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    DRUG CLASS:

    Selective estrogen receptor covalent antagonist

    Related drugs:
    over2years
    Phase I study of HRS8807, an oral selective ER covalent antagonist (SERCA), in ER+/HER2- locally advanced (LA) or metastatic (M) breast cancer (BC) (ESMO 2023)
    3 pts achieved PR (1 at 75 mg and 2 at 150 mg; in which 2 had prior SERD [fulvestrant] and all had prior CDK4/6i in the M setting; treatment duration was 8.4, 8.6+, and 7.0+ mo). 18F-FES PET-CT SUVmax decreased significantly after treatment. Conclusions HRS8807 was well-tolerated and showed early signs of robust antitumor activity, favorable PK properties (both parent and active metabolite), and high ER occupancy in pretreated ER+/HER2- LA/M BC.
    P1 data • Metastases
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    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • CDK4 (Cyclin-dependent kinase 4)
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    HER-2 negative
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    fulvestrant • HRS8807