Immuno drugs Flashcards
What is the MoA of cyclosporine?
Cyclosporine binds cyclophlin → inhibition of calcineurin → no IL-2 transcription → blocked T cell activation
What are the toxicities of cyclosporine?
NEPHROTOXICITY Hypertension Hyperlipidemia Hyperglycemia Tremor Hirsutism Gingival hyperplasia
What is the MoA of tacrolimus?
Binds FKBP → inhibition of calcineurin → no IL-2 transcription → blocked T cell activation
Notice: after the initial step this is the same as cyclosporine
What toxicities that ARE seen with cyclosporine are NOT seen with tacrolimus?
No gingival hyperplasia or hirsutism
What is the MoA of sirolimus (rapamycin)?
Binds FKBP → inhibits mTOR → no IL-2 signal transduction → blocked T cell activation and B cell differentiation
What toxicities are seen with sirolimus?
Anemia/thrombocytopenia/leukopenia
Insulin resistance
Hyperlipidemia
NON-NEPHROTOXIC
What is basiliximab an Ab to?
IL-2R
What is azathioprine?
Antimetabolite precursor of 6-MP
How do glucocorticoids suppress the immune system?
Glucocorticoids inhibit NF-kB → decreased tsx of many cytokines
How is NF-kB activated? What does it usually do?
NF-kB is phosphorylated, and then ubquinated → proteosomal cleavage to active form → tsx regulator
What is oprelvekin?
IL-11…used with thrombocytopenia
What can be used for the recovery of bone marrow?
Filgrastim (Granulocyte Colon-Stimulating Factor…G-CSF)
Sargramostim (GM-CSF…Granulocyte-Macrophage Colony-Stimulating Factor)
What is aldesleukin? When is it used?
IL-2
Used in Renal Cell Carcinoma and metastatic melanoma
When is IFN-α used?
Chronic HBV/HCV Kaposi sarcoma Hairy cell leukemia Condyloma acuminatum Renal cell carcinoma Malignant melanoma
When is IFN-β used?
Multiple Sclerosis
When is IFN-γ used?
Chronic granulomatous disease
What are some therapeutic antibodies used for various cancers?
Alemtuzumab Bevacizumab Cetuximab Rituximab Trastuzumab
Alemtuzumab?
CD52
CLL
Bevacizumab?
VEGF
CRC and RCC
Cetuximab?
EGFR
Stage IV CRC and head/neck cancer
Rituximab?
CD20
Non-Hodgkin lymphoma, rheumatoid arthritis (w/ MTX), ITP
Trastuzumab?
HER2/neu
Breast cancer or gastric cancer
What are some therapeutic antibodies used for autoimmune diseases?
Infliximab, adalimumab
Natalizumab
Infliximab, adalimumab?
TNF-α
IBD, RA, ankylosing spondylitis, psoriasis
