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    DRUG:

    caxmotabart entudotin (IKS014)

    i
    Other names: IKS014, LCB14, FS-1502
    Company:
    Fosun Pharma, Iksuda Therap, LigaChem Biosci
    Drug class:
    Microtubule inhibitor, HER2-targeted antibody-drug conjugate
    Related drugs:
    3ms
    FS-CY1502-Ph1-01: Phase 1 Study of FS-1502 in Patients With HER2 Expressed Advanced Solid Tumors and Breast Cancer. (clinicaltrials.gov)
    P1, N=161, Completed, Shanghai Fosun Pharmaceutical Industrial Development Co. Ltd. | Active, not recruiting --> Completed | N=297 --> 161
    Trial completion • Enrollment change
    |
    HER-2 positive • HER-2 expression
    |
    caxmotabart entudotin (IKS014)
    6ms
    A multicenter, open-label, double-cohort, phase II study: to evaluate the efficacy and safety of FS-1502 in patients with HER2-overexpressing locally advanced or metastatic gastric/gastroesophageal junction adenocarcinoma (ChiCTR2500101151)
    P2, N=79, Completed, Sir Run Run Shaw Hospital , Zhejiang University School of Medicine; Shanghai Fosun Pharmaceutical Industrial Development Co., Ltd.
    New P2 trial
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 overexpression
    |
    caxmotabart entudotin (IKS014)
    7ms
    IKS014 in Advanced Solid Tumors That Express HER2 (clinicaltrials.gov)
    P1, N=165, Recruiting, Iksuda Therapeutics Ltd. | Trial primary completion date: Sep 2025 --> Sep 2026
    Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive • HR positive • HER-2 amplification • HER-2 expression • HER-2 amplification + HR-positive
    |
    caxmotabart entudotin (IKS014)
    8ms
    An open, two-cohort, multicenter Phase II study of FS-1502 in combination with Srulizumab and chemotherapy in patients with HER2-expressing advanced gastric cancer (ChiCTR2500099447)
    P2, N=58, Completed, Beijing Cancer Hospital; Shanghai Fosun Pharmaceutical (Group) Limited by Share Ltd
    New P2 trial
    |
    HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • TMB (Tumor Mutational Burden)
    |
    PD-L1 expression • HER-2 positive • HER-2 expression
    |
    5-fluorouracil • capecitabine • caxmotabart entudotin (IKS014)
    over1year
    Phase 1 Study of FS-1502 in Patients With HER2 Expressed Advanced Solid Tumors and Breast Cancer. (clinicaltrials.gov)
    P1, N=297, Active, not recruiting, Shanghai Fosun Pharmaceutical Industrial Development Co. Ltd. | Recruiting --> Active, not recruiting | Trial primary completion date: Sep 2023 --> Apr 2024
    Enrollment closed • Trial primary completion date • Metastases
    |
    HER-2 positive • HER-2 expression
    |
    caxmotabart entudotin (IKS014)
    2years
    Model-Informed Dose Selection for an Investigational HER2 ADC FS-1502 in Patients with HER2 Expressed Advanced Malignant Solid Tumors. (PubMed, Br J Clin Pharmacol)
    This PopPK and E-R analysis guided the recommended phase II dose (RP2D) selection of 2.3 mg/kg Q3W and supported body weight based dosing for an investigational HER2 ADC FS-1502.
    Journal • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 expression
    |
    caxmotabart entudotin (IKS014)
    2years
    IKS014 in Advanced Solid Tumors That Express HER2 (clinicaltrials.gov)
    P1, N=165, Recruiting, Iksuda Therapeutics Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive • HR positive • HER-2 amplification • HER-2 expression
    |
    caxmotabart entudotin (IKS014)
    over2years
    FS-1502 Versus T-DM1 for HER2-Positive Unresectable Locally Advanced or Metastatic Breast Cancer (clinicaltrials.gov)
    P3, N=314, Recruiting, Shanghai Fosun Pharmaceutical Industrial Development Co. Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive
    |
    Kadcyla (ado-trastuzumab emtansine) • caxmotabart entudotin (IKS014)
    over2years
    IKS014 in Advanced Solid Tumors That Express HER2 (clinicaltrials.gov)
    P1, N=165, Not yet recruiting, Iksuda Therapeutics Ltd.
    New P1 trial • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive • HR positive • HER-2 amplification • HER-2 expression
    |
    caxmotabart entudotin (IKS014)
    over2years
    FS-1502 in HER2-positive advanced breast cancer: Results from an open-label, phase 1 study. (ASCO 2023)
    All pts had previously received anti-HER2 therapy, among which trastuzumab ± pertuzumab (n = 67, 96%) and pyrotinib (n = 52, 74%) were the most common. FS-1502 demonstrated very promising antitumor activity and was well tolerated in heavily pretreated HER2-positive BC, with mild eye toxicity and no related interstitial lung disease reported. A Phase 3 clinical trial is under planning to further confirm efficacy and safety of FS-1502 in pts with advanced HER2-positive BC. Clinical trial information: NCT03944499.
    Clinical • P1 data • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive • HER-2 expression
    |
    Herceptin (trastuzumab) • Perjeta (pertuzumab) • Irene (pyrotinib) • caxmotabart entudotin (IKS014)
    almost3years
    FS-1502 Versus T-DM1 for HER2-Positive Unresectable Locally Advanced or Metastatic Breast Cancer (clinicaltrials.gov)
    P3, N=314, Not yet recruiting, Shanghai Fosun Pharmaceutical Industrial Development Co. Ltd.
    New P3 trial • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive
    |
    Kadcyla (ado-trastuzumab emtansine) • caxmotabart entudotin (IKS014)
    over3years
    IKS014, a HER2-targeting antibody drug conjugate incorporating novel bioconjugation and tumor-selective linker technology with improved in vivo efficacy and tolerability (AACR 2022)
    While trastuzumab and ado-trastuzumab emtansine (T-DM1) have become an integral part of treatment paradigms for HER2-positive cancer, the more recent approvals of the fam-trastuzumab deruxtecan (DS-8201) ADC and the Fc-engineered margetuximab antibody have highlighted the potential for continued improvement over existing HER2-targeting therapies. In cynomolgus monkeys, IKS014 was tolerated at 12 mg/kg single dose and 5 mg/kg repeat dose without ocular or lung toxicity findings.IKS014 was highly efficacious against HER2-positive tumor xenografts in vivo, including models with moderate target expression, and compared favorably to clinically validated benchmark ADCs. This improved preclinical efficacy combined with stable PK and good tolerability profile warrants further development of this novel ADC for HER2-positive cancers.
    Preclinical
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive • HER-2 expression
    |
    Kadcyla (ado-trastuzumab emtansine) • Enhertu (fam-trastuzumab deruxtecan-nxki) • Margenza (margetuximab-cmkb) • caxmotabart entudotin (IKS014)