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European Heart Journal Advance Access published online on June 17, 2008
European Heart Journal, doi:10.1093/eurheartj/ehn234
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Published on behalf of the European Society of Cardiology. All rights reserved. © The Author 2008. For permissions please email: journals.permissions@oxfordjournals.org
The online version of this article has been published under an open access model. Users are entitled to use, reproduce, disseminate, or display the open access version of this article for non-commercial purposes provided that the original authorship is properly and fully attributed; the Journal, Learned Society and Oxford University Press are attributed as the original place of publication with correct citation details given; if an article is subsequently reproduced or disseminated not in its entirety but only in part or as a derivative work this must be clearly indicated. For commercial re-use, please contact journals.permissions@oxfordjournals.org.

Inhibition of endothelin receptors in the treatment of pulmonary arterial hypertension: does selectivity matter?

Christian F. Opitz1,*, Ralf Ewert2, Wilhelm Kirch3 and David Pittrow3

1 Department of Internal Medicine, DRK-Kliniken Berlin, Köpenick, Berlin, Germany
2 Department of Internal Medicine B, Ernst-Moritz-Arndt University Greifswald, Greifswald, Germany
3 Institute for Clinical Pharmacology, Medical Faculty Carl Gustav Carus, Technical University, Dresden, Germany

Received 19 November 2007; revised 7 May 2008; accepted 15 May 2008.

* Corresponding author: Tel: +49 30 303 54305, Fax: +49 30 30 354 309, Email: c.opitz{at}drk-kliniken-berlin.de

Treatment options for pulmonary arterial hypertension (PAH) have considerably improved in the past few years. Endothelin (ET)-receptor antagonism has been established as a first-line option for the majority of PAH patients. Endothelin-receptor antagonists (ETRAs) comprise sulfonamide and non-sulfonamide agents with different affinities for ET-receptor subtypes (ETA and ETB), and the focus of development has shifted from drugs with less selectivity to those with high selectivity. There is ongoing debate as to whether selective or non-selective ET-receptor antagonism is more beneficial in the treatment of PAH. This paper reviews the current evidence from experimental and clinical studies obtained from a thorough literature search focusing on the three marketed drugs bosentan, sitaxentan, and ambrisentan. A clinically meaningful difference among the three approved ETRAs with respect to their ET-receptor selectivity could not be demonstrated to date. Therefore, in clinical practice, other features are likely to be of greater relevance when considering treatment, such as the potential for serious drug–drug interactions, convenience of dosing schedule, or rates of limiting side effects. These characteristics bear more relation to the chemical or pharmacological properties of the drugs than to receptor selectivity itself.

Key Words: Endothelin • Receptor selectivity • Pulmonary arterial hypertension • ETA/ETB • ETRA • ET-1 • Bosentan • Sitaxentan • Ambrisentan


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