ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM. 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. ARN-509 displayed dose-proportional pharmacokinetics, and demonstrated pharmacodynamic and antitumor activity across all dose levels tested. ARN-509 is currently in a Phase I clinical trial.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Phase I study of ARN-509, a novel antiandrogen, in the treatment of castration-resistant prostate cancer.
Rathkopf DE, et al. J Clin Oncol. 2013 Oct 1;31(28):3525-30. PMID: 24002508.
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