Phase I study of ARN-509, a novel antiandrogen, in the treatment of castration-resistant prostate cancer.

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.

Patients and methods

Thirty patients with progressive CRPC received continuous daily oral ARN-509 at doses between 30 and 480 mg, preceded by administration of a single dose followed by a 1-week observation period with pharmacokinetic sampling. Positron emission tomography/computed tomography imaging was co

SUBMITTER: Rathkopf DE 

PROVIDER: S-EPMC3782148 | biostudies-literature | 2013 Oct

REPOSITORIES: biostudies-literature