Deferasirox

EXJADE

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What it isOral iron chelator; transfusional iron overload.

Why this oneOral once-daily chelation replacing overnight subcutaneous infusions.

What limits itRenal and hepatic failure and GI hemorrhage require monitoring. GI upset and rash are common.

FDA label

BOXED WARNING Renal failure (incl. fatal), hepatic failure (incl. fatal), and GI hemorrhage; monitor renal/hepatic function; contraindicated if eGFR <40.

FDA dosing	Population	Start	Target	Max
Transfusional iron overload	>=2 yr, eGFR >60	20 mg/kg QD	adjust q3-6 mo by ferritin trend	per titration
Non-transfusion-dependent thalassemia (NTDT) iron overload	eGFR >60	10 mg/kg QD	adjust by ferritin/LIC	per titration

Titration Adjust every 3-6 months based on serum ferritin trends.

Renal Contraindicated if eGFR <40. eGFR 40-60: reduce starting dose by 50%. Evaluate baseline renal function; monitor at least monthly.

Hepatic Severe (Child-Pugh C): avoid. Moderate (Child-Pugh B): reduce starting dose by 50%. Mild (Child-Pugh A): monitor closely.

Instructions

Take orally once daily as an oral suspension; calculate dose to nearest whole tablet.
Obtain baseline renal function (serum creatinine in duplicate), LFTs/bilirubin, auditory and ophthalmic exams before starting.

Contraindications

Estimated GFR <40 mL/min/1.73 m2
Poor performance status
High-risk myelodysplastic syndrome
Advanced malignancies
Platelet count <50 x 10^9/L

Cautions

Acute kidney injury/renal failure and renal tubular toxicity (Fanconi syndrome)
Hepatic toxicity and failure
GI hemorrhage/ulceration
Bone marrow suppression
Hypersensitivity
Severe skin reactions (SJS/TEN/DRESS)
Auditory and ocular abnormalities

Adverse reactions

Diarrhea
Vomiting
Nausea
Abdominal pain
Skin rash
Increased serum creatinine

Pregnancy Use only if potential benefit justifies fetal risk; animal decreased offspring viability and renal anomalies.

Lactation Undefined

⚠ BOXED WARNINGS

Renal failure
Hepatic failure
Gastrointestinal hemorrhage

Cost, est. cash$20–$2,000/month

Generic entry2016

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger3 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk1 / 4

Legacy pregnancy categoryUnknown / historical label unavailable

Defining liabilityAgent-specific cardiovascular, neurologic or metabolic toxicity requires monitored use in poisoning or overload.

Mechanism of action: Deferasirox ballicule

Deferasirox ballicule: receptor binding, kinetics and half-life diagram

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