Table 1. MAJOR TK INHIBITORS TARGETING CANCER-ASSOCIATED TKs.
| Name | Main Target(s) | FDA Approval | Indication(s) |
|---|---|---|---|
| Bcr-Abl1 Inhibitors | |||
| Imatinib | BCR-Abl1, Abl, KIT, PDGFRs | 2001 | CML, GIST |
| Dasatinib | BCR-Abl1, Abl, Src, Kit, PDGFRs, EPH, CSK | 2006 | CML, ALL |
| Nilotinib | BCR-Abl1, Abl, Kit, Lck, EPHA3, DDR1 | 2007 | CML |
| Bosutinib | BCR-Abl1, Abl, Src, Lyn, Hck | 2012 | CML |
| Ponatinib | BCR-Abl1, Abl, PDGFRα, Src, KIT, FGFR, VEGFRs | 2012 | CML, Ph+ ALL |
| EGFR Inhibitors | |||
| Erlotinib | EGFR | 2004 | NSCLC, pancreatic cancer |
| Gefitinib | EGFR | 2005 | NSCLC, AML |
| Afatinib | HER2, EGFR, T790M mutated EGFR | 2013 | NSCLC, squamous cell carcinoma of the head and neck, breast cancer |
| Osimertinib | EGFR, T790M mutated EGFR | 2015 | NSCLC |
| Dacomitinib | EGFR | -- | NSCLC, gastric cancer, head and neck cancer, glioma |
| Rociletinib | EGFR, T790M mutated EGFR | -- | NSCLC |
| HM61713 | EGFR, T790M mutated EGFR | -- | NSCLC |
| ASP8273 | EGFR, T790M mutated EGFR | -- | NSCLC |
| EGF816 | L858R, Ex19del, and T790M mutated EGFR | -- | NSCLC |
| PF-06747775 | EGFR, T790M mutated EGFR | -- | NSCLC |
| Alk Inhibitors | |||
| Crizotinib | ALK, MET | 2011 | ALCL, NSCLC, Neuroblastoma |
| Ceritinib | ALK | 2014 | NSCLC |
| Alectinib | ALK | 2015 | NSCLC |
| Brigatinib | ALK, EGFR | -- | ALCL, NSCLC, Neuroblastoma |
| CEP-28122/CEP-37440 | ALK | -- | ALCL, NSCLC |
| Entrectinib | TrkA, TrkB, TrkC, ROS1, ALK | -- | Neuroblastoma |
| PF-06463922 | ROS1, ALK | -- | NSCLC |
| TSR-011 | ALK, TRK | -- | NSCLC |
| X-376/X-396 | ALK | -- | NSCLC |
| HER/ErbB Receptor Inhibitors | |||
| Lapatinib | HER2 | 2007 | Breast Cancer |
| Neratinib | HER2 | -- | Breast Cancer |
| VEGFR and PDGFR Inhibitors | |||
| Sorafenib | VEGFR, PDGFR and Raf kinases | 2005 | Renal cell carcinoma, hepatocellular carcinoma, iodine resistant advanced thyroid carcinoma |
| Sunitinib | PDGF-Rs, VEGFRs | 2006 | Kidney cancer, GIST, pancreatic neuroendocrine tumors |
| Pazopanib | c-KIT, FGFR, PDGFR and VEGFR | 2009 | Renal cell carcinoma, soft tissue sarcomas |
| Vandetanib | VEGFR. EGFR, c-Ret | 2011 | Unresectable, locally advanced, or metastatic medullary thyroid cancer |
| Sunutinib | VEGFR, KIT, PDGFR | 2011 | Pancreatic neuroendocrine tumors, kidney cancer, GIST |
| Pazopanib | VEGFR, KIT, FGFR, PDGFR | 2012 | Renal cell carcinoma, soft tissue sarcomas |
| Regorafenib | VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR FGFR1, FGFR2, |
2012 | Metastatic colorectal cancer, GIST |
| Cabozantinib | VEGFR2, c-Met | 2012 | Thyroid cancer, advanced renal cell carcinoma, prostate cancer, glioblastoma multiforme |
| Axitinib | VEGFR1, VEGFR2, VEGFR3 | 2012 | Renal cell carcinoma, CML |
| Lenvatinib | VEGFR1, VEGFR2, VEGFR3, PDGFRs, FGFRs, c-Kit, RET, | 2015 | Thyroid cancer |
| Linifanib | VEGFR, PDGFR | -- | NSCLC, liver cancer, breast cancer, colorectal cancer |
| Bruton's tyrosine kinase Inhibitor | |||
| Ibrutinib | Bruton's tyrosine kinase | 2013 | CLL, mantle cell lymphoma, B-cell malignancies |
CML, Chronic Myelogenous Leukemia; GIST, Gastrointestinal Stromal Tumour; ALL, Acute Lymphocytic Leukemia; Ph+ ALL, Philadelphia positive ALL; NSCLC, Non Small Cell Lung Carcinoma; AML, Acute Myelogenous Leukemia; ALCL, Anaplastic Large Cell Lymphoma