ARV-102 Targets LRRK2 Beyond the Blood-Brain Barrier
This oral LRRK2 degrader developed by Arvinas exhibits outstanding clinical potential. At an 80 mg dose, it achieves 70% LRRK2 degradation in the cerebrospinal fluid of Parkinson’s patients, with degradation rates exceeding 50% across all dose groups.
Build LRRK2 Degraders
| Product Name: 1-(6-Bromo-5-fluoro-1-methyl-1H-indazol-3-yl)dihydropyrimidine-2,4(1H,3H)-dione Product Code: F551531 CAS: 276050-50-6 | Product Name: 1-(2-(2,6-Dioxopiperidin-3-yl)-4-fluoro-1-oxoisoindolin-5-yl)piperidine-4-carbaldehyde Product Code: F575091 CAS: 2839670-59-4 | Product Name: 3-(5-(4-(Dimethoxymethyl)piperidin-1-yl)-4-fluoro-1-oxoisoindolin-2-yl)piperidine-2,6-dione Product Code: F575092 CAS: 2839670-58-3 |
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| Product Name: 5-(1-Methylcyclopropoxy)-1H-indazole Product Code: F601257 CAS: 1626355-74-5 | Product Name: 3-(5-Bromo-4-fluoro-1-oxoisoindolin-2-yl)piperidine-2,6-dione Product Code: F738115 CAS: 2408391-89-7 | Product Name: 3-(6-Chloro-3-oxo-1H-pyrrolo[3,4-c]pyridin-2(3H)-yl)piperidine-2,6-dione Product Code: F5738117 CAS: 2154343-21-0 |
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LRRK2 is a key kinase regulating neuronal function. It’s aberrant expression and mutations are closely associated with neurodegenerative diseases including Parkinson’s disease and progressive supranuclear palsy. Conventional targeted drugs struggle to balance central nervous system efficacy and safety. ARV-102, a PROTAC degrader, demonstrates favorable pharmacokinetic properties and can effectively penetrate the blood brain barrier. By directly degrading LRRK2 protein, it achieves a more durable and precise blockade of pathogenic pathways.
ARV-102 also displays excellent safety profiles, without the pulmonary adverse reactions commonly observed with traditional inhibitors. The development of LRRK2 targeted PROTAC degraders has emerged as a highly promising cutting edge direction in the treatment of neurodegenerative diseases.
In response to the latest research advances of ARV-102, an LRRK2 PROTAC degrader, we have expanded our catalogue at Fluorochem to include a newly developed series of novel dedicated building blocks.
