Drug intelligence / Profile preview

cedazuridine + azacitidine

Development stage
Phase 3
Lead developer
Astex Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Cedazuridine + azacitidine is an investigational oral fixed-dose combination of two agents for the treatment of myelodysplastic syndromes (MDS), chronic myelomonocytic leukemia (CMML), and potentially acute myeloid leukemia (AML). Azacitidine is a pyrimidine nucleoside analogue and hypomethylating agent that incorporates into DNA and RNA, inhibiting DNA methyltransferase, leading to hypomethylation of DNA, disruption of abnormal cell growth, and induction of apoptosis in malignant cells. Cedazuridine is a cytidine deaminase inhibitor that prevents the rapid degradation of azacitidine in the gastrointestinal tract and liver, enabling effective systemic exposure when administered orally. The combination aims to provide pharmacokinetic equivalence to parenteral azacitidine while reducing treatment burden for patients[1][2][6].

Other names
cedazuridine/azacitidine combination agentoral azacitidine with cedazuridine
02

Targets

DNMT (DNA methyltransferase)CDA (Cytidine deaminase)

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