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Clofarabine

Last updated on September 23, 2021

(British Approved Name, US Adopted Name, rINN)

ClofarabineDrug Nomenclature

International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):

Synonyms: Cl-F-Ara-A; Clofarabina
BAN: Clofarabine
USAN: Clofarabine
INN: Clofarabine [rINN (en)]
INN: Clofarabina [rINN (es)]
INN: Clofarabine [rINN (fr)]
INN: Clofarabinum [rINN (la)]
INN: Кльофарабин [rINN (ru)]
Chemical name: 2-Chloro-9-(2-deoxy-2-fluoro-β-d-arabinofuranosyl)-9H-purin-6-amine
Molecular formula: C10H11ClFN5O3 =303.7
CAS: 123318-82-1
ATC code: L01BB06

Adverse Effects, Treatment, and Precautions

As for Fludarabine Phosphate, although neurotoxicity is less severe. Capillary leak syndrome resulting from cytokine release has occurred with clofarabine, causing respiratory distress, hypotension, pleural and pericardial effusions, and multi-organ failure. Prophylactic corticosteroids may be useful, but clofarabine must be stopped immediately if signs or symptoms of capillary leak syndrome develop (respiratory status and blood pressure should be monitored during infusion). Other adverse effects include anxiety, flushing, tachycardia, hypotension, hepatotoxicity, haematuria, myalgia, arthralgia, and headache. Renal and hepatic function, and complete blood counts, should be monitored during clofarabine therapy. Hydration should be maintained during treatment to minimise the risk of tumour lysis syndrome and other adverse effects.

Pharmacokinetics

Clofarabine is about 47% bound to plasma proteins. About 50 to 60% of a dose is excreted unchanged in the urine and it has a terminal half-life of about 5 hours.

Uses and Administration

Clofarabine, a purine nucleoside analogue, is used as an antimetabolite antineoplastic in the treatment of relapsed or refractory acute lymphoblastic leukaemia in patients aged 1 to 21 years. A dose of 52 mg/m is given daily for 5 days, by intravenous in fusion over 2 hours. A longer infusion time should be considered in children weighing less than 20 kg to reduce anxiety and irritability, and to avoid high clofarabine concentrations. The course may be repeated every 2 to 6 weeks, depending on the patient’s recovery from bone-marrow depression and other adverse effects. Treatment is usually assessed after 2 treatment cycles. Clofarabine is under investigation for the treatment of acute myeloid leukaemia, myelodysplastic syndrome, and solid tumours.

Proprietary Preparations

Czech Republic: Evoltra;

France: Evoltra;

Portugal: Evoltra;

United Kingdom (UK): Evoltra;

United States of America (US and USA): Clolar

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