Exjade
Exjade - General Information
Exjade is an oral iron chelator. Its main use is to reduce chronic iron overload in patients who are receiving long term blood transfusions for conditions such as beta-thalassemia and other chronic anemias. It is the first oral medication approved in the USA for this purpose.
Pharmacology of Exjade
Exjade is an orally active chelator that is selective for iron (as Fe3+). It is a tridentate ligand that binds iron with high affinity in a 2:1 ratio. Although deferasirox has very low affinity for zinc and copper there are variable decreases in the serum concentration of these trace metals after the administration of deferasirox. The clinical significance of these decreases is uncertain.
Exjade for patients
Exjade should be taken once daily on an empty stomach at least 30 minutes prior to food, preferably at the same time every day. The tablets should not be chewed or swallowed whole. The tablets should first be completely dispersed in water, orange juice, or apple juice, and the resulting suspension drunk immediately. After swallowing the suspension, any residue should be resuspended in a small volume of the liquid and swallowed.
Patients should be cautioned not to take aluminum-containing antacids and Exjade simultaneously. Because auditory and ocular disturbances have been reported with Exjade, patients should have auditory and ophthalmic testing before starting Exjade treatment and thereafter at regular intervals.
Patients experiencing dizziness should exercise caution when driving or operating machinery.
Exjade Interactions
The concomitant administration of Exjade and aluminum-containing antacid preparations has not been formally studied. Although deferasirox has a lower affinity for aluminum than for iron, Exjade should not be taken with aluminum-containing antacid preparations.
In healthy volunteers, Exjade had no effect on the pharmacokinetics of digoxin. The effect of digoxin on Exjade pharmacokinetics has not been studied.
The concomitant administration of Exjade and vitamin C has not been formally studied. Doses of vitamin C up to 200 mg were allowed in clinical studies without negative consequences.
The interaction of Exjade with hydroxyurea has not been formally studied. No inhibition of deferasirox metabolism by hydroxyurea is expected based on the results of an in vitro study.
Exjade should not be combined with other iron chelator therapies, as safety of such combinations has not been established.
Drug/Food Interactions
The bioavailability (AUC) of deferasirox was variably increased when taken with a meal. Deferasirox should be taken on an empty stomach 30 minutes before eating.
Exjade tablets for oral suspension can be dispersed in water, orange juice, or apple juice.
Exjade Contraindications
Use of Exjade® (deferasirox) is contraindicated in patients with hypersensitivity to deferasirox or to any other component of Exjade.
Additional information about Exjade
Exjade Indication: For the treatment of chronic iron overload due to blood transfusions (transfusional hemosiderosis) in patients 2 years of age and older.
Mechanism Of Action: Exjade works in treating iron toxicity by binding trivalent (ferric) iron (for which it has a strong affinity), forming a stable complex which is eliminated via the kidneys.
Drug Interactions: Aluminium Possible physicochemical interaction
Food Interactions: Tablets should be taken on an empty stomach at least 30 minutes before a meal, preferably at the same time everyday.
Food causes inconsistent increases in the bioavailability of this product.
Tablets should be completely dispersed in water, orange juice or apple juice and the resulting suspension should be ingested immediately (after swallowing the suspension, any residue should be resuspended in a small volume of liquid and swallowed).
Dispersion in carbonated drinks or milk is not recommended due to foaming and slow dispersion, respectively.
Generic Name: Deferasirox
Synonyms: Deferasiroxum [inn-latin]
Drug Category: Iron Chelating Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Deferasirox: Exjde;
Absorption: The absolute bioavailability (AUC) of deferasirox tablets for oral suspension is 70% compared to an intravenous dose.
Toxicity (Overdose): Not Available
Protein Binding: Deferasirox is highly (~99%) protein bound almost exclusively to serum albumin.
Biotransformation: Hepatic. CYP450-catalyzed (oxidative) metabolism of deferasirox appears to be minor in humans (about 8%). Glucuronidation is the main metabolic pathway for deferasirox, with subsequent biliary excretion.
Half Life: The mean elimination half-life ranged from 8 to 16 hours following oral administration.
Dosage Forms of Exjade: Tablet, for suspension Oral
Chemical IUPAC Name: 4-[(3Z,5E)-3,5-bis(6-oxo-1-cyclohexa-2,4-dienylidene)-1,2,4-triazolidin-1-yl]benzoic acid
Chemical Formula: C21H15N3O4
Deferasirox on Wikipedia: https://en.wikipedia.org/wiki/Deferasirox
Organisms Affected: Humans and other mammals
