Imatinib
GLEEVEC
Pronunciation: i-MAT-in-ib
“I'm a tiny nibbler, a Gleeful vector”
derived from Vector character (Despicable Me)
What it isBCR-ABL tyrosine kinase inhibitor; chronic myeloid leukemia and GIST.
Why this oneTurned fatal CML into a chronic disease; archetype of targeted therapy.
What limits itEdema, particularly periorbital, and myelosuppression. CYP3A4-dependent; take with food and a large glass of water.
Imatinib prescription history
Animated chart of estimated U.S. prescriptions per year, Tyrosine kinase inhibitors (2001–2026). Imatinib enters in 2001 (estimated).
FDA-approved for
- CML/GIST (2001)
Principal riskPeriorbital edema and myelosuppression
Classes and tags
Clinical profile
Legacy pregnancy categoryD
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
FDA label
Read the full label on DailyMed ↗
NO BOXED WARNINGS
| 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
Available strengths
- tab 100, 400 mg
- sol 80 mg/mL
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
Cost
Generic entry2015
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Memory aids: interaction avatars
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Self-check
- How should imatinib be taken?
With food and a large glass of water. - Where is imatinib edema particularly characteristic?
Around the eyes.