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Cedazuridine is an inhibitor of cytidine deaminase (IC50 = 0.4 µM).1 It increases plasma levels of decitabine via inhibition of its metabolism by cytidine deaminase in rhesus monkeys when administered at doses of 1 and 10 mg/kg. Cedazuridine (3 mg/kg) induces decreases in leukemic cell expansion in combination with orally administered 5-azacytidine (Item No. 11164), which is inactive as a single agent, in the bone marrow and spleen in a MOLM-13 acute myeloid leukemia (AML) mouse xenograft model.2 Formulations containing cedazuridine in combination with decitabine have been used in the treatment of myelodysplastic syndrome (MDS).
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1. Design, synthesis, and pharmacological evaluation of fluorinated tetrahydrouridine derivatives as inhibitors of cytidine deaminase. J. Med. Chem. 57(6), 2582-2588 (2014).
2. Oral azacitidine and cedazuridine approximate parenteral azacitidine efficacy in murine model. Target Oncol. 15(2), 231-240 (2020).