Cited by 2,292Prostate Cancer Treatment and ResearchHeterocyclic Compound Synthesis and BioactivityHormonal and reproductive studies

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Development of a second-generation antiandrogen for treatment of advanced prostate cancer.

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Tran, Chris, Ouk, Samedy, Clegg, Nicola J., Chen, Yu, Watson, Philip A., Arora, Vivek, Wongvipat, John, Smith-Jones, Peter M., Yoo, Dongwon, Kwon, Andrew, Wasielewska, Teresa, Welsbie, Derek, Chen, Charlie Degui, Higano, Celestia S., Beer, Tomasz M., Hung, David T., Scher, Howard I., Jung, Michael E., Sawyers, Charles L.·2009·Science

DOI 10.1126/science.1168175PMC PMC2981508

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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.

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Self-citation
Androgen Receptor Directed Therapies in Castration-Resistant Metastatic Prostate Cancer
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Authors: Tran, C., Ouk, S., Clegg, N. J., Chen, Y., Watson, P. A., Arora, V., Wongvipat, J., Smith-Jones, P. M., Yoo, D., Kwon, A., Wasielewska, T., Welsbie, D., Chen, C. D., Higano, C. S., Beer, T. M., Hung, D. T., Scher, H. I., Jung, M. E., & Sawyers, C. L.
Affiliations: Memorial Sloan Kettering Cancer Center (US)
University of California, Los Angeles (US)
University of Washington (US)
Oregon Health & Science University (US)
Medivation, Inc. (United States) (US)
Corresponding author: Tran, Chris
Ouk, Samedy
Chen, Charlie Degui
Jung, Michael E.
Sawyers, Charles L.
ORCID: Ouk, Samedy
Chen, Yu
Watson, Philip A.
Arora, Vivek
Yoo, Dongwon
Welsbie, Derek
Chen, Charlie Degui
Higano, Celestia S.
Beer, Tomasz M.
Scher, Howard I.
Jung, Michael E.
Sawyers, Charles L.
Venue: Science
Publisher: American Association for the Advancement of Science (AAAS)
Published: 2009-05-08
Volume: 324
Issue: 5928
Pages: 787-790
ISSN: 0036-8075 (ISSN-L)
1095-9203
DOI: 10.1126/science.1168175
PMC: PMC2981508
OpenAlex: W2119504728
Cited by: 2,292
References: 21
Citations by year: 2026: 58 · 2025: 91 · 2024: 110 · 2023: 141 · 2022: 139 · 2021: 150 · 2020: 152 · 2019: 131 · 2018: 146 · 2017: 145 · 2016: 157 · 2015: 134 · 2014: 163 · 2013: 163 · 2012: 160
FWCI: 116.20
Type: journal article
Language: en
Open access: bronze
doi.org
Locations: Science (publishedVersion)
PubMed (publishedVersion)
PubMed Central (acceptedVersion)
Funders: National Cancer Institute (P50CA092629)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Prostate Cancer Treatment and Research
Physical Sciences › Chemistry › Organic Chemistry › Heterocyclic Compound Synthesis and Bioactivity
Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Hormonal and reproductive studies
Keywords: castration-resistant prostate cancer, androgen receptor antagonists, enzalutamide, androgen receptor, bicalutamide, nonsteroidal antiandrogens, androgen receptor nuclear translocation, coactivator recruitment, prostate-specific antigen, oral anticancer drugs, drug development
MeSH terms: Androgen Antagonists, Anilides, Animals, Antineoplastic Agents, Benzamides, Biological Availability, Cell Nucleus, DNA, Drug Screening Assays, Antitumor, Humans, Male, Nitriles, Phenylthiohydantoin, Prostatic Neoplasms, Receptors, Androgen, Tosyl Compounds, Transcription, Genetic, Gene Expression Regulation, Neoplastic, Xenograft Model Antitumor Assays, Cell Line, Tumor, Cell Proliferation, Mice

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Development of a second-generation antiandrogen for treatment of advanced prostate cancer.

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