Thursday, August 1, 2013
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Androgen receptor mutations that convey resistance to
second-generation anti-androgen receptor compounds
Studies in cell culture and
in patient samples identified drug resistance mutations that could help guide
prostate cancer treatment. In cells, chronic exposure to the anti-androgen
receptor compounds Xtandi enzalutamide or ARN-509 resulted in the
acquisition of the F876L androgen receptor mutation. In cells with the F976L
mutation, the drugs acted as agonists, whereas in wild-type cells the drugs
acted as antagonists and inhibited cell proliferation. In circulating tumor
DNA obtained from patients' plasma, the mutation was identified after
treatment with ARN-509. Next steps include determining the frequency of the
mutation in patients receiving second-generation anti-androgen receptor
Xtandi enzalutamide is marketed by Astellas Pharma Inc. and Medivation Inc. for
castration-resistant prostate cancer. ARN-509 from Aragon Pharmaceuticals Inc.
is in Phase II testing.
Published online Aug. 1, 2013
Patent application filed;
licensing status undisclosed
Joseph, J.D. et al.
Cancer Discov.; published online June 18, 2013;
Contact: James D. Joseph, Aragon Pharmaceuticals Inc., San
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