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INCB057643 + gemcitabine is an investigational combination of a selective small molecule bromodomain and extra-terminal (BET) protein inhibitor (INCB057643) with the cytotoxic chemotherapeutic agent gemcitabine. INCB057643 inhibits BET family proteins, which regulate oncogenic gene transcription, thereby potentially suppressing cancer cell proliferation and survival. Gemcitabine is a nucleoside analog that interferes with DNA synthesis, resulting in cell death, and is standard-of-care for various solid tumors. The combination is under clinical investigation to determine safety, tolerability, and preliminary efficacy in patients with relapsed or refractory advanced or metastatic solid tumors and hematologic malignancies for which gemcitabine is relevant[1][4][7][9].
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