Protacs In 2025: From The Laboratory Concept To Clinical Breakthrough

    April 2026 in “ Future Medicinal Chemistry
    Yan Xu, Xinyu Li, Jian Song, Sai‐Yang Zhang
    TLDR PROTACs have become a breakthrough in medicine by effectively targeting and degrading specific proteins to treat diseases.
    Proteolysis-Targeting Chimeras (PROTACs) have made significant strides in drug discovery by targeting previously "undruggable" proteins. In 2025, a New Drug Application was submitted for Vepdegestrant, a PROTAC targeting estrogen receptors in breast cancer, which reduced disease progression risk by 40% compared to standard therapy. Other PROTACs, like BMS-986365 for prostate cancer and BGB-16673 for leukemia, showed promising Phase III trial results. Innovations such as PolyTACs and VIPER-TACs have broadened PROTACs' target range, and linker-free designs have enhanced drug properties. Despite challenges like the "hook effect," ongoing research is expected to further improve PROTACs' clinical applications, potentially revolutionizing precision medicine.
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