The DOI matches its Crossref record; 6 of the 6 references it cites were found in a registry or an index.
ARN-509: A Novel Antiandrogen for Prostate Cancer Treatment
Open accessAbstract
Continued reliance on the androgen receptor (AR) is now understood as a core mechanism in castration-resistant prostate cancer (CRPC), the most advanced form of this disease. While established and novel AR pathway–targeting agents display clinical efficacy in metastatic CRPC, dose-limiting side effects remain problematic for all current agents. In this study, we report the discovery and development of ARN-509, a competitive AR inhibitor that is fully antagonistic to AR overexpression, a common and important feature of CRPC. ARN-509 was optimized for inhibition of AR transcriptional activity and prostate cancer cell proliferation, pharmacokinetics, and in vivo efficacy. In contrast to bicalutamide, ARN-509 lacked significant agonist activity in preclinical models of CRPC. Moreover, ARN-509 lacked inducing activity for AR nuclear localization or DNA binding. In a clinically valid murine xenograft model of human CRPC, ARN-509 showed greater efficacy than MDV3100. Maximal therapeutic response in this model was achieved at 30 mg/kg/d of ARN-509, whereas the same response required 100 mg/kg/d of MDV3100 and higher steady-state plasma concentrations. Thus, ARN-509 exhibits characteristics predicting a higher therapeutic index with a greater potential to reach maximally efficacious doses in man than current AR antagonists. Our findings offer preclinical proof of principle for ARN-509 as a promising therapeutic in both castration-sensitive and castration-resistant forms of prostate cancer. Cancer Res; 72(6); 1494–503. ©2012 AACR.
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Jemal, A., Siegel, R., Xu, J., & Ward, E. (2010) · CA: A Cancer Journal for Clinicians · doi:10.3322/caac.20073 · Cited by 12,596
Abiraterone and Increased Survival in Metastatic Prostate Cancer
de Bono, J. S., Logothetis, C. J., Molina, A., Fizazi, K., North, S., Chu, L., Chi, K. N., Jones, R. J., Goodman, O. B., Saad, F., et al. (2011) · New England Journal of Medicine · doi:10.1056/nejmoa1014618 · Cited by 4,407 · cited 2×
“9 months over control (prednisone only) in CRPC patients previously treated with docetaxel (8).”
Self-citationDevelopment of a second-generation antiandrogen for treatment of advanced prostate cancer.
Tran, C., Ouk, S., Clegg, N. J., Chen, Y., Watson, P. A., Arora, V., Wongvipat, J., Smith-Jones, P. M., Yoo, D., Kwon, A., et al. (2009) · Science · doi:10.1126/science.1168175 · Cited by 2,292
Self-citationMolecular determinants of resistance to antiandrogen therapy
Chen, C. D., Welsbie, D. S., Tran, C., Baek, S. H., Chen, R., Vessella, R., Rosenfeld, M. G., & Sawyers, C. L. (2004) · Nature Medicine · doi:10.1038/nm972 · Cited by 2,278
Self-citationScher, H. I., & Sawyers, C. L. (2005) · Journal of Clinical Oncology · doi:10.1200/jco.2005.03.4777 · Cited by 1,025
Self-citationReid, A. H. M., Attard, G., Danila, D. C., Oommen, N. B., Olmos, D., Fong, P. C., Molife, L. R., Hunt, J., Messiou, C., Parker, C., et al. (2010) · Journal of Clinical Oncology · doi:10.1200/jco.2009.24.6819 · Cited by 394
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Apalutamide for Metastatic, Castration-Sensitive Prostate Cancer
Chi, K. N., Agarwal, N., Bjartell, A., Chung, B. H., Pereira de Santana Gomes, A. J., Given, R., Juárez Soto, Á., Merseburger, A. S., Özgüroğlu, M., Uemura, H., et al. (2019) · New England Journal of Medicine · doi:10.1056/nejmoa1903307 · Cited by 1,564
Emerging mechanisms of resistance to androgen receptor inhibitors in prostate cancer
Watson, P. A., Arora, V. K., & Sawyers, C. L. (2015) · Nature Reviews Cancer · doi:10.1038/nrc4016 · Cited by 1,536
Self-citationApalutamide Treatment and Metastasis-free Survival in Prostate Cancer
Smith, M. R., Saad, F., Chowdhury, S., Oudard, S., Hadaschik, B. A., Graff, J. N., Olmos, D., Mainwaring, P. N., Lee, J. Y., Uemura, H., et al. (2018) · New England Journal of Medicine · doi:10.1056/nejmoa1715546 · Cited by 1,344
Korpal, M., Korn, J. M., Gao, X., Rakiec, D. P., Ruddy, D. A., Doshi, S., Yuan, J., Kovats, S. G., Kim, S., Cooke, V. G., et al. (2013) · Cancer Discovery · doi:10.1158/2159-8290.cd-13-0142 · Cited by 561
Role of Androgen Receptor in Prostate Cancer: A Review
Fujita, K., & Nonomura, N. (2019) · The World Journal of Men's Health · doi:10.5534/wjmh.180040 · Cited by 483
Metadata
- Authors
- Clegg, N. J., Wongvipat, J., Joseph, J. D., Tran, C., Ouk, S., Dilhas, A., Chen, Y., Grillot, K., Bischoff, E. D., Cai, L., Aparicio, A., Dorow, S., Arora, V., Shao, G., Qian, J., Zhao, H., Yang, G., Cao, C., Sensintaffar, J., Wasielewska, T., Herbert, M. R., Bonnefous, C., Darimont, B., Scher, H. I., Smith-Jones, P., Klang, M., Smith, N. D., De Stanchina, E., Wu, N., Ouerfelli, O., Rix, P. J., Heyman, R. A., Jung, M. E., Sawyers, C. L., & Hager, J. H.
- Venue
- Cancer Research
- Published
- 2012-03-14
- Volume
- 72
- Issue
- 6
- Pages
- 1494-1503
- ISSN
- 0008-5472 (ISSN-L)
- 1538-7445
- OpenAlex
- W2084637523
- Cited by
- 662
- References
- 6
- FWCI
- 45.53
- Type
- journal article
- Language
- en
- Open access
- green
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- Clegg, N. J., Wongvipat, J., Joseph, J. D., Tran, C., Ouk, S., Dilhas, A., Chen, Y., Grillot, K., Bischoff, E. D., Cai, L., Aparicio, A., Dorow, S., Arora, V., Shao, G., Qian, J., Zhao, H., Yang, G., Cao, C., Sensintaffar, J., . . . Hager, J. H. (2012). ARN-509: A Novel Antiandrogen for Prostate Cancer Treatment. Cancer Research. https://doi.org/10.1158/0008-5472.can-11-3948
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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