Colorectal Cancer: From Genetic Landscape to Targeted Therapy

Table 1

Antiangiogenic RTKIs agents under clinical trials investigation in mCRC.

Drugs	Target	Number of participants	Setting	Treatment	Primary outcome measures	Phase	Identifiers
Vatalanib (PTK787/ZK 222584)	VEGFR1-3, FGFR1-3, PDGFRα-β	1168	1st line mCRC	Oxaliplatin/5FU/Leucovorin ± vatalanib	PFS	III	NCT00056459
		855	2nd line mCRC		OS		NCT00056446
Nintedanib (BIBF1120)	VEGFR1-3, FGFR1-3, PDGFRα-β	768	Refractory mCRC	BSC ± Nintedanib	PFS/OS	III	NCT02149108
		54	Refractory mCRC	mFOLFOX6 ± Nintedanib	PFS	III	NCT01362361
Semaxanib (SU5416)	VEGFR2	710	1st line mCRC	Leucovorin and Fluorouracil ± Semaxanib	OS	III	NCT00004252
Brivanib	VEGFR2/FGFR1	750	mCRC kRAS wild-type (refractory)	Cetuximab ± Brivanib	OS	III	NCT00640471
Sunitinib	PDGFR-β, VEGFR2,	768	1st line mCRC	FOLFIRI ± Sunitinib	PFS	III	NCT00457691
Fruquintinib	VEGFR1-3	416	3rd line mCRC	Fruquintinib vs. placebo	OS	III	NCT02314819
Cediranib (AZD2171)	VEGFR1-3	1814	1st line mCRC	Beva + folfox vs. beva + Cediranib	PFS	II/III	NCT00384176
Sorafenib	VEGFR1-3 PDGFR-β BRAF	101	2nd line mCRC	FOLFOX6/FOLFIRI ± Sorafenib	PFS	II	NCT00889343
Vanucizumab	VEGF-A Angiopoietin-2	197	1st line mCRC	mFOLFOX6 + beva vs. mFOLFOX6 + Vancizumab	PFS	II	NCT02141295
Famitinib	VEGFR2-3, c-Kit, PDGFR	154	3rd line advanced mCRC	Famitinib vs. placebo	PFS	II	NCT01762293
Axitinib	VEGFR1-3	70	1st line maintenance therapy	Axitinib alone after FOLFOX/beva in 1st line	PFS	II	NCT01490866
Apatinib	VEGFR2	54	Refractory mCRC progressed after 2nd line	Apatinib alone	PFS	II	NCT03190616

mCRC: metastatic colorectal cancer; 5FU: 5-fluorouracil; FOLFOX: oxaliplatin in combination with 5-fluorouracil and folinic acid; FOLFIRI: irinotecan in combination with 5-fluorouracil and folinic acid; BSC: best supportive care; Beva: bevacizumab; PFS: progression-free survival; OS: overall survival; VEGFR: vascular endothelial growth factor receptor; FGFR: fibroblast growth factor receptor; PDGFR: platelet-derived growth factor receptor.