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Pharmacokinetic evaluation of ambrisentan.

Author(s): Buckley MS, Wicks LM, Staib RL, Kirejczyk AK, Varker AS, Gibson JJ, Feldman JP

Affiliation(s): Banner Good Samaritan Medical Center, Department of Pharmacy, 1111 E. McDowell Rd, Phoenix, AZ 85006, USA.

Publication date & source: 2011-03, Expert Opin Drug Metab Toxicol., 7(3):371-80. Epub 2011 Feb 8.

Publication type: Review

INTRODUCTION: Pulmonary arterial hypertension (PAH) is a life-threatening and progressive disease characterized by increasing pulmonary vascular resistance leading to right ventricular failure and premature death. Current therapies target three major pathways involving endothelin, prostacyclin and NO. Ambrisentan is an oral, once daily, selective endothelin receptor antagonist. AREAS COVERED: This review focuses on, and critically appraises, the clinical efficacy and safety of ambrisentan as well as its pharmacokinetic and pharmacodynamic properties. The article also gives an expert perspective on the role of ambrisentan in the management of PAH. EXPERT OPINION: Ambrisentan is an effective and safe treatment which is, in the authors' opinion, a valuable addition to the armamentarium against PAH. Ambrisentan offers a relative lack of drug interactions, once daily dosing and reassuring liver safety, offering safety and convenience advantages over bosentan. Presently, there is a lack of comparative studies between PDE5 inhibitors and endothelin receptor antagonists and a lack of data comparing bosentan with ambrisentan. This is hindering data-based conclusions regarding relative efficacy and further studies are needed to define the role of ambrisentan in the management of PAH.

Page last updated: 2011-12-09

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