Ambrisentan, also known as BSF-208075 and LU-208075, is a drug indicated for use in the treatment of pulmonary hypertension. Ambrisentan, which relaxes those muscles, is an endothelin receptor antagonist, and is selective for the type A endothelin receptor (ETA). Ambrisentan significantly improved exercise capacity (6-minute walk distance) compared with placebo in two double-blind, multicenter trials (ARIES-1 and ARIES-2). Ambrisentan was approved by the U.S. Food and Drug Administration (FDA) and European Medicines Agency, and designated an orphan drug, for the treatment of pulmonary hypertension.
Isolation, identification, characterization, synthesis and quality control strategy of new process-related impurities in ambrisentan; Feng, Wei-Dong; Zhuo, Song-Ming; Zhang, Fu-Li Journal of Pharmaceutical and Biomedical Analysis Volume 165 Pages 325-337 Journal; 2019
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Study on the synthesis of ambrisentan; Li, Xiao-gang; Yingyong Huagong; Volume 43; Issue 9; Pages 1675-1678; Journal; 2014
Process for preparation of Ambrisentan and intermediates thereof; Lin, Feng; Zhu, Xiaofeng; Chen, Jianli; Xu, Qiulong; Assignee Shanghai Institute of Pharmaceutical Industry, Peop. Rep. China; 2013; Patent Information; Nov 21, 2013; WO 2013170778 A1
Method for preparation of (S)-2-hydroxy-3-methoxy-3,3-diphenylpropanoic acid and ambrisentan via optical resolution of its racemate using commercially available (S)-(+)-1,2,3,4-tetrahydro-1-naphthylamine; Amagasa, Katsuaki; Oonami, Toshihiko; Assignee Toa Eiyo, Ltd., Japan, 2017; Patent Information; Jul 27, 2017; JP 2017128528 A
LC-MS/MS characterization of forced degradation products of ambrisentan: development and validation of a stability-indicating RP-HPLC method; Ramisetti, Nageswara Rao; Kuntamukkala, Ramakrishna; New Journal of Chemistry; Volume 38; Issue 7; Pages 3050-3061; Journal; 2014