Our Science

OUR SCIENCE

Publications

This section includes publications related to Arvinas’ PROTAC science, discovery compounds, and clinical-stage assets. View our congress presentations here.

Discovery of oral PROTAC LRRK2 degraders as potential treatments for neurodegenerative disorders

Journal/Conference: Michael J. Fox Foundation 2024 Parkinson’s Disease Therapeutics Conference

Author: Angela Cacace, PhD

Date: October 17, 2024

New therapies on the horizon: Targeted protein degradation in neuroscience

Journal/Conference: Cell Chemical Biology

Author: James A. Gregory, Christopher M. Hickey, Juan Chavez, and Angela M. Cacace

September 19, 2024

Development of potent, orally bioavailable PROTAC® LRRK2 degrader molecules as potential disease modifying therapeutics for neurodegeneration

Journal/Conference: Biennial International LRRK2 Meeting

Author: Kaela Kelly, PhD

June 21, 2024

Development of potent, orally bioavailable, and highly selective LRRK2 PROTAC® degrader molecules as potential disease modifying therapeutics for Parkinson’s disease

Journal/Conference: International Congress of Parkinson’s Disease and Movement Disorders

Author: Jere Meredith Jr., Kaela Kelly, Val Guss, Adrianna DeSantis, Lida Kimmel, Sierra Soletsky, Dianne Bryce, Rashaun Wilson, John Corradi, Stefanie Keenan, Greg Cadelina, Jennifer Pizzano, Juan Chavez, Steve Sparks, Angela M. Cacace

March 8, 2024

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

Journal/Conference: J Med Chem

Author: Michael Berlin*, Jennifer Cantley, Mark Bookbinder, Elizabeth Bortolon, Fabio Broccatelli, Greg Cadelina, Emily W. Chan, Huifen Chen, Xin Chen, Yunxing Cheng, Tommy K. Cheung, Kim Davenport, Dean DiNicola, Debbie Gordon, Brian D. Hamman, Alicia Harbin, Roy Haskell, Mingtao He, Alison J. Hole, Thomas Januario, Philip S. Kerry, Stefan G. Koenig, Limei Li, Mark Merchant, Inmaculada Pérez-Dorado, Jennifer Pizzano, Connor Quinn, Christopher M. Rose, Emma Rousseau, Leofal Soto, Leanna R. Staben, Hongming Sun, Qingping Tian, Jing Wang, Weifeng Wang, Crystal S. Ye, Xiaofen Ye, Penghong Zhang, Yuhui Zhou, Robert Yauch and Peter S. Dragovich*

January 5, 2024

Co-Opting The E3 Ligase KLHDC2 For Targeted Protein Degradation By Small Molecules

Journal/Conference: Nature Structural & Molecular Biology

Author: Christopher M. Hickey, Katherine M. Digianantonio, Kurt Zimmermann, Alicia Harbin, Connor Quinn, Avani Patel, Peter Gareiss, Amanda Chapman, Bernadette Tiberi, Jennifer Dobrodziej, John Corradi, Angela M. Cacace, David R. Langley & Miklós Békés

January 4, 2024

Physicochemical Property Determinants Of Oral Absorption For PROTAC® Protein Degraders

Journal/Conference: Journal of Medicinal Chemistry

Author: Keith R. Hornberger and Erika M. V. Araujo

June 6, 2023

Small Molecule PROTAC® Hijacking And Structural Characterization Of An E3 Ligase, KLHDC2, For Targeted Protein Degradation

Journal/Conference: Cold Spring Harbor Ubiquitin Meeting

Author: Katie Digianantonio

April 25, 2023

The Arvinas PROTAC® Discovery Engine: PROTAC® Biophysical Characterization Fuels The Discovery Of Target And E3 Ligase Ligands For Optimized PROTAC® Degrader Molecules

Journal/Conference: American Chemical Society (ACS) Spring 2023

Author: Alicia Harbin

March 28, 2023

KRAS-Targeted PROTAC® Degraders Are Broadly Efficacious Against KRAS Dependent Tumor Models

Journal/Conference: Targeting RAS Conference (AACR Special Conference)

Author: Katie Smith

March 8, 2023

Structural Insights Into PROTAC®-Induced Proximity

Journal/Conference: New England Structural Biology Association (NESBA)

Author: Katie Digianantonio

January 25, 2023

PROTAC® Targeted Protein Degraders: The Past Is Prologue. Nature Reviews Drug Discovery

Journal/Conference: Nature Reviews Drug Discovery

Author: Miklós Békés, et al.

January 18, 2022

August 18, 2025

British Journal of Clinical Pharmacology

Effect of Vepdegestrant, a PROTAC Oestrogen Receptor Degrader, on Dabigatran and Rosuvastatin Pharmacokinetics in Healthy Participants

DZ Yang et al.

READ NOW

May 31, 2025

New England Journal of Medicine

Vepdegestrant, a PROTAC Estrogen Receptor Degrader, in Advanced Breast Cancer

M Campone et al.

READ NOW

May 6, 2025

Targeted Oncology

PROteolysis TArgeting Chimera (PROTAC) Estrogen Receptor Degraders for Treatment of Estrogen Receptor–Positive Advanced Breast Cancer

EP Hamilton et al.

READ NOW

December 13, 2024

Molecular Cancer Therapeutics

Preclinical Evaluation of Bavdegalutamide (ARV-110), a Novel PROteolysis TArgeting Chimera Androgen Receptor Degrader

LB Snyder et al.

READ NOW

November 20, 2024

International Journal of Clinical Oncology

Safety and Pharmacokinetics of Vepdegestrant in Japanese Patients with ER+ Advanced Breast Cancer: A Phase 1 Study

H Iwata et al.

READ NOW

November 5, 2024

Organic Process Research & Development

Development of a Commercial Manufacturing Process for Vepdegestrant, an Orally Bioavailable PROTAC Estrogen Receptor Degrader for the Treatment of Breast Cancer

S Avery et al.

READ NOW

September 19, 2024

Cell Chemical Biology

New Therapies on the Horizon: Targeted Protein Degradation in Neuroscience

JA Gregory et al.

READ NOW

July 29, 2024

Future Oncology

VERITAC-2: A Phase III Study of Vepdegestrant, a PROTAC ER Degrader, Versus Fulvestrant in ER+/ HER2- Advanced Breast Cancer

EP Hamilton et al.

READ NOW

May 31, 2024

Clinical Cancer Research

Oral Estrogen Receptor PROTAC® Vepdegestrant (ARV-471) is Highly Efficacious as Monotherapy and in Combination with CDK4/6 or P13K/mTOR Pathway Inhibitors in Preclinical ER+ Breast Cancer Models

SM Gough et al.

READ NOW
1 2