Immunomodulatory Drugs Flashcards
Which immunomodulatory drugs decrease T cell activation?
BEST BCD
Belatacept
Everolimus
Sirolimus
Tacrolimus
Basiliximab
Cyclosporine
Daclizumab
Which immunosuppressants target cytokines?
I TEAA
Infliximab Adalimumab Etanercept Anakinra Tocilizumab
Which drugs target oncogenic growth factors?
Cetuximab
Trastuzumab
Erlotinib
What are the MOA of Cyclosporine and Tacrolimus?
Inhibit calcineurin, a phosphatase required for activation of NFAT
What are the indications for cyclosporine and tacrolimus?
Transplant rejection prophylaxis
Autoimmune diseases: RA (cyclosporine)
What AEs are associated with cyclosporine and tacrolimus?
⬛️⬛️⬛️
⬛️ inc. risk of infections
⬛️ nephrotoxicity (cyclosporine)
⬛️ HTN (tacrolimus)
Inc. risk of malignancies
What is the MOA of belatacept?
Fusion protein between CTLA-4 and Fc; binds B7 and prevents activation by CD28
What are indications for belatacept?
Transplant rejection prophylaxis
What AEs are associated with belatacept?
Inc. risk of infections
Inc. risk of malignancies
What is the MOA of muromonab?
An anti-CD3 antibody
Binding of CD3 antibody to CD3 initiates activation of T cell = strong signal 1
(Causes cytokine secretion first, and since there is only 1 signal, cell undergoes apoptosis)
What is Muromonab indicated for?
Transplant rejection
Type 1 DM
What AEs are associated with Muromonab?
“Cytokine Storm”
What is the MOA of rituximab?
depletes B cells
Anti-CD20 antibody activates ADCC for killing of B cells by NK cells
What is rituximab indicated for?
Autoimmune diseases: RA, SLE, MS
Certain B cell lymphomas
What AEs are associated with Rituximab?
⬛️⬛️⬛️
Inc. risk of infections
(⬛️= HBV exacerbation)
⬛️Inc. risk of PML
(Progressive multifocal leukoencephalopathy)
⬛️serious rash
What is the MOA of glucocorticoids?
Binds to glucocorticoid receptor and regulates gene transcription, resulting in
Inc. apoptosis
Dec. inflamm. Cytokines from macrophages and Tecells
Dec. T cell activation
What are indications for glucocorticoids?
Transplant rejection
Chronic inflammatory disease (IBD)
Autoimmune diseases (MS, RA)
What AEs are associated with glucocorticoids?
Diabetes
Weight gain
Osteoporosis
Fluid retention
What are the MOA of infliximab and adalimumab?
TNF antibodies
What is the MOA of Etanercept?
TNF receptor fusion protein
What is the MOA of anakinra?
IL-1 receptor antagonist
What is the MOA of tocilizumab?
IL-6 receptor antibody
What is the MOA of natalizumab?
VLA-4 antibody
What are indications and CI for infliximab and adalimumab?
Indications:
inflammatory diseases
RA, IBD, psoriatic arthritis
CI: heart failure