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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › BCR-ABL tyrosine kinase inhibitors
imatinib
L01EA01
Forms & Strengths
- Oral tablets: 100 mg
- Oral tablets: 400 mg
Adult Dosing
- Newly diagnosed CML-CP: 400 mg orally once daily
- CML blast crisis or accelerated phase: 600 mg orally once daily
- GIST: 400 mg to 600 mg orally once daily
Pediatric Dosing
- CML in pediatric patients: 340 mg/m² orally once daily (max 600 mg/day)
- Administer either once daily or divided into two daily doses (morning and evening)
Indications
- Newly diagnosed chronic myeloid leukemia (CML) Philadelphia chromosome-positive
- CML in blast crisis, accelerated phase, or in chronic phase after failure of interferon-alpha therapy
- Kit (CD117)-positive unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST)
Mechanism of Action
- Inhibitor of the Bcr-Abl tyrosine kinase, the constitutive abnormal tyrosine kinase created by the Philadelphia chromosome abnormality in CML
- Inhibits receptor tyrosine kinases for platelet-derived growth factor (PDGF) and stem cell factor (SCF), c-Kit
Contraindications
- Hypersensitivity to imatinib or any excipient
Adverse Reactions
- Fluid retention and severe superficial edema
- Nausea, vomiting, diarrhea, abdominal pain, and dyspepsia
- Musculoskeletal pain, muscle cramps, and arthralgia
- Myelosuppression including neutropenia, thrombocytopenia, and anemia
- Hepatotoxicity and elevated liver transaminases
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole) may increase imatinib plasma concentrations
- Strong CYP3A4 inducers (e.g., rifampin) may significantly decrease imatinib plasma concentrations
- Imatinib inhibits CYP3A4, CYP2C9, and CYP2D6, potentially increasing plasma levels of substrates such as simvastatin, warfarin, and metoprolol
Curated Content: Needs Vetting Before Put to Clinical Use