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Ref Type Journal Article
PMID (31588020)
Authors Robichaux JP, Elamin YY, Vijayan RSK, Nilsson MB, Hu L, He J, Zhang F, Pisegna M, Poteete A, Sun H, Li S, Chen T, Han H, Negrao MV, Ahnert JR, Diao L, Wang J, Le X, Meric-Bernstam F, Routbort M, Roeck B, Yang Z, Raymond VM, Lanman RB, Frampton GM, Miller VA, Schrock AB, Albacker LA, Wong KK, Cross JB, Heymach JV
Title Pan-Cancer Landscape and Analysis of ERBB2 Mutations Identifies Poziotinib as a Clinically Active Inhibitor and Enhancer of T-DM1 Activity.
Journal Cancer cell
Vol 36
Issue 4
Date 2019 Oct 14
URL
Abstract Text We characterized the landscape and drug sensitivity of ERBB2 (HER2) mutations in cancers. In 11 datasets (n = 211,726), ERBB2 mutational hotspots varied across 25 tumor types. Common HER2 mutants yielded differential sensitivities to eleven EGFR/HER2 tyrosine kinase inhibitors (TKIs) in vitro, and molecular dynamics simulations revealed that mutants with a reduced drug-binding pocket volume were associated with decreased affinity for larger TKIs. Overall, poziotinib was the most potent HER2 mutant-selective TKI tested. Phase II clinical testing in ERBB2 exon 20-mutant non-small cell lung cancer resulted in a confirmed objective response rate of 42% in the first 12 evaluable patients. In pre-clinical models, poziotinib upregulated HER2 cell-surface expression and potentiated the activity of T-DM1, resulting in complete tumor regression with combination treatment.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
ERBB2 D769H missense unknown ERBB2 (HER2) D769H lies within the protein kinase domain of the Erbb2 (Her2) protein (UniProt.org). D769H confers resistance to selected tyrosine kinase inhibitors (PMID: 31588020), results in constitutive phosphorylation of Erbb2 (Her2), activation of downstream signaling, is transforming in cell culture (PMID: 29967253, PMID: 31588020), and promotes tumor formation in xenograft models (PMID: 23220880), however, in another study, induces similar cell proliferation and cell viability to wild-type Erbb2 (Her2) in two different cell lines (PMID: 29533785), and therefore, its effect on Erbb2 (Her2) protein function is unknown. Y
ERBB2 D769N missense unknown ERBB2 (HER2) D769N lies within the protein kinase domain of the Erbb2 (Her2) protein (UniProt.org). D769N confers resistance to selected tyrosine kinase inhibitors, results in activation of Erbb2 (Her2) downstream signaling, and is transforming in culture in one study (PMID: 31588020), but results in similar cell proliferation and viability levels as wild-type Erbb2 (Her2) in another study (PMID: 29533785), and therefore, its effect on Erbb2 (Her2) protein function is unknown. Y
ERBB2 D769Y missense gain of function ERBB2 (HER2) D769Y lies within the protein kinase domain of the Erbb2 (Her2) protein (UniProt.org). D769Y results in constitutive phosphorylation of Erbb2 (Her2), increased downstream signaling, is transforming in cell culture (PMID: 23220880, PMID: 29967253, PMID: 31588020), and confers resistance to selected tyrosine kinase inhibitors (PMID: 31588020). Y
ERBB2 G776delinsLC indel gain of function ERBB2 (HER2) G776delinsLC results in a deletion of a glycine (G) at amino acid 776 within the protein kinase domain of the Erbb2 (Her2) protein, combined with the insertion of a leucine (L) and a cystine (C) at the same site (UniProt.org). G776delinsLC leads to constitutive activation of Erbb2 (Her2), increased downstream signaling, is transforming in cell culture (PMID: 26545934, PMID: 29967253, PMID: 31588020), and confers resistance to selected tyrosine kinase inhibitors (PMID: 31588020). Y
ERBB2 G776delinsVC indel gain of function ERBB2 (HER2) G776delinsVC results in a deletion of a glycine (G) at amino acid 776 within the protein kinase domain of the Erbb2 (Her2) protein, combined with the insertion of a valine (V) and a cystine (C) at the same site (UniProt.org). G776delinsVC leads to constitutive activation of Erbb2 (Her2), increased downstream signaling (PMID: 26545934, PMID: 31588020), is transforming in cell culture (PMID: 29533785, PMID: 29967253), and confers resistance to selected tyrosine kinase inhibitors (PMID: 31588020). Y
ERBB2 G776delinsVV indel gain of function ERBB2 (HER2) G776delinsVV results in a deletion of a glycine (G) at amino acid 776 within the protein kinase domain of the Erbb2 (Her2) protein, combined with the insertion of two valines (V) at the same site (UniProt.org). G776delinsVV results in constitutive ERbb2 (Her2) phosphorylation, activation of downstream signaling, is transforming in cell culture (PMID: 29686424, PMID: 31588020), and confers resistance to selected tyrosine kinase inhibitors (PMID: 31588020). Y
ERBB2 G778_P780dup duplication gain of function ERBB2 (HER2) G778_P780dup (also referred to as P780_Y781insGSP and V777_G778insGSP) indicates the insertion of 3 duplicate amino acids, glycine (G)-778 through proline (P)-781, in the protein kinase domain of the Erbb2 (Her2) protein (UniProt.org). G778_P780dup results in constitutive activation of Erbb2 (Her2), increased downstream signaling, is transforming in cell culture (PMID: 23220880, PMID: 31588020), and confers resistance to selected tyrosine kinase inhibitors (PMID: 31588020). Y
ERBB2 G778_S779insLPS insertion gain of function ERBB2 (HER2) G778_S779insLPS results in the insertion of three amino acids in the protein kinase domain of the Erbb2 (Her2) protein between amino acids 778 and 779 (UniProt.org). G778_S779insLPS results in constitutive phosphorylation of Erbb2 (Her2), activation of downstream signaling, is transforming in cell culture, and confers resistance to selected tyrosine kinase inhibitors (PMID: 31588020). Y
ERBB2 L755P missense gain of function ERBB2 (HER2) L755P lies within the protein kinase domain of the Erbb2 (Her2) protein (UniProt.org). L755P results in increased phosphorylation of Erbb2 (Her2), activation of downstream signaling, is transforming in cell culture (PMID: 22046346, PMID: 29967253, PMID: 31588020), and confers resistance to selected tyrosine kinase inhibitors (PMID: 31588020). Y
ERBB2 L755S missense gain of function ERBB2 (HER2) L755S lies within the protein kinase domain of the Erbb2 (Her2) protein (UniProt.org). L755S results in increased phosphorylation of Erbb2 (Her2), activation of downstream signaling, is transforming in cell culture (PMID: 29967253, PMID: 31588020), and is associated with resistance to Erbb2 (Her2)-targeted therapies (PMID: 22046346, PMID: 28487443). Y
ERBB2 L786V missense gain of function ERBB2 (HER2) L786V lies within the protein kinase domain of the Erbb2 (Her2) protein (UniProt.org). L786V results in constitutive phosphorylation of Erbb2 (Her2), increased downstream signaling, is transforming in cell culture, and confers resistance to selected tyrosine kinase inhibitors (PMID: 31588020). Y
ERBB2 L869R missense gain of function ERBB2 (HER2) L869R lies within the protein kinase domain of the Erbb2 (Her2) protein (UniProt.org). L869R results in constitutive Erbb2 (Her2) phosphorylation, activation of downstream signaling, transformation of cultured cells (PMID: 31588020), enhanced tumor formation and metastasis in animal models (PMID: 27900369), and confers resistance to selected tyrosine kinase inhibitors (PMID: 31588020). Y
ERBB2 R678Q missense unknown ERBB2 (HER2) R678Q lies within the juxtamembrane domain of the Erbb2 (Her2) protein (PMID: 30449325). The functional effect of R678Q is conflicting, as it demonstrates phosphorylation levels and transformation potential comparable to wild-type Erbb2 (Her2) protein in cell culture and xenograft models (PMID: 29533785, PMID: 23220880), however, in other studies, results in increased phosphorylation of Erbb2 (Her2) and activation of downstream signaling (PMID: 24971884), and is transforming in culture (PMID: 30449325, PMID: 31588020). Y
ERBB2 V754M missense gain of function ERBB2 (HER2) V754M lies within the protein kinase domain of the Erbb2 (Her2) protein (UniProt.org). V754M results in increased Erbb2 (Her2) phosphorylation and activation of downstream signaling, and is transforming in cell culutre (PMID: 31588020).
ERBB2 V773M missense unknown ERBB2 (HER2) V773M lies within the protein kinase domain of the Erbb2 (Her2) protein (UniProt.org). V773M results in activation of Erbb2 downstream signaling, is transforming in cell culture, and confers resistance to selected tyrosine kinase inhibitors (PMID: 31588020), but also demonstrates similar levels of cell proliferation and viability as wild-type Erbb2 (Her2) (PMID: 29533785), and therefore, its effect on Erbb2 (Her2) protein function is unknown. Y
ERBB2 V777L missense gain of function ERBB2 (HER2) V777L lies within the protein kinase domain of the Erbb2 (Her2) protein (UniProt.org). V777L results in increased Erbb2 (Her2) activity, activation of downstream signaling, transformation of cultured cells (PMID: 29967253, PMID: 31588020), increased tumor growth in xenograft models (PMID: 23220880), and confers resistance to selected tyrosine kinase inhibitors (PMID: 31588020). Y
ERBB2 V842I missense unknown ERBB2 (HER2) V842I lies within the protein kinase domain of the Erbb2 (Her2) protein (UniProt.org). V842I confers resistance to selected tyrosine kinase inhibitors (PMID: 31588020), results in increased Erbb2 (Her2) activity, downstream pathway activation, and transformation of cultured cells (PMID: 23220880, PMID: 31588020), however, in another study, demonstrates similar cell proliferation and viability levels to wild-type Erbb2 (Her2) in two different cell lines (PMID: 29533785), and therefore, its effect on Erbb2 (Her2) protein function is unknown. Y
ERBB2 Y772_A775dup duplication gain of function ERBB2 (HER2) Y772_A775dup (also referred to as A775_G776insYVMA, M774_A775insAYVM, and E770delinsEAYVM) indicates the insertion of 4 duplicate amino acids, tyrosine (Y)-772 through alanine (A)-775, in the protein kinase domain of the Erbb2 (Her2) protein (UniProt.org). Y772_A775dup results in the constitutive phosphorylation of Erbb2 (Her2), activation of downstream signaling, is transforming in cell culture (PMID: 17311002, PMID: 31588020), and confers resistance to selected tyrosine kinase inhibitors (PMID: 31588020). Y
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Imbruvica (ibrutinib) in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup Advanced Solid Tumor resistant Nazartinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup were resistant to Nazartinib (EGF816) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, Gilotrif (afatinib) inhibited survival of transformed cells expressing ERBB2 (HER2) G776delinsLC in culture (PMID: 31588020). 31588020
ERBB2 V842I Advanced Solid Tumor sensitive Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) V842I in culture (PMID: 31588020). 31588020
ERBB2 L786V Advanced Solid Tumor sensitive Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) L786V in culture (PMID: 31588020). 31588020
ERBB2 D769H Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor sensitive Nazartinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Nazartinib (EGF816) in culture (PMID: 31588020). 31588020
ERBB2 L755S Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) L755S in culture (PMID: 31588020). 31588020
ERBB2 D769H Advanced Solid Tumor sensitive Nazartinib Preclinical - Cell culture Actionable In a preclinical study, Nazartinib (EGF816) inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 V777L Advanced Solid Tumor sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, Gilotrif (afatinib) inhibited survival of transformed cells expressing ERBB2 (HER2) V777L in culture (PMID: 31588020). 31588020
ERBB2 D769Y Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) D769Y were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor resistant Nazartinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Nazartinib (EGF816) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsLC were resistant to Imbruvica (ibrutinib) in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Vizimpro (dacomitinib) in culture (PMID: 31588020). 31588020
ERBB2 D769N Advanced Solid Tumor sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, Gilotrif (afatinib) inhibited survival of transformed cells expressing ERBB2 (HER2) D769N in culture (PMID: 31588020). 31588020
ERBB2 V773M Advanced Solid Tumor resistant Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V773M were resistant to Tagrisso (osimertinib) in culture (PMID: 31588020). 31588020
ERBB2 V842I Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V842I were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor resistant Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Vizimpro (dacomitinib) in culture (PMID: 31588020). 31588020
ERBB2 L755S Advanced Solid Tumor sensitive Osimertinib Preclinical - Cell culture Actionable In a preclinical study, Tagrisso (osimertinib) inhibited survival of transformed cells expressing ERBB2 (HER2) L755S in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup lung non-small cell carcinoma sensitive Ado-trastuzumab emtansine + Poziotinib Preclinical - Pdx Actionable In a preclinical study, Poziotinib (HM781-36B) and Kadcyla (ado-trastuzumab emtansine) combination treatment resulted in sustained tumor regression in patient-derived xenograft models of non-small cell lung cancer harboring ERBB2 (HER2) Y772_A775dup (PMID: 31588020). 31588020
ERBB2 D769H Advanced Solid Tumor sensitive Osimertinib Preclinical - Cell culture Actionable In a preclinical study, Tagrisso (osimertinib) inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 L786V Advanced Solid Tumor sensitive Nazartinib Preclinical - Cell culture Actionable In a preclinical study, Nazartinib (EGF816) inhibited survival of transformed cells expressing ERBB2 (HER2) L786V in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) G776delinsVV in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P80dup were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) L755P in culture (PMID: 31588020). 31588020
ERBB2 V777L Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V777L were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 D769Y Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) D769Y in culture (PMID: 31588020). 31588020
ERBB2 L869R Advanced Solid Tumor sensitive Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L869R were resistant to Tagrisso (osimertinib) in culture (PMID: 31588020). 31588020
ERBB2 L786V Advanced Solid Tumor sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, Gilotrif (afatinib) inhibited survival of transformed cells expressing ERBB2 (HER2) L786V in culture (PMID: 31588020). 31588020
ERBB2 V842I Advanced Solid Tumor resistant Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V842I were resistant to Tagrisso (osimertinib) in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor resistant Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Nerlynx (neratinib) in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor resistant Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Tagrisso (osimertinib) in culture (PMID: 31588020). 31588020
ERBB2 V773M Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) V773M in culture (PMID: 31588020). 31588020
ERBB2 L869R Advanced Solid Tumor sensitive Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) L869R in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup Advanced Solid Tumor sensitive Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) G778_P780dup in culture (PMID: 31588020). 31588020
ERBB2 V777L Advanced Solid Tumor conflicting Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V777L were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 V777L Advanced Solid Tumor sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, Imbruvica (ibrutinib) inhibited survival of transformed cells expressing ERBB2 (HER2) V777L in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup breast cancer sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited viability of breast cancer cells expressing ERBB2 (HER2) Y772_A775dup in culture (PMID: 31588020). 31588020
ERBB2 D769N Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) D769N in culture (PMID: 31588020). 31588020
ERBB2 D769Y Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) D769Y were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Imbruvica (ibrutinib) in culture (PMID: 31588020). 31588020
ERBB2 V773M Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) V773M in culture (PMID: 31588020). 31588020
ERBB2 G778_S779insLPS Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) G778_S779insLPS in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) G776delinsLC in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor resistant Afatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Gilotrif (afatinib) in culture (PMID: 31588020). 31588020
ERBB2 V777L Advanced Solid Tumor sensitive Nazartinib Preclinical - Cell culture Actionable In a preclinical study, Nazartinib (EGF816) inhibited survival of transformed cells expressing ERBB2 (HER2) V777L in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor resistant Nazartinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Nazartinib (EGF816) in culture (PMID: 31588020). 31588020
ERBB2 L755S Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) L755S in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 V777L Advanced Solid Tumor sensitive Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, Vizimpro (dacomitinib) inhibited survival of transformed cells expressing ERBB2 (HER2) V777L in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Imbruvica (ibrutinib) in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup Advanced Solid Tumor conflicting Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup were resistant to Vizimpro (dacomitinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor conflicting Afatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Gilotrif (afatinib) in culture (PMID: 31588020). 31588020
ERBB2 D769Y Advanced Solid Tumor sensitive Nazartinib Preclinical - Cell culture Actionable In a preclinical study, Nazartinib (EGF816) inhibited survival of transformed cells expressing ERBB2 (HER2) D769Y in culture (PMID: 31588020). 31588020
ERBB2 L786V Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) L786V in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup Advanced Solid Tumor conflicting Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y722_A755dup were resistant to Pyrotinib in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) G778_P780dup in culture (PMID: 31588020). 31588020
ERBB2 V773M Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V773M were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 V777L Advanced Solid Tumor sensitive Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) V777L in culture (PMID: 31588020). 31588020
ERBB2 D769Y Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) D769Y in culture (PMID: 31588020). 31588020
ERBB2 L755S Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755S were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 D769H Advanced Solid Tumor sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, Imbruvica (ibrutinib) inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor conflicting Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Nerlynx (neratinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor resistant Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsLC were resistant to Tagrisso (osimertinib) in culture (PMID: 31588020). 31588020
ERBB2 D769N Advanced Solid Tumor sensitive Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, Vizimpro (dacomitinib) inhibited survival of transformed cells expressing ERBB2 (HER2) D769N in culture (PMID: 31588020). 31588020
ERBB2 V773M Advanced Solid Tumor sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, Imbruvica (ibrutinib) inhibited survival of transformed cells expressing ERBB2 (HER2) V773M in culture (PMID: 31588020). 31588020
ERBB2 V842I Advanced Solid Tumor sensitive Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, Vizimpro (dacomitinib) inhibited survival of transformed cells expressing ERBB2 (HER2) V842I in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup breast cancer sensitive Ado-trastuzumab emtansine + Poziotinib Preclinical - Cell culture Actionable In a preclinical study, addition of Poziotinib (HM781-36B) enhanced growth inhibition by Kadcyla (ado-trastuzumab emtansine) treatment in breast cancer cells expressing ERBB2 (HER2) Y772_A775dup in culture (PMID: 31588020). 31588020
ERBB2 L755S Advanced Solid Tumor sensitive Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, Vizimpro (dacomitinib) inhibited survival of transformed cells expressing ERBB2 (HER2) L755S in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup Advanced Solid Tumor resistant Afatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup were resistant to Gilotrif (afatinib) in culture (PMID: 31588020). 31588020
ERBB2 L755S Advanced Solid Tumor resistant Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755S were resistant to Pyrotinib in culture (PMID: 31588020). 31588020
ERBB2 L786V Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L786V were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 D769N Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) D769N in culture (PMID: 31588020). 31588020
ERBB2 L869R Advanced Solid Tumor sensitive Nazartinib Preclinical - Cell culture Actionable In a preclinical study, Nazartinib (EGF816) inhibited survival of transformed cells expressing ERBB2 (HER2) L869R in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) P780_Y781insGSP in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) G776delinsLC in culture (PMID: 31588020). 31588020
ERBB2 L755S Advanced Solid Tumor sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, Gilotrif (afatinib) inhibited survival of transformed cells expressing ERBB2 (HER2) L755S in culture (PMID: 31588020). 31588020
ERBB2 L869R Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) L755S in culture (PMID: 31588020). 31588020
ERBB2 V842I Advanced Solid Tumor sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, Gilotrif (afatinib) inhibited survival of transformed cells expressing ERBB2 (HER2) V842I in culture (PMID: 31588020). 31588020
ERBB2 D769H Advanced Solid Tumor sensitive Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, Vizimpro (dacomitinib) inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 D769N Advanced Solid Tumor sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, Imbruvica (ibrutinib) inhibited survival of transformed cells expressing ERBB2 (HER2) D769N in culture (PMID: 31588020). 31588020
ERBB2 V773M Advanced Solid Tumor resistant Nazartinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V773M were resistant to Nazartinib (EGF816) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 L786V Advanced Solid Tumor sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, Imbruvica (ibrutinib) inhibited survival of transformed cells expressing ERBB2 (HER2) L768V in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 G778_S779insLPS Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_S779insLPS were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 V842I Advanced Solid Tumor sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, Imbruvica (ibrutinib) inhibited survival of transformed cells expressing ERBB2 (HER2) V842I in culture (PMID: 31588020). 31588020
ERBB2 L869R Advanced Solid Tumor sensitive Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, Vizimpro (dacomitinib) inhibited survival of transformed cells expressing ERBB2 (HER2) L869R in culture (PMID: 31588020). 31588020
ERBB2 D769H Advanced Solid Tumor sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, Gilotrif (afatinib) inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 V773M Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V773M were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup lung non-small cell carcinoma predicted - sensitive Poziotinib Phase II Actionable In a Phase II trial, Poziotinib (HM781-36B) treatment resulted in a confirmed objective response rate of 42% (5/12) in patients with non-small cell lung cancer harboring ERBB2 (HER2) Y772_A775dup (n=9) or ERBB2 (HER2) G778_P780dup (n=3), with a median progression-free survival of 5.6 months (PMID: 31588020; NCT03066206). 31588020
ERBB2 G778_S779insLPS Advanced Solid Tumor resistant Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_S779insLPS were resistant to Tagrisso (osimertinib) in culture (PMID: 31588020). 31588020
ERBB2 V842I Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) V842I in culture (PMID: 31588020). 31588020
ERBB2 D769H Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup Advanced Solid Tumor decreased response Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) P780_Y781insGSP were resistant to Tagrisso (osimertinib) in culture (PMID: 31588020). 31588020
ERBB2 D769H Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) D769H were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 L869R Advanced Solid Tumor sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, Gilotrif (afatinib) inhibited survival of transformed cells expressing ERBB2 (HER2) L869R in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor resistant Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Vizimpro (dacomitinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor resistant Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsLC were resistant to Vizimpro (dacomitinib) in culture (PMID: 31588020). 31588020
ERBB2 D769N Advanced Solid Tumor sensitive Nazartinib Preclinical - Cell culture Actionable In a preclinical study, Nazartinib (EGF816) inhibited survival of transformed cells expressing ERBB2 (HER2) D769N in culture (PMID: 31588020). 31588020
ERBB2 D769Y Advanced Solid Tumor sensitive Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) D769Y in culture (PMID: 31588020). 31588020
ERBB2 L755S Advanced Solid Tumor resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755S were resistant to Imbruvica (ibrutinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor resistant Nazartinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsLC were resistant to Nazartinib (EGF816) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor sensitive Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) G776delinsLC in culture (PMID: 31588020). 31588020
ERBB2 L786V Advanced Solid Tumor sensitive Osimertinib Preclinical - Cell culture Actionable In a preclinical study, Tagrisso (osimertinib) inhibited survival of transformed cells expressing ERBB2 (HER2) L786V in culture (PMID: 31588020). 31588020
ERBB2 V842I Advanced Solid Tumor resistant Nazartinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V842I were resistant to Nazartinib (EGF816) in culture (PMID: 31588020). 31588020
ERBB2 D769Y Advanced Solid Tumor sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, Imbruvica (ibrutinib) inhibited survival of transformed cells expressing ERBB2 (HER2) D769Y in culture (PMID: 31588020). 31588020
ERBB2 D769Y Advanced Solid Tumor sensitive Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, Vizimpro (dacomitinib) inhibited survival of transformed cells expressing ERBB2 (HER2) D769Y in culture (PMID: 31588020). 31588020
ERBB2 L869R Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) L869R in culture (PMID: 31588020). 31588020
ERBB2 V773M Advanced Solid Tumor sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, Gilotrif (afatinib) inhibited survival of transformed cells expressing ERBB2 (HER2) V773M in culture (PMID: 31588020). 31588020
ERBB2 L786V Advanced Solid Tumor sensitive Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, Vizimpro (dacomitinib) inhibited survival of transformed cells expressing ERBB2 (HER2) L786V in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup breast cancer sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited viability of breast cancer cells expressing ERBB2 (HER2) G778_P780dup in culture (PMID: 31588020). 31588020
ERBB2 D769Y Advanced Solid Tumor sensitive Osimertinib Preclinical - Cell culture Actionable In a preclinical study, Tagrisso (osimertinib) inhibited survival of transformed cells expressing ERBB2 (HER2) D769Y in culture (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor resistant Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Pyrotinib in culture (PMID: 31588020). 31588020
ERBB2 L869R Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L869R were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Afatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Gilotrif (afatinib) in culture (PMID: 31588020). 31588020
ERBB2 G778_S779insLPS Advanced Solid Tumor resistant Nazartinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_S779insLPS were resistant to Nazartinib (EGF816) in culture (PMID: 31588020). 31588020
ERBB2 L755S colorectal cancer conflicting Afatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Gilotrif (afatinib) did not significantly inhibit tumor growth compared to vehicle control in cell line xenograft models of colorectal cancer harboring ERBB2 (HER2) L755S (PMID: 31588020). 31588020
ERBB2 V777L Advanced Solid Tumor sensitive Osimertinib Preclinical - Cell culture Actionable In a preclinical study, Tagrisso (osimertinib) inhibited survival of transformed cells expressing ERBB2 (HER2) V777L in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup Advanced Solid Tumor conflicting Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Nerlynx (neratinib) in culture (PMID: 31588020). 31588020
ERBB2 L755S Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L755S were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Tarloxotinib (TRLX) in culture (PMID: 31588020). 31588020
ERBB2 V777L Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) V777L in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Gilotrif (afatinib) in culture (PMID: 31588020). 31588020
ERBB2 L786V Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L786V were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor resistant Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Tarloxotinib (TRLX) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 31588020). 31588020
ERBB2 V842I Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) V842I in culture (PMID: 31588020). 31588020
ERBB2 G778_S779insLPS Advanced Solid Tumor sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, Imbruvica (ibrutinib) inhibited survival of transformed cells expressing ERBB2 (HER2) G778_S779insLPS in culture (PMID: 31588020). 31588020
ERBB2 V773M Advanced Solid Tumor sensitive Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) V773M in culture (PMID: 31588020). 31588020
ERBB2 V842I Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) V842I were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup breast cancer sensitive Ado-trastuzumab emtansine + Poziotinib Preclinical - Cell culture Actionable In a preclinical study, addition of Poziotinib (HM781-36B) enhanced growth inhibition by Kadcyla (ado-trastuzumab emtansine) treatment in breast cancer cells expressing ERBB2 (HER2) G778_P780dup in culture (PMID: 31588020). 31588020
ERBB2 L755S colorectal cancer sensitive Poziotinib Preclinical - Cell line xenograft Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited viability of colorectal cancer cells harboring ERBB2 (HER2) L755S in culture, and reduced tumor size by 58% in a cell line xenograft model (PMID: 31588020). 31588020
ERBB2 L755P Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) L755P in culture (PMID: 31588020). 31588020
ERBB2 L869R Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L869R were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor resistant Lapatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsLC were resistant to Tykerb (lapatinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor conflicting Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Tagrisso (osimertinib) in culture (PMID: 31588020). 31588020
ERBB2 D769Y Advanced Solid Tumor sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, Gilotrif (afatinib) inhibited survival of transformed cells expressing ERBB2 (HER2) D769Y in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor conflicting Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Vizimpro (dacomitinib) in culture (PMID: 31588020). 31588020
ERBB2 L755S colorectal cancer conflicting Neratinib Preclinical - Cell line xenograft Actionable In a preclinical study, Nerlynx (neratinib) treatment resulted in increased tumor growth compared to vehicle control in cell line xenograft models of colorectal cancer harboring ERBB2 (HER2) L755S (PMID: 31588020). 31588020
ERBB2 G778_S779insLPS Advanced Solid Tumor sensitive Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, Vizimpro (dacomitinib) inhibited survival of transformed cells expressing ERBB2 (HER2) G778_S779insLPS in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC breast cancer sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited Erbb2 (Her2) phosphorylation and viability of breast cancer cells expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Nazartinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Nazartinib (EGF816) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor resistant Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Tagrisso (osimertinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) G776delinsVV in culture (PMID: 31588020). 31588020
ERBB2 G778_S779insLPS Advanced Solid Tumor sensitive Afatinib Preclinical - Cell culture Actionable In a preclinical study, Gilotrif (afatinib) inhibited survival of transformed cells expressing ERBB2 (HER2) G778_S779insLPS in culture (PMID: 31588020). 31588020
ERBB2 D769N Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) D769N were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 V777L Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) V777L in culture (PMID: 31588020). 31588020
ERBB2 G778_S779insLPS Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_S779insLPS were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup Advanced Solid Tumor resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup were resistant to Imbruvica (ibrutinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor resistant Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Nerlynx (neratinib) in culture (PMID: 31588020). 31588020
ERBB2 L755S Advanced Solid Tumor sensitive Nazartinib Preclinical - Cell culture Actionable In a preclinical study, Nazartinib (EGF816) inhibited survival of transformed cells expressing ERBB2 (HER2) L755S in culture (PMID: 31588020). 31588020
ERBB2 L786V Advanced Solid Tumor sensitive Tarloxotinib Preclinical - Cell culture Actionable In a preclinical study, Tarloxotinib (TRLX) inhibited survival of transformed cells expressing ERBB2 (HER2) L786V in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) Y772_A775dup in culture (PMID: 31588020). 31588020
ERBB2 G778_P780dup Advanced Solid Tumor conflicting Neratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup were resistant to Nerlynx (neratinib) in culture (PMID: 31588020). 31588020
ERBB2 D769N Advanced Solid Tumor sensitive Lapatinib Preclinical - Cell culture Actionable In a preclinical study, Tykerb (lapatinib) inhibited growth of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor resistant Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Pyrotinib in culture (PMID: 31588020). 31588020
ERBB2 G778_S779insLPS Advanced Solid Tumor sensitive Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) G778_S779insLPS in culture (PMID: 31588020). 31588020
ERBB2 D769H Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) D769H were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 L755P lung non-small cell carcinoma predicted - sensitive Poziotinib Case Reports/Case Series Actionable In a Phase II trial, Poziotinib (HM781-36B) treatment resulted in stable disease lasted more than 7 months in a patient with non-small cell lung cancer harboring ERBB2 (HER2) L755P (PMID: 31588020; NCT03066206). 31588020
ERBB2 G776delinsVC Advanced Solid Tumor conflicting Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Pyrotinib in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup Advanced Solid Tumor resistant Osimertinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup were resistant to Tagrisso (osimertinib) in culture (PMID: 31588020). 31588020
ERBB2 D769H Advanced Solid Tumor sensitive Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVV Advanced Solid Tumor resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Imbruvica (ibrutinib) in culture (PMID: 31588020). 31588020
ERBB2 G778_S779insLPS Advanced Solid Tumor sensitive Poziotinib Preclinical - Cell culture Actionable In a preclinical study, Poziotinib (HM781-36B) inhibited survival of transformed cells expressing ERBB2 (HER2) G778_S779insLPS in culture (PMID: 31588020). 31588020
ERBB2 V773M Advanced Solid Tumor sensitive Dacomitinib Preclinical - Cell culture Actionable In a preclinical study, Vizimpro (dacomitinib) inhibited survival of transformed cells expressing ERBB2 (HER2) V773M in culture (PMID: 31588020). 31588020
ERBB2 L869R Advanced Solid Tumor resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) L869R were resistant to Imbruvica (ibrutinib) in culture (PMID: 31588020). 31588020
ERBB2 G776delinsVC breast cancer sensitive Ado-trastuzumab emtansine + Poziotinib Preclinical - Cell culture Actionable In a preclinical study, addition of Poziotinib (HM781-36B) enhanced growth inhibition by Kadcyla (ado-trastuzumab emtansine) treatment in breast cancer cells expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 31588020). 31588020
ERBB2 Y772_A775dup lung non-small cell carcinoma predicted - sensitive Poziotinib Phase II Actionable In a Phase II trial, Poziotinib (HM781-36B) treatment resulted in a confirmed objective response rate of 42% (5/12) in patients with non-small cell lung cancer harboring ERBB2 (HER2) Y772_A775dup (n=9) or ERBB2 (HER2) G778_P780dup (n=3), with a median progression-free survival of 5.6 months (PMID: 31588020; NCT03066206). 31588020
ERBB2 D769N Advanced Solid Tumor sensitive Pyrotinib Preclinical - Cell culture Actionable In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) D769N in culture (PMID: 31588020). 31588020
ERBB2 G776delinsLC Advanced Solid Tumor resistant Sapitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsLC were resistant to Sapitinib (AZD8931) in culture (PMID: 31588020). 31588020
ERBB2 D769N Advanced Solid Tumor sensitive Osimertinib Preclinical - Cell culture Actionable In a preclinical study, Tagrisso (osimertinib) inhibited survival of transformed cells expressing ERBB2 (HER2) D769N in culture (PMID: 31588020). 31588020