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Dalpiciclib + apatinib is a combination therapy comprising two small-molecule targeted agents: dalpiciclib, a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), and apatinib, a tyrosine kinase inhibitor (TKI) specifically targeting vascular endothelial growth factor receptor-2 (VEGFR-2). Dalpiciclib induces cell cycle arrest in the G1 phase by preventing the phosphorylation of the retinoblastoma (Rb) protein, thereby inhibiting tumor cell proliferation. Apatinib acts as an anti-angiogenic agent by blocking VEGFR-2 signaling, which is critical for tumor-associated neoangiogenesis and vascular permeability. This combination is primarily developed by Jiangsu Hengrui Pharmaceuticals and is being evaluated in clinical trials, including those led by Peking University Third Hospital, for the treatment of advanced or refractory sarcomas and other solid tumors. The rationale for the combination lies in the potential synergy between cell cycle inhibition and the disruption of the tumor microenvironment through anti-angiogenesis.
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