Table 2.
Approved kinase inhibitor drugs for inflammatory diseases, malignancies and haematological disorders
| Drug class | Drug | Specificity | Inflammatory disease | Malignancy and haematological disorder |
|---|---|---|---|---|
| ABL | Dasatinib | ABL | None | CML, ALL |
| Imatinib | ABL | ASM, HES | CML, GIST | |
| Nilotinib | ABL | None | CML | |
| Ponatinib | ABL | None | Refractory CML | |
| Bosutinib | ABL | None | CML | |
| CSF1R | Edicotinib | CSF1R | None | GCT |
| Pexidartinib | CSF1R, FLT, KIT | None | GCT | |
| JAK | Abrocitinib | JAK1 | AD | None |
| Baricitinib | JAK1, JAK2 | RA, COVID-19, AA, AD | None | |
| Delgocitinib | Pan-JAK | AD (topical only, Japan) | None | |
| Deucravacitinib | TYK2 | Psoriasis | None | |
| Fedratinib | JAK2 | None | MF, PV, ET | |
| Filgotinib | JAK1 | RA (Europe, Japan), UC (Japan) | None | |
| Momelitinib | JAK1, JAK2 | None | MF | |
| Pacritinib | JAK2, FLT3 | None | MF | |
| Peficitinib | Pan-JAK | RA (Japan) | None | |
| Ruxolitinib | JAK1/JAK2 > TYK2 > JAK3 | GVHD, AD (topical only), vitiligo (topical only) | MF, PP, PRV, ET, PT | |
| Tofacitinib | JAK3/JAK1 > JAK2, TYK2 | RA, UC; PsA, AS, JIA (USA, Europe) | None | |
| Upadacitinib | JAK1 > JAK2 | RA; PsA, AD (USA, Japan); AS, UC (USA) | None | |
| MAPK | Vemurafenib | BRAF | None | Metastatic melanoma, Erdheim–Chester disease |
| Dabrafenib | BRAF | None | Metastatic melanoma | |
| ROCK | Belumosudil | ROCK2 | GVHD | None |
| Fasudil | ROCK1, ROCK2 | None | Cerebral vasospasm (Japan, China) | |
| RSK | Galunisertib | TGFβR | IPF (EU, Canada) | None |
| RTK | Nintedanib | PDGFR | ILD, IPF | None |
| SYK | Fostamatinib | SYK | ITP | None |
| TEC | Acalabrutinib | BTK | None | CLL/SLL, MCL |
| Ibrutinib | BTK, ITK | GVHD | CLL/SLL, MCL, MZL, WM | |
| Orelabrutinib | BTK | None | Relapsed/refractory MCL (China) | |
| Zanubrutinib | BTK | None | MCL, MZL, WM |
AA, alopecia areata; AD, atopic dermatitis; ALL, acute lymphoblastic leukaemia; AS, ankylosing spondylitis; ASM, advanced systemic mastocytosis; BTK, Bruton’s tyrosine kinase; CLL, chronic lymphocytic leukaemia; CML, chronic myeloid leukaemia; CSF1R, colony-stimulating factor 1 receptor; ET, essential or post-essential thrombocytopenia; GCT, giant cell tumour; GIST, gastrointestinal stromal tumour; GVHD, graft versus host disease; HES, hypereosinophilic syndrome; ILD, interstitial lung disease; IPF, idiopathic pulmonary fibrosis; ITP, idiopathic thrombocytopenia; JAK, Janus kinase; JIA, juvenile idiopathic arthritis; MAPK, mitogen-activated protein kinase; MCL, mantle-cell lymphoma; MF, myelofibrosis; MZL, marginal zone leukaemia; PDGFR, platelet-derived growth factor receptor; PP, primary polycythemia; PRV, polycythemia rubra vera; PsA, psoriatic arthritis; PT, primary thrombocythemia; PV, pemphigus vulgaris; RA, rheumatoid arthritis; ROCK, RHO-associated coiled–coiled containing protein kinase; RSK, receptor serine kinase; RTK, receptor tyrosine kinase; SLL, small lymphocytic leukaemia; SYK, spleen tyrosine kinase; TGFβR, transforming growth factor-β receptor; UC, ulcerative colitis; WM, Waldenström macroglobulinaemia.