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Emzadirib (CYT-0851) is an orally bioavailable small molecule inhibitor of RAD51-mediated homologous recombination and DNA repair. Developed by Cyteir Therapeutics, it was designed to exploit synthetic lethality in cancer cells by inhibiting RAD51, a protein essential for repairing DNA double-strand breaks. By blocking this repair pathway, emzadirib leads to the accumulation of unrepaired DNA damage and subsequent apoptosis in tumor cells. It was evaluated in Phase 1/2 clinical trials for various B-cell malignancies and advanced solid tumors, both as a monotherapy and in combination with chemotherapy agents like gemcitabine and capecitabine. However, development was discontinued in 2023 after Cyteir Therapeutics determined that continuation was not feasible given the resources required and the overall clinical efficacy data, subsequently leading to the company's liquidation.
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