As a specific Endothelin A, zibotentan can binds to endothelin A receptor (ETA) with Ki of 13 nM.But zibotentan do not shows inihbition to endothelin B receptor (ETB). Zibotentan can block ET-1 induced EGFR transactivation and mitogenic activity in ovarian carcinoma cell lines HEY and OVCA 433 at the concentration of 1 uM.
In vivo
Administration of Zibotentan(10 mg/kg/day)can potently inhibits the growth of HEY ovarian carcinoma xenografts in mice by 69%.