clofarabine

Description: Clofarabine(formerly C1 F-Ara-A; C1 F-Ara-A; CAFdA; trade names: Clofarex; Clolar) is an antimetabolite anticancer chemotherapeutic drug and a purine nucleoside approved for the treatment of relapsed or refractory acute lymphoblastic leukemia. It acts as a DNA synthesis inhibitor as well as a substrate of Deoxycytidine kinase (dCK). Clofarabine is phosphorylated to form clofarabine triphosphate, which competes with dATP for DNA polymerase-alpha and -epsilon. At the same time, clofarabine-monophosphate is incorporated into internal and terminal DNA sites, which impaired DNA elongation and repair. Clofarabine triphosphate inhibits ribonucleotide reductase with IC50 value of 65 nM, which then reduced dCTP and dATP. Clofarabine is efficiently transported into cells through nucleoside transporters hENT1, hENT2, and hCNT2.

References: Nat Rev Drug Discov. 2006 Oct; 5(10):855-63; Clin Cancer Res. 2001 Nov; 7(11):3580-9.

C1-F-Ara-A; Clofarabine, C1 F-Ara-A; C1 F-Ara-A; trade names: Clofarex; Clolar. Abbreviation: CAFdA