NCIt definition : An orally bioavailable pyrimidine analogue prodrug with potential antineoplastic activity.
Sapacitabine is hydrolyzed by amidases to the deoxycytosine analogue CNDAC (2'-Cyano-2'-deoxyarabinofuranosylcytosine),
which is then phosphorylated into the active triphosphate form. As an analogue of
deoxycytidine triphosphate, CNDAC triphosphate incorporates into DNA strands during
replication, resulting in single-stranded DNA breaks during polymerization due to
beta-elimination during the fidelity checkpoint process; cell cycle arrest in the
G2 phase and apoptosis ensue. The unmetabolized prodrug may exhibit antineoplastic
activity as well.;