Arvinas announced that the first subject was dosed in its Phase 1 clinical trial of ARV-102, the Company’s first oral PROTAC 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. 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 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.
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