Arvinas, Inc. presented first-in-human data from its Phase 1 clinical trial of ARV-102, an investigational PROTAC leucine-rich repeat kinase 2 (LRRK2) degrader. The data, shared at the 2025 International Conference on Alzheimer’s and Parkinson’s Diseases, showed ARV-102 was well tolerated, orally bioavailable, and brain-penetrant in healthy volunteers.
ARV-102 achieved substantial reduction of LRRK2 in cerebral spinal fluid (CSF), a key indicator for neurodegenerative disease targets. A single oral dose of at least 60 mg, and repeated doses of at least 20 mg, resulted in greater than 50% LRRK2 reduction in the CSF and over 90% reduction in peripheral blood mononuclear cells (PBMCs).
The safety profile was promising, with no serious adverse events reported after single or multiple doses. These findings support the continued evaluation of ARV-102 in neurodegenerative diseases associated with LRRK2 dysfunction, including Parkinson's disease, for which a Phase 1 trial in patients has already been initiated.
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