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BIOMARKER:

SDC4-NRG1 fusion

i
Other names: SDC4, Syndecan 4, Syndecan 4 (Amphiglycan, Ryudocan), Syndecan Proteoglycan 4, Ryudocan Core Protein, Amphiglycan, Syndecan-4, SYND4, Ryudocan Amphiglycan 3, NRG1, GGF, HGL, HRG, NDF, NRG1-IT2, Neuregulin 1, Heregulin
Entrez ID:
3ms
Zongertinib (BI 1810631), an irreversible HER2 TKI, spares EGFR signaling and improves therapeutic response in preclinical models and patients with HER2-driven cancers. (PubMed, Cancer Discov)
Zongertinib potently and selectively blocks HER2, while sparing EGFR, and inhibits the growth of cells dependent on HER2 oncogenic driver events, including HER2-dependent human cancer cells resistant to trastuzumab deruxtecan. Zongertinib displays potent anti-tumor activity in HER2-dependent human NSCLC xenograft models and enhances the activities of antibody-drug conjugates and KRASG12C inhibitors, without causing obvious toxicities. The preclinical efficacy of zongertinib translates in objective responses in patients with HER2-dependent tumors, including cholangiocarcinoma (SDC4-NRG1 fusion) and breast cancer (V777L HER2 mutation) thus supporting the ongoing clinical development of zongertinib.
Preclinical • Journal
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HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • NRG1 (Neuregulin 1) • SDC4 (Syndecan 4)
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HER-2 mutation • NRG1 fusion • HER-2 V777L • NRG1 fusion • SDC4-NRG1 fusion
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Enhertu (fam-trastuzumab deruxtecan-nxki) • zongertinib (BI 1810631)