Exam 1 Drugs

adalimumab

Humira

human mab to TNFa cytokine

golimumab

Simponi, Aria

mab to TNFa cytokine

infliximab

Remicade

chimeric mab to TNFa cytokine → mouse variable, human Fc

certolizumab pegol

Cimzia

humanized Fab, mouse variable

conjugated to PEG → stability

etanercept

Enbrel

fusion protein TNFa receptor, Fc of IgG → stability

anakinra

Kinaret

recombinant human IL-1R antagonist

tocilizumab

Actemra

humanized mab to IL-6R soluble and membrane

sarilumab

Kevzara

human mab to IL-6R soluble and membrane

secukinumab

Cosentyx

human mab to IL-17A

ustekinumab

Stelara

human mab to IL-12 and IL-23 → p40 subunit

guselkumab

Tremfya

human mab to IL-23 → p19 subunit

vedolizumab

Entyvio

mab to a4B7 integrin → block T cell migration to GI tract

tofacitinib

Zeljanz

JAK1 and JAK3 small molecule inhibitor → less cytokines

baricitinib

Olumiant

JAK1 and JAK2 inhibitor

for RA non-responsive to anti-TNFa

alemtuzumab

Campath, Lemtrada

humanized mab to CD52 on lymphocytes → ADCC, apoptosis → deplete lymphocyte

rituximab

Rituxan

chimeric mab to CD20 antigen on B cells → deplete lymphocyte

abatacept

Orencia

fusion protein of CTLA-4 receptor, Fc of IgG → block T cell CD28 costimulation pathway

belatacept

Nujolix

fusion protein of CTLA-4 receptor, Fc of IgG → block T cell CD28 costimulation pathway

basiliximab

Simulect

chimeric mab to IL-2R alpha chain (CD25) → block high affinity IL-2R signaling

tacrolimus

macrolide abx

binds FKBP → inhibit calcineurin

nephrotoxic

cyclosporine

cyclic peptide

binds cyclophilin → inhibit calcineurin

nephrotoxic

sirolimus

macrolide abx

binds FKBP → inhibit mTOR → IL-2 pathway

not directly nephrotoxic

methotrexate

antiproliferative → inhibit DHFR → less purine/pyrimidine synthesis

anti-inflammatory → accumulate adenosine → suppress T cell activation

azathioprine

antimetabolite blocks purine synthesis

thioguanine incorporated to growing DNA strand