In vitro: In biochemical assays, Upadacitinib is 74-fold more selective for JAK-1 than for JAK-2 (which is involved in erythropoiesis) and 58-fold more selective for JAK-1 than for JAK-3 (which is involved in immunosurveillance). The enhanced selectivity of Upadacitinib for JAK-1 over JAK-2 and JAK-3 may offer an improved benefit–risk profile in patients with RA range.
In vivo: AbbVie’s second JAK inhibitor in development Upadacitinib has been described as a second-generation inhibitor. Multiple-dose Phase I studies are completed in 2013. In phase I trials, Upadacitinib is found to be safe and well-tolerated up to multiple doses of 24 mg twice daily using the immediate release formulation. Upadacitinib exposure is dose proportional in the evaluated multiple dose.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||22 mg/mL in DMSO|
Assessment of effect of CYP3A inhibition, CYP induction, OATP1B inhibition, and high-fat meal on pharmacokinetics of the JAK1 inhibitor upadacitinib.
Mohamed MF, et al. Br J Clin Pharmacol. 2017 Oct;83(10):2242-2248. PMID: 28503781.
JAK inhibitors: A broadening approach in rheumatoid arthritis.
Lam S. Drugs Today. 2016 Aug;52(8):467-469. PMID: 27722215.
|Related JAK Products|
Delphinidin (chloride) is an anthocyanidin, a natural plant pigment which can modulate JAK/STAT3 and MAPKinase signaling to induce apoptosis in HCT116 cells.
AZD4205 is a novel potent and selective janus kinase 1 (JAK1) inhibitor, with IC50 value of 73 nM.
PF-06826647, also known as Tyk2-IN-8, is a selective and orally administered tyrosine kinase 2 (TYK2) inhibitor, with IC50 of 17 nM.
PF-06700841 (Brepocitinib) tosylate is a dual inhibitor of JAK1 and TYK2, with IC50 values of 17 nM and 23 nM, respectively.
|JAK3-IN-6 (Compound 2)
JAK3-IN-6 (Compound 2) CAS#: 1443235-95-7 is a potent and highly selective JAK3 inhibitor, with an IC50 of 0.15 nM.
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