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azacitidine + temozolomide
- Development stage
- Unknown
- Lead developer
- Bristol Myers Squibb
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Intravenous, Oral, Subcutaneous
01
Overview
Azacitidine + temozolomide is an investigational combination therapy involving two small molecule chemotherapeutic agents. Azacitidine is a pyrimidine nucleoside analogue and DNA methyltransferase inhibitor that incorporates into RNA and DNA, disrupting their metabolism and inhibiting protein synthesis, as well as impairing DNA methylation. It is primarily used in the treatment of myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML)[3]. Temozolomide is an oral alkylating agent that acts by methylating DNA at several sites, most notably the O6 position of guanine, leading to tumor cell apoptosis[4][6]. The combination has been studied in early-phase clinical trials for various cancers, including glioma and other solid tumors[1][2]. The rationale for combining these drugs includes potential synergistic effects through epigenetic modification (demethylation) by azacitidine enhancing the cytotoxicity of temozolomide[2].
- Other names
- 5-azacytidine + temozolomide5-AZA + TMZ
02
Targets
DNMT (DNA methyltransferase)
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