Bifunctional small molecules for protein degradation

Arvinas Inc. is at the forefront of biotechnology, specializing in the development of targeted protein degradation therapies through its proprietary PROTAC (PROteolysis-TArgeted Chimera) platform. This innovative approach leverages the body's natural ubiquitin-proteasome system to selectively degrade disease-causing proteins, which can lead to transformative treatments for serious conditions, particularly in oncology and neuroscience. The company is focused on creating a new class of medicines that can address previously "undruggable" targets, thereby expanding the possibilities of drug discovery and offering hope to patients with limited treatment options.

In the realm of neuroscience, Arvinas is pioneering the development of PROTACs that can penetrate the blood-brain barrier, targeting proteins implicated in neurodegenerative diseases such as Alzheimer's, Parkinson's, and Huntington's disease. Their research aims to create oral PROTACs that can effectively degrade pathogenic proteins within the central nervous system, potentially improving clinical outcomes for patients suffering from these debilitating conditions. By exploring differentiated pharmacology and the ability to selectively degrade harmful proteins while sparing healthy ones, Arvinas is positioning itself as a leader in the quest for innovative therapies that could significantly alter the treatment landscape for serious diseases.

United States

Arvinas is a clinical-stage biotechnology company dedicated to improving the lives of patients suffering from debilitating and life-threatening diseases through the discovery, development, and commercialization of therapies that degrade disease-causing proteins. Arvinas uses its PROTAC Discovery Engine to engineer proteolysis targeting chimeras, or PROTAC targeted protein degraders, that are designed to harness the body’s own natural protein disposal system to selectively and efficiently degrade and remove disease-causing proteins. Arvinas is currently progressing multiple investigational drugs through clinical development programs, including vepdegestrant, targeting estrogen receptor for patients with locally advanced or metastatic ER+/HER2- breast cancer; ARV-102, targeting LRRK2 for neurodegenerative disorders; and ARV-393, targeting BCL6 for relapsed/refractory non-Hodgkin Lymphoma.

Based in the biotech hub of New Haven, CT, Arvinas is driven by an industry-leading team dedicated to improving the lives of people living with serious diseases. For more information, visit www.arvinas.com. 

Community Guidelines: http://bit.ly/ArvinasCG

Cancer

Central Nervous System (CNS)

Genetic Diseases

Immune System Diseases

Lung Diseases

Arvinas Inc.

Breast cancer

Solid tumor/s

ARV-471 is an investigational orally bioavailable PROTAC® protein degrader designed to specifically target and degrade the estrogen receptor (ER) for the treatment of patients with locally advanced or metastatic ER+/HER2- breast cancer.
 
In preclinical studies, ARV-471 demonstrated near-complete ER degradation in tumor cells, induced robust tumor shrinkage when dosed as a single agent in multiple ER-driven xenograft models, and showed superior anti-tumor activity when compared to a standard of care agent, fulvestrant, both as a single agent and in combination with a CDK4/6 inhibitor.

Vepdegestrant (ARV-471) + Palbociclib

Vepdegestrant (Mono)

Vepdegestrant + Atirmociclib (1L)

Vepdegestrant (ARV-471)

Castration-resistant prostate cancer

Prostate cancer

ARV-766 is an investigational orally bioavailable PROTAC® protein degrader designed to selectively target and degrade AR. In preclinical studies, ARV-766 degraded all resistance-driving point mutations of AR, including L702H, a mutation associated with treatment with abiraterone and other AR-pathway therapies.
 
ARV-766 is being developed as a potential treatment for men with metastatic castration-resistant prostate cancer, and ARV-766 may also have applicability in other AR-driven diseases both in and outside oncology. ARV-766 has demonstrated activity in preclinical models of resistance to currently available AR-targeted therapies.

ARV-766 +/- Abiraterone 

ARV-110 is an investigational orally bioavailable PROTAC® protein degrader designed to selectively target and degrade the androgen receptor (AR). ARV-110 is being developed as a potential treatment for men with metastatic castration-resistant prostate cancer.
 
ARV-110 has demonstrated activity in preclinical models of AR mutation or overexpression, both common mechanisms of resistance to currently available AR-targeted therapies.

Bavdegalutamide (ARV-110) +/- Aabiraterone  

Vepdegestrant (ARV-471)+CDK4 inhibitor

Neurodegenerative disease

Parkinson's disease

ARV-102 is an investigational oral PROTAC degrader uniquely designed to cross the blood-brain barrier and degrade the LRRK2 protein
 
In non-human primates, orally administered ARV-102 has been shown to reach deep-brain regions and degrade LRRK2 by nearly 90%. The Phase 1 clinical trial of ARV-102 is enrolling healthy volunteers at the Centre for Human Drug Research (CHDR) in Leiden, the Netherlands. The trial will evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of ARV-102, including the evaluation of LRRK2 degradation and exploratory LRRK2 pathway biomarkers.

Arvinas Inc.

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