PF-06685360

PF-06685360 (also known as PF-360) is a potent, selective, and brain-penetrant small-molecule inhibitor of leucine-rich repeat kinase 2 (LRRK2), developed by Pfizer. It is primarily utilized as a preclinical research tool to investigate the role of LRRK2 in the pathogenesis of Parkinson's disease, particularly in cases associated with the G2019S mutation. With an IC50 of 3 nM, it demonstrates high potency for LRRK2 kinase inhibition. While orally bioavailable, preclinical studies in rodents have identified potential renal toxicity, characterized by morphological changes in the proximal tubular epithelium, such as the accumulation of hyaline droplets. It is not currently an approved therapeutic drug.