[HTML][HTML] Phase I study of ARN-509, a novel antiandrogen, in the treatment of castration-resistant prostate cancer
Journal of clinical oncology, 2013•ncbi.nlm.nih.gov
Purpose ARN-509 is a novel androgen receptor (AR) antagonist for the treatment of
castration-resistant prostate cancer (CRPC). ARN-509 inhibits AR nuclear translocation and
AR binding to androgen response elements and, unlike bicalutamide, does not exhibit
agonist properties in the context of AR overexpression. This first-in-human phase I study
assessed safety, tolerability, pharmacokinetics, pharmacodynamics, and antitumor activity of
ARN-509 in men with metastatic CRPC.
castration-resistant prostate cancer (CRPC). ARN-509 inhibits AR nuclear translocation and
AR binding to androgen response elements and, unlike bicalutamide, does not exhibit
agonist properties in the context of AR overexpression. This first-in-human phase I study
assessed safety, tolerability, pharmacokinetics, pharmacodynamics, and antitumor activity of
ARN-509 in men with metastatic CRPC.
Abstract
Purpose
ARN-509 is a novel androgen receptor (AR) antagonist for the treatment of castration-resistant prostate cancer (CRPC). ARN-509 inhibits AR nuclear translocation and AR binding to androgen response elements and, unlike bicalutamide, does not exhibit agonist properties in the context of AR overexpression. This first-in-human phase I study assessed safety, tolerability, pharmacokinetics, pharmacodynamics, and antitumor activity of ARN-509 in men with metastatic CRPC.
ncbi.nlm.nih.gov