SPL Set ID: e20ab2fe-bc9f-48a3-b15a-e4bc9532c2ac
1 drug(s) with this SPL Set ID
Ambrisentan is an endothelin receptor antagonist that is selective for the endothelin type-A (ET A ) receptor. The chemical name of ambrisentan is (+)-(2 S )-2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropanoic acid. It has a molecular formula of C 22 H 22 N 2 O 4 and a molecular weight of 378.42. It contains a single chiral center determined to be the ( S ) configuration and has the following structural formula: Figure 1 Ambrisentan Structural Formula Ambrisentan is a white to off-white, crystalline solid. It is a carboxylic acid with a pKa of 4.0. Ambrisentan is practically insoluble in water and in aqueous solutions at low pH. Solubility increases in aqueous solutions at higher pH. In the solid state ambrisentan is very stable, is not hygroscopic, and is not light sensitive. Ambrisentan tablets are available as 5 mg and 10 mg film-coated tablets for once daily oral administration. The tablets include the following inactive ingredients: croscarmellose sodium, lactose monohydrate, magnesium stearate and microcrystalline cellulose. The tablets are film-coated with a coating material containing FD&C Red #40 aluminum lake, polyethylene glycol, polyvinyl alcohol, talc, and titanium dioxide. Ambrisentan tablets, 5 mg tablets also contain FD&C Blue #2. Each square shaped, light pink ambrisentan tablet contains 5 mg of ambrisentan. Each oval shaped, dark pink ambrisentan tablet contains 10 mg of ambrisentan. Ambrisentan tablets are unscored. figure1