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. Author manuscript; available in PMC: 2018 Jul 11.
Published in final edited form as: Oncogene. 2018 Jan 11;37(12):1561–1575. doi: 10.1038/s41388-017-0045-7

Table 2.

EGFR/EGFRvIII-targeted therapies

EGFR/EGFRvIII targeted therapy Effects in GBM References
Inhibitors 1st generation Gefitinib Not very effective in GBM clinical trials. 108109
Erlotinib
Lapatinib
2nd generation Afatinib Good safety but limited single-reagent activity on GBM patients. Promising in combination with TMZ in a case report. 115
Dacomitinib Promising in pre-clinical models. 116
3rd generation Rociletinib Effects on GBM to be evaluated.
AZD9291 In phase I/II clinical trial
Antibodies Targeting the L2 domain of EGFR Cetuximab Not very effective in GBM clinical trials. 119122
Panitumumab
Nimotuzumab
Targeting the EGFRvIII-specific sequence mAB806 Good safety. Anti-GBM effects to be evaluated. 123
Toxin or radioactive isotope conjugated 125I mAB425 When used singly or in combination with TMZ, significantly prolonged patient survival. 124
BisAbs bscEGFRvIIIxCD3 Promising in pre-clinical models. 126
Vaccines Rindopepimut (CDX110) Significantly prolonged patient survival when co-administrated with TMZ. Failed phase III trial. 130133
CARs CAR-T cells targeting EGFRvIII Promising in pre-clinical models. Currently under phase I clinical trial. 134136
RNA-based therapies Antisense oligonucleotides, RNAi, ribozymes and adjuvant miRNA based therapy Feasibility to be further evaluated in pre-clinical models. 137138