TABLE 3.

Summary of approved multikinase small molecule inhibitors

Class	Drug name	Company	First approval	Targets	Protein substrate	Administration pathway	Indications
VEGFR multikinase	Sorafenib (Nexavar)	Bayer Healthcare	2005	c‐CRAF, BRAF, mutant BRAF, KIT, FLT‐ 3, RET, RET/PTC, VEGFR1, VEGFR2, VEGFR3, PDGFRβ	Tyrosine	Oral	HCC, RCC, radioiodine‐ refractory DTC
VEGFR multikinase	Sunitinib (Sutent)	CPPI CV (Pfizer)	2006	PDGFRα, PDGFRβ, VEGFR1, VEGFR2, VEGFR3, KIT, FLT3, CSF‐1R, RET	Tyrosine	Oral	GIST, RCC, pNET
VEGFR multikinase	Pazopanib (Votrient)	Novartis	2009	VEGFR1, VEGFR2, VEGFR3, PDGFRα, PDGFRβ, FGFR1, FGFR3, Kit, Itk, Lck, c‐Fms	Tyrosine	Oral	RCC, soft tissue sarcoma
VEGFR multikinase	Vandetanib (Caprelsa)	Genzyme Corp	2011	EGFR, VEGFR, RET, BRK, TIE2, EPH receptor, Src,	Tyrosine	Oral	MTC
VEGFR multikinase	Axitinib (Inlyta)	PF Prism CV	2012	VEGFR1, VEGFR2, VEGFR3	Tyrosine	Oral	RCC
VEGFR multikinase	Regorafenib (Stivarga)	Bayer Healthcare	2012	RET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR‐alpha, PDGFR‐beta, FGFR1, FGFR2, TIE2, DDR2, TrkA, Eph2A, RAF‐1, BRAF, BRAF V600E, SAPK2, PTK5, Abl, CSF1R	Tyrosine	Oral	CRC, GIST, HCC
VEGFR multikinase	Cabozantinib (Cabometyx, Comertiq)	Exelixis	2012	MET, VEGFR1, VEGFR2, VEGFR3, AXL, RET, ROS1, TYRO3, MER, KIT, TRKB, FLT‐3, TIE‐2	Tyrosine	Oral	RCC, HCC, radioiodine‐ refractory DTC
VEGFR multikinase	Lenvatinib (Lenvima)	Eisai	2015	VEGFR1, VEGFR2, VEGFR3, FGFR1, FGFR2, FGFR3, FGFR4, PDGFRα, KIT, RET	Tyrosine	Oral	Radioiodine‐ refractory DTC, RCC, HCC, endometrial carcinoma
VEGFR multikinase	Tivozanib (Fotvida)	Aveo Pharms	2021	VEGFR1, VEGFR2, VEGFR3, c‐kit, PDGFRβ	Tyrosine	Oral	RCC

Abbreviations: HCC, hepatocellular carcinoma; RCC, renal cell carcinoma; DTC, differentiated thyroid carcinoma; GIST, gastrointestinal stromal tumor; pNET, pancreatic neuroendocrine tumor; MTC, medullary thyroid cancer; CRC, colorectal cancer. Data sources: https://www.fda.gov/drugs/development‐approval‐process‐drugs/drug‐approvals‐and‐databases.