Dangerous Drug: Imatinib Mesylate(eh mat’eh nib mess’ ah late)
GleevecDNC
PREGNANCY CATEGORY D
Drug Classes
Antineoplastic
Protein tyrosine kinase inhibitor
Therapeutic Actions
A protein tyrosine kinase inhibitor that selectively inhibits the Bcr-Abl tyrosine kinase created by the Philadelphia chromosome abnormality in CML; this inhibits proliferation and induces apoptosis in the Bcr-Abl positive cell lines as well as fresh leukemic cells, leading to an inhibition of tumor growth in CML patients in blast crisis.
Indications
Treatment of patients with Philadelphia-chromosome–positive CML in blast crisis, accelerated phase or in chronic phase after failure with interferon-alfa therapy
Treatment of patients with Kit (CD117) positive unresectable or metastatic malignant GI stromal tumors (GISTs)
NEW INDICATION: • Treatment of adult patients as adjunct therapy following resection of Kit (CD117) positive GISTs
Treatment of patients with newly diagnosed or relapsed or refractory Philadelphia chromosome–positive ALL
Treatment of aggressive systemic mastocytosis (ASM)
Treatment of adults with unresectable, recurrent, or metastatic dermatofibrosarcoma protuberans (DFSP)
Treatment of adults with myelodysplastic/myeloproliferative diseases (MDS/MPD)
Treatment of hypereosinophilic syndrome and chronic eosinophilic leukemia (HES/CEL) in adults
Treatment of pediatric patients with Philadelphia chromosome positive CML in chronic phase, whose disease recurred after stem cell transplant or who are resistant to interferon alfa therapy
Unlabeled uses: Rectal administration of twice-daily doses; polycythemia vera
Contraindications and Cautions
Contraindicated with allergy to imatinib or any of its components, pregnancy, lactation.
Use cautiously with hepatic or renal impairment; bone marrow suppression; cardiac disease, risk factors for heart failure.
Available Forms
TabletsDNC—100, 400 mg
Dosages
Dosage should be adjusted based on bone marrow function and liver toxicity.
When used with CYP3A4 inducers, increase imatinib dosage by 50% and carefully monitor patient. For dosages of 800 mg or more, use 400 mg tablets to avoid increase in iron.
Adults
Chronic phase CML: 400 mg/day PO as a once-a-day dose; increase to 600 mg/day may be considered if response is not satisfactory and patient can tolerate the drug.
Accelerated phase or blast crisis CML: 600 mg/day PO as a single dose; increase to
400 mg PO bid may be considered if response is not satisfactory and patient can tolerate the drug.
ALL: 600 mg/day PO.
ASM: 400 mg/day PO.
ASM with eosinophilia: 100 mg/day PO.
DFSP: 800 mg/day PO.
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