Deferasirox

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Substrate of
  • Inhibits
  • Induces
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

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

North America

Canada: Exjade; USA: Exjade.

Latin America

Argentina: Exjade; Brazil: Exjade.

Asia

Japan: Exjade.

Drug combinations

Chemistry

Deferasirox: C~21~H~15~N~3~O~4~. Mw: 373.36. (1) Benzoic acid, 4-[3,5-bis(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl]-; (2) 4-[3,5-bis(2-Hydroxyphenyl)-1H-1,2,4-triazol-1-yl]benzoic acid. CAS-201530-41-8 (2004).

Pharmacologic Category

Heavy Metal Antagonists; Chelating Agent. Antidotes. (ATC-Code: V03AC03).

Mechanism of action

Heavy metal antagonist; chelating agent for iron. Selectively binds iron, forming a complex which is excreted through the feces.

Therapeutic use

Treatment of chronic iron overload due to blood transfusions in thalassemia or other chronic anemias (designated an orphan drug by FDA for this use).

Pregnancy and lactiation implications

Teratogenic effects not observed in animal studies. There are no adequate, well-controlled studies in pregnant women. Use during pregnancy only if clearly needed.

Unlabeled use

Contraindications

Hypersensitivity to deferasirox or any component of the formulation.

Warnings and precautions

Decreased hearing and high frequency hearing loss reported. Cytopenias (agranulocytosis, neutropenia, and thrombocytopenia) in preexisting hematologic disorders reported. Hepatic dysfunction or failure, mostly in patients >55 years of age with underlying comorbidities (including hepatic cirrhosis and multiorgan failure). Hepatitis and elevated transaminases also reported. Hypersensitivity reactions (anaphylaxis and angioedema) may occur, usually within the first month of treatment. Cases of nephrotoxicity reported. May cause proteinuria. Ocular disturbances (lens opacities, cataracts, intraocular pressure elevation, and retinal disorders) reported. May cause skin rash (dose-related). Avoid combination with other iron chelation therapies.

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