[PDF][PDF] ARV-110: An oral androgen receptor PROTAC degrader for prostate cancer

…, RR Willard, N Vitale, J Pizzano… - J. Clin …, 2019 - s3.us-east-1.amazonaws.com
Background: The Androgen Receptor (AR) remains the principal driver of castrationresistant
prostate cancer during the transition from a localized to metastatic disease. Most patients …

Abstract P5-04-18: ARV-471, an oral estrogen receptor PROTAC degrader for breast cancer

…, J Bradley, E Rousseau, R Willard, J Pizzano… - Cancer research, 2019 - AACR
ARV-471, an estrogen receptor (ER) alpha PROTAC, is a hetero-bifunctional molecule that
facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase …

[HTML][HTML] Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers

…, M Grimmer, F Broccatelli, J Wang, J Pizzano… - Nature …, 2022 - nature.com
The mammalian SWItch/Sucrose Non-Fermentable (SWI/SNF) helicase SMARCA4 is
frequently mutated in cancer and inactivation results in a cellular dependence on its paralog, …

[PDF][PDF] Discovery of ARV-110, a first in class androgen receptor degrading PROTAC for the treatment of men with metastatic castration resistant prostate cancer

…, J Macaluso, J Pizzano, J Wang… - Cancer …, 2021 - s3.us-east-1.amazonaws.com
This presentation contains forward-looking statements within the meaning of The Private
Securities Litigation Reform Act of 1995 that involve substantial risks and uncertainties, …

ARV-110: An androgen receptor PROTAC degrader for prostate cancer

…, J Pizzano, D Gordon, M Bookbinder, J Macaluso… - Cancer research, 2018 - AACR
The Androgen Receptor (AR) remains the principal driver of castration-resistant prostate
cancer during the transition from a localized to metastatic disease. Most patients initially …

Evaluation of cynomolgus monkey pregnane X receptor, primary hepatocyte, and in vivo pharmacokinetic changes in predicting human CYP3A4 induction

…, J Simmermacher, HA Dulac, J Pizzano… - Drug metabolism and …, 2010 - ASPET
Monkeys have been proposed as an animal model to predict the magnitude of human clinical
drug-drug interactions caused by CYP3A4 enzyme induction. To evaluate whether the …

PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models

…, M Merchant, I Pérez-Dorado, J Pizzano… - Journal of Medicinal …, 2024 - ACS Publications
The identification of VHL-binding proteolysis targeting chimeras (PROTACs) that potently
degrade the BRM protein (also known as SMARCA2) in SW1573 cell-based experiments is …

[HTML][HTML] Development of Liposome Systems for Enhancing the PK Properties of Bivalent PROTACs

…, Y Cui, X Zhang, F Broccatelli, J Pizzano, J Cantley… - Pharmaceutics, 2023 - mdpi.com
Proteolysis-Targeting Chimeras (PROTACs) are a promising new technology in drug development.
They have rapidly evolved in recent years, with several of them in clinical trials. While …

An oral androgen receptor PROTAC degrader for prostate cancer.

…, J Pizzano, DA Gordon, M Bookbinder, J Macaluso… - 2018 - ascopubs.org
381 Background: The Androgen Receptor (AR) remains the principal driver of castration-resistant
prostate cancer during the transition from a localized to metastatic disease. Most …

Abstract ND03: Discovery of ARV-766, an androgen receptor degrading PROTAC® for the treatment of men with metastatic castration resistant prostate cancer

…, C Ferraro, DA Gordon, J Macaluso, J Pizzano, J Wang… - Cancer Research, 2023 - AACR
Prostate cancer is the second leading cause of cancer death in men in the United States.
The androgen receptor (AR) plays critical roles in both early disease and advanced prostate …