Generic Name and Formulations:
Bosutinib 100mg, 500mg; tabs.
Treatment of chronic, accelerated, or blast phase Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML) with resistance or intolerance to prior therapy.
Take with food. Initially 500mg once daily until disease progression or patient intolerance. Consider dose escalation to 600mg once daily in patients who do not reach complete hematological response (CHR) by Week 8 or a complete cytogenetic response (CCyR) by Week 12, who did not have Grade 3 or higher adverse reactions. Hepatic impairment: initially 200mg daily. Renal impairment (CrCl 30–50mL/min): initially 400mg daily; (CrCl <30mL/min): initially 300mg daily. Dose modifications for toxicity: see full labeling.
<18yrs: not established.
Monitor and manage GI toxicity, fluid retention; withhold, reduce dose, or discontinue as necessary. Perform CBC weekly for first month, then monthly; hepatic enzyme tests monthly for first three months (more frequently if transaminase elevations occur); withhold, reduce dose, or discontinue as necessary. Monitor renal function at baseline and during therapy; consider adjusting dose if renal impairment occurs. Dialysis: not studied. Pregnancy (Cat.D); avoid. Use effective contraception during and for ≥30 days after last dose. Nursing mothers: not recommended.
Potentiated by concomitant strong or moderate CYP3A inhibitors (eg, boceprevir, clarithromycin, conivaptan, indinavir, itraconazole, ketoconazole, lopinavir/ritonavir, mibefradil, nefazodone, nelfinavir, posaconazole, ritonavir, saquinavir, telaprevir, telithromycin, voriconazole, or amprenavir, aprepitant, atazanavir, ciprofloxacin, crizotinib, darunavir/ritonavir, diltiazem, erythromycin, fluconazole, fosamprenavir, imatinib, verapamil, grapefruit products); avoid. Antagonized by concomitant strong or moderate CYP3A inducers (eg, carbamazepine, phenytoin, rifampin, St. John’s Wort, or bosentan, efavirenz, etravirine, modafinil, nafcillin); avoid. Antagonized by proton pump inhibitors (eg, lansoprazole); consider short-acting antacids or H2 blockers instead; separate dosing by ≥2hrs.
Tyrosine kinase inhibitor.
Diarrhea, nausea, thrombocytopenia, rash, vomiting, abdominal pain, RTI, anemia, pyrexia, abnormal LFTs, fatigue, cough, headache; fluid retention, hepatic or renal toxicity.
Hepatic (CYP3A4); 94% protein bound.
Fecal (primary), renal.
Tabs 100mg—120; 500mg—30
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