Endothelin Receptors As Therapeutic Targets In Castration-Resistant Prostate Cancer

New, effective therapies for castration-resistant prostate cancer are needed to treat this lethal form of the disease. Through an understanding of the biology of endothelin-1 and the endothelin receptors (the endothelin axis) in prostate cancer, this axis has emerged as a promising target for therapeutic intervention. Clinical trials of potent, selective, or specific endothelin receptor A subtype (ETA) antagonists have demonstrated clinical activity, but such agents have not yet been approved for the treatment of prostate cancer. These generally well-tolerated, oral agents are ideal for chronic administration. This chapter will discuss the biology of the endothelin axis, several of the preclinical observations supporting the therapeutic rationale, and some of the available clinical trial data on this promising new approach.