Cedazuridine CAS# 1141397-80-9 西达尿苷
Cedazuridine (E7727) is an oral cytidine deaminase (CDA) inhibitor developed to enhance the bioavailability of the hypomethylating agent decitabine. In preclinical studies, cedazuridine potently inhibited CDA activity with a Ki of ~0.2 µM, preventing rapid degradation of decitabine in the gastrointestinal tract and liver. In rodent and primate models, co-administration of cedazuridine with decitabine increased systemic decitabine exposure by 7–10 fold compared to decitabine alone, while maintaining hypomethylating activity. Cedazuridine itself showed no cytotoxic or DNA hypomethylating effects, confirming its role as a metabolic modulator. These findings supported its development as an oral fixed-dose decitabine–cedazuridine combination.
📌 参考资料/链接:
Design, Synthesis, and Pharmacological Evaluation of Fluorinated Tetrahydrouridine Derivatives as Inhibitors of Cytidine DeaminaseBy: Ferraris, Dana; et alJournal of Medicinal Chemistry (2014), 57(6), 2582-2588
📄 详细内容
CAS No. 1141397-80-9 西达尿苷Cedazuridine synthetic routes

Design, Synthesis, and Pharmacological Evaluation of Fluorinated Tetrahydrouridine Derivatives as Inhibitors of Cytidine DeaminaseBy: Ferraris, Dana; et alJournal of Medicinal Chemistry (2014), 57(6), 2582-2588
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