Table 1.
A brief description [27,30,31,62,63] of selected TKIs arranged alphabetically by their international nonproprietary names (INN) formulated into lipid-based nanosystems.
| INN | Brand Name | Approval for the 1st Indication | Type | Kinase Target | Major Therapeutical Uses |
|---|---|---|---|---|---|
| afatinib | Gilotrif | 2013 | V | EGFR, HER2 | NSCLC |
| axitinib | Inlyta | 2012 | II | VEGFR1-3, PDGFR | RCC |
| brigatinib | Alunbrig | 2017 | I | ALK, ROS1, IGF-1R, Flt3, EGFR | NSCLC |
| bortezomib | Velcade | 2003 | I | proteasome | multiple myeloma, MCL |
| cabozantinib | Cometriq, Cabometyx | 2012 | I | RET, HGFR, VEGFR1-3, Kit, TrkB, Flt3, Axl, Tie2, ROS1 | MTC, RCC, HCC |
| crizotinib | Xalkori | 2011 | II | ALK, HGFR, ROS1, MST1R | NSCLC |
| dasatinib | Sprycel | 2006 | I | BCR-ABL, EGFR, PDGFR Src, Lck, Yes, Fyn, Kit, EphA2 | CML, ALL |
| erlotinib | Tarceva | 2004 | I | EGFR, HER1 | NSCLC, SCLC, PaC |
| gefitinib | Iressa | 2009 | I | EGFR | NSCLC |
| imatinib | Gleevec | 2001 | II | BCR-ABL, c-Kit, PDGFR | CML, ALL, DFSP, HES, GIST, MDS/MDP |
| lapatinib | Tykerb | 2007 | II | EGFR, HER2 | breast cancer |
| nintedanib | Ofev | 2014 | I | VEGFR, FGFR, PDGFR | pulmonary fibrosis |
| osimertinib | Tagrisso | 2015 | V | EGFR | NSCLC |
| pazopanib | Votrient | 2009 | I | VEGFR1-3, PDGFR, FGFR1/3, Kit, Lck, Fms, Itk | RCC, STS |
| ponatinib | Iclusig | 2013 | II | BCR-ABL, VEGFR, PDGFR, FGFR, EphR, Src, Kit, RET, Tie2, Flt3 | CML, ALL |
| regorafenib | Stivarga | 2012 | II | BCR-ABL, VEGFR, BRAF, c-Kit, PDGFR, RET, FGFR, Tie2, Eph | CRC, GIST |
| selumetinib | Koselugo | 2020 | V | MEK1/2 | NF1 |
| sorafenib | Nexavar | 2005 | II | B/C-Raf, BRAF, c-Kit, Flt3, RET, VEGFR1-3, PDGFR | RCC, DTC, HCC, ThC |
| sunitinib | Sutent | 2006 | II | PDGF, VEGFR1-3, c-Kit, Flt3, CSF-1R, RET | CML, RCC, GIST, PNET |
| trametinib | Mekinist | 2013 | III | MEK1/2 | melanoma, NSCLC |
ALL = acute lymphoid leukemia; CML = chronic myeloid leukemia; CRC = colorectal carcinoma; DFSP = dermatofibrosarcoma protuberans; DTC = differentiated thyroid carcinoma; GIST = gastrointestinal stromal tumor; HCC = hepatocellular carcinoma; HES = hypereosinophilic syndrome; MCL = mantle cell lymphoma; MDS/MDP = myelodysplastic/myeloproliferative neoplasms; MTC = medullary thyroid cancer; NF1 = neurofibromatosis type 1; NSCLC = non-small cell lung cancer; PaC = pancreatic cancer; PNET = primitive neuroectodermal tumor; RCC = renal cell carcinoma; STS = soft tissue sarcoma; ThC = thyroid cancer.