Imatinib
- Atc Codes:L01XE01
- CAS Codes:152459-95-5
- PHARMGKB ID:152459-95-5
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Glivec; Belgium: Glivec; Bulgaria: Glivec; Cyprus: Glivec; Czech Republic: Glivec; Denmark: Glivec; Estonia: Glivec; Finland: Glivec; France: Glivec; Germany: Glivec; Greece: Glivec; Hungary: Glivec; Ireland: Glivec; Italy: Glivec; Latvia: Glivec; Lithuania: Glivec; Malta: Glivec; Netherlands: Glivec; Poland: Glivec; Portugal: Glivec; Romania: Glivec; Slovakia: Glivec; Slovenia: Glivec; Spain: Glivec; Sweden: Glivec; UK: Glivec.
North America
Canada: Gleevec; USA: Gleevec.
Latin America
Argentina: Glivec, Imatinib, Timab, Ziatir; Brazil: Glivec; Mexico: Glivec.
Asia
Japan: Glivec.
Drug combinations
Chemistry
Imatinib: C~29~H~31~N~7~O. Mw: 493.60. α-(4-Methyl-1-piperazinyl)-3′-[[4-(3-pyridyl)-2-pyrimidinyl]amino]-p-tolu-p-toluidide. CAS-152459-95-5.
Pharmacologic Category
Other Antineoplastic Agents; Protein Kinase Inhibitors. Tyrosine Kinase Inhibitor. (ATC-Code: L01XE01).
Mechanism of action
Inhibits BCR-ABL tyrosine kinase, constitutive abnormal gene product of Philadelphia chromosome in chronic myeloid leukemia (CML). Inhibition of this enzyme blocks proliferation and induces apoptosis in BCR-ABL-positive cell lines as well as in fresh leukemic cells in Philadelphia chromosome positive CML. Also inhibits tyrosine kinase for platelet-derived growth factor (PDGF), stem cell factor (SCF), c-Kit, and cellular events mediated by PDGF and SCF.
Therapeutic use
Treatment of newly diagnosed Philadelphia chromosome-positive (Ph^+^) CML in chronic phase of disease. Treatment of Ph^+^ CML in blast crisis, in accelerated phase, or in chronic phase of disease after failure of interferon alpha therapy. Treatment of pediatric patients with Ph^+^ chronic phase CML whose disease has recurred after stem cell transplantation or who are resistant to interferon alpha therapy. Treatment of Kit (CD117)-positive unresectable and/or metastatic malignant gastrointestinal stromal tumors.
Pregnancy and lactiation implications
May cause fetal harm. Teratogenicity and embryolethality demonstrated in animals. Use not recommended during lactation.
Unlabeled use
Treatment of desmoid tumors (soft tissue sarcoma).
Contraindications
Hypersensitivity to imatinib or any component of the formulation.
Warnings and precautions
Hazardous agent. May cause bone marrow suppression (anemia, neutropenia, and thrombocytopenia). Cardiovascular effects possible (usually reported in comorbidities and/or risk factors). Dermatologic reactions (erythema multiforme and Stevens-Johnson syndrome) reported. Often associated with fluid retention, weight gain, and edema (use with caution in patients where fluid accumulation may be poorly tolerated, such as in cardiovascular disease (HF or hypertension) and pulmonary disease). May cause GI irritation. Severe hemorrhage reported with use, including GI hemorrhage and/or tumor hemorrhage. Hepatotoxicity might occur (may be severe). Acute liver failure also reported. Opportunistic infections might develop. Use with caution in bone marrow suppression. Use with caution in hepatic or renal impairment. Hypothyroidism reported in thyroidectomy patients (receiving thyroid hormone replacement therapy) during imatinib therapy. High potential for CYP interactions. Risk of severe superficial edema (e.g. rapid weight gain, facial edema, anasarca), severe fluid retention (i.e. pleural effusion, pericardial effusion, pulmonary edema, ascites), cerebral edema, increased intracranial pressure, and papilledema (including fatalities).