GI stromal tumor (GIST) after failure of imatinib mesylate treatment due to resistance or intolerance. Metastatic renal cell carcinoma (MRCC) after failure of cytokine-based therapy. Pancreatic neuroendocrine tumors (pNET).
GIST & MRCC 50 mg once daily for 4 wk followed by 2 wk off (schedule 4/2) to complete 6-wk cycle. May be increased or decreased by 12.5 mg up to 75 mg or down to 25 mg. pNET 37.5 mg (3 cap of 12.5 mg concomitantly) once daily w/o a schedule rest period. May be increased or decreased by 12.5 mg. Max: 50 mg daily. Co-administration w/ potent CYP3A4 inducers eg, rifampin Increase dose by 12.5 mg increments to max of 87.5 mg daily (GIST & RCC) or 62.5 mg daily (pNET). Co-administration w/ potent CYP3A4 inhibitors eg, ketoconazole Reduce dose by 12.5 mg decrements to min of 37.5 mg daily (3 cap of 12.5 mg concomitantly) (GIST & MRCC) or 25 mg daily (pNET).
Not for use in patients w/ NSCLC. Discontinue if CHF, pancreatitis & hepatic failure occur. Interrupt treatment &/or reduce dose in patients w/o clinical evidence of CHF but w/ ejection fraction of <50% & >20% below baseline. Hemorrhagic events, thyroid dysfunction, GI disorders, other dermatologic effects. Aneurysms & artery dissections. Hair or skin depigmentation may occur. Patients w/ cardiac events w/in 12 mth prior to treatment eg, MI (including severe/unstable angina), coronary/peripheral artery bypass graft, symptomatic CHF, CVA/transient ischemic attack, or pulmonary embolism; history of QT interval prolongation, taking antiarrhythmics or w/ preexisting cardiac disease, bradycardia or electrolyte disturbances. Concomitant use w/ strong CYP3A4 inhibitors. Consider baseline & periodic evaluations of LVEF during treatment. Perform CBC w/ platelet count & serum chemistries including phosphate at the beginning of each cycle. Monitor for CHF, HTN, adrenal insufficiency, thyroid dysfunction. May affect ability to drive or operate machinery. Severe (Child-Pugh class C) hepatic impairment. Impaired renal function. May impair fertility. Women of childbearing potential should avoid becoming pregnant while on treatment. Pregnancy & lactation. Ped patients.
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