zibotentan

Zibotentan is an orally available, highly selective antagonist of the endothelin A (ETA) receptor developed by AstraZeneca. It works by blocking the ETA receptor, thereby inhibiting endothelin-mediated mechanisms that promote tumor cell proliferation, survival, angiogenesis, migration, invasion, and metastasis. Originally investigated as an anti-cancer agent—particularly for hormone-resistant prostate cancer—it was also studied in other cancers such as breast cancer, ovarian cancer, colorectal cancer, and non-small cell lung cancer. Although it failed to show efficacy in a phase III trial for advanced prostate cancer and development for oncology indications was discontinued, zibotentan has more recently been investigated in combination with dapagliflozin for chronic kidney disease (CKD) with proteinuria/albuminuria. The combination demonstrated significant reductions in albuminuria compared to dapagliflozin alone and is progressing to phase III trials[1][2][3][4][5][6].

Other names

zibotentan