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azacitidine
- Development stage
- Approved
- Lead developer
- Bristol Myers Squibb
- 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
- Subcutaneous, Intravenous, Oral
01
Overview
Azacitidine is a pyrimidine nucleoside analogue and antimetabolite chemotherapy drug used primarily for the treatment of myelodysplastic syndromes (MDS), acute myeloid leukemia (AML), chronic myelomonocytic leukemia (CMML), and juvenile myelomonocytic leukemia (JMML). It acts as a chemical analog of cytidine and exerts its antineoplastic effects through two main mechanisms. At low doses, it inhibits DNA methyltransferase enzymes, leading to hypomethylation of DNA and reactivation of silenced genes. At higher doses, it incorporates into RNA and DNA, disrupting their metabolism and synthesis—resulting in cytotoxicity to abnormal hematopoietic cells. Azacitidine is administered either by subcutaneous or intravenous injection or as an oral tablet. The drug was originally developed by Pharmacia & Upjohn.
- Brand names
- VidazaOnureg
- Other names
- 5-azacytidine5-azaCazacytidine
02
Targets
DNMT1 (DNA (cytosine-5)-methyltransferase 1)TRDMT1 (DNA methyltransferase 2)
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