Drug intelligence / Profile preview

azacitidine + cytarabine

Development stage
Unknown
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous, Subcutaneous
01

Overview

Azacitidine + cytarabine is a combination of two antineoplastic agents used primarily in the treatment of acute myeloid leukemia (AML), especially in patients who are older or unfit for intensive chemotherapy. Azacitidine is a DNA hypomethylating agent that incorporates into DNA and RNA, leading to hypomethylation and direct cytotoxicity to abnormal hematopoietic cells. Cytarabine is an antimetabolite that inhibits DNA synthesis by acting as a cytosine nucleoside analog, resulting in cell death during the S-phase of the cell cycle. This combination exploits complementary mechanisms—epigenetic modulation by azacitidine and inhibition of DNA replication by cytarabine—to enhance anti-leukemic efficacy[1][5]. The regimen has been studied both alone and as part of multi-drug protocols for AML.

02

Targets

DNMT1 (DNA (cytosine-5)-methyltransferase 1)DNA polymerase family

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