Table 1 Kinase inhibitors approved by FDA and NMPA
From: An overview of kinase downregulators and recent advances in discovery approaches
Year | Name | Binding mode | Target | PDB ID |
|---|---|---|---|---|
2001 | Imatinib | Type II | ABL/KIT/PDGFR | 2HYY |
2003 | Gefitinib | Type I | EGFR | 4WKQ |
2004 | Erlotinib | Type I | EGFR | 4HJO |
2005 | Sorafenib | Type II | FLT3/KIT/RET/PDGFR/VEGFR | 3WZE |
2006 | sunitinib | Type I | FLT3/KIT/RET/PDGFR | 3G0E,6JOK |
Dasatinib | Type I | ABL/KIT/LCK/Src/PDGFR | 3G6D | |
2007 | Nilotinib | Type II | ABL/KIT/PDGFR | 3CS9 |
Lapatinib | Type1/2 | EGFR/HER2 | 3BBT, 1XKK | |
2009 | Pazopanib | Type I | KIT/VEGFR | PDB ID of its analog:204 3CJG |
2011 | Icotinib | Type I | EGFR | |
Crizotinib | Type I | ALK/ROS/c-MET | 3ZBF | |
Ruxolitinib | Type I | Pan-JAK | Ref. 205 | |
Vemurafenib | Type I | BRAF | 3OG7 | |
2012 | Axitinib | Type II | KIT/PDGFR/VEGFR | 4AG8 |
Radotinib | Type II | ABL | ||
Bosutinib | Type I | ABL/Src | 3UE4, 4MXO | |
Regorafenib | Type II | FLT3/KIT/VEGFR/PDFGR | Ref. 9 | |
Tofacitinib | Type I | JAK | 3LXK,3FUP | |
Cabozantinib | Type II | FLT3/KIT/VEGFR/FGFR/PDFGR/RET/c-Met/TRK2 | 4MXC | |
Ponatinib | Type II | ABL/FLT3/KIT/PDGFR/ FGFR/Src | 3OXZ | |
2013 | Afatinib | Covalent | EGFR/HER2 | 4G5J, 4G5P |
Ibrutinib | Covalent | BTK | 6DI9 | |
Trametinib | Type III | MEK1/2 | Ref. 206 | |
2014 | Ceritinib | Type I | ALK/ROS | 4MKC |
Apatinib | Type I | VEGFR2 | ||
Idelalisib | Type I | PI3Kδ | 4XE0 | |
Dabrafenib | Type1/2 | BRAF-V600E | 5CSW | |
2015 | Alectinib | Type I | ALK | 3AOX |
Cobimetinib | Type III | MEK1/2 | 4AN2 | |
Palbociclib | Type I | CDK4/6 | 5L2I | |
Osimertinib | Covalent | EGFR | 6JXT | |
Lenvatinib | Type I | KIT/RET/FGFR/PDGFR/ VEGFR | 3WZD, 5ZV2 | |
Nintedanib | Type I | KIT/FGFR/VEGFR | 3C7Q | |
2016 | Olmutinib | Covalent | EGFR | |
2017 | Brigatinib | Type I | ALK/EGFR/FLT3/IGF1R/ ROS1 | BMX8 |
Acalabrutinib | Covalent | BTK | Ref. 207 | |
Ribociclib | Type I | CDK4/6 | 5L2T | |
Neratinib | Covalent | EGFR/HER2 | 2JIV, 3W2Q | |
Midostaurin | Type I | FLT3/KIT | 4NCT | |
Copanlisib | Type I | PI3K | 5G2N | |
2018 | Anlotinib | Type I | FGFR/PDGFR/VEGFR | |
Lorlatinib | Type I | ALK | 4UXL | |
Fruquintinib | Type I | VEGFR | ||
Binimetinib | Type III | BRAF | 7M0U | |
Pyrotinib | Covalent | HER1/2/4 | Ref. 208 | |
Dacomitinib | Covalent | EGFR | 4I24 | |
Gilteritinib | Type I | FLT3/ALX | 6JQR | |
Larotrectinib | Type I | TRK | Ref. 209 | |
Duvelisib | Unreported | PI3Kδ/γ | ||
Fostamatinib | Type I | SYK | ||
Encorafenib | Type I | BRAF/V600E | ||
Baricitinib | Unreported | JAK1/2 | ||
2019 | Pexidartinib | Type II | CSF1R/KIT/FLT3 | 4R7H |
Zanubrutinib | Covalent | BTK | 6J6M | |
Entrectinib | Type I | TRK | 5FTO | |
Erdafitinib | Type I | FGFR | 5EW8 | |
Quizartinib | Type II | FLT3 | 4XUF | |
Fedratinib | Type I | JAK2 | 6VNE | |
Alpelisib | Type I | PI3Kα | 4JPS | |
Upadacitinib | Unreported | JAK1 | ||
Flumatinib | Type II | ABL/KIT/PDGFR | ||
Netarsudil | Unreported | ROCK1/2 | ||
2020 | Pemigatinib | Type I | pan-FGFRs | |
Avapritinib | Unreported | KIT/PDGFR | ||
Ripretinib | Type II | KIT/PDGFR | 6MOB | |
Selumetinib | Type III | MEK1/2 | 4U7Z | |
Capmatinib | Unreported | MET | ||
Tucatinib | Unreported | HER2 | ||
Almonertinib | Covalent | EGFR | Ref. 208 | |
Ensartinib | Unreported | ALK | ||
Orelabrutinib | Covalent | BTK | Ref. 210 | |
Sulfatinib | Unreported | VEGFR/FGFR | ||
Selpercatinib | Type I | RET | 7JU6 | |
Pralsetinib | Type I | RET | 7JU5 | |
2021 | Trilaciclib | Unreported | CDK4/6 | |
Furmonertinib | Covalent | EGFR | Ref. 211 | |
Infigratinib | Type I | FGFRs | 3TT0 | |
Tepotinib | Type I | MET | 4R1V | |
Tivozanib | Type II | VEGFR2 | 4ASE | |
Umbralisib | Type I | PI3Kδ |
