Drug intelligence / Profile preview

sapacitabine

Development stage
Discontinued
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
Administration
Oral
01

Overview

Sapacitabine is an orally administered small molecule nucleoside analog prodrug developed primarily for the treatment of various cancers, including acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS). It is a derivative of 2'-deoxycytidine and acts as a DNA-damaging agent. After administration, sapacitabine is converted in the body to its active metabolite CNDAC (2'-C-cyano-2'-deoxy-1-β-D-arabino-pentofuranosyl-cytosine), which incorporates into DNA during replication. This incorporation leads to single-strand breaks that are subsequently converted into double-strand breaks during subsequent rounds of DNA replication, resulting in cell cycle arrest and apoptosis of cancer cells. Sapacitabine has been investigated mainly for hematological malignancies but also for some solid tumors. It is developed and manufactured by Cyclacel Pharmaceuticals.

02

Targets

DNA polymerase family

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