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. 2023 May 23;98(5):656–677. doi: 10.1016/j.abd.2023.03.001

Table 2.

Pharmacological characteristics of the main JAK-STAT pathway inhibitors available on the market

Drug Inhibitory concentration (IC50) Metabolism Plasma half-life
Tofacitinib JAK1: 2.9 nM Hepatic CYP3A4 > CYP2C19 6 to 8h
JAK2: 1.2 nM
JAK3: 1.1 nM
TYK2: 42 nM
Baricitinib JAK1: 4.0 nM Hepatic CYP3A4 10 to 13h
JAK2: 6.6 nM
JAK3: 787 nM
TYK2: 61 nM
Ruxolitinib JAK1: 6.4 nM Hepatic CYP3A4 3 to 4h
JAK2: 8.8 nM
JAK3: 487.0 nM
TYK2: 30.0 nM
Ritlecitinib JAK1: 1.638 nM Hepatic: CYP450; Serum: glutathione-S-transferase 2 to 3h
JAK2: 1.507 nM
JAK3: 0.3 nM
TYK2: 3.779 nM
Abrocitinib JAK1: 29 nM Hepatic CYP2C19 > CYP2C9 > CYP3A4 > CYP2D6 3 to 5h
JAK2: 803 nM
JAK3: > 10.000 nM
TYK2: 1.259 nM
Upadacitinib JAK1: 14 nM Hepatic CYP3A4 > CYP2D6 6 to 15h
JAK2: 593 nM
JAK3: 1.860 nM
TYK2: 2.715 nM
Delgocitinib JAK1: 2.8 nM NA: topical use NA: topical use
JAK2: 2.6 nM
JAK3: 13.0 nM
TYK2: 58.0 nM