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 |