Oclacitinib maleate (PF-03394197 maleate) 是一种新型 JAK 抑制剂。Oclacitinib maleate (PF-03394197 maleate) 抑制 JAK1 最有效。 Information Oclacitinib maleate (PF-03394197) is a novel inhibitor ofJAKfamily members withIC50ranging from 10 to 99 nM and JAK1-dependent cytokines withIC50ranging from 36 to 249 nM. It does not inhibit a panel of 38 non-JAK kinases. Targets JAK1 (Cell-free assay); JAK2 (Cell-free assay); TYK2 (Cell-free assay); JAK3 (Cell-free assay) 10nM; 18nM; 84nM; 99nM In vitro PF-03394197 inhibits JAK family members by 50% at concentrations ranging from 10 to 99 nM and does not inhibit a panel of 38 non-JAK kinases. PF-03394197 is most potent at inhibiting JAK1. PF-03394197 also inhibits the function of JAK1-dependent cytokines involved in allergy and inflammation as well as pruritus. PF-03394197 has minimal effects on cytokines which does not activate the JAK1 enzyme in cells. In vivo PF-03394197 administered orally at a dose of 0.4–0.6 mg/kg twice daily is safe and efficacious in controlling the pruritus associated with allergic dermatitis. PF-03394197 provides itch relief within 24 h that persistes through the treatment period, with over 70% of the treated dogs achieving a >50% reduction in pruritus by day 7.