Generic Name and Formulations:
Imatinib (as mesylate) 100mg, 400mg; tabs.
Company:
Novartis Pharmaceuticals Corp
| 03/12/13 |
| Approved Indication and dosing for pediatric patients with newly diagnosed Ph+ALL. |
Kit (CD117) (+) unresectable and/or metastatic malignant GI stromal tumors (GIST). Adjuvant treatment of adults following complete gross resection of Kit (CD117) (+) GIST.
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%.
Not recommended.
Signal transduction inhibitor.
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.
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).
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.
Hepatic (CYP3A4, 1A2, 2D6, 2C9, 2C19); 95% protein bound.
Fecal (primarily), renal.
NO
100mg—90
400mg—30
| 03/12/13 |
| Approved Indication and dosing for pediatric patients with newly diagnosed Ph+ALL. |
Philadelphia-chromosome (+) chronic myeloid leukemia (CML): in newly-diagnosed adults and children in chronic phase; in patients in blast crisis, accelerated phase, or chronic phase after failure of interferon-alpha therapy. Adults with relapsed or refractory Ph (+) acute lymphoblastic leukemia (ALL). Children with newly diagnosed Ph+ ALL in combination with chemotherapy. Adults with myelodysplastic/myeloproliferative diseases (MDS/MPD) associated with PDGFR (platelet-derived growth factor receptor) gene rearrangements. Adults with hypereosinophilic syndrome (HES) and/or chronic eosinophilic leukemia (CEL) who have the FIP1L1-PDGFRα fusion kinase and for patients with HES and/or CEL who are FIP1L1-PDGFRα fusion kinase negative or unkown.
Take with food and water. May disperse tab in water or apple juice and take promptly. ≥18yrs: Chronic phase CML: 400mg once daily. Accelerated phase or blast crisis: 600mg once daily. Relapsed/refractory Ph+ ALL: 600mg once daily. MDS/MPD: 400mg once daily. HES/CEL: 400mg once daily. HES/CEL w. FIP1L1-PDGFRα fusion kinase: initially 100mg once daily; may increase to 400mg once daily if insufficient response. 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%.
Take with food and water in 1 or 2 divided doses; may disperse tab in water or apple juice and take promptly. <1yrs: not recommended. ≥1yrs: Newly diagnosed Ph+CML: 340mg/m2 per day (max 600mg). Newly diagnosed Ph+ALL: 340mg/m2 per day (max 600mg); give with chemotherapy. If severe non-hematologic reactions develop: interrupt dose; resume at a lower dose in hepatic dysfunction. Renal or hematologic reactions: see full labeling. Potent CYP3A4 inducers (eg, phenytoin): increase imatinib dose by at least 50%; monitor closely.
Signal transduction inhibitor.
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.
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).
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.
Testing considerations: BCR-Abl t(9;22) in Ph+ CML patients
Hepatic (CYP3A4, 1A2, 2D6, 2C9, 2C19); 95% protein bound.
Fecal (primarily), renal.
NO
100mg—90
400mg—30
| 03/12/13 |
| Approved Indication and dosing for pediatric patients with newly diagnosed Ph+ALL. |
Adults with aggressive systemic mastocytosis (ASM) without the D816V c-Kit mutation or with c-Kit mutational status unknown. Adults with unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans (DFSP).
Take with food and water. May disperse tab in water or apple juice and take promptly. ≥18yrs: ASM without D816V c-Kit mutation or status unknown: 400mg once daily. ASM associated with eosinophilia: initially 100mg once daily; may increase to 400mg once daily if insufficient response. 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%.
Not recommended.
Signal transduction inhibitor.
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.
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).
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.
Hepatic (CYP3A4, 1A2, 2D6, 2C9, 2C19); 95% protein bound.
Fecal (primarily), renal.
NO
100mg—90
400mg—30