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azacitidine + decitabine
- Development stage
- Unknown
- Lead developer
- Bristol Myers Squibb
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral, Intravenous, Subcutaneous
01
Overview
Azacitidine and decitabine are antimetabolite chemotherapeutic agents classified as hypomethylating agents. Both drugs are nucleoside analogues that inhibit DNA methyltransferases, leading to DNA hypomethylation and reactivation of tumor suppressor genes. Azacitidine is primarily incorporated into RNA, with a smaller fraction incorporated into DNA, while decitabine is incorporated only into DNA. Their main clinical use is in the treatment of myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML), particularly in patients who are not candidates for intensive chemotherapy. These drugs help restore normal blood cell production by altering gene expression patterns through epigenetic modulation[1][2][3][4][6].
- Other names
- 5-azacytidine + 5-aza-2'-deoxycytidine
02
Targets
DNMT1 (DNA (cytosine-5)-methyltransferase 1)DNMT3B (DNA (cytosine-5)-methyltransferase 3B)DNMT3A (DNA methyltransferase 3 alpha)
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