First Subject Dosed in Phase I Clinical Trial of Investigational Protein Degrader for Neurodegenerative Disease
ARV-102 is a novel oral PROTAC protein degrader designed to cross the blood-brain barrier and target leucine-rich repeat kinase 2.
Arvinas has announced that the first subject was dosed in its Phase I clinical trial of ARV-102, according to a company press release.1 ARV-102 is the company’s first oral PROTAC (PROteolysis-TArgeting Chimera) protein degrader in development to treat neurodegenerative diseases.
In preclinical studies, ARV-102 has been shown to cross the blood-brain barrier and degrade leucine-rich repeat kinase 2 (LRRK2), which is a large multidomain scaffolding kinase. Increased activity and expressions of LRRK2 is genetically involved in the pathogenesis of neurological diseases including Parkinson’s disease and progressive supranuclear palsy.
According to the press release, orally administered ARV-102 has been shown to reach deep-brain regions and degrade LRRK2 by nearly 90% in non-human primates.
“Parkinson’s disease and progressive supranuclear palsy are devastating diseases and this important step of dosing the first healthy volunteer with ARV-102 marks a significant milestone in our commitment to develop transformative therapies for patients living with neurodegenerative diseases,” said Angela M. Cacace, PhD, senior vice president, neuroscience and platform biology, Arvinas in the press release. “There is a high unmet need in many neurologic diseases, and unlike other therapeutic modalities designed to inhibit LRRK2 activity, ARV-102 is an investigational oral PROTAC degrader uniquely designed to cross the blood-brain barrier and degrade the LRRK2 protein. As a pioneer in targeted protein degradation, we believe that PROTAC degraders have great potential to change the treatment paradigm for patients with neurodegenerative diseases.”
The Phase I trial of ARV-102 will evaluate its safety, tolerability, pharmacokinetics, and pharmacodynamics, including the evaluation of LRRK2 degradation and exploratory LRRK2 pathway biomarkers in healthy volunteers. The study is enrolling healthy volunteers at the Centre for Human Drug Research (CHDR) in Leiden, the Netherlands.
Reference
- Arvinas Announces First-in-Human Dosing of ARV-102, an Investigational PROTAC® Protein Degrader for Neurodegenerative Disease. News release. February 20, 2024. Accessed February 21, 2024. https://www.globenewswire.com/news-release/2024/02/20/2831684/0/en/Arvinas-Announces-First-in-Human-Dosing-of-ARV-102-an-Investigational-PROTAC-Protein-Degrader-for-Neurodegenerative-Disease.html
Behind the Buzz: Why Clinical Research Leaders Flock to SCOPE Summit
February 7th 2025In this episode, we meet with Micah Lieberman, Executive Conference Director for SCOPE Summit (Summit for Clinical Ops Executives) at Cambridge Innovation Institute. We will dive deep into the critical role of collaboration within the clinical research ecosystem. How do we bring together diverse stakeholders—sponsors, CROs, clinical trial tech innovators, suppliers, patients, sites, advocacy organizations, investors, and non-profits—to share best practices in trial design, program planning, innovation, and clinical operations? We’ll explore why it’s vital for thought leaders to step beyond their own organizations and learn from others, exchanging ideas that drive advancements in clinical research. Additionally, we’ll discuss the pivotal role of scientific conferences like SCOPE Summit in fostering these essential connections and collaborations, helping shape the future of clinical trials. Join us as we uncover how collective wisdom and cross-industry partnerships are transforming the landscape of clinical research.
Reaching Diverse Patient Populations With Personalized Treatment Methods
January 20th 2025Daejin Abidoye, head of solid tumors, oncology development, AbbVie, discusses a number of topics around diversity in clinical research including industry’s greatest challenges in reaching diverse patient populations, personalized treatment methods, recruitment strategies, and more.
POETYK PsA-2 Trial Shows Efficacy of Sotyktu as an Oral Therapy for Psoriatic Arthritis
March 11th 2025Sotyktu (deucravacitinib) demonstrated significant efficacy in improving psoriatic arthritis symptoms compared to placebo in the Phase III POETYK PsA-2 trial, with a well-tolerated safety profile.
