アンブリセンタン 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
効能
血圧降下薬, エンドセリンA受容体拮抗薬
商品名
ヴォリブリス (グラクソ・スミスクライン)
説明
Ambrisentan is a selective endothelin-A (ETA) receptor antagonist introduced for the oral treatment of patients with pulmonary arterial
hypertension (PAH), to improve exercise capacity and delay clinical worsening.
It is the third ET-receptor antagonist to be marketed for this indication behind
bosentan and sitaxsentan. PAH is a rare disease of the small pulmonary arteries
characterized by vascular proliferation and remodeling, resulting in a
progressive increase in pulmonary vascular resistance and pulmonary arterial
pressure, and ultimately, right ventricular failure and premature death. Early symptoms of PAH include gradual onset of shortness of breath, fatigue,
palpitation, edema, and fainting. Endothelin-1 (ET-1), a potent vasoconstrictor
and smooth muscle mitogen, is a key contributor to the acceleration of the
disease, and its effects are mediated through activation ofET
A and ET
B
receptors.
化学的特性
White to Off White Solid
使用
Nonpeptide endothelin ETA receptor antagonist. Antihypertensive
一般的な説明
Ambrisentan, (+)-(2S)-2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropanoic acid(Letairis), is a potent ETA selective endothelin antagonist that,is indicated, in the treatment of pulmonary arterial hypertension(PAH). PAH is a rare disease that if left untreated has ahigh mortality rate. In June of 2007, the FDA granted approvalof ambrisentan for once-daily treatment of PAH.Studies have shown that it improves a 6-minute walk by about30 to 60 m for patients receiving placebo.
アンブリセンタン 上流と下流の製品情報
原材料
準備製品