Nelarabine

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
  • Toxicological Effects
  • Genes that may be involved
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

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

North America

Canada: Atriance; USA: Arranon.

Asia

Japan: Arranon.

Drug combinations

Chemistry

Nelarabine: C~11~H~15~N~5~O~5~. Mw: 297.27. (1) 9-β-D-Arabinofuranosyl-6-methoxy-9H-purin-2-amine; (2) 2-Amino-9-β-D-arabinofuranosyl-6-methoxy-9H-purine. CAS-121032-29-9 (1998).

Pharmacologic Category

Antineoplastic Agents; Antimetabolites. (ATC-Code: L01BB07).

Mechanism of action

Nelarabine, prodrug of ara-G, is demethylated by adenosine deaminase to ara-G and then converted to ara-GTP. Ara-GTP is incorporated into DNA of leukemic blasts, leading to inhibition of DNA synthesis and inducing apoptosis. Ara-GTP appears to accumulate at higher levels in T-cells, which correlates to clinical response.

Therapeutic use

Treatment of relapsed or refractory T-cell acute lymphoblastic leukemia and T-cell lymphoblastic lymphoma.

Pregnancy and lactiation implications

Teratogenic effects observed in animal studies. There are no adequate, well-controlled studies in pregnant women. Excretion in breast milk unknown (not recommended in nursing women).

Unlabeled use

CML (Philadelphia chromosome positive) T-Cell blast phase.

Contraindications

Hypersensitivity to nelarabine or any component of the formulation.

Warnings and precautions

Leukopenia, thrombocytopenia, anemia, and neutropenia commonly occur in bone marrow suppression. Neurotoxicity is dose-limiting toxicity (risk of neurotoxicity may increase in concurrent or previous intrathecal chemotherapy or history of craniospinal irradiation). Appropriate measures must be taken to prevent hyperuricemia and tumor lysis syndrome (use extreme caution in increased uric acid, gout, and history of uric acid stones). Use with caution in hepatic impairment (risk of adverse reactions may be higher with hepatic dysfunction), and in renal impairment. Ara-G clearance may be reduced with renal dysfunction. Administration of live vaccines should be avoided.

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