From: Tyrosine kinase inhibitors for solid tumors in the past 20 years (2001–2020)
Drug | Brand name | Manufacturer | Targets | Applications of diseases | Approval year or current phase of clinical trials |
---|---|---|---|---|---|
Imatinib | Gleevec | Novartis Oncology | Bcr-Abl, KIT, PDGFR | Advanced Philadelphia chromosome positive chronic myeloid leukemia | 2001 |
1L KIT + unrectable or metastatic GIST | 2002 | ||||
Other hematological cancer | |||||
Sunitinib | Sutent | Pfizer Inc | KIT, PDGFR, VEGFR1-2, FLT3 | GIST after disease progression on or intolerance to imatinib | 2006 [172] |
Regorafenib | Stivarga | Bayer | KIT, PDGFR, VEGFR1-3, TIE2, FGFR, BRAF, RET | Locally advanced, unresectable, or metastatic GIST previously treated with imatinib and sunitinib | 2013 [173] |
Avapritinib | Ayvakit | Blueprint Medicines | KIT, PDGFR | Unresectable or metastatic GIST harboring PDGFRA exon 18 mutation | 2020 [176] |
≥ 4L and PDGFRA exon 18 mutant GIST | I [176] | ||||
Locally advanced unresectable or metastatic GIST who previously received imatinib and 1 or 2 other TKIs | III (NCT03465722) | ||||
Ripretinib (DCC-2618) | Qinlock | Deciphera | KIT, PDGFR | Advanced GIST who have received prior treatment with 3 or more TKIs including imatinib | 2020 [177] |
Advanced GIST after disease progression on or intolerance to imatinib | III (NCT03673501) | ||||
Investigational drugs | |||||
PLX-9486 | – | Plexxikon | KIT | Combined with pexidartinib for KIT + GIST | [179] |