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Science 324 (5928): 787-790

Copyright © 2009 by the American Association for the Advancement of Science

Development of a Second-Generation Antiandrogen for Treatment of Advanced Prostate Cancer

Chris Tran,1,* Samedy Ouk,5,* Nicola J. Clegg,1 Yu Chen,1,3 Philip A. Watson,1 Vivek Arora,1 John Wongvipat,1 Peter M. Smith-Jones,2 Dongwon Yoo,5 Andrew Kwon,1 Teresa Wasielewska,1 Derek Welsbie,6 Charlie Degui Chen,6,{dagger} Celestia S. Higano,7 Tomasz M. Beer,8 David T. Hung,9 Howard I. Scher,3 Michael E. Jung,5,{ddagger} Charles L. Sawyers1,4,{ddagger}

Abstract: Metastatic prostate cancer is treated with drugs that antagonize androgen action, but most patients progress to a more aggressive form of the disease called castration-resistant prostate cancer, driven by elevated expression of the androgen receptor. Here we characterize the diarylthiohydantoins RD162 and MDV3100, two compounds optimized from a screen for nonsteroidal antiandrogens that retain activity in the setting of increased androgen receptor expression. Both compounds bind to the androgen receptor with greater relative affinity than the clinically used antiandrogen bicalutamide, reduce the efficiency of its nuclear translocation, and impair both DNA binding to androgen response elements and recruitment of coactivators. RD162 and MDV3100 are orally available and induce tumor regression in mouse models of castration-resistant human prostate cancer. Of the first 30 patients treated with MDV3100 in a Phase I/II clinical trial, 13 of 30 (43%) showed sustained declines (by >50%) in serum concentrations of prostate-specific antigen, a biomarker of prostate cancer. These compounds thus appear to be promising candidates for treatment of advanced prostate cancer.

1 Human Oncology and Pathogenesis Program, Memorial Sloan-Kettering Cancer Center, New York, NY 10065, USA.
2 Department of Radiology, Memorial Sloan-Kettering Cancer Center, New York, NY 10065, USA.
3 Genitourinary Oncology Service, Division of Solid Tumor Oncology and Sidney Kimmel Center for Prostate and Urologic Cancers, Memorial Sloan-Kettering Cancer Center, New York, NY 10065, USA.
4 Howard Hughes Medical Institute, Memorial Sloan-Kettering Cancer Center, New York, NY 10065, USA.
5 Department of Chemistry and Biochemistry, University of California Los Angeles, Los Angeles, CA 90095, USA.
6 Molecular Biology Institute, University of California Los Angeles, Los Angeles, CA 90095, USA.
7 Division of Oncology, Departments of Medicine and Urology, University of Washington, Fred Hutchinson Cancer Center, Seattle, WA 98109, USA.
8 OHSU Knight Cancer Institute, Oregon Health and Science University, Portland, OR 97239, USA.
9 Medivation, Inc., 201 Spear Street, San Francisco, CA 94105, USA.

* These authors contributed equally to this work.

{dagger} Present address: State Key Laboratory of Molecular Biology, Institute of Biochemistry and Cell Biology, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200031, China.

{ddagger} To whom correspondence should be addressed. E-mail: sawyersc{at}; jung{at}

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Identification of a Clinically Relevant Androgen-Dependent Gene Signature in Prostate Cancer.
H. V. Heemers, L. J. Schmidt, Z. Sun, K. M. Regan, S. K. Anderson, K. Duncan, D. Wang, S. Liu, K. V. Ballman, and D. J. Tindall (2011)
Cancer Res. 71, 1978-1988
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Systematic Analysis of MicroRNAs Targeting the Androgen Receptor in Prostate Cancer Cells.
P. Ostling, S.-K. Leivonen, A. Aakula, P. Kohonen, R. Makela, Z. Hagman, A. Edsjo, S. Kangaspeska, H. Edgren, D. Nicorici, et al. (2011)
Cancer Res. 71, 1956-1967
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Castration-Resistant Prostate Cancer: Targeted Therapies and Individualized Treatment.
R. Aggarwal and C. J. Ryan (2011)
Oncologist 16, 264-275
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Phase I Dose-Escalation Study of the Novel Antiandrogen BMS-641988 in Patients with Castration-Resistant Prostate Cancer.
D. Rathkopf, G. Liu, M. A. Carducci, M. A. Eisenberger, A. Anand, M. J. Morris, S. F. Slovin, Y. Sasaki, S. Takahashi, S. Ozono, et al. (2011)
Clin. Cancer Res. 17, 880-887
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Small Molecule Inhibitors as Probes for Estrogen and Androgen Receptor Action.
D. J. Shapiro, C. Mao, and M. T. Cherian (2011)
J. Biol. Chem. 286, 4043-4048
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An update on androgen deprivation therapy for prostate cancer.
N. Sharifi, J. L. Gulley, and W. L. Dahut (2010)
Endocr. Relat. Cancer 17, R305-R315
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Tubulin-Targeting Chemotherapy Impairs Androgen Receptor Activity in Prostate Cancer.
M.-L. Zhu, C. M. Horbinski, M. Garzotto, D. Z. Qian, T. M. Beer, and N. Kyprianou (2010)
Cancer Res. 70, 7992-8002
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Nuclear androgen receptor staining in bone metastases is related to a poor outcome in prostate cancer patients.
S. Crnalic, E. Hornberg, P. Wikstrom, U. H. Lerner, A. Tieva, O. Svensson, A. Widmark, and A. Bergh (2010)
Endocr. Relat. Cancer 17, 885-895
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