Article: Ambrisentan, a non-peptide endothelin receptor antagonist.
2006 Volume 24, Issue 1, Page(s) 63–76
Abstract: ... of disease states, mainly of the cardiovascular system. Ambrisentan (LU 208075), a selective ET(A)-receptor ... suggest an integral involvement of the endothelin (ET)-system in the pathophysiology of a variety ... antagonist, is an orally active diphenyl propionic acid derivative. It has been shown to have a very ...
Abstract | Increasing numbers of experimental investigations and recently also of clinical trials strongly suggest an integral involvement of the endothelin (ET)-system in the pathophysiology of a variety of disease states, mainly of the cardiovascular system. Ambrisentan (LU 208075), a selective ET(A)-receptor antagonist, is an orally active diphenyl propionic acid derivative. It has been shown to have a very promising efficacy to safety ratio in the initial clinical trials. Phase II and Phase III trials with ambrisentan in pulmonary arterial hypertension have been performed. The pharmacological properties and data from the experimental investigations suggest additional possible uses of ambrisentan in the prevention of reperfusion injury after organ transplantation and in restenosis following coronary artery dilatation. Furthermore, the pharmacological profile of ambrisentan indicates that this drug may also be suitable in the treatment of cerebrovascular disorders. In the present article basic investigations, animal studies and clinical trials with ambrisentan are reviewed. This review may help to define pathophysiological conditions, in which ambrisentan could be indicated and further evaluated in appropriate preclinical and clinical trials. |
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MeSH term(s) | Animals ; CHO Cells ; Clinical Trials as Topic ; Cricetinae ; Cricetulus ; Endothelin A Receptor Antagonists ; Humans ; Myocardial Ischemia/drug therapy ; Phenylpropionates/chemistry ; Phenylpropionates/pharmacology ; Phenylpropionates/therapeutic use ; Pyridazines ; Renal Insufficiency/drug therapy ; Structure-Activity Relationship |
Chemical Substances | Endothelin A Receptor Antagonists ; Phenylpropionates ; Pyridazines ; ambrisentan (HW6NV07QEC) |
Language | English |
Publishing date | 2006 |
Publishing country | United States |
Document type | Journal Article ; Review |
ZDB-ID | 645099-4 |
ISSN | 0897-5957 |
ISSN | 0897-5957 |
DOI | 10.1111/j.1527-3466.2006.00063.x |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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