• Alias: Rapamycin
    • A natural macrocyclic lactone produced by the bacterium Streptomyces hygroscopicus that binds to the immunophilin FKBP-12 to generate an immunosuppressive complex that binds to and inhibits the activation of mTOR
    • FDA approved for the prevention of organ rejection in kidney transplant (immunosuppressive agent)
    • Currently under investigation in phase 1/2 clinical trials in different cancer types including gynecologic tumors and breast cancer
    • Recommended oncology dose: 4 mg PO daily
    • Half-life: 57 to 63 hours
    • Metabolism: Major CYP3A4 substrate
    • Common side effects in cancer patients: Peripheral edema, hypertriglyceridemia, hypertension, hypercholesterolemia, tinine increase, abdominal pain, diarrhea
    Other topics in Targeted and Immunotherapy Agents