TABLE 1

List of the EGFR inhibitors, their properties, and clinical indications

Drug NameBrand NameInhibition SiteClinical IndicationBBB Penetration
CSF Penetration Rate (%) in PatientsBrain Penetration Rate (%) in Animal Models
ErlotinibTarcevaATP binding siteNSCLC and pancreatic cancer2.77–5.113.7
GefitinibIressaATP binding siteNSCLC1.07–3.5827
AfatinibGilotrifATP binding siteNSCLC0.7ND
BrigatinibAlunbrigATP binding site of ALKNSCLCNDND
IcotinibConmanaATP binding siteNSCLC0.352.69
CetuximabErbituxDomain III of sEGFRColorectal cancer, NSCLC, head and neck cancerNDND
OsimertinibTagrissoATP binding siteNSCLCND180
LapatinibTykerb and TyverbATP-binding pocket of the EGFR/HER2 protein kinase domainBreast cancerNDND
PanitumumabVectibixExtracellular domain of the EGFRColorectal cancerNDND
NeratinibNerlynxCysteine side chain of EGFR/HER2 protein kinase domainBreast cancerNDND
VandetanibCaprelsaATP binding site: inhibits RET, VEGFR-2, VEGFR-3, EGFR and VEGFR-1Medullary thyroid cancer1.2–2.421
NecitumumabPortrazzaDomain III of sEGFRNSCLCNDND
DacomitinibVizimproATP binding siteNSCLCNDND
AZD3759 (Phase I Clinical Trial)ATP binding siteNSCLC111282

  • ND, not determined. ALK: anaplastic lymphoma kinase; RET: rearranged during transfection; VEGFR: vascular endothelial growth factor