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BIOMARKER:

EGFR overexpression + HER-2 overexpression

i
Other names: ERBB2, CD340, HER-2, HER2, NEU, NGL, V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 2, EGFR, ERBB, ERBB1, Epidermal growth factor receptor
Entrez ID:
7ms
MICROSATELLITE INSTABILITY ASSOCIATED GASTRIC CANCERS ARE ACCOMPANIED WITH OVER-EXPRESSION OF HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR(HER)-2 (IASGO 2023)
The frequencies of MSI and HER-2 over-expression were 21.8% (71/ 326), and 12.6% (41/ 326), respectively. The frequency of EGFR over-expression was 45.4% (148/ 326). In microsatellite stable (MSS) GCs, the over-expression of HER-2 and EGFR of AGCs was more frequent than EGCs (P< 0.01) (P= 0.03).
Microsatellite instability
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HER-2 (Human epidermal growth factor receptor 2) • MSI (Microsatellite instability)
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HER-2 positive • HER-2 overexpression • EGFR overexpression • EGFR positive • EGFR overexpression + HER-2 overexpression
over1year
Multicenter phase Ib/II study of second-line varlitinib and paclitaxel in patients with EGFR/HER2 co-expressing advanced gastric cancer (K-MASTER-13) (ESMO 2022)
Conclusions Varlitinib combined with paclitaxel revealed manageable toxicities and antitumor activity in patients with EGFR/HER2 co-expressing AGC who progressed after first-line chemotherapy. Updated outcomes for ongoing patients and biomarker analysis will be presented.
Clinical • P1/2 data
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • ERBB4 (erb-b2 receptor tyrosine kinase 4)
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HER-2 overexpression • HER-2 expression • EGFR expression • EGFR overexpression • EGFR overexpression + HER-2 overexpression • HER-2-H
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paclitaxel • varlitinib (ASLAN001)
almost2years
Construction of a Mass-Tagged Oligo Probe Set for Revealing Protein Ratiometric Relationship Associated with EGFR-HER2 Heterodimerization in Living Cells. (PubMed, Anal Chem)
Using the assay, the expression level of EGFR-HER2 dimer and its relationship with individual protein monomers were determined in four breast cancer cell lines. We are among the first to obtain the absolute level of protein heterodimer, and this quantitative information may be vital in understanding the molecular basis of cancer.
Journal
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
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HER-2 overexpression • HER-2 expression • EGFR expression • EGFR overexpression • EGFR overexpression + HER-2 overexpression
over2years
An anti-EGFR/anti- HER2 Bispecific Antibody with Enhanced Antitumor Activity Against Acquired Gefitinib-Resistant NSCLC Cells. (PubMed, Protein Pept Lett)
Our results suggest that HECrossMAb may function as a potential therapeutic agent for the treatment of NSCLC overexpressing EGFR and HER2.
Journal
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • FOS (Fos Proto-Oncogene AP-1 Transcription Factor Subunit 2) • MTDH (Metadherin)
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HER-2 overexpression • EGFR overexpression • EGFR overexpression + HER-2 overexpression
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Herceptin (trastuzumab) • Erbitux (cetuximab) • gefitinib
3years
H-Ferritin nanoparticle-mediated delivery of antibodies across a BBB in vitro model for treatment of brain malignancies. (PubMed, Biomater Sci)
Moreover, after crossing the endothelial monolayer, HFn-conjugated mAbs retain their biological activity against targets, as assessed by MTS and ADCC assays. Our data support the use of HFn as efficient carrier to enhance the BBB crossing of mAbs, without affecting their antitumoral activity.
Preclinical • Journal
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
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HER-2 overexpression • EGFR expression • EGFR overexpression • EGFR overexpression + HER-2 overexpression
over3years
[VIRTUAL] Phase Ib trial of varlitinib plus weekly paclitaxel in EGFR/HER2 co-expressing advanced gastric cancer (AGC). (ASCO-GI 2021)
Background: EGFR and HER2 are over-expressed in gastric cancer, and activation of EGFR signaling in HER2-overexpressing gastric cancer can confer resistance to HER2-directed treatment like trastuzumab. The combination of varlitinib 300mg bid and weekly paclitaxel 80mg showed manageable safety profiles and determined as RP2D. Currently, multi-site phase 2 part is now underway.
P1 data
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
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HER-2 overexpression • HER-2 expression • EGFR expression • EGFR overexpression • EGFR overexpression + HER-2 overexpression
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Herceptin (trastuzumab) • paclitaxel • varlitinib (ASLAN001)