Table 11.

Advances of KIT/PDGFR-TKIs

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]

In the last column of “Approval years or current phases of clinical trials”: if a drug has been approved, we provided data of the year of its approval by Food and Drug Administration (FDA); if a drug is under investigation, we provided current phases of its clinical trials

GIST Gastrointestinal stromal tumor, TKIs tyrosine kinase inhibitors, PDGFR platelet-derived growth factor receptor

Data source: www.fda.gov, www.drugs.com, and www.clinicaltrials.gov (cutoff date: 19 July 2020)