ARV-102

ARV-102 is a novel, oral, brain-penetrant investigational PROTAC (PROteolysis TArgeting Chimera) small molecule designed to selectively degrade leucine-rich repeat kinase 2 (LRRK2), a large multidomain scaffolding kinase implicated in the pathogenesis of neurodegenerative diseases such as Parkinson’s disease and progressive supranuclear palsy. Unlike traditional inhibitors that block enzyme activity, PROTACs like ARV-102 facilitate the targeted degradation of disease-causing proteins by harnessing the body’s natural protein disposal system. Preclinical and early clinical data demonstrate that ARV-102 crosses the blood-brain barrier, achieves substantial reduction of LRRK2 in both central nervous system and peripheral blood compartments, and impacts downstream biomarkers associated with LRRK2 activity. The drug is being developed by Arvinas for neurodegenerative disorders where LRRK2 dysfunction plays a role[1][3][4][5][6][7][8][9].

Other names

LRRK2 protein modulator - ArvinasLRRK-2 protein modulator - ArvinasLRRK 2 protein modulator - Arvinas