Scientific Literature & Abstracts

2017

  • Chi K, et. al. Efficacy, safety, tolerability, and pharmacokinetics of EPI-506 (ralaniten acetate), a novel androgen receptor (AR) N-terminal domain (NTD) inhibitor, in men with metastatic castration-resistant prostate cancer (mCRPC) progressing after enzalutamide and/or abiraterone. ASCO Annual Meeting 2017 (Abstract# 5032). Read More > ASCO Poster >

2016

  • Antonarakis, et. al. Targeting the N-terminal Domain of the Androgen Receptor: A New Approach for the Treatment of Advanced Prostate Cancer. The Oncologist 2016. Read More >
  • Banuelos CA, et. al. Sintokamide A is a novel antagonist of androgen receptor that uniquely binds activation function-1 in its amino-terminal domain. JBC 2016. Read More >
  • Imamura Y, et. al. An imaging agent to detect androgen receptor and its active splice variants in prostate cancer. JCI Insight 2016. Read More >
  • Imamura Y, Sadar MD. Androgen receptor targeted therapies in castration-resistant prostate cancer: Bench to clinic. International Journal of Urology 2016. Read More >
  • De Mol E, et. al. EPI-001, a compound active against castration-resistant prostate cancer, targets transactivation unit 5 of the androgen receptor. ACS Chem Biol 2016. Read More >
  • Chi K, et. al. Analysis of AR-driven resistance mechanisms in a phase 1/2 study of EPI-506, a novel AR N-terminal domain inhibitor, in men with metastatic castration-resistant prostate cancer (mCRPC) with progression after enzalutamide or abiraterone. ASCO Annual Meeting 2016 (Abstract# TPS5030). Read More >
  • Yang YC, et. al. Targeting androgen receptor activation function-1 with EPI to overcome resistance mechanisms in castration-resistant prostate cancer. Clin Cancer Res 2016. Read More >

2015

  • Kato M, et. al. Co-targeting Androgen Receptor Splice Variants and mTOR signaling pathway for the Treatment of Castration-Resistant Prostate Cancer. Clin Cancer Res 2015. Read More >
  • Montgomery RB, et. al. A phase 1/2 open-label study of safety and antitumor activity of EPI-506, a novel AR N-terminal domain inhibitor, in men with metastatic castration-resistant prostate cancer (mCRPC) with progression after enzalutamide or abiraterone. ASCO Annual Meeting 2015. J Clin Oncol 33, 2015 (suppl; abstr TPS5072). Read More >

2014

  • Martin SK, et. al. N-terminal targeting of androgen receptor variant enhances response of castration resistant prostate cancer to taxane chemotherapy. Mol Oncol 2014. Read More >
  • Banuelos, CA, et. al. Characterization of niphatenones that inhibit androgen receptor N-terminal domain. PLoS One 2014. Read More >

2013

  • Myung JK, et. al. An androgen receptor N-terminal domain antagonist for treating prostate cancer. J Clin Invest 2013. Read More >
  • Yang YC, et. al. Spongian diterpenoids inhibit androgen receptor activity. Mol Cancer Ther 2013. Read More >

2012

  • Sadar MD. Advances in small molecule inhibitors of androgen receptor for the treatment of advanced prostate cancer. World J Urol 2012. Read More >
  • Meimetis LG, et. al. Niphatenones, glycerol ethers from the sponge Niphates digitalis block androgen receptor
    transcriptional activity in prostate cancer cells: structure elucidation, synthesis, and biological activity. J Med Chem 2012. Read More >

2011

  • Sadar MD. Small molecule inhibitors targeting the “Achilles’ heel” of androgen receptor activity. Cancer Res 2011. Read More >

2010

  • Andersen RJ, et. al. Regression of castrate-recurrent prostate cancer by a small molecule inhibitor of the amino-terminus domain of the androgen receptor. Cancer Cell 2010. Read More >