1527475-61-1

PFE-360 (PF-06685360) is a poten and elective inhibitor of LRRK2 kinase.

PFE-360 (PF-06685360) is a potent, selective, brain penetrated and orally active leucine-rich repeat kinase 2 (LRRK2) inhibitor with a mean IC50 of 2.3 nM in vivo[1][2].

PFE-360 (4 mg/kg and 7.5 mg/kg, orally, BID, 10-12 weeks) treatment potently decreases the LRRK2-pSer935/total LRRK2 ratio, with no significant adverse effects.
animal Model: Female Sprague Dawley rats (NTac:SD) weighed 225-250 g.
Dosage: 4 mg/kg and 7.5 mg/kg (pharmacokinetics and pharmacodynamics).
Administration: Orally BID for 10-12 weeks.
Result: The LRRK2-pSer935/total LRRK2 ratio was significantly decreased at both 1 h and 12 h after dosing.
The terminal bodyweights exhibited no significant changes.

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[1] Marco A.S. Baptista, et al. LRRK2 Kinase Inhibitors of Different Structural Classes Induce Abnormal Accumulation of Lamellar Bodies in Type II Pneumocytes in Non-Human Primates but are Reversible and Without Pulmonary Functional Consequences.
[2] Andersen MA, et al. Parkinson's disease-like burst firing activity in subthalamic nucleus induced by AAV-α-synuclein is normalized by LRRK2 modulation. Neurobiol Dis. 2018 Aug;116:13-27. DOI:10.1016/j.nbd.2018.04.011
[3] Andersen MA, et al. PFE-360-induced LRRK2 inhibition induces reversible, non-adverse renal changes in rats. Toxicology. 2018 Feb 15;395:15-22. DOI:10.1016/j.tox.2018.01.003