Clofarabine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Evoltra; Belgium: Evoltra; Bulgaria: Evoltra; Cyprus: Evoltra; Czech Republic: Evoltra; Denmark: Evoltra; Estonia: Evoltra; France: Evoltra; Germany: Evoltra; Greece: Evoltra; Hungary: Evoltra; Ireland: Evoltra; Italy: Evoltra; Latvia: Evoltra; Lithuania: Evoltra; Luxembourg: Evoltra; Malta: Evoltra; Netherlands: Evoltra; Poland: Evoltra; Portugal: Evoltra; Romania: Evoltra; Slovakia: Evoltra; Slovenia: Evoltra; Spain: Evoltra; Sweden: Evoltra; UK: Evoltra.

North America

USA: Clolar.

Drug combinations

Chemistry

Clofarabine: C~10~H~11~ClFN~5~O~3~. Mw: 303.68. (1) 9H-Purin-6-amine, 2-chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-; (2) 2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine. CAS-123318-82-1 (2003).

Pharmacologic Category

Antineoplastic Agents; Antimetabolite Agent; Purine Antagonist. (ATC-Code: L01BB06).

Mechanism of action

Clofarabine, a purine nucleoside analog is metabolized to clofarabine 5′-triphosphate, which competes with deoxyadenosine triphosphate for binding to ribonucleotide reductase and DNA polymerase. Clofarabine inhibits DNA synthesis, terminates DNA chain elongation, and inhibits DNA repair resulting in decreased cell replication and repair. Clofarabine disrupts the mitochondrial membrane, which results in the release of proteins, cytochrome C and apoptosis-inducing factor leading to cell death.

Therapeutic use

Relapsed or refractory acute lymphoblastic leukemia.

Pregnancy and lactiation implications

Teratogenic effects observed in animals. There are no adequate tests in pregnant women. Not recommended during lactation.

Unlabeled use

Relapsed and refractory acute myeloid leukemia, chronic myeloid leukemia in blast phase, acute lymphocytic leukemia, myelodysplastic syndrome.

Contraindications

Hypersensitivity to clofarabine or any component of the formulation.

Warnings and precautions

Hazardous agent. Myelosuppression (dose-dependent) is common. Cytokine release may develop into systemic inflammatory response syndrome/capillary leak syndrome, and organ dysfunction. Tumor lysis syndrome may occur. Use with caution in hepatic/renal impairment.

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