Topic Highlight
Copyright ©The Author(s) 2016.
World J Gastroenterol. Jul 14, 2016; 22(26): 5896-5908
Published online Jul 14, 2016. doi: 10.3748/wjg.v22.i26.5896
Table 2 Molecularly-targeted drugs evaluated in clinical trials for gastric cancer
Drug nameTypeMolecular effectPrimary cancer which it is usedEffect on gastric cancer in studies
Trastuzumab[17]Fully humanized monoclonal antibodyAnti-HER-2 receptor proteinBreast cancerEffective
First approved molecular therapy
Sunitinib[17]Oral multi-tyrosine kinase inhibitorAnti- VEGF, PDGF and KIT receptorsGastrintestinal stromal tumors, renal cell carcinoma and pancreatic neuroendocrine tumorsLimited therapeutic effect
Bevacizumab[131,132]Fully humanized monoclonal antibodyAnti-VEGFColorectal cancer, non small cell lung cancer and breast cancerGives better survival in peritoneal metastatic disease or combined with anti-HER-2 therapy
Lapatinib[17]Oral dual tyrosine kinase inhibitorAnti-EGFR and HER-2HER-2 positive advanced breast cancerNot effective
Everolimus[17]Oral mTOR inhibitorAnti-intracellular receptor FKBP12Renal cancerEffective in advanced gastric cancer
Ramucirumab[17]Fully humanized IgG1 monoclonal antibodyAnti-VEGFR-2Gastric and lung cancerEffective approved
Cetuximab[17]Monoclonal IgG antibodyAnti-EGFRColorectal cancerNot effective
Panitumumab[17]Fully humanized IgG2 monoclonal antibodyAnti-EGFRAdvanced colorectal cancerNot effective
Gefitinib[133]Tyrosine kinase inhibitorAnti- EGFREGFR mutation positive lung cancerNot effective
Matuzumab[134]Fully humanized monoclonal antibodyAnti-EGFRNot yet approved in any other indicationModerately effective
Tivantinib[94]Tyrosine kinase inhibitorSelective c-Met inhibitorNot yet approved in any other indicationmoderately effective
Onartuzumab[135]Fully humanized monoclonal antibodyAnti-extracellulardomain of the tyrosine kinase receptor METNot yet approved in any other indicationNot effective
Regorafenib[73]Tyrosine kinase inhibitorAnti-angiogenic factorGastrointestinal stromal tumorsFound effective when tested on xenograft model with GC
Pembrolizumab[100]Monoclonal antibodyPD-1 inhibitorAdvanced melanoma, advanced lung cancerPromising phase IB results.
Phase III results are awaited
Apatinib[72]Tyrosine kinase inhibitorMultikinase inhibitorNot yet approved in any other indicationShown to be effective in a phase III Chinese study