Ambrisentan Chemical formula
Synonyms: Ambrisentán; Ambrisentanum; BSF-208075; LU-208075. (+)(2S)-2-[(4,6-Dimethylpyrimidin-2yl)oxy]-3-methoxy-3,3-diphenylpropanoic acid.
Cyrillic synonym: Амбризентан.

💊 Chemical information

Chemical formula: C22H22N2O4 = 378.4.
CAS — 177036-94-1.
ATC — C02KX02.
ATC Vet — QC02KX02.

💊 Adverse Effects and Precautions

As for Bosentan.

💊 Interactions

Ambrisentan is a substrate for a number of enzymes and transporters and interactions could potentially occur with inducers or inhibitors of the cytochrome P450 isoenzymes CYP3A4 and CYP2C19, P-glycoprotein, uridine diphosphate glucuronosyltransferases, and organic anion transporting polypeptide (OATP).

💊 Pharmacokinetics

Ambrisentan is rapidly absorbed from the gastrointestinal tract and peak plasma concentrations occur about 2 hours after oral doses. It is about 99% bound to plasma proteins. Ambrisentan is excreted mainly by the liver, although the relative contribution of hepatic metabolism and biliary excretion is not known. The terminal elimination half-life is about 15 hours.

💊 Uses and Administration

Ambrisentan is an endothelin receptor antagonist with similar actions to bosentan, although it has a higher selectivity for the endothelin ETA-receptor. It is used in the management of pulmonary hypertension functional class II or III. It is given orally in an initial dose of 5 mg once daily; the dose may be increased to 10 mg once daily if tolerated.
1. Galié N, et al. Ambrisentan therapy for pulmonary arterial hypertension. J Am Coll Cardiol 2005; 46: 529–35
2. Vatter H, Seifert V. Ambrisentan, a non-peptide endothelin receptor antagonist. Cardiovasc Drug Rev 2006; 24: 63–76
3. Barst RJ. A review of pulmonary arterial hypertension: role of ambrisentan. Vasc Health Risk Manag 2007; 3: 11–22
4. Anonymous. Ambrisentan (Letairis) for pulmonary arterial hypertension. Med Lett Drugs Ther 2007; 49: 87–8.

💊 Preparations

Proprietary Preparations

UK: Volibris; USA: Letairis.
Published November 11, 2018.