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20 Cards in this Set

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sirolimus

specific lymphocyte-signaling inhibitors




binds to FK binding protein (FKBP)


blocks the molecular target of rapamycin (mTOR) receptor in the IL2 receptor signaling pathway, inhibit T-cell proliferation

TNF- α neutralization





anti-cytokine therapy


Treats RA




TNFa secreted by macrophages, mast cells, activated TH cells.


RA TNFa secreted by activated macrophages in affected joint.





Etanercept

Soluble TNFa receptor dimer


TNF ligand binding domain + Fc domain of IgG1


Binds and inactivatees TNFa




can have mild to moderate erythema, pruritus, pain and swelling at site of injection

Infliximab

Chimeric anti-TNFa monoclonal antibody


human FC and mouse variable region


binds with high affinity to TNFa




Tx for RA, crohn's dz, ulcerative colitis




Hypersensitivity reaction can occur

Adalimumab

fully humanized recombined IgG1 against TNFa


similar to infliximab with smaller risk of hypersensitivity




All TNFa blocking agents can cause serious infections, sepsis, tuberculosis and fungal infection (opportunistic)

TNFa neutralizing agents (3)

Infliximab




Adalimumab




Etanercept

anakinra

interleukin-1 Receptor antagonist (IL-1Ra)




Competitively inhibits IL1B (immune function) binding to receptor


Lowers inflammatory reaction in RA




adverse effect similar to TNF blocker, serious infection





MAB

against cell surface receptors expressed on malignant activated immune cells.




Preferentially deplete receptors.


Depletion of specific immune cells




Adverse Effect:


Antibody bind to T Cell receptor causing cytokine release before they are destroyed.

Anti-thymocyte globulin (ATG)

Polyclonal Antibodies


injecting rabbits with human thymocytes


target many epitopes on human T cells, target essentially all T cells




For depletion of specific immune Cells




Can cause cytokine release syndrome


Development of antibodies against rabbit-specific epitopes



OKT3 (muromonab-CD3)

A type of MAB




mouse monoclonal antibody against human CD3


CD3 expressed by both CD4 and CD8 T cell




cause transient immunosuppression, T Cell level return to normal within a week of discontinuing use




Can cause cytokine release syndrome


Antibody against mouse



rituximab

a type of MAB


anti-CD20 chimeric murine/human monoclonal




CD20 found on B lymphocytes, rituximab result in B-cell depletion




treats RA, B cells perpetuate inflammatory response.


Rituximab used with methotrexate to treat RA thats refractory to TNFa inhibitor


Also treats Non-Hodgkins

Basiliximab

A type of MAB


Chimeric Anti-CD25, a IL-2 receptor




CD25 ONLY on activated T cells, IL-2 binding allow clonal expansion.





abatacept

Inhibition of costimulation




fully human recombinant fusion protein




binds to B7 and keeps it from interacting with CD28.


disrupts the activation pathway of T cells and causes antigen to make T cell become anergic

belatacept

Inhibition of costimulation




Similar mechanism to abatacept




only indicated for use in Epstein-Barr virus (EBV) seropositive patients because of the risk of post-transplant lymphoproliferative disorder

natalizumab

cell adhesion blockade



blocks alpha-4 integrins


critical to immune-cel1 adhesion




treatment of multiple sclerosis and Crohn's disease




several patients developed progressive multifocal leukoencephalopathy (PML)

eculizumab

Suppression of Complement Activation




humanized monoclonal antibody against C5,


late complement trigger protein that causes assembly of the MAC


Treat paroxysmal nocturnal hemoglobinuria (PNH); decreases hemoglobinuria and the need for erythrocyte transfusions

Ibalizumab

MAB for CD4




down-modulates cell surface expression of CD4 andblocks binding of residual CD4 to MHC class II




makes T cells anergic but does not deplete

Alemtuzumab

MAB against CD52




Present on mature B and T cells




severely depletes T and B cells




Tx for lymphocytic leukemia (-tu-)

Bortezomib

Proteasome inhibitor




depletion of plasma cells




tx for multiple myeloma

tocilizumab

anti-IL-6 Receptor MAB




Prevents inflammatory effects of IL-6


For patient with high PRA (panel Reactive antibody)