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Drug Evaluation

Ambrisentan for pulmonary arterial hypertension

    Lewis J Rubin

    University of California, San Diego School of Medicine, Pulomary Vascular Center and Division of Pulmonary and Critical Care Medicine, 9300 Campus Point Dr., La Jolla, CA 92037, USA.

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    Email the corresponding author at ljrubin@ucsd.edu

    ,
    Christopher Dufton

    Myogen, Inc., Westminster, Colorado, USA

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    &
    Michael J Gerber

    Myogen, Inc., Westminster, Colorado, USA

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    Published Online:24 Nov 2005https://doi.org/10.2217/14796678.1.4.425

    Abstract

    Endothelin receptor antagonists (ERAs) are an important class of agents used for the treatment of pulmonary arterial hypertension (PAH). Ambrisentan is an oral, once-daily, endothelin type-A receptor (ETA)-selective, propanoic acid class ERA under clinical investigation for the treatment of PAH. In a Phase II study, ambrisentan improved 6-minute walk distance, Borg dyspnea index, World Health Organization Functional Class, and hemodynamics. Ambrisentan was well tolerated and adverse events were not dose related, including a low incidence and severity of liver function test abnormalities. There are no relevant interactions between ambrisentan and cytochrome P450 isoenzymes (metabolism, induction or inhibition) that might alter the activity of P450-metabolized drugs. Potential benefits of ambrisentan include oral, once-daily dosing, ETA-receptor selectivity, and the decreased risks of liver toxicity and adverse drug–drug interactions compared with other ERAs.

    Papers of special note have been highlighted as either of interest (•) or of considerable interest (••) to readers.

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