Table 1 Targets for some US FDA-approved kinase inhibitors
From: Recent advances in pharmacological diversification of Src family kinase inhibitors
Target | US FDA approved kinase inhibitors | Disease targeted |
|---|---|---|
Bcr-Abl Tyrosine kinase inhibitors | Imatinib, Nilotinib, Dasatinib, Bosutinib, Ponatinib | Acute myeloid leukemia (AML), chronic myeloid leukemia (CML), acute lymphoblastic leukemia (ALL) |
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors | Gefitinib, Erlotinib, Afatinib, Osimertinib, Lapatinib, Neratinib | Lung cancer, breast cancer |
Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors | Sorafenib, Sunitinib, Pazopanib, Axitinib, Cabozantinib, Lenvatinib, Vandetanib, Regorafenib | Angiogenesis inhibitors, renal carcinoma, glioblastoma |
Platelet-derived growth factor receptors (PDGFR) tyrosine kinase inhibitors | Regorafenib, Cabozantinib, Lenvatinib, Pazopanib, Sunitinib, Sorafenib, Imatinib, Nilotinib, Dasatinib | Pulmonary tumor thrombotic microangiopathy, soft tissue sarcoma |
Fibroblast growth factor receptors (FGFR) tyrosine kinase inhibitors | Regorafenib, Lenvatinib | Bladder, lung, and gastric cancers |
BRAF kinase inhibitors | Vemurafenib, Dabrafenib, Regorafenib, Sorafenib | Advanced melanoma |
MEK inhibitors | Trametinib, Cobimetinib | Advanced melanoma |
Anaplastic lymphoma kinase (ALK) TKIs | Crizotinib, Ceritinib, Alectinib, Brigatinib, Lorlatinib | Non-small-cell lung carcinoma |
Bruton tyrosine kinase inhibitors (BTK) | Ibrutinib, Acalibrutinib | Relapsed and refractory (Mantle cell lymphoma, Waldenstrom macroglobulinemia) |
FMS-like tyrosine kinase 3 (FLT3) inhibitors | Midostaurin | In combination with chemotherapy for acute myeloid leukemia |
JAK2 kinase inhibitors | Ruxolitinib | Mycosis fungoides |
Phosphoinositide 3-kinase (PI3K) inhibitors | Idelalisib, Copanlisib | Relapsed (of chronic lymphocytic leukemia, non-Hodgkin lymphoma, follicular lymphoma) |
Cyclin-dependent kinase (CDK) 4/6 inhibitors | Palbociclib, Ribociclib, Abemaciclib | Metastatic breast cancer of Postmenopausal women |