1-(2-cyano-2-deoxy-β- D-arabinofuranosyl)-4-(palmitoylamino)pyrimidin-2(1 H)-one
Legal status ?
ATC code None
N-[1-[(2 R,3 S,4 S,5 R)-3-Cyano-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-2-oxopyrimidin-4-yl]hexadecanamide
C 26 H 42 N 4 O 5
Mol. mass 490.64 g/mol
(what is this?) (verify)
Sapacitabine is a drug undergoing research for potential use in chemotherapy. [1 ] [2 ]
Sapacitabine is an oral
nucleoside analog prodrug that acts through a dual mechanism. The compound interferes with DNA synthesis by causing single-strand DNA breaks and induces arrest of the cell division cycle at G2 phase.
Both sapacitabine and its major
metabolite, CNDAC, have demonstrated potent anti-tumor activity in both blood and solid tumors in preclinical studies. In a liver metastatic mouse model, sapacitabine was shown to be superior to gemcitabine (Gemzar; Lilly) or 5-FU, two widely used nucleoside analogs, in delaying the onset and growth of liver metastasis.
Clinical trials [ edit ]
Cyclacel has initiated a number of
clinical trials to evaluate sapacitabine in both solid and hematological tumors laying the foundation for future Phase 2 studies and combination studies with other anti-cancer agents. Three Phase 1 studies have been completed, which evaluated safety and pharmacokinetics of a variety of dosing schedules in approximately 120 patients with solid tumors.
Sapacitabine is currently being evaluated in two Phase 2 trials in patients with advanced
cutaneous T-cell lymphoma (CTCL) and in elderly patients with acute myeloid leukemias (AML).
As of February 2013
phase 3 trial for AML. [3 ]
it is in a
References [ edit ]