Tyrosine kinase inhibitors: Multi-targeted or single-targeted?

Table 4 Tyrosine kinase inhibitors of the vascular endothelial growth factor receptor tyrosine kinase families

Inhibitor	Tyrosine kinase target	Neoplasm(s) targeted	Clinical status
Sunitinib (Sutent,	VEGFR1/2/3, PDGFRα/β, Kit,	GIST (imatinib resist)	Approved
SU11248)	Flt3, CSF1R, RET	Adv RCC	Approved
		NSCLC	Phase III
Vandetanib (ZD6474)	VEGFR2, EGFR, RET	Solid tumors	Phase I/II
		Adv NSCLC	Approved
		Medullary thyroid	Phase II
Vatalanib (PTK787/ZK222584)	VEGFR1/2/3, PDGFRβ, Kit	Colorectal, prostate, RCC, MDS, AML, MM	Phase III
			Phase I/II
Sorafenib (BAY 43-9006)	B-Raf, VEGFR2/3, PDGFRβ,	Adv RCC	Approved
	Flt3, Kit, RAF, RET	NSCLC	Phase III
		Melanoma, prostate	Diff phases
Semaxinib (SU5416)	VEGFR2, Kit, Flt3, Stat5, AKT	AML	Phase II
Cediranib (AZD2171)	VEGFR1/2/3, PDGFRβ, Kit	Solid tumors	Phase I/II/III
CEP-7055	VEGFR1/2/3, Flt3	Solid tumors	Phase  I/II
Dovitinib lactate	VEGFR1/2, FGFR1/3, PDGFRβ,	Multiple myeloma	Phase II/III
(TKI258; CHIR258)	Flt3, Kit, CSFR1
CP-547,632	VEGFR2, FGFR	Ovarian, lung	Phase I/II
Pazopanib (GW786034)	VEGFR1/2/3, PDGFRα/β, Kit	RCC,	Approved;
		Multiple myeloma;	Phase I/II
		solid tumors	Phase I/II
OSI-930	VEGFR, Kit	Cancer, anti-angiogenic	Phase I/II
Foretinib (XL-880; GSK 1363089)	VEGFR, c-MET	HCC, gastric	Phase I/II
KRN-951	VEGFR1/2/3, PDGFRβ, Kit	Adv cancer	Phase I/II
SU10944	VEGFR	Solid tumors	Preclinical
ZK-CDK	VEGFR1/2/3, PDGFRβ, Cdks	Breast, prostate	Phase I/II, suspended
Axitinib (AG-13736)	VEGFR1/2, PDGFRβ, Kit	Solid tumors	Phase II/III
Motesanib diphosphate	VEGFR1/2, PDGFRβ, Kit, RET	Anti-angiogenic	Phase II
(AMG706)		GIST (Imatinib resist)	Phase II
		NSCLC	Phase III
Brivanib (BMS-582664)	VEGFR2, FGFR	Solid tumors	Phase I/II
PD173074	VEGFR, FGFR	Solid tumors, anti-angio	Preclinical
Linifanib (M10-963; ABT-869	PDGFRβ, VEGFR2, CSF1R	NSCLC, HCC, RCC	Phase II/III
BAY57-9352	VEGFR2/3, PDGFRβ, Kit	Anti-angiogenic	Phase I
SU11657	TELPDGFRβ, VEGFR, Kit, Flt3	CMML	Preclinical
Regorafenib (BAY 73-4506)	VEGFR-2, Tie-2	RCC; HCC	Phase II
XL-184	VEGFR-2, c-MET, c-Kit, Tie-2	NSCLC, Glioblastoma, lymphoma	Phase II
BIBF1120	VEGFR2, PDGFR, FGFR	Ovarian	Phase II
		Adv solid tumors	Phase I
AZD6244	MEK	NSCLC, pancreas melanoma	Phase II
TSU-68 (SU6668)	VEGFR2, PDGFRβ, FGFR, Kit	Adv solid tumors	Phase I/II/III

CMML: Chronic myelomonocytic leukemia; MDS: Myelodysplastic syndromes; MM: Multiple myeloma; HCC: Hepatocellular carcinoma; RCC: Renal cell carcinoma; NSCLC: Non small cell lung cancer; PDGFR: Platelet derived growth factor receptor; EGFR: Epidermal growth factor receptor; AML: Acute myeloid leukaemia.