Tyrosine kinase inhibitors for solid tumors in the past 20 years (2001–2020)

Huang, Liling; Jiang, Shiyu; Shi, Yuankai

doi:10.1186/s13045-020-00977-0

Journal of Hematology & Oncology

Table 5 Advances of VEGFR-associated multi-targeted TKIs

From: Tyrosine kinase inhibitors for solid tumors in the past 20 years (2001–2020)

Drug	Brand name	Manufacturer	Targets	Applications of diseases	Approved years or current phases of clinical trials
Sorafenib	Nexavar	Bayer	VEGFR1-3, TIE2, PDGFR, FGFR, BRAF, CRAF, KIT, FLT-3	mRCC	2005 [203]
				Unresectable HCC	2007 [109, 110]
				metastatic DTC	2013 [204]
Sunitinib	Sutent	Pfizer Inc	VEGFR-1–2, PDGFR, FLT3, KIT	GIST after disease progression on or intolerance to imatinib	2006 [172]
				mRCC	2006 [172]
				unresectable or metastatic pancreatic neuroendocrine tumor	2011 [205]
				Adjuvant treatment for RCC	2017
Vandetanib	Caprelsa	AstraZeneca	EGFR, VEGFR2-3, RET	Unresectable or metastatic MTC	2011 [206]
Regorafenib	Stivarga	Bayer	VEGFR1-3, TIE2, PDGFR, FGFR, BRAF, KIT, RET	Recurrent or metastatic CRC, locally advanced/unresectable or metastatic GIST previously treated with imatinib and sunitinib, advanced HCC who has been previously treated with sorafenib	2012 [207] , 2013 [173], 2017 [114]
Lenvatinib	Lenvima	Eisai Inc	VEGFR1-3, PDGFR, FGFR 1–4, RET, KIT	Radioactive iodine refractory DTC	2015 [208]
				2L combined with everolimus for mRCC	2016 [209]
				1L unresectable HCC	2018 [111]
				Combined with pembrolizumab for certain types of endometrial cancer	2019 [210]
Cabozantinib	Cometriq/Cabometyx	Exelixis Inc	VEGFR1-3, MET, ROS1, RET, AXL, NTRK, KIT	Progressive metastatic MTC	2012 [211]
				2L mRCC	2016 [212]
				1L mRCC	2017
				HCC who has been previously treated with sorafenib	2019 [115]
Axitinib	Inlyta	Pfizer Inc	VEGFR1-3, PDGFR, KIT, FLT-3	2L advanced RCC	2012 [213]
				1L combined with pembrolizumab for advanced RCC	2019 [214]
				1L combined with avalumab for advanced RCC	2019 [215]
Pazopanib	Votrient	GlaxoSmithKline	VEGFR, PDGFR, KIT	Advanced RCC	2009
Pazopanib	Votrient	GlaxoSmithKline	VEGFR, PDGFR, KIT	Advanced STS who has previously received chemotherapy	2012
Anlotinib	-	Jiangsu ChiaTai Tianqing	VEGFR2-3, FGFR1-4, PDGFR, KIT, RET	≥ 3L metastatic NSCLC	2018^& [117]
				≥ 2L metastatic STS	2018^& [216]
				≥ 3L relapsed SCLC	2019^& [118]
				Many other solid tumors	ongoing
Fruquintinib	-	Chi-Med	VEGFR1-3	≥ 3L mCRC	2018^& [217]
Apatinib	-	Jiangsu Hengrui	VEGFR2, KIT, RET, c-Src	≥3L adenocarcinoma of the stomach or gastroesophageal junction	2014^& [218]
Apatinib	-	Jiangsu Hengrui	VEGFR2, KIT, RET, c-Src	2L HCC	2020^& Applying for approval [116]
Investigational drugs
Surufatinib	-	Chi-Med	VEGFR1-3, FGFR, CSF-1R	1L non-pancreatic NET	2019^& Received a NDA [219]
Surufatinib	-	Chi-Med	VEGFR1-3, FGFR, CSF-1R	Pancreatic NET, solid tumors, biliary tract cancer	I-III ongoing
Famitinib	-	Jiangsu Hengrui	VEGFR2-3, PDGFR, FLT1, FLT3, KIT	CRC, NSCLC	III ongoing
Famitinib	-	Jiangsu Hengrui	VEGFR2-3, PDGFR, FLT1, FLT3, KIT	Multiple solid tumors	I-II ongoing
Donafenib	-	Suzhou Zelgen	VEGFR, PDGFR	HCC, CRC, DTC, NPC	I-III ongoing
Cediranib	-	AstraZeneca	VEGFR1-3, KIT, PDGFR	Combined with olaparib for ≥ 2L SCLC	II [220]

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), except those with a superscript “&” which means they were firstly approved by National Medical Products Administration (NMPA); if a drug is under investigation, we provided current phases of its clinical trials
NSCLC non-small cell lung cancer, SCLC small cell lung cancer, mRCC metastatic renal cell carcinoma, HCC hepatocellular carcinoma, DTC differentiated thyroid cancer, MTC medullary thyroid cancer, CRC colorectal cancer, GIST gastrointestinal stromal tumor, STS soft tissue sarcoma, NPC nasopharyngeal carcinoma, NET neuroendocrine tumors, FLT3 fetal liver tyrosine kinase receptor 3, NDA new drug application, VEGFR vascular endothelial growth factor receptor
Data source: www.fda.gov, www.drugs.com, and www.clinicaltrials.gov (cutoff date: 19 July 2020)

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ISSN: 1756-8722

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