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- binds to cyclophilin --> complexe inhibit calcineurin (a cytoplasmic phosphatase, regulates the ability of the nuclear factor of activated T cells to translocate to the nucleus and inc the production of key cytokines such as IL-2, IL-3 and IFN-gamma)
- Use: suppresses organ rejection, selected autoimmune disorders
- Toxicity: predisposes patietns to viral infections and lymphoma; nephrotoxic (preventable w/ mannitol diuresis); gout
- binds to FK-binding protein --> complexe inhibit calcineurin (a cytoplasmic phosphatase, regulates the ability of the nuclear factor of activated T cells to translocate to the nucleus and inc the production of key cytokines such as IL-2, IL-3 and IFN-gamma)
- Use: organ transplant
- Toxicity: nephrotoxicity, peripheral neurophathy, hypertension, pleural effusion, hyperglycemia
- inhibits mTOR. inhibits T-cell proliferation in response to IL-2
- Use: kidney transplant, drug-eluting stents
- Toxicity: hyperlipidemia, thrombocytopenia, leukopenia
- inhibits inosine monophosphate dehydrogenase, an enzyme in the de novo pathway of GTP synthesis.
- Use: sole agent in kidney, liver and heart transplantations.
- Toxicity: myelosuppression, gastrointestinal disturbances
- immunosuppressant converted to 6-mercaptopurine (purine antimetabolites). inhibit several enzymes involved in purine metabolism.
- Use: kidney transplantation, autoimmune disorders (glomerulonephritis and hemolytic anemia)
- Toxicity: Bone marrow suppression. Metabolized by xanthine oxidase thus toxic effects may be inc by allopurinol
- target CD3
- prevent acute transplant rejection
- target IL-2 receptor
- prevent acute rejection of renal transplant
- Crohn's disease, rheumatoid arthritis, psoratic arthritis, ankylosing spondylitis, arthritis
- Glycoprotein IIb/IIIa
- prevent cardiac ischemia in unstable angina and in patients treated with percutaneous coronary intervention
- HER-2 overexpressing breast cancer
- B-cell non-Hodgkin's lymphoma
respiratory syncytial virus- blocks RSV F protein
- target IgE
- additional line of treatment for severe asthma
hepatitis B and C, Kaposi's sarcoma, leukemias, malignant melanoma
chronic granulomatous disease
oprelvekin (IL-11), thrombopoietin