Arvinas Begins Human Trials for ARV-102, a PROTAC® Degrader Targeting Neurodegeneration

Arvinas Inc. has initiated its Phase 1 clinical trial of ARV-102, a novel oral PROTAC® protein degrader aimed at treating neurodegenerative diseases. ARV-102 has shown promise in preclinical studies, demonstrating its ability to breach the blood-brain barrier and degrade leucine-rich repeat kinase 2 (LRRK2), a protein linked to neurological disorders like Parkinson’s disease and progressive supranuclear palsy.

In tests on non-human primates, orally administered ARV-102 managed to penetrate deep-brain regions and reduce LRRK2 levels by almost 90%. The initial Phase 1 trial focuses on enrolling healthy volunteers to study the safety, tolerability, pharmacokinetics, and pharmacodynamics of ARV-102 at the Centre for Human Drug Research in Leiden, Netherlands.

Angela M. Cacace, Ph.D., Senior Vice President of Neuroscience and Platform Biology, emphasized the importance of this milestone for advancing treatments for neurodegenerative diseases. Unlike other therapeutics that merely inhibit LRRK2 activity, ARV-102 is designed to cross the blood-brain barrier and effectively degrade the LRRK2 protein, offering a potentially transformative approach to treating these challenging conditions.

In a recent update, John Houston, Ph.D., Chairperson, CEO, and President, along with Angela M. Cacace, provided insights into the progress of ARV-102 and other preclinical PROTAC protein degraders targeting neurological disorders. These updates were made available through a webcast.

Arvinas, a clinical-stage biotechnology firm, focuses on developing therapies for debilitating and life-threatening diseases by leveraging their proprietary PROTAC Discovery Engine platform. This technology aims to create PROTAC degraders that harness the body's natural protein disposal system to eliminate disease-causing proteins. The company's clinical-stage programs include treatments for diseases related to historically “undruggable” targets, such as ARV-471 for ER+/HER2- breast cancer, ARV-766 and bavdegalutamide for metastatic castration-resistant prostate cancer, and ARV-102 for neurodegenerative disorders.

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