Imatinib

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What it isBCR-ABL tyrosine kinase inhibitor; chronic myeloid leukemia and GIST.

Why this oneIt turned CML from a fatal disease into a chronic one, and it is the archetype of targeted therapy.

What limits itEdema, particularly periorbital, and myelosuppression. CYP3A4-dependent; take with food and a large glass of water.

FDA-approved for

CML/GIST (2001)

FDA label

Read the full label on DailyMed ↗

FDA dosing	Population	Start	Target	Max
Ph+ CML chronic phase	Adults	400 mg QD	400 mg QD	600 mg QD
Ph+ CML accelerated phase/blast crisis	Adults	600 mg QD	600 mg QD	800 mg/day (400 mg BID)
Ph+ CML chronic phase	Pediatrics	340 mg/m²/day	340 mg/m²/day	600 mg/day
Ph+ ALL (relapsed/refractory)	Adults	600 mg QD	600 mg QD
Ph+ ALL (newly diagnosed, with chemotherapy)	Pediatrics	340 mg/m²/day	340 mg/m²/day	600 mg/day
MDS/MPD	Adults	400 mg QD	400 mg QD
ASM	Adults	400 mg QD (100 mg QD if FIP1L1-PDGFRα+)	400 mg QD
HES/CEL	Adults	400 mg QD (100 mg QD if FIP1L1-PDGFRα+)	400 mg QD
DFSP	Adults	800 mg/day (400 mg BID)	800 mg/day
GIST (metastatic/unresectable)	Adults	400 mg QD	400 mg QD	800 mg/day (400 mg BID)
GIST adjuvant	Adults	400 mg QD	400 mg QD (3 years)

Renal Moderate (CrCl 20–39): reduce starting dose 50%, max 400 mg; mild (40–59): max 600 mg; severe: use with caution (100 mg/day tolerated)

Hepatic Mild/moderate: no adjustment; severe: reduce dose 25% (e.g., 300 mg)

Instructions

Take with a meal and a large glass of water
May disperse tablets in water or apple juice if swallowing is difficult
Doses ≥800 mg/day: use 400 mg tablets to reduce iron exposure
Increase dose by ≥50% if a strong CYP3A4 inducer must be coadministered

Cautions

Fluid retention/edema
Cytopenias (anemia, neutropenia, thrombocytopenia)
CHF/left ventricular dysfunction
Hepatotoxicity (fatal liver failure reported)
Hemorrhage (incl GI)
GI perforation
Bullous dermatologic reactions (erythema multiforme, SJS)
Hypothyroidism (thyroidectomy patients)
Embryo-fetal toxicity
Growth retardation in children
Tumor lysis syndrome
Renal toxicity

Adverse reactions

Edema
Nausea
Vomiting
Muscle cramps
Musculoskeletal pain
Diarrhea
Rash
Fatigue
Abdominal pain

Pregnancy Can cause fetal harm; avoid pregnancy; effective contraception during and 14 days after last dose

Lactation Do not breastfeed during and for 1 month after last dose

NO BOXED WARNINGS

Principal riskPeriorbital edema and myelosuppression

Cost, est. cash$50–$10,000/month or cycle

Generic entry2015

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades2 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryD

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.