Second generation purine nucleoside analogue which integrates fludarabine and cladribine.
Retains 2-halogenated adenine making it resistant to deamination and has a fluoride molecule at the 2’ position of the carbohydrate prevents phosphorylation improving bioavailability and prevents release of neurotoxic halogenat4d adenine moiety.
Inhibits DNA polymerases and ribonucleotide reductase.
Disrupts the integrity of the mitochondria membrane, releasing proapoptotic mitochondria proteins and cytochrome C.
Has activity in adult acute myelogenous leukemia.
Not susceptible to metabolic deactivation by phosphorolytic cleavage.
Resistant to deamination by adenosine deaminase.
Oral bioavailabilty 50-60%.
Administered intravenously, as an anti metabolite, for acute lymphoblastic leukemia.
Has activity in adult acute myelogenous leukemia.
Study of older patients with relapsed or refractory AML, a combination of clofarabine plus cytarabine compared with cytarabine alone: Overall survival did not differ, but the combination significantly improved response rates of 46.9% versus 22.9%, and increased event free survival as well Faderi S et al).