journal or magazin.
Publication sub-type
Review (review): journal as complete as possible of one specific subject, written based on exhaustive analyses from published work.
Collection
Publications
Institution
Title
Therapeutic potential of endothelin receptor modulators: lessons from human clinical trials.
Journal
Expert Opinion on Therapeutic Targets
Author(s)
Aubert J.D., Juillerat-Jeanneret L.
ISSN
1744-7631 (Electronic)
ISSN-L
1472-8222
Publication state
Published
Issued date
2009
Volume
13
Number
9
Pages
1069-1084
Language
english
Notes
Publication types: Journal Article ; Review
Publication Status: ppublish
Abstract
The endothelin system, and in particular endothelin receptors, are targets for therapeutic intervention in human diseases. Endothelin receptor antagonists have reached clinical use for treating pulmonary arterial hypertension, and are under clinical investigation for several other diseases, such as cancer, vasospasm or fibrogenic diseases. We review the molecules that have been evaluated in the main clinical trials, from the point of view of receptor selectivity and of their chemical characteristics which were important for efficacy in pulmonary hypertension. We will also discuss future use of antagonists to endothelin receptor(s) in several human diseases and what should be the necessary properties of the future molecules for efficacy in diseases where the presently tested molecules displayed suboptimal efficacy.
Keywords
Animals, Clinical Trials as Topic, Drug Delivery Systems, Endothelins/metabolism, Humans, Hypertension, Pulmonary/drug therapy, Hypertension, Pulmonary/physiopathology, Neoplasms/drug therapy, Neoplasms/physiopathology, Receptors, Endothelin/antagonists & inhibitors
Pubmed
Web of science
Create date
08/10/2009 14:32
Last modification date
20/08/2019 15:37
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