TA-0201

TA-0201 is an orally active, selective, small molecule endothelin A (ET(A)) receptor antagonist, structurally classified as a pyrimidine sulfonamide derivative. It displays extremely high affinity for the endothelin ET(A) receptor (pK(i)=10.7) relative to the endothelin ET(B) receptor (pK(i)=7.8). Preclinical studies demonstrated activity in models using human recombinant and prostate endothelin receptors, inhibiting contraction responses triggered by endothelin-1, which implicates potential utility in treating cardiovascular or prostate-related disorders as an anti-ischaemic agent or in heart failure. TA-0201 was developed by Tanabe Seiyaku in Japan and is a derivative of TA-0115. There are no reported approvals or late-stage clinical development for any indication.

Other names

N-(6-(2-(5-bromopyrimidine-2-yloxy)ethoxy)-5-(4-methylphenyl)pyrimidin-4-yl)-4-(2-hydroxy-1,1-dimethylethyl) benzensulfonamide sodium salt sesquihydrate