Atrasentan: a rationally designed targeted therapy for cancer.
Endothelin axis deregulation triggers a series of events that ultimately activates proliferation, invasion, escape from programmed cell death, new vessel formation, abnormal osteogenesis and alteration of nociceptive stimuli. Atrasentan is a novel agent that effectively targets this pathway and is able to inhibit and/or reverse several of these events. Biologic and clinical activity in patients with prostate cancer have been demonstrated in a phase III, placebo-controlled setting by the suppression of markers of biochemical prostate cancer progression and a delay in time to disease progression. Atrasentan may represent a therapeutic option in the management of prostate and other cancers that is worthy of continued investigation.
Jimeno
Antonio
A
Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University, Baltimore, Maryland 21231-1000, USA. ajimeno1@jhmi.edu
Carducci
Michael
M
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000627:therapeutic use; D000077868:Atrasentan; D016503:Drug Delivery Systems; D015195:Drug Design; D019332:Endothelin-1 / Q000037:antagonists & inhibitors / Q000378:metabolism; D006801:Humans; D008297:Male; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D011759:Pyrrolidines / Q000008:administration & dosage* / Q000627:therapeutic use; D016032:Randomized Controlled Trials as Topic
D000970:Antineoplastic Agents; D019332:Endothelin-1; D011759:Pyrrolidines; D000077868:Atrasentan