Clofarabine

General information

Clofarabine (Clolar®) is a purine nucleoside analogue, which has been approved for the treatment of relapsed or refractory acute lymphoblastic leukemia in children after at least two prior regimens. The active 5′-triphosphate metabolite inhibits DNA synthesis by reducing cellular pools of deoxynucleotide triphosphate. In addition, drug-related inhibition of ribonucleotide reductase and termination of DNA chain elongation contribute to clofarabine’s antineoplastic activity. After intravenous administration of 52 mg/m ² /day for 5 days the half-life averages 5.2 hours. More than 50% of the dose is excreted in the urine unchanged, and the dosage must be modified in patients with reduced renal function [ ].

Severe myelosuppression, including neutropenia, anemia, and thrombocytopenia, has been described as a dose-limiting adverse effect. The risk of severe infection may therefore be increased. In addition, dose-limiting non-hematological adverse effects, including rashes and reversible hyperbilirubinemia and raised aminotransferase activities, have been described [ ].