Science

Publications

2023

  • . Phase 1/2 Trial of Oral EPI-7386 (masofaniten) in Combination with Enzalutamide (Enz) Compared with Enz Alone in Subjects with Metastatic Castration-Resistant Prostate Cancer (mCRPC): Current Phase 1 (P1) results.

    PCF 2023 Poster Presentation

  • . Phase 1/2 Trial of Oral EPI-7386 (masofaniten) in Combination with Enzalutamide (Enz) Compared with Enz Alone in Subjects with Metastatic Castration-Resistant Prostate Cancer (mCRPC): Current Phase 1 (P1) results. ESMO Virtual Congress 2023.

    ESMO 2023 Poster Presentation

  • Lacetti, Andrew et al. Phase 1/2 Trial of Oral EPI-7386 in Combination with Enzalutamide (Enz) Compared with Enz Alone in Subjects with Metastatic Castration-Resistant Prostate Cancer (mCRPC): Preliminary Results from the Phase 1 (P1) Dose-optimization Component of the Study. 2023 American Society of Clinical Oncology Genitourinary (ASCO GU) Symposium.

    ASCO GU 2023 Poster Presentation

  • Pachynski, Russel et al. A Phase 1 Trial of Oral EPI-7386 in Patients with Metastatic Castration-Resistant Prostate Cancer (mCRPC): Update From the First-in-Human Study. 2023 American Society of Clinical Oncology Genitourinary (ASCO GU) Cancers Symposium.

    ASCO GU 2023 Poster Presentation

2022

  • Hong, NH. et al. Advances in the Development of a Targeted N-Terminal Domain Androgen Receptor Degrader (ANITAC) for the Treatment of Prostate Cancer. 34th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics.

    EORTC-NCI-AACR 2022 Poster Presentation

  • Hong, NH. et al. Advances in the Development of a Targeted N-Terminal Domain Androgen Receptor Degrader (ANITAC) for the Treatment of Prostate Cancer. Prostate Cancer Foundation (PCF) 2022 Scientific Retreat.

    PCF 2022 Poster Presentation

  • Laccetti, A. et al. Phase 1/2 Study of EPI-7386 in Combination with Enzalutamide (Enz) Compared with Enz Alone in Subjects with Metastatic Castration-Resistant Prostate Cancer (mCRPC): Preliminary Results from the Phase 1 (P1) Dose-optimization Component of the Study. Prostate Cancer Foundation (PCF) 2022 Scientific Retreat.

    PCF 2022 Poster Presentation

  • Laccetti, A. et al. Oral EPI-7386 in Patients with Metastatic Castration-Resistant Prostate Cancer: Results From the First-in-Human Dose Escalation Phase 1a Study. Prostate Cancer Foundation (PCF) 2022 Scientific Retreat.

    PCF 2022 Poster Presentation

  • Hong, NH. et al. Androgen receptor (AR) N-Terminal Domain degraders can degrade AR full length and AR splice variants in CRPC preclinical models. 2022 American Association for Cancer Research (AACR) Annual Meeting.

    AACR 2022 Poster Presentation

2021

  • Hong, NH. et al. Comprehensive preclinical characterization of the mechanism of action of EPI-7386, an androgen receptor N-terminal domain inhibitor. 2021 Prostate Cancer Foundation (PCF) Annual Scientific Retreat.

    PCF 2021 Poster Presentation

  • Hong, NH. et al. Comprehensive preclinical characterization of the mechanism of action of EPI-7386, an androgen receptor N-terminal domain inhibitor. 2021 AACR-NCI-EORTC Virtual International Conference on Molecular Targets and Cancer Therapeutics. (Abstract: P192).

    AACR-NCI-EORTC 2021 Poster Presentation

  • . Comprehensive in vitro characterization of the mechanism of action of EPI-7386, an androgen receptor N-terminal inhibitor. 2021 AACR. (Abstract Number: 1209).

    AACR 2021 Poster Presentation

  • . Preclinical and clinical pharmacology of EPI-7386, an androgen receptor N-terminal domain inhibitor for castration-resistant prostate cancer. ASCO GU 2021. (Abstract Number: 119).

    ASCO-GU Poster Presentation

2020

  • . The preclinical characterization of the N-terminal domain androgen receptor inhibitor, EPI-7386, for the treatment of prostate cancer. ENA 2020 – 32nd Symposium. (EORTC-NCI-AACR) (Abstract ID #181).

    EORTC-NCI-AACR 32nd Symposium Poster

  • . EPI-7386, a potent N-terminal domain androgen receptor inhibitor, with a favorable preclinical safety and superior in vitro/in vivo profile, in clinical development for prostate cancer. Prostate Cancer Foundation 27th Annual Scientific Retreat.

    Prostate Cancer Foundation 27th Annual Scientific Retreat Poster

  • . Pre-clinical profile of EPI-7386, a second-generation N-terminal domain androgen receptor inhibitor for the treatment of prostate cancer. ESMO Virtual Congress 2020. (Poster ID #11P).

    ESMO Virtual Congress 2020 Poster

  • . Pre-clinical development of the second-generation N-terminal domain androgen receptor inhibitor, EPI-7386, for the treatment of prostate cancer. American Association for Cancer Research Virtual Annual Meeting II 2020. (Abstract ID #1953).

    2020 AACR Virtual Annual Meeting II Poster

  • . The preclinical characterization and development of EPI-7386, an N-terminal domain androgen receptor inhibitor for the treatment of prostate cancer. [Poster Session]. American Urology Association Annual Conference, Washington, DC, United States.

    2020 American Urology Association Annual Conference Poster

  • . IND Candidate EPI-7386 as an N-terminal Domain Androgen Receptor Inhibitor in Development for the Treatment of Prostate Cancer. American Society of Clinical Oncology Genitourinary Cancers Symposium 2020. (Abstract ID #142).

    2020 Genitourinary Cancers Symposium Poster

2019

  • . Treatment of castrated resistant prostate cancer, with EPI-7386, a second generation N-terminal domain androgen receptor inhibitor. AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics. (Abstract ID B117).

    AACR-NCI-EORTC Poster

  • . Treatment of castrated resistant prostate cancer, with EPI-7386, a second generation N-terminal domain androgen receptor inhibitor. The 26th Annual Scientific Retreat | Prostate Cancer Foundation.

    Prostate Cancer Foundation Annual Retreat Poster

  • . EPI-7386 is a novel N-terminal domain androgen receptor inhibitor for the treatment of prostate cancer. European Society of Medical Oncology (ESMO) 2019 Congress. (Abstract ID 503P).

    European Society of Medical Oncology 2019 Congress Poster

  • . Next generation N-terminal domain androgen receptor inhibitor with improved potency and metabolic stability in castration-resistant poster cancers models. Genitourinary Cancers Symposium 2019. (Abstract# MP34-04).

    American Urological Association Poster

  • . Next generation N-terminal domain androgen receptor inhibitor with improved potency and metabolic stability in castration-resistant poster cancers models. Genitourinary Cancers Symposium 2016. (Abstract# 220).

    American Association for Cancer Research Poster

  • . Next generation N-terminal domain androgen receptor inhibitor with improved potency and metabolic stability in castration-resistant poster cancers models. Genitourinary Cancers Symposium 2019. (Abstract# 220).

    Genitouronary Cancers Symposium Poster

  • . Lessons Learned from the metastatic castration-resistant phase 1 of EPI-506, a first-generation androgen receptor N-terminal domain inhibitor. Genitourinary Cancers Symposium 2019. (Abstract# 257).

    Genitouronary Cancers Symposium Poster

2017

  • . 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).

    ASCO Poster

2016

  • . Targeting the N-terminal Domain of the Androgen Receptor: A New Approach for the Treatment of Advanced Prostate Cancer. The Oncologist 2016

  • . Sintokamide A is a novel antagonist of androgen receptor that uniquely binds activation function-1 in its amino-terminal domain. JBC 2016

  • . An imaging agent to detect androgen receptor and its active splice variants in prostate cancer. JCI Insight 2016

  • . Androgen receptor targeted therapies in castration-resistant prostate cancer: Bench to clinic. International Journal of Urology 2016

  • . EPI-001, a compound active against castration-resistant prostate cancer, targets transactivation unit 5 of the androgen receptor. ACS Chem Biol 2016

  • . 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).

  • . Targeting androgen receptor activation function-1 with EPI to overcome resistance mechanisms in castration-resistant prostate cancer. Clin Cancer Res 2016

2015

  • . Co-targeting Androgen Receptor Splice Variants and mTOR signaling pathway for the Treatment of Castration-Resistant Prostate Cancer. Clin Cancer Res 2015

  • . 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 2016. J Clin Oncol 33, 2015 (suppl; abstr TPS5072)

2014

  • . N-terminal targeting of androgen receptor variant enhances response of castration resistant prostate cancer to taxane chemotherapy. Mol Oncol 2014

  • . Characterization of niphatenones that inhibit androgen receptor N-terminal domain. PLoS One 2014

2013

  • . An androgen receptor N-terminal domain antagonist for treating prostate cancer. J Clin Invest 2013

  • . Spongian diterpenoids inhibit androgen receptor activity. Mol Cancer Ther 2013

2012

  • . Advances in small molecule inhibitors of androgen receptor for the treatment of advanced prostate cancer. World J Urol 2012

  • . 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

2011

  • . Small molecule inhibitors targeting the “Achilles’ heel” of androgen receptor activity. ancer Res 2011

2010

  • . Regression of castrate-recurrent prostate cancer by a small molecule inhibitor of the amino-terminus domain of the androgen receptor. Cancer Cell 2010