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Description: Abrocitinib (formerly also known as PF-04965842) is a novel, potent and orally bioavailable JAK1 (Janus Kinase 1) inhibitor with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM for JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2, respectively. It is being investigated for treatment of plaque psoriasis. Physicochemical properties and pharmacokinetic parameters of PF-04965842 are examined in rats following doses of 1 mg/kg iv or 3 mg/kg po. Clearance of PF-04965842 is low relative to total liver blood flow (CL = 26.6 mL/min/kg). Vdss = 1.04 L/kg. T1/2 = 1.1 h. The oral availability of PF-04965842 is 95.6%. PF-04965842 demonstrates efficacy in a dose-responsive manner in a therapeutic rat adjuvant-induced arthritis model.
References: J Med Chem. 2018, 61(3):1130-1152.
Related CAS#:2204280-33-9 (trans-isomer)
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