nebentan potassium

Nebentan potassium (YM598) is an orally active synthetic substituted phenylethenesulfonamide that acts as a highly potent and selective antagonist of the endothelin A (ETA) receptor. By selectively blocking ETA receptors, YM598 inhibits endothelin-mediated mechanisms involved in tumor cell growth and progression, angiogenesis, metastasis, and has demonstrated efficacy in models of pulmonary arterial hypertension and renal protection. It exhibits a high selectivity for ETA over ETB receptors with a selectivity ratio of 222. In preclinical studies, it showed superior antagonistic activity compared to bosentan and comparable oral bioavailability to atrasentan. The drug was investigated primarily for the treatment of castration-resistant prostate cancer but development was discontinued after phase 2 trials[1][3][5][6][7].

Other names

nebentan potassium