Role of receptor tyrosine kinases in gastric cancer: New targets for a selective therapy

Table 1 FDA-licensed tyrosine kinase inhibitors, their targets, modes of action, and clinical use

Agent	Target	Mode of action	Established clinicalapplication
Imatinib mesylate	bcr-abl; PDGFR, c-kit	Kinase inhibitor	CML, GIST, hypereosinophilic syndrome
Gefitinib	erbB1/EGFR	Kinase inhibitor	NSCLC
Erlotinib	erbB1/EGFR	Kinase inhibitor	NSCLC
Cetuximab	erbB1/EGFR	Blocking antibody	Colorectal cancer
Trastuzumab	erbB2/HER	Blocking antibody	Breast cancer
Bevacizumab	VEGF	Neutralizing antibody	Colorectal cancer

Table 2 Therapeutics targeting the EGFR family

Agent	Type	Target	Status
Trastuzumab	Humanized mAb	erbB2	Approved for breast cancer
Pertuzumab	Humanized mAb	erbB2	Phase II trials
Cetuximab	Chimeric mAb	EGFR	Approved for colorectal cancer
Matuzumab	Humanized mAb	EGFR	Phase II trials
Panitumab	Humanized mAb	EGFR	Trials ongoing
Gefitinib	TKI	EGFR	Approved for NSCLC
Erlotinib	TKI	EGFR	Approved for NSCLC
Lapatinib	TKI	EGFR/erbB2	Phase III trial / breast cancer
AEE788	TKI	EGFR/ erbB2/ VEGFR	Phase I trials
CI-1033	Irreversible TKI	EGFR/erbB2	Phase II trials
EKB-569	Irreversible TKI	EGFR/erbB2	Phase II trials
EXEL 7647 / EXEL 0999	TKI	EGFR/ erbB2/ VEGFR	Phase I trials

(incomplete list; modified according to ref. 44)