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    ZN-1041

    Other names: RG6596; RO7771950

    Modality: Tyrosine Kinase Inhibitor (TKI)

    Disease State: Human Epidermal Growth Factor Receptor 2 (HER2)-positive Breast Cancer, Advanced Solid Tumors

    Summary

    ZN-1041(RG6596/RO7771950) is an investigational, orally administered TKI selective for HER2. It is designed to be delivered across the blood-brain barrier (BBB) being evaluated to treat HER2+ breast cancer brain metastases (BCBM).1

    Clinical Trials

    ZN-1041
    NCT ID Study Phase Enrollment Status Study Title
    NCT07413939 Phase II / Phase III Recruiting RO7771950 Versus Tucatinib in Combination With Trastuzumab and Capecitabine in People With Locally Advanced or Metastatic Breast Cancer That is Human Epidermal Growth Factor Receptor 2 (HER2)-Positive View details

    Proposed Mechanism of Action

    ZN-1041 (RG6596/RO7771950) is an investigational, orally administered TKI.1 It is designed to target the intracellular kinase domain of homo- or hetero-dimerised HER2, preventing autophosphorylation and de-activating downstream signaling of the receptors.2

    1. Ma F, Li Y, Yao H, et al. Preclinical and early clinical data of ZN-1041, a best-in-class BBB penetrable HER2 inhibitor to treat breast cancer with CNS metastases. Poster presented at: ASCO Annual Meeting; June 2-6, 2023; Chicago, IL. Abstract 1040. Accessed April 2, 2026. https://medically.roche.com/​global/​en/​oncology/​oncology-annual-meeting-2023/​medical-material/​oncology-annual-meeting-2023-poster-ma-preclinical-and-early-clinical-data-pdf.html
    2. Xuhong JC, Qi XW, Zhang Y, Jiang J. Mechanism, safety and efficacy of three tyrosine kinase inhibitors lapatinib, neratinib and pyrotinib in HER2-positive breast cancer. Am J Cancer Res. 2019;9(10):2103-2119.

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    TOP

    • BBB
      Blood-brain barrier

    • BCBM
      Breast cancer brain metastases

    • HER2
      Human epidermal growth factor receptor 2

    • TKI
      Tyrosine kinase inhibitor

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