Generic Name and Formulations:
Imatinib (as mesylate) 100mg, 400mg; tabs.

Company:
Novartis Pharmaceuticals Corp

Indications for GLEEVEC:
Kit (CD117) (+) unresectable and/or metastatic malignant GI stromal tumors (GIST). Adjuvant treatment of adults following complete gross resection of Kit (CD117) (+) GIST.

Adult Dose for GLEEVEC:
Take with food and water. May disperse tab in water or apple juice and take promptly. ≥18yrs: GIST: 400mg once daily; up to 800mg daily (given as 400mg twice daily) may be considered if clinically indicated. Adjuvant GIST treatment: 400mg once daily; 36 months of treatment recommended (see full labeling). If severe non-hematologic reactions develop: interrupt dose; resume at a lower dose in hepatic dysfunction. Severe hepatic impairment: reduce dose by 25%. Renal or hematologic reactions: see full labeling. Potent CYP3A4 inducers (eg, rifampin): increase imatinib dose by at least 50%.

Children's Dose for GLEEVEC:
Not recommended.

Pharmacological Class:
Signal transduction inhibitor.

Warnings/Precautions:
Hepatic or renal impairment. Immunosuppressed. Monitor weight and for fluid retention regularly; CBCs weekly for 1st month, bi-weekly for 2nd month, then periodically (eg, every 2–3 months); liver function at baseline then monthly or as needed. Monitor for tumor lysis syndrome; correct clinically significant dehydration and treat high uric acid levels before initiating therapy. Monitor growth in children. Cardiovascular disease. Elderly. Avoid pregnancy (Cat.D); nursing mothers: not recommended; see full labeling.

Interactions:
Potentiated by CYP3A4 inhibitors (eg, azole antifungals, macrolides). Antagonized by CYP3A4 inducers (eg, dexamethasone, phenytoin, phenobarbital, carbamazepine, St. John's wort, rifampin). May potentiate drugs metabolized by CYP3A4 (eg, acetaminophen, benzodiazepines, dihydropyridine calcium channel blockers, cyclosporine, pimozide, statins), CYP2D6, or CYP2C9 (use heparin instead of warfarin).

Adverse Reactions:
GI disturbances, edema (may be severe), bleeding, muscle cramps, fever, pain, rash (may be severe; eg, erythema multiforme, Stevens-Johnson syndrome), fatigue, dizziness, blurred vision, somnolence, headache, cough, arthralgia/myalgia, dyspnea, hypokalemia, night sweats, anorexia, pruritus, neutropenia, thrombocytopenia, weight gain, renal or hepatotoxicity, immunosuppression, hypothyroidism in thyroidectomy patients undergoing levothyroxine replacement (monitor TSH levels); rare: severe CHF, left ventricular dysfunction.

Metabolism:
Hepatic (CYP3A4, 1A2, 2D6, 2C9, 2C19); 95% protein bound.

Elimination:
Fecal (primarily), renal.

Generic Availability:
NO

How Supplied:
100mg—90
400mg—30