• Aliases: RAD001, Zortress (kidney and liver transplantation)
    • Binds to the immunophilin FKBP-12 to generate an immunosuppressive complex that binds to and inhibits the activation of mTOR
    • FDA approved for kidney and pancreatic neuroendocrine carcinomas and for breast cancer in combination with exemestane
    • Recommended dose: 10 mg once daily with or without food. Avoid grapefruit juice.
    • Half-life: 30 hours
    • Metabolism: Major CYP3A4 substrate and P-glycoprotein
    • Common side effects: Mouth ulcers, rash (acneiform), delayed wound healing, nausea/vomiting, fatigue, anorexia (decreased appetite), cough, shortness of breath, thrombocytopenia, diarrhea or constipation, hypercholesterolemia
    • Clinical pearls: Monitor cholesterol. Levels may increase while on treatment despite the patient’s dietary habits. Initiate oral care early on (soft toothbrush, salt, and soda swish).
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