Ambrisentan for the Treatment of Pulmonary Arterial ... | 合法藥品大搜索

由NGaliè著作·2008·被引用1065次—Ambrisentanisanonsulfonamide,propanoicacid–based,A-selectiveendothelinreceptorantagonistwithabioavailabilityandhalf-lifethatallowonce-dailydosing​ ...

Pulmonary arterial hypertension (PAH) is a progressive disease characterized by an elevated pulmonary vascular resistance leading to right ventricular failure and premature death.1 Current therapies approved for the treatment of PAH in the United States and/or Europe include prostacyclin analogues administered by intravenous, inhaled, and subcutaneous routes; the oral endothelin-receptor antagonists bosentan and sitaxsentan; and the oral phosphodiesterase type 5 inhibitor sildenafil. Although these agents are efficacious, each has safety-, tolerability-, or drug delivery–related adverse effects.2–6[1]

Clinical Perspective p 3019

Endothelin-1 is a 21–amino acid peptide that plays a key role in the pathobiology of PAH,7,8 exerting vasoconstrictor and mitogenic effects by binding to 2 distinct receptor isoforms in the pulmonary vascular smooth muscle cells, endothelin A and B receptors.9 Endothelin B receptors also are present in endothelial cells, and their activation lead...