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Imatinib

    Brands

    DEA Class; Rx

    Common Brand Names; Gleevec

    • Antineoplastics, Tyrosine Kinase Inhibitor; 
    • PDGFR-alpha Inhibitors

    Oral BCR-ABL tyrosine kinase inhibitor
    Used in Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia and Ph+ acute lymphoblastic leukemia in adults and pediatric patients, and myelodysplastic/myeloproliferative diseases, aggressive systemic mastocytosis, hypereosinophilic syndrome and/or chronic eosinophilic leukemia, dermatofibrosarcoma protuberans, and malignant gastrointestinal stromal tumors in adults
    Severe myelosuppression, congestive heart failure, and hepatotoxicity have been reported

    Indicated for adults with relapsed or refractory Philadelphia chromosome positive (Ph+) acute lymphoblastic leukemia (ALL)

    Indicated for patients with hypereosinophilic syndrome (HES) and/or chronic eosinophilic leukemia (CEL) who have the FIP1L1-PDGFRα fusion kinase (mutational analysis or FISH demonstration of CHIC2 allele deletion) and for patients with HES and/or CEL who are FIP1L1-PDGFRα fusion kinase negative or unknown

    Indicated for patients with Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) who are newly-diagnosed in chronic phase, or who are in blast crisis, accelerated phase, or chronic phase after interferon-alpha therapy

    Indicated for adults with unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans

    Indicated for adults with aggressive systemic mastocytosis without the D816V c-Kit mutation as determined with an FDA-approved test or with c-Kit mutational status unknown

    —

    • Decreased hemoglobin (46.9-72.2%)
    • Fluid retention (61.7%)
    • Diarrhea (43.8-59.3%)
    • Periorbital edema (47.2-59.3%)
    • Fatigue (38.8-57%)
    • Nausea (41-53.1%)
    • Rash and related terms (19-40.1%)
    • Decreased WBC count (14.5-34.5%)
    • Musculoskeletal pain (47%)
    • Headache (23-37%)
    • Abdominal pain (14-36.5%)
    • Joint pain (31.4%)
    • Muscle spasms (30.9%)
    • Increased AST (12.2-30.9%)
    • Nasopharyngitis (30.5%)
    • Increased blood creatinine (11.6-30.4%)
    • Dermatitis (29.4%)
    • Increased ALT (16.6-28.9%)
    • Hemorrhage (28.9%)
    • Peripheral edema (26.7%)
    • Pain (25.8%)
    • Decreased neutrophils (16-24.2%)
    • Myalgia (12.2-24.1%)
    • Hypoproteinemia (23.7%)
    • Vomiting (10.8-22.5%)
    • Upper respiratory tract infection (5-21.2%)
    • Cough (20%)
    • Dizziness (4.6-19.4%)
    • Flatulence (8.9-19.1%)
    • Dyspepsia (12-18.9%)
    • Increased lacrimation (9.8-18%)
    • Pharyngeal pain (18.1%)
    • Pyrexia (6.2-17.8%)
    • Anorexia (16.9%)
    • Increased weight (16.9%)
    • Increased weight (13.4-15.6%)
    • Arthralgia (15.1%)
    • Depression (6.8-14.9%)
    • Insomnia (9.8-14.7%)
    • Facial edema (14%)
    • Infection (13.9%)
    • Pruritus (7-12.9%)
    • Constipation (8-12.8%)
    • Dizziness (12.5%)
    • Asthenia (12%)
    • Hypoalbuminemia (11.9%)
    • Sinusitis (11.4%)
    • Alopecia (7-11.3%)
    • Decreased platelets (5-11.3%)
    • Increased bilirubin (11.3%)
    • Bone pain (11.3%)
    • Cough (11%)
    • Increased blood alkaline phosphate (6.5-10.8%)
    • Blurred vision (5-10.8%)
    • Decreased weight (10.1%)

    Hypothyroidism reported in patients post-thyroidectomy on levothyroxine replacement; closely monitor TSH levels

    Risk of severe CHF or left ventricular dysfunction, especially in patients with comorbidities; monitor and treat patients with cardiac disease or risk factors for cardiac failure

    Cardiac adverse reactions were more frequent in patients with advanced age or co-morbidities, including previous medical history of cardiac disease; carefully monitor patients with cardiac disease or risk factors for cardiac or history of renal failure; evaluate and treat any patient with signs or symptoms consistent with cardiac or renal failure

    In patients with hypereosinophilic syndrome with occult infiltration of HES cells within the myocardium, cases of cardiogenic shock/left ventricular dysfunction have been associated with HES cell degranulation upon initiation of imatinib therapy; reported to be reversible with the administration of systemic steroids, circulatory support measures, and temporarily withholding imatinib

    Myelodysplastic/myeloproliferative disease and systemic mastocytosis may be associated with high eosinophil levels; consider performing an echocardiogram and determining serum troponin in patients with HES/CEL, and in patients with MDS/MPD or ASM associated with high eosinophil levels; if either is abnormal, consider prophylactic use of systemic steroids (1–2 mg/kg) for one to two weeks concomitantly with drug at the initiation of therapy

    If anticoagulation required, use LMW or standard heparin instead of warfarin

    Fetal harm when administered to a pregnant woman based on human and animal data

    Imatinib and its active metabolite are excreted into human milk

    Adults

    800 mg/day PO.

    Geriatric

    800 mg/day PO.

    Adolescents

    340 mg/m2 per day PO (maximum of 600 mg/day) for Ph+ ALL or chronic-phase CML.

    Children

    340 mg/m2 per day PO (maximum of 600 mg/day) for Ph+ ALL or chronic-phase CML.

    Infants

    Safety and efficacy not established.

    Imatinib mesylate 

    tablet

    • 100mg
    • 400mg