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    DRUG CLASS:

    β-catenin inhibitor

    Related drugs:
    7d
    A first-in-human, open-label multicentre Phase 1 study of the orally administered E7386 in patients with selected advanced neoplasms. (PubMed, Br J Cancer)
    E7386 demonstrated a manageable safety profile, a dose-dependent pharmacokinetic profile, and some disease stabilisation in heavily pretreated patients with advanced solid tumours.
    P1 data • Journal • First-in-human
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    CTNNB1 (Catenin (cadherin-associated protein), beta 1)
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    E7386
    25d
    A Phase 1 Oral Mass Balance and Combined Intravenous [14C] Microtracer Study to Characterize the Absorption, Metabolism, Excretion, and Pharmacokinetics of Antitumor Drug E7386 in Humans. (PubMed, J Clin Pharmacol)
    These results suggest that [14C]E7386-related material is predominantly excreted in feces after oral administration. Overall, IV administration and oral administration of a single E7386 dose was tolerable in healthy participants, and adverse events were manageable.
    Clinical • P1 data • PK/PD data • Journal
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    CREBBP (CREB binding protein)
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    E7386
    2ms
    Phase III Trial of Camrelizumab+Apatinib+Eribulin vs. Physician's Choice Chemotherapy in Advanced Triple-Negative Breast Cancer (clinicaltrials.gov)
    P3, N=246, Recruiting, Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University | Active, not recruiting --> Recruiting | Trial completion date: Mar 2031 --> Jun 2029 | Trial primary completion date: Sep 2030 --> Dec 2028
    Enrollment open • Trial completion date • Trial primary completion date
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    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
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    ER positive • HER-2 negative • ER negative • HER-2 negative + AR positive + ER positive • HER-2 negative + ER positive
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    AiRuiKa (camrelizumab) • AiTan (rivoceranib) • eribulin mesylate
    2ms
    A multicenter, single-arm phase II clinical study of eribulin combined with inituzumab and pyrotinib in the treatment of HER2-positive advanced breast cancer (ChiCTR2600121825)
    P2, N=76, Recruiting, Fifth Affiliated Hospital, Sun Yat-Sen University; Fifth Affiliated Hospital, Sun Yat-Sen University
    New P2 trial
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    HER-2 (Human epidermal growth factor receptor 2)
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    HER-2 expression
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    Irene (pyrotinib) • eribulin mesylate • TheraCIM (nimotuzumab)
    2ms
    NUP62 promotes breast cancer progression and inhibits ferroptosis by stabilizing NRF2 in a KEAP1-dependent way. (PubMed, iScience)
    In vivo, eribulin or NUP62 silencing significantly suppressed tumor growth in xenograft models. Our findings establish the NUP62-KEAP1-NRF2 axis as a master regulator of ferroptosis in BC, positioning eribulin as a promising therapeutic agent for NUP62-high tumors.
    Journal
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    KEAP1 (Kelch Like ECH Associated Protein 1) • NUP62 (Nucleoporin 62)
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    eribulin mesylate
    2ms
    Safety and Antitumor Activity of Farletuzumab Ecteribulin in Patients With NSCLC: Phase I Expansion Results. (PubMed, JTO Clin Res Rep)
    FZEC demonstrated modest antitumor activity, and observed AEs were generally manageable in patients with heavily pretreated NSCLC. NCT03386942.
    P1 data • Journal
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    FOLR1 ( Folate receptor alpha )
    |
    FOLR1 expression
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    eribulin mesylate • farletuzumab ecteribulin (MORAb-202)
    2ms
    Role of the cross-regulation between Wnt pathway activation and androgen receptor signaling in prostate cancer treatment resistance. (PubMed, Cell Death Differ)
    Targeting β-catenin interactions with co-activators p300/CBP using selective inhibitors (IQ-1 and ICG-001) effectively mitigated Wnt-driven ARSI resistance, restoring sensitivity to therapy in preclinical models...The identified Wnt signature holds potential as a biomarker for predicting and monitoring therapeutic outcomes. Concurrent targeting of AR and Wnt signaling represents a promising strategy to overcome treatment resistance, particularly in patients with Wnt-activating mutations.
    Journal
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    RNF43 (Ring Finger Protein 43) • ZNRF3 (Zinc And Ring Finger 3)
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    foscenvivint (PRI724)
    2ms
    MBC-EA: A Multicenter, Single-Arm, Phase II Exploratory Study of Eribulin in Combination With Anlotinib for HER2-Negative Recurrent/Metastatic Breast Cancer Previously Treated With Antibody-Drug Conjugates (clinicaltrials.gov)
    P2, N=52, Recruiting, Sun Yat-sen University
    New P2 trial
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    HER-2 (Human epidermal growth factor receptor 2)
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    HER-2 negative
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    Focus V (anlotinib) • eribulin mesylate
    3ms
    JAZMINE: Phase Ib/II Study of Zanidatamab Plus Tucatinib and Chemotherapy in HER2-Positive Advanced Breast Cancer (clinicaltrials.gov)
    P1/2, N=24, Not yet recruiting, MedSIR
    New P1/2 trial
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    HER-2 positive • HER-2 amplification
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    capecitabine • eribulin mesylate • Tukysa (tucatinib) • Ziihera (zanidatamab-hrii)
    3ms
    CSF1R Inhibition with Chemotherapy Relieves Systemic Immune Suppression in Patients with Metastatic Triple-Negative Breast Cancer and Boosts anti-PD-1 Efficacy in Transgenic Mammary Tumors. (PubMed, Clin Cancer Res)
    These clinical and preclinical findings provide rationale for therapies to increase therapeutic index of aPD-1 therapy by diminishing presence of T cell-suppressive myelomonocytic cells to improve outcomes for patients with refractory disease.
    Journal • PD(L)-1 Biomarker • IO biomarker
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    CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule)
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    eribulin mesylate • Turalio (pexidartinib)
    3ms
    Eribulin Mesylate-based Therapy in Patients With Advanced HER2-negative Breast Cancer Previously Treated With ADC (clinicaltrials.gov)
    P=N/A, N=400, Not yet recruiting, Fudan University
    New trial • Real-world evidence
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    eribulin mesylate
    3ms
    SWOG S1937: Comparing the New Anti-cancer Drug Eribulin With Chemotherapy Against the Usual Chemotherapy Alone in Metastatic Urothelial Cancer (clinicaltrials.gov)
    P3, N=184, Active, not recruiting, National Cancer Institute (NCI) | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    gemcitabine • paclitaxel • docetaxel • eribulin mesylate • Trodelvy (sacituzumab govitecan-hziy)