| Macitentan, a tissue-targeting endothelin receptor antagonist for the potential oral treatment of pulmonary arterial hypertension and idiopathic pulmonary fibrosis. | |
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MedLine Citation:
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PMID: 20730702 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Macitentan (ACT-064992), under development by Actelion Ltd in collaboration with Japanese licensee Nippon Shinyaku Co Ltd, is an orally active, non-peptide dual endothelin (ET)(A) and ET(B) receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). Scientific evidence suggests that the ET system may play an important role in the pathobiology of several cardiovascular diseases. A major therapeutic advance for the treatment of patients with PAH and IPF has been the pharmacological control of the activated ET system with ET receptor antagonists. Macitentan, because of its ability to target the tissues and to block both ET(A) and ET(B) receptors, is emerging as a new agent to treat cardiovascular disorders associated with chronic tissue ET system activation. The phase I and II clinical trials conducted to date have demonstrated that macitentan increases plasma levels of ET-1, displays dose-dependent pharmacokinetics, and was well tolerated in healthy volunteers and patients. At the time of publication, a phase II trial in patients with IPF and a phase III trial in patients with PAH was ongoing. It is expected that the results of these trials will validate the safety and efficacy of macitentan. |
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Authors:
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Shahzad G Raja |
Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Current opinion in investigational drugs (London, England : 2000) Volume: 11 ISSN: 2040-3429 ISO Abbreviation: Curr Opin Investig Drugs Publication Date: 2010 Sep |
Date Detail:
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Created Date: 2010-08-23 Completed Date: 2011-02-02 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 100965718 Medline TA: Curr Opin Investig Drugs Country: England |
Other Details:
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Languages: eng Pagination: 1066-73 Citation Subset: IM |
Affiliation:
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Harefield Hospital, Department of Cardiothoracic Surgery, Royal Brompton & Harefield NHS Trust, Hill End Road, Harefield, London, UB9 6JH, UK. drrajashahzad@hotmail.com |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Oral Animals Cardiovascular Diseases / drug therapy Clinical Trials as Topic Dogs Drug Evaluation, Preclinical Humans Hypertension, Pulmonary / drug therapy Idiopathic Pulmonary Fibrosis / drug therapy* Male Pyrimidines / administration & dosage, adverse effects, pharmacokinetics, therapeutic use* Rats Receptors, Endothelin / antagonists & inhibitors*, metabolism Sulfonamides / administration & dosage, adverse effects, pharmacokinetics, therapeutic use* |
| Chemical | |
Reg. No./Substance:
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0/N-(5-(4-bromophenyl)-6-(2-(5-bromopyrimidin-2-yloxy)ethoxy)pyrimidin-4-yl)-N'-propylaminosulfonamide; 0/Pyrimidines; 0/Receptors, Endothelin; 0/Sulfonamides |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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