^
    Contact us  to learn more about
    our Premium Content:  News alerts, weekly reports and conference planners
    BIOMARKER:

    ESR1 mutation

    i
    Other names: ESR1, Era, ESR, NR3A1, ER, ER beta
    Entrez ID:
    2099
    Related biomarkers:
    Expression
    Mutation
    CNA
    Fusion
    Others
    Related tests:
    6d
    ELAINE 1: Evaluation of Lasofoxifene Versus Fulvestrant in Advanced or Metastatic ER+/HER2- Breast Cancer With an ESR1 Mutation (clinicaltrials.gov)
    P2, N=100, Completed, Sermonix Pharmaceuticals Inc. | Active, not recruiting --> Completed | Trial completion date: Dec 2024 --> May 2025 | Trial primary completion date: Dec 2024 --> May 2025
    Trial completion • Trial completion date • Trial primary completion date • First-in-human
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HER-2 negative • ESR1 mutation
    |
    fulvestrant • Fablyn (lasofoxifene)
    12d
    PhII Randomized CAPecitabine + ELAcestrant vs. Capecitabine Alone in ER+ Breast Cancer (CAPELA) (clinicaltrials.gov)
    P2, N=297, Recruiting, Kristina A. Fanucci | Trial completion date: Oct 2029 --> Oct 2030 | Trial primary completion date: Dec 2028 --> Dec 2029
    Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • CD4 (CD4 Molecule)
    |
    ER positive • HER-2 negative • ESR1 mutation • HER-2 negative + ER positive • HER-2 negative + ER positive + ESR1 mutation
    |
    capecitabine • Orserdu (elacestrant)
    12d
    Serial analysis of ESR1 mutations in cell-free DNA from hormone receptor-positive, HER2-negative metastatic breast cancer during palliative endocrine therapy. (PubMed, Front Oncol)
    bESR1 was detected prior to clinical progression in half of patients. Our study suggests the benefit of bESR1 monitoring during palliative endocrine therapy.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HR positive • HER-2 negative • ESR1 mutation • EGFR positive • HR positive + HER-2 negative • HER-2 negative + HR positive + ESR1 mutation
    13d
    PhII Randomized CAPecitabine + ELAcestrant vs. Capecitabine Alone in ER+ Breast Cancer (CAPELA) (clinicaltrials.gov)
    P2, N=297, Recruiting, Kristina A. Fanucci | Not yet recruiting --> Recruiting
    Enrollment open
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • CD4 (CD4 Molecule)
    |
    ER positive • HER-2 negative • ESR1 mutation • HER-2 negative + ER positive • HER-2 negative + ER positive + ESR1 mutation
    |
    capecitabine • Orserdu (elacestrant)
    14d
    Characterization of ESR1 alterations in patients with breast and gynecologic cancers. (PubMed, Breast Cancer Res)
    ESR1 alterations were most frequent in HR + /HER2- BC samples and missense mutations were more frequent in metastatic samples, consistent with their role in ET resistance and disease progression. ESR1 alterations co-occurred with therapeutically relevant alterations in other genes that may help inform clinical decision-making. Gynecologic tumors harbored ESR1 alterations that have prognostic and potentially therapeutic relevance.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • CCND1 (Cyclin D1) • FGF3 (Fibroblast growth factor 3) • CCDC170(Coiled-Coil Domain Containing 170)
    |
    HER-2 amplification • HER-2 negative • HER-2 mutation • ESR1 mutation
    18d
    Comparative efficacy and safety of novel oral selective estrogen receptor degraders in ER+/HER2- advanced breast cancer: An updated systematic review and meta-analysis of randomized controlled trials. (PubMed, Cancer Treat Rev)
    Novel oral SERDs may represent a paradigm shift in managing PD after 1 L therapy, showing potential to improve PFS in selected patients.
    Retrospective data • Review • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HER-2 negative • ESR1 mutation
    |
    fulvestrant
    24d
    Calcium and Cadmium Activate ESRRB to Mediate Cell Stemness and Pluripotency. (PubMed, Int J Mol Sci)
    Mutational analysis and molecular docking identified potential metal interaction sites within ESRRB's ligand-binding domain. Together, these results suggest calcium acts as a natural ligand for ESRRB and cadmium, which mimics calcium, activate ESRRB to mediate cell stemness and pluripotency.
    Journal
    |
    ER (Estrogen receptor) • ESRRB (Estrogen Related Receptor Beta)
    |
    ESR1 mutation
    24d
    Human Cancers Derived from Either Genetic or Lifestyle Factors Are Initiated by Impaired Estrogen Signaling. (PubMed, Cancers (Basel))
    Increased cancer risk, insulin resistance, and infertility all originate from defective estrogen signaling.
    Review • Journal • BRCA Biomarker
    |
    ER (Estrogen receptor) • BRCA1 (Breast cancer 1, early onset) • IGF1 (Insulin-like growth factor 1)
    |
    ESR1 mutation
    25d
    Selective Estrogen Receptor Degraders Induce Bradycardia by Modulating Nuclear Estrogen Signaling. (PubMed, JACC Basic Transl Sci)
    Giredestrant and camizestrant induced significant bradycardia in wild-type zebrafish embryos, whereas fulvestrant and amcenestrant (SERDs that do not induce bradycardia in patients) did not alter heart rate. Mutations in gper, esr2a, and esr2b did not confer resistance to SERD-induced bradycardia, whereas esr1 mutant embryos were protected. These findings demonstrate that SERD-associated bradycardia is mediated through Esr1 signaling, supporting an on-target adverse effect.
    Journal
    |
    ER (Estrogen receptor)
    |
    ER positive • BRAF wild-type • ESR1 mutation
    |
    fulvestrant • amcenestrant (SAR439859) • camizestrant (AZD9833) • giredestrant (RG6171)
    26d
    ESR1 mutation in Endocrine treatment naive Endometrial Cancer: Prevalence, Characteristics and Prognostic Implications, results from the UTOLA phase II GINECO trial. (PubMed, Clin Cancer Res)
    ESR1 mutations, while rare overall in treatment-naïve EC, are more prevalent in NSMP LGEC, potentially affecting AI efficacy. ESR1 status should be considered in selecting hormonotherapy and as a stratification factor in AI trials.
    P2 data • Journal
    |
    ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    ER positive • MSI-H/dMMR • ESR1 mutation
    26d
    A Phase Ib/II Study to Evaluate Multiple Combination Therapies of FWD1802 in Patients With ER+/HER2- BC (clinicaltrials.gov)
    P1/2, N=196, Recruiting, Forward Pharmaceuticals Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    HER-2 positive • ER positive • HER-2 negative • ESR1 mutation • ER positive + HER-2 negative • HER-2 negative + ER positive • HER-2 negative + ER positive + ESR1 mutation
    |
    Ibrance (palbociclib) • everolimus • Verzenio (abemaciclib) • Kisqali (ribociclib)