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Phase I Study of ARN-509, a Novel Antiandrogen, in the Treatment of Castration-Resistant Prostate Cancer
Author(s) -
Dana E. Rathkopf,
Michael J. Morris,
Josef J. Fox,
Daniel C. Danila,
Susan F. Slovin,
Jeffrey H. Hager,
Peter J. Rix,
Edna Chow Maneval,
Isan Chen,
Mithat Gönen,
Martin Fleisher,
Steven M. Larson,
Charles L. Sawyers,
Howard I. Scher
Publication year - 2013
Publication title -
journal of clinical oncology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 10.482
H-Index - 548
eISSN - 1527-7755
pISSN - 0732-183X
DOI - 10.1200/jco.2013.50.1684
Subject(s) - medicine , tolerability , pharmacokinetics , prostate cancer , pharmacodynamics , antiandrogen , adverse effect , bicalutamide , urology , pharmacology , androgen receptor , context (archaeology) , androgen deprivation therapy , cancer , paleontology , biology
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.

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