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BIOMARKER:

ERBB3 expression

i
Other names: ERBB3, HER3, LCCS2, V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3
Entrez ID:
Related biomarkers:
7d
Assessing the Immunogenicity of pING-hHER3FL (clinicaltrials.gov)
P1, N=24, Recruiting, Herbert Lyerly | Trial completion date: Mar 2025 --> Sep 2025 | Trial primary completion date: Mar 2024 --> Sep 2024
Trial completion date • Trial primary completion date
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ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
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ERBB3 expression
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pING-hHER3FL
10d
HER3 overexpression: a predictive marker for poor prognosis in advanced ALK-positive non-small cell lung cancer treated with ALK inhibitors. (PubMed, Transl Lung Cancer Res)
Combination treatment with lorlatinib and erlotinib significantly reduced HRG1-induced activation of RTK signaling in ALK-positive NSCLC cells. HER3 overexpression has potential as a prognostic marker in ALK-positive NSCLCs, including ALK-TKI naïve and treated cases, especially those with EML4-ALK V1/V2. Assessing HER3 expression may be crucial for treatment planning and outcome prediction in these patients.
Journal • Metastases
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HER-2 (Human epidermal growth factor receptor 2) • ALK (Anaplastic lymphoma kinase) • MET (MET proto-oncogene, receptor tyrosine kinase) • EML4 (EMAP Like 4) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
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HER-2 expression • ALK positive • EGFR overexpression • MET overexpression • EML4-ALK fusion • ALK fusion • ERBB3 expression • MET expression • ERBB3 overexpression • EML4-ALK fusion + ALK positive • EML4-ALK variant 1
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erlotinib • Lorbrena (lorlatinib)
23d
Immunohistochemistry expression of membrane targets for novel therapeutic agents in RET-rearranged NSCLC (AACR 2024)
cMET and TROP2 were frequently expressed in RET+ aNSCLC, EGFR and HER3 were present in a lower proportion, HER2 was rarely found. These markers were not associated with a prognostic or predictive impact on RETi outcomes. The activity of novel therapeutic agents should be evaluated in this setting.
PD(L)-1 Biomarker • IO biomarker
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • MET (MET proto-oncogene, receptor tyrosine kinase) • RET (Ret Proto-Oncogene) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • TACSTD2 (Tumor Associated Calcium Signal Transducer 2)
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PD-L1 expression • HER-2 expression • MET amplification • RET fusion • EGFR expression • ERBB3 expression • MET expression • RET expression
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Dako EGFR pharmDx™ • PATHWAY antiHer2/neu (4B5) Rabbit Monoclonal Primary Antibody
1m
Translational Insights and Overall Survival in the U31402-A-U102 Study of Patritumab Deruxtecan (HER3-DXd) in EGFR-Mutated NSCLC. (PubMed, Ann Oncol)
In patients with EGFR-mutated NSCLC after EGFR TKI and PBC, HER3-DXd treatment was associated with a clinically meaningful OS. The tumor biomarker characterization comprised the first description of potential mechanisms of resistance to HER3-DXd therapy.
Journal
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EGFR (Epidermal growth factor receptor) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
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EGFR mutation • ERBB3 expression • ERBB3 mutation
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patritumab deruxtecan (U3-1402)
2ms
ERBB3 overexpression is enriched in diverse patient populations with castration-sensitive prostate cancer and is associated with a unique AR activity signature. (PubMed, Clin Cancer Res)
In diverse CSPC patient populations, ERBB3 OE was associated with high AR signaling despite low intraprostatic androgen. Mechanistic studies demonstrated a direct link between HER3 and enzalutamide resistance. ERBB3 OE as a biomarker could thus stratify patients for intensification of therapy in castration-sensitive disease, including targeting HER3 directly to improve sensitivity to AR-targeted therapies.
Journal
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ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
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ERBB3 expression • ERBB3 overexpression • AR expression
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enzalutamide capsule • patritumab (U3-1287)
2ms
The Therapeutic Significance of HER3 in Non-small Cell Lung Cancer (NSCLC): A Review Study. (PubMed, Curr Med Chem)
Monoclonal antibodies such as lumretuzumab, seribantumab, and patritumab have shown potential in targeting HER3 to overcome resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs). Additionally, antibody-drug conjugates (ADCs) like HER3-DXd (patritumab deruxtecan) are new drug candidates that have demonstrated selective delivery of cytotoxic chemicals to NSCLC cells by exploiting HER3's widespread expression, minimizing cytotoxicity. This review aims to evaluate the efficacy of current HER3 therapeutics in development and their therapeutic potential in NSCLC, incorporating evidence from clinical trials.
Review • Journal
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HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
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ERBB3 expression
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patritumab deruxtecan (U3-1402) • seribantumab (MM-121) • lumretuzumab (RG7116)
2ms
Enrollment open • Metastases
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • TACSTD2 (Tumor Associated Calcium Signal Transducer 2)
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HER-2 positive • EGFR mutation • HER-2 expression • EGFR T790M • ERBB3 expression • TROP2 expression • ER expression • PGR expression
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patritumab deruxtecan (U3-1402)
3ms
Fluorescent in situ hybridization has limitations in screening NRG1 gene rearrangements. (PubMed, Diagn Pathol)
Considering the high cost of NGS, FISH remains a useful method for screening NRG1 fusions in various types of tumors. This study provides valuable insights into the molecular mechanisms of NRG1 fusion and identifies potential treatment targets for patients suffering from this disease.
Journal
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ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • NRG1 (Neuregulin 1)
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ERBB3 expression • NRG1 fusion • ERBB3 positive • NRG1 rearrangement • NRG1 fusion
4ms
HERTHENA-Lung02: phase III study of patritumab deruxtecan in advanced EGFR-mutated NSCLC after a third-generation EGFR TKI. (PubMed, Future Oncol)
HERTHENA-Lung02 is the first phase III trial to evaluate the safety and efficacy of HER3-DXd versus PBC in patients with progression on a third-generation EGFR TKI. Clinical Trial Registration: NCT05338970 (clinicaltrials.gov); 2021-005879-40 (EudraCT Number).
P3 data • Review • Journal • Metastases
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ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
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EGFR mutation • EGFR expression • ERBB3 expression • ERBB3 mutation
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patritumab deruxtecan (U3-1402)
4ms
ERBB3 expression in racially diverse patients with castration-sensitive prostate cancer and its association with a unique AR activity signature. (ASCO-GU 2024)
In diverse CSPC patient populations, ERBB3 OE was associated with high AR signaling and serum PSA despite low intraprostatic androgen, suggesting ERBB3 OE as a prospective biomarker for ligand-independent AR activation. In this context, ERBB3 OE could stratify patients for intensification of therapy in castration-sensitive disease and emphasizes the importance of biomarker-directed clinical trials with diverse populations.
Clinical
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ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
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ERBB3 expression • ERBB3 overexpression • AR expression
4ms
Therapeutic target biomarkers of patient-derived xenograft models of gastric-type cervical adenocarcinoma. (PubMed, Gynecol Oncol Rep)
In summary, we evaluated biomarkers for therapeutic targets using newly established PDX models of GAS. Frequent HER3 overexpression and HER2 expression in GAS tumors suggest the possibility of new treatments for patients with GAS by targeting HER3 and HER2.
Preclinical • Journal
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HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • ARID1A (AT-rich interaction domain 1A) • MSH6 (MutS homolog 6) • PMS2 (PMS1 protein homolog 2)
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HER-2 overexpression • ERBB3 expression • ERBB3 overexpression • GAST expression
4ms
Prognostic and predictive biomarkers for anti-EGFR monoclonal antibody therapy in RAS wild-type metastatic colorectal cancer: a systematic review and meta-analysis. (PubMed, BMC Cancer)
In RAS wt mCRC patients receiving EGFR-targeted therapy, BRAF mutation is a powerful prognostic and therapy-predictive biomarker, with no effect found for PIK3CA mutation, PTEN mutation or deletion, but the combined biomarker KRAS/NRAS/BRAF/PIK3CA mutations predict resistance to anti-EGFR therapy. Low miR-31-3p expression may have positive prognostic and therapy predictive effects. Evidence on the prognostic and predictive roles of EGFR and its ligands, and HER2/3/4 is insufficient.
Retrospective data • Review • Journal • Metastases
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HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • NRAS (Neuroblastoma RAS viral oncogene homolog) • PTEN (Phosphatase and tensin homolog) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • ERBB4 (erb-b2 receptor tyrosine kinase 4) • EREG (Epiregulin) • MIR31 (MicroRNA 31)
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KRAS mutation • BRAF mutation • NRAS mutation • PIK3CA mutation • HER-2 expression • PTEN mutation • ERBB3 expression • RAS mutation • RAS wild-type • ERBB3 mutation • PIK3CA mutation + PTEN mutation • AREG expression • ERBB4 expression • KRAS deletion
5ms
Coordinate transcriptional regulation of ErbB2/3 by C-terminal binding protein 2 signals sensitivity to ErbB2 inhibition in pancreatic adenocarcinoma. (PubMed, Oncogenesis)
ErbB3 expression in human PDAC cell lines was similarly dependent on CtBP2 and depletion of ErbB3 in a human PDAC cell line severely attenuated growth, demonstrating the critical role of ErbB3 signaling in maintaining PDAC cell growth. Sensitivity to the ErbB2-targeted tyrosine kinase inhibitor lapatinib, but not the EGFR-targeted agent erlotinib, varied in proportion to the level of ErbB3 expression in mouse and human PDAC cells, suggesting that an ErBb2 inhibitor can effectively leverage CtBP2-driven transcriptional activation of physiologic ErbB2/3 expression and signaling in PDAC cells for therapeutic benefit.
Journal
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ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • NRG1 (Neuregulin 1) • CTBP2 (C-Terminal Binding Protein 2)
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HER-2 expression • ERBB3 expression
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erlotinib • lapatinib
5ms
Suppression of GATA2/3-FOXA1-HER3 Axis by Histone Deacetylase (HDAC) Inhibitors shows Antitumor Activity in Basal-like Breast Cancer (SABCS 2023)
We recently found that panobinostat and romidepsin potently induced TNBC cell growth inhibition and apoptosis via downregulation of HER3 through suppression of forkhead box protein A1 (FOXA1), a pioneering transcription factor...Notably, the combination of HDACis with an EGFR inhibitor (gefitinib) or an anti-HER3 antibody synergistically enhanced the anti-survival effects on BLBC cells... HDACis exhibit potent inhibitory effects on BLBC cells via downregulation of GATA2/3-mediated repression of FOXA1 gene transcription, which in turn suppresses HER3 expression and signaling. Our findings indicate that epigenetic targeting of the GATA2/3-FOXA1-HER3 axis may be an effective therapeutic strategy for the eradication of BLBC tumors.
Epigenetic controller
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ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • FOXA1 (Forkhead Box A1) • GATA2 (GATA Binding Protein 2)
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ERBB3 expression
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gefitinib • Farydak (panobinostat) • Istodax (romidepsin)
5ms
Novel Metrics of HER2 Heterogeneity in HER2-Positive and HER2-Low Breast Cancer via High Dimensional Multiplexed Immunofluorescence Spatial Profiling (SABCS 2023)
We present novel metrics of HER2 heterogeneity via HDmIF, which offer detailed characterization of the diversity of HER2 expression in a large, clinically-annotated cohort with long-term follow-up. Identification of a strong association between immunophenotype and RFS supports further investigation of the highly immune activated subsets of ER-/HER2+ breast cancer. Strong correspondence of HER2 IF and IHC and our HAIQu methodology offers a pathway to translation of HER2het metrics to clinical practice.
PD(L)-1 Biomarker • IO biomarker
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • ER (Estrogen receptor) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
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HER-2 positive • HER-2 expression • PD-L1 underexpression • HR negative • ERBB3 expression • PD-1-L • PD-L1-L
5ms
TAS0612, a novel RSK, AKT, and S6K inhibitor, exhibits antitumor effects in preclinical tumor models. (PubMed, Mol Cancer Ther)
Additionally, TAS0612 demonstrated the persistence of blockade of downstream growth and anti-apoptotic signals, despite activation of upstream effectors in the signaling pathway and FoxO-dependent re-expression of HER3. In conclusion, TAS0612 with RSK/AKT/S6K inhibitory activity may provide a novel therapeutic strategy for cancer patients to improve clinical responses and overcome resistance mechanisms.
Preclinical • Journal
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • PTEN (Phosphatase and tensin homolog) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
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KRAS mutation • BRAF mutation • ERBB3 expression
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TAS0612
5ms
A Study of YL202 in Selected Patients With Advanced Solid Tumors (clinicaltrials.gov)
P2, N=200, Not yet recruiting, MediLink Therapeutics (Suzhou) Co., Ltd.
New P2 trial • Metastases
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HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
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HER-2 positive • ERBB3 expression
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BNT326
5ms
HER-3 surface expression increases in advanced colorectal cancer representing a potential therapeutic target. (PubMed, Cell Death Discov)
Overall, this study confirms that surface HER-3 is highly expressed in CRC and reveals that HER-3 expression increases in metastatic CRC patients compared to early stage. Importantly, the results suggest that HER-3 has a prognostic and therapeutic value in patients developing MM liver metastases.
Journal • Metastases
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HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
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ERBB3 expression
5ms
Assessing the Immunogenicity of pING-hHER3FL (clinicaltrials.gov)
P1, N=24, Recruiting, Herbert Lyerly | Trial completion date: Dec 2024 --> Mar 2025 | Trial primary completion date: Dec 2023 --> Mar 2024
Trial completion date • Trial primary completion date
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ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
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ERBB3 expression
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pING-hHER3FL
5ms
Systematic Characterization of Antibody-Drug Conjugate Targets in Central Nervous System Tumors. (PubMed, Neuro Oncol)
CNS tumors exhibit subtype-specific expression of ADC targets including several FDA-approved for other indications. Clinical trials of ADCs in CNS tumors may therefore be warranted.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • CLDN18 (Claudin 18) • CD276 (CD276 Molecule) • CLDN6 (Claudin 6) • NECTIN4 (Nectin Cell Adhesion Molecule 4) • TACSTD2 (Tumor Associated Calcium Signal Transducer 2)
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HER-2 expression • ERBB3 expression • TROP2 expression • CLDN6 expression
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Enhertu (fam-trastuzumab deruxtecan-nxki)
5ms
Stromal-derived NRG1 enables oncogenic KRAS bypass in pancreas cancer. (PubMed, Genes Dev)
Genetic depletion or pharmacological inhibition of ERBB2/3 or NRG1 abolished KRAS* bypass and synergized with KRAS inhibitors in combination treatments in mouse and human PDAC models. Thus, we found that CAFs can contribute to KRAS* inhibitor therapy resistance via paracrine mechanisms, providing an actionable therapeutic strategy to improve the effectiveness of KRAS* inhibitors in PDAC patients.
Journal • Stroma
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KRAS (KRAS proto-oncogene GTPase) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • NRG1 (Neuregulin 1)
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KRAS mutation • HER-2 expression • ERBB3 expression
5ms
Clinico-Pathological and Prognostic Significance of a Combination of Tumor Biomarkers in Iranian Patients With Breast Cancer. (PubMed, Clin Breast Cancer)
ROR1 and HER3 displayed significant association with different clinic-pathological features and in addition to the other tumor biomarkers could be considered as diagnostic and prognostic biomarkers in breast cancer patients.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • TP53 (Tumor protein P53) • PGR (Progesterone receptor) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • ROR1 (Receptor Tyrosine Kinase Like Orphan Receptor 1)
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HER-2 expression • ERBB3 expression • ROR1 expression • TP53 expression
5ms
Association of the m A reader IGF2BP3 with tumor progression and brain-specific metastasis in breast cancer. (PubMed, Cancer)
As an m A reader, IGF2BP3 is dysregulated and implicated in various cancers but its role in breast cancer has not been fully clarified. In this study, we found that IGF2BP3 was upregulated in breast cancer and IGF2BP3 expression increased gradually during breast cancer progression. IGF2BP3 expression exerted no effect on the overall survival and breast cancer-specific survival of breast cancer patients; however, IGF2BP3-positive patients were more likely to develop distant metastasis than IGF2BP3-negative patients. In addition, IGF2BP3 was associated with brain-specific metastasis in breast cancer patients. These findings warrant further investigation because they provide a rationale for novel predictive or therapeutic approaches.
Journal • PD(L)-1 Biomarker • IO biomarker
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HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • IGF2BP3 (Insulin Like Growth Factor 2 MRNA Binding Protein 3)
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ERBB3 expression
6ms
EFFECTS OF HEPATOCYTE-SPECIFIC DELETION OF EGFR IN A DIET-INDUCED NAFLD MOUSE MODEL (AASLD 2023)
In our previous study, we found that chemical inhibition of EGFR utilizing Canertinib, dramatically reduced hepatocyte steatosis, liver injury, and fibrosis, in a murine fast-food diet (FFD) model, indicating a potential role for EGFR in regulating NAFLD... The hepatocyte-specific deletion of EGFR alters lipid metabolism and fibrosis signaling in a murine FFD model of NAFLD, but is much less effective compared to pharmacological inhibition of EGFR.
Preclinical
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • FASN (Fatty acid synthase) • PPARG (Peroxisome Proliferator Activated Receptor Gamma)
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ERBB3 expression
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canertinib (CI-1033)
6ms
Patritumab Deruxtecan (HER3-DXd), a Human Epidermal Growth Factor Receptor 3-Directed Antibody-Drug Conjugate, in Patients With Previously Treated Human Epidermal Growth Factor Receptor 3-Expressing Metastatic Breast Cancer: A Multicenter, Phase I/II Trial. (PubMed, J Clin Oncol)
HER3-DXd demonstrated a manageable safety profile and durable efficacy in heavily pretreated patients across clinical subtypes. These data warrant further evaluation of HER3-DXd in patients with HER3-expressing metastatic breast cancer.
P1/2 data • Journal • Metastases
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HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
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HER-2 positive • HR positive • HER-2 negative • ERBB3 expression
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patritumab deruxtecan (U3-1402)
6ms
Potential impact of HercepTest™ mAb PharmDx (Dako Omnis) (ge001) in breast cancer diagnosis. (PubMed, Pol J Pathol)
We have reason to believe that the new antibody will reduce the diagnostic time and avoid unnecessary costs. Due to the small study group, further investigation is needed.
Journal
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HER-2 overexpression • HER-2 amplification • ERBB3 expression
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HercepTest • PATHWAY antiHer2/neu (4B5) Rabbit Monoclonal Primary Antibody
6ms
Enrollment closed
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
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ER positive • HER-2 negative • ERBB3 expression • PGR positive
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paclitaxel • doxorubicin hydrochloride • cyclophosphamide • letrozole • epirubicin • patritumab deruxtecan (U3-1402)
6ms
HER3 functions as an effective therapeutic target in triple negative breast cancer to potentiate the antitumor activity of gefitinib and paclitaxel. (PubMed, Cancer Cell Int)
Our data demonstrate that increased HER3 is an effective therapeutic target for TNBC and our anti-HER3 mAb (4A7) may enhance the efficacy of gefitinib or paclitaxel in TNBC.
Journal
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EGFR (Epidermal growth factor receptor) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • CXCR4 (Chemokine (C-X-C motif) receptor 4) • CXCL12 (C-X-C Motif Chemokine Ligand 12)
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ERBB3 expression
|
gefitinib • paclitaxel • R3Mab
7ms
A Study of U3-1402 (Patritumab Deruxtecan) in Subjects With Metastatic Breast Cancer (clinicaltrials.gov)
P2, N=121, Recruiting, SCRI Development Innovations, LLC | Trial completion date: Nov 2023 --> Nov 2025 | Trial primary completion date: Nov 2023 --> Nov 2025
Trial completion date • Trial primary completion date • Metastases
|
ER (Estrogen receptor) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
|
HER-2 positive • HER-2 negative • HER-2 expression • ERBB3 expression
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patritumab deruxtecan (U3-1402)
7ms
HERTHENA-Lung01, a Phase II Trial of Patritumab Deruxtecan (HER3-DXd) in Epidermal Growth Factor Receptor-Mutated Non-Small-Cell Lung Cancer After Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor Therapy and Platinum-Based Chemotherapy. (PubMed, J Clin Oncol)
After tumor progression with EGFR TKI therapy and PBC in patients with EGFR-mutated NSCLC, HER3-DXd once every 3 weeks demonstrated clinically meaningful efficacy with durable responses, including in CNS metastases. A phase III trial in EGFR-mutated NSCLC after progression on an EGFR TKI is ongoing (HERTHENA-Lung02; ClinicalTrials.gov identifier: NCT05338970).
P2 data • Journal
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
|
EGFR mutation • ERBB3 expression • ERBB3 mutation
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Tagrisso (osimertinib) • patritumab deruxtecan (U3-1402)
7ms
AMT-562, a novel HER3-targeting antibody drug conjugate, demonstrates a potential to broaden therapeutic opportunities for HER3-expressing tumors. (PubMed, Mol Cancer Ther)
Pharmacokinetics and safety profiles of AMT-562 were favorable and the highest dose lacking severe toxicity was 30 mg/kg in cynomolgus monkeys. AMT-562 has potential to be a superior HER3-targeting ADC with a higher therapeutic window that can overcome resistance to generate higher percentage and more durable responses in U3-1402-insensitive tumors.
Journal
|
EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase)
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ERBB3 expression
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patritumab deruxtecan (U3-1402) • AMT-562
7ms
Human Epidermal Growth Factor Receptor 2/Human Epidermal Growth Factor Receptor 3 PET Imaging: Challenges and Opportunities. (PubMed, PET Clin)
Numerous PET radiopharmaceuticals have been developed to evaluate (or target for therapy) HER2 and HER3 expression. This review seeks to inform on challenges and opportunities in HER2 and HER3 PET imaging in both clinical and preclinical settings.
Review • Journal
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HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
|
HER-2 expression • ERBB3 expression
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Herceptin (trastuzumab) • Perjeta (pertuzumab)
7ms
Androgen receptor transcriptional activity is required for heregulin-1β-mediated nuclear localization of the HER3/ErbB3 receptor tyrosine kinase. (PubMed, J Biol Chem)
Mutations of ErbB3's kinase domain did not affect its localization but was responsible for cell viability in CRPC cells. Taken together, we conclude that AR expression regulated ErbB3 expression, its transcriptional activity suppressed ErbB3 nuclear translocation, and HRG binding to ErbB3 promoted it.
Journal
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EGFR (Epidermal growth factor receptor) • AR (Androgen receptor) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
|
ERBB3 expression • ERBB3 mutation • AR expression
7ms
Keeping it in the family: HER3 as a target in brain metastases. (PubMed, Clin Cancer Res)
HER3-targeting antibody-drug conjugates have demonstrated efficacy in HER3-expressing metastatic breast cancer and NSCLC. Thus, HER3 expression by IHC may be a biomarker for development of HER3-targeting BM-specific therapeutics.
Journal
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ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
|
ERBB3 expression
8ms
HER3 targeting augments the efficacy of panobinostat in claudin-low triple-negative breast cancer cells. (PubMed, NPJ Precis Oncol)
Tumor xenograft models were used to test the in vivo antitumor activity of panobinostat alone or its combinations with gefitinib, an EGFR-tyrosine kinase inhibitor (TKI). Upregulation of HER3 compromises the efficacy of panobinostat in CL TNBC. Inactivation of HER3 combined with panobinostat represents a practical approach to combat CL TNBC.
Journal
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EGFR (Epidermal growth factor receptor) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
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ERBB3 expression
|
gefitinib • Farydak (panobinostat)
8ms
HERTHENA-Lung01: a phase II study of patritumab deruxtecan (HER3-DXd) in previously treated metastatic EGFR-mutated NSCLC. (PubMed, Future Oncol)
HERTHENA-Lung01 is a global, registrational, phase II trial further evaluating HER3-DXd in previously treated advanced EGFR-mutated NSCLC. Clinical Trial Registration: NCT04619004 (ClinicalTrials.gov); 2020-000730-17 (EudraCT).
P2 data • Review • Journal • Metastases
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EGFR (Epidermal growth factor receptor) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
|
EGFR mutation • EGFR expression • EGFR overexpression • ERBB3 expression • ERBB3 mutation
|
patritumab deruxtecan (U3-1402)
8ms
Phase I study of SHR-A2009, a HER3-targeted ADC, in advanced solid tumors (ESMO 2023)
Conclusions SHR-A2009 showed a tolerable safety profile and encouraging anti-tumor activity in pts with heavily pretreated advanced solid tumors. The trial is ongoing to assess SHR-A2009 at higher doses and in selected cancer types (NSCLC and other solid tumors).
P1 data • Metastases
|
ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
|
EGFR mutation • ERBB3 expression
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SHR-A2009
8ms
Combining Anti-HER3 Antibody, HMBD-001, with EGFR Inhibition and Chemotherapy may Improve Treatment Outcomes in SqNSCLC (IASLC-WCLC 2023)
Potency of HMBD-001 to inhibit tumor growth as monotherapy or in combination with cetuximab and/or docetaxel was evaluated using murine CDX and PDX models. An analysis of copy number variations and expression of genes in Chr3q, Chr3p and Chr7p confirms that genes involved in HER3 signaling are frequently amplified and have higher expression in squamous compared to non-squamous NSCLC. Several genetic alterations in sqNSCLC lead to HER3 and EGFR pathway activation. HMBD-001, a potent anti-HER3 mAb, in combination with EGFR inhibition and chemotherapy, has the potential to greatly improve clinical outcomes following immune-chemotherapy. Hummingbird Bioscience plans to initiate Phase Ib clinical trials in biomarker selected populations of sqNSCLC in H2, 2023.
Clinical • IO biomarker
|
PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
|
EGFR amplification • EGFR overexpression • ERBB3 expression • PIK3CA amplification
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Erbitux (cetuximab) • docetaxel • HMBD-001 • R3Mab
8ms
HER3 Expression in Archived Tissue Samples from Patients with NSCLC Across Various Genomic Subtypes and Characteristics (IASLC-WCLC 2023)
This study found that HER3 membrane was expressed in 98% of NSCLC tumors across all included genomic subtypes. HER3 expression was seen in patients regardless of prior treatment with systemic anticancer therapy. The observation that HER3 membrane is broadly expressed in NSCLC confirms results of previous studies indicating that targeting this cell surface protein might be broadly applicable to patients with diverse subtypes of NSCLC.
Clinical • PD(L)-1 Biomarker • IO biomarker
|
EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • ALK (Anaplastic lymphoma kinase) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
|
PD-L1 expression • KRAS mutation • EGFR mutation • KRAS G12C • EGFR exon 20 insertion • ALK rearrangement • ERBB3 expression • KRAS G12 • EGFR exon 20 mutation • ERBB3 mutation
8ms
HER3/Akt/mTOR pathway is a key therapeutic target for the reduction of triple‑negative breast cancer metastasis via the inhibition of CXCR4 expression. (PubMed, Int J Mol Med)
Furthermore, treatment of metastatic TNBC cells with everolimus inhibited their migration, invasion and metastasis by decreasing CXCR4 expression. Thus, targeting the HER3/Akt/mTOR pathway opens up a new avenue for the development of therapeutics against TNBC metastasis; in addition, everolimus may prove to be an effective therapeutic agent for the suppression of TNBC metastasis.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • CXCR4 (Chemokine (C-X-C motif) receptor 4)
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ERBB3 expression • CXCR4 expression
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everolimus