Sapacitabine

**Semantic type:** Organic Chemical|Pharmacologic Substance

**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.

**Synonyms:** - CS 682 - CS-682 - CS682 - CYC682 - N-(1-(2-Cyano-2-deoxy-beta-D-arabinofuranosyl)-2-oxo-1,2-dihydropyrimidin-4-yl)-hexadecanamide - SAPACITABINE