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sapacitabine + decitabine
- Development stage
- Unknown
- Lead developer
- Cyclacel 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, Covalent Small Molecules → Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Sapacitabine + decitabine is an investigational combination of two small molecule chemotherapeutic agents. Decitabine is a pyrimidine nucleoside analogue and hypomethylating agent that incorporates into DNA and inhibits DNA methyltransferases, leading to global DNA hypomethylation and reactivation of silenced tumor suppressor genes. This results in decreased neoplastic cell proliferation and increased cellular differentiation or apoptosis[4][5][6]. Sapacitabine is also a nucleoside analogue with antitumor activity (not detailed in the provided search results). The combination has been studied primarily for hematologic malignancies such as myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML).
02
Targets
DNMT3A (DNA methyltransferase 3 alpha)DNMT3B (DNA (cytosine-5)-methyltransferase 3B)DNMT1 (DNA (cytosine-5)-methyltransferase 1)
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