• Alias: BAY 73-4506
    • Orally bioavailable VEGFR, TIE2, KIT, RAF, RET, PDGFR, FGFR inhibitor
    • FDA approved for mCRC (2012) and unresectable or metastatic GI stromal tumors (2013)
    • Recommended dose: 160 mg orally with food, once daily for the first 21 days of each 28-day cycle
    • Half-life: 28 hours (range 14–58 hours)
    • Metabolism: Major CYP3A4 substrate
    • Common side effects: Hepatotoxicity (US box warning), asthenia/fatigue, diarrhea, anorexia, hypertension, mucositis, dysphonia
    • Clinical pearls: Assure liver function tests prior to initiation; monitor blood pressure closely; for diarrhea, prescribe imodium—up to 8 tabs/day. If resistant,   d. For mucositis, avoid sodas, acidic fruits, tomatoes, and spicy food. Gargle with baking soda/water mixture am/pm and after each meal. Swish with carafate after baking soda to coat the mouth and protect. May also add viscous lidocaine to assist with diminishing painful eating. For anorexia, add supplemental nutrition to each meal: ensure/boost three times a day if feasible.
    Other topics in Targeted and Immunotherapy Agents