Deferasirox

Deferasirox Brand Names- Exjade | JADENU

What is Deferasirox

Deferasirox is a first in class, tridentate, oral, iron-chelating agent used in the treatment of chronic iron overload secondary to multiple RBC transfusions (i.e., transfusional iron overload) and non-transfusion dependent thalassemia syndromes.

Iron overload is a serious complication caused by frequent blood transfusions in patients with blood transfusion-dependent anemias, such as ß-thalassemia, sickle cell disease, other rare anemias, and myeloproliferative disorders.

Deferasirox has been developed as an alternative to deferoxamine, the standard treatment of chronic iron overload, which is administered parenterally.

In patients with chronic iron toxicity, chelation treatments are effective for rapid iron removal, maintenance of low iron stores, prevention of heart and other organ damage caused by iron overload, and ultimately improved survival.

A large number of patients that require iron chelation therapy with deferoxamine often do not receive adequate therapy due to noncompliance.

Because deferasirox is administered orally once daily, it will likely be a more acceptable regimen for chronic use, thus enhancing the management of chronic iron toxicity.

Additionally, the quality of life of patients who require lifelong iron-chelating therapy may be considerably improved.

Despite the benefits, health care providers are urged to consider the risks versus benefits of prescribing deferasirox.

To highlight these risks, the product labeling contains a Black Box Warning regarding potential for renal failure, hepatic failure, and gastrointestinal hemorrhages. In some cases these adverse events have resulted in fatalities, particularly in elderly and pediatric patients.

Indications

  1. iron toxicity
  2. transfusional iron overload

For the treatment of chronic iron toxicity secondary to transfusional iron overload or non-transfusion-dependent thalassemia syndromes

for the initiation of therapy for chronic iron toxicity secondary to transfusional iron overload (transfusional hemisiderosis)

Side Effects

  1. abdominal pain
  2. agranulocytosis
  3. alopecia
  4. anaphylactoid reactions
  5. angioedema
  6. anxiety
  7. cataracts
  8. cholelithiasis
  9. diarrhea
  10. dizziness
  11. Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)
  12. edema
  13. elevated hepatic enzymes
  14. erythema multiforme
  15. esophagitis
  16. Fanconi syndrome
  17. fatigue
  18. fever
  19. gastritis
  20. GI bleeding
  21. GI perforation
  22. glycosuria
  23. hearing loss
  24. hematuria
  25. hepatic failure
  26. hepatitis
  27. hepatotoxicity
  28. hypokalemia
  29. insomnia
  30. interstitial nephritis
  31. maculopapular rash
  32. nausea
  33. nephrotoxicity
  34. neutropenia
  35. optic neuritis
  36. pancreatitis
  37. peptic ulcer
  38. proteinuria
  39. purpura
  40. rash
  41. renal failure (unspecified)
  42. Stevens-Johnson syndrome
  43. thrombocytopenia
  44. toxic epidermal necrolysis
  45. urticaria
  46. vasculitis
  47. visual impairment
  48. vomiting

Monitoring Parameters

  • audiometry
  • CBC with differential
  • ferritin
  • LFTs
  • ophthalmologic exam
  • serum creatinine/BUN
  • serum electrolytes
  • urinalysis

Contraindications

  • agranulocytosis
  • anemia
  • angioedema
  • anticoagulant therapy
  • bone marrow suppression
  • breast-feeding
  • cataracts
  • children
  • corticosteroid therapy
  • diarrhea
  • driving or operating machinery
  • geriatric
  • GI bleeding
  • GI perforation
  • glaucoma
  • hearing impairment
  • hepatic decompensation
  • hepatic disease
  • hepatitis
  • hepatotoxicity
  • hypovolemia
  • infants
  • myelodysplastic syndrome (MDS)
  • neonates
  • neoplastic disease
  • nephrotoxicity
  • neutropenia
  • peptic ulcer disease
  • pregnancy
  • proteinuria
  • renal disease
  • renal failure
  • renal impairment
  • serious hypersensitivity reactions or anaphylaxis
  • serious rash
  • thrombocytopenia
  • visual disturbance
  • vomiting

Interactions

  • Acetaminophen; Aspirin, ASA; Caffeine
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  • Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
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