drugs Flashcards
(26 cards)
muromonab
Indication: transplant rejection
MOA
- anti-CD3
- Binds surface protein present on all T cells that normally binds antigen leading to hyper stimulation
- Hyperstimulation leads to T cell death and new organ is accepted
First approved therapeutic Ab
fingolimod
Indication: MS
MOA
- Sphingosine analog, S1PR1 agonist
- Triggers Gai to inhibit RacI GTPase function in cell motility
- Results in sequestering lymphocytes in lymph nodes
- Can’t go to CNS and contribute to disease
corticosteroids
Indication: inflammation
MOA
- Agonist of glucocorticoid receptor
- Decrease transcription of pro-inflammatory molecules
- TNFa
- Increase transcription of anti-inflammatory molecules
- IL-10, IL-1
NSAIDs
Indication: inflammation
MOA
- Decrease prostaglandins
- Inhibit COX 1 and 2 enzymes
Salicylic acid- natural product from willow bark
anti-IL5s (mepolizumab, reslizumab, benralizumab)
Indication: eosinophilic asthma
MOA
- Block IL5 binding to IL5R
- Prevents activation and degranulation of eosinophils
infliximab (Remicade)
Infliximab (Remicade)
Indication: Crohn’s disease
MOA
- anti-TNF, binds to extracellular TNF and neutralizes it
- If TNF can’t bind receptor, can’t cause inflammation
anakinra (Kineret)
Indication: RA
MOA
- IL-1 receptor antagonist
- Competitively inhibits binding to receptor
- Reduces inflammation
nivolumab
Indication: cancer
MOA
- Prevents PD-1R from interacting with ligand
- Blocking inhibitory signal increases T cell activation
Immune checkpoint therapy
lifitegrast (Xiidra)
Indication: dry eye
MOA
- Prevents LFA-1 ICAM interaction
- Decreases T cell activation by blocking immune synapse formation
- Decrease local eye inflammation
aldesleukin
Indication: metastatic renal carcinoma
MOA
- Stimulates T cell response
- Recombinant form of IL-2, stimulating T cell proliferation
basiliximab (Simulect)
Indication: transplant rejection
MOA
- Antibody to IL-2 receptor of T cells
- Binding drug to receptor means that antigen can’t bind and there’s no activation of T cells
dupilumab (Dupixant)
Indication: atopic dermatitis
MOA
- IL-4 antibody
- Decreases Th2 cells
ixekizumab (Taltz)
Indication: plaque psoriasis
MOA
- Binds IL-17, preventing inflammation
- Prevents progression of disease
conjugate vaccines
T cell dependent response gives a stronger B cell response
- May have stronger efficacy against pathogen
Some pathogens express polysaccharides
- Can use to directly activate B cells
- T cell independent- weaker, short lived
Conjugating polysaccharide to stronger antigen will get cells to produce a stronger antibody response to a weaker antigen
- Makes T cell independent into dependent
Ex. Tetanus toxoid protein can be conjugated to a weaker epitope
- Will be presented by B cells to activate tetanus toxoid specific Th cells
- Then leads to stronger response
Hib vaccine
Haemophilus influenzae type B vaccine is a conjugate of tetanus toxoid and polyribosyl ribitol phosphate
For prevention of meningitis
Initial vaccines with PRP gave weak antibody response that diminished rapidly
Reformulation in 1990 as conjugate vaccine boosted efficacy
- Changed from T-independent to T-dependent response
etanercept (Enbrel)
Indication: RA
MOA
- Combined anti-TNF IgG with TNF receptor
- Extended stability due to fusion
rituximab
Indication: autoimmune diseases and cancer
MOA
- Monoclonal Ab targeting CD20 on B cells
- Healthy or malignant
ADCC is mediated by Fc portion which triggers NK cells to kill B cells
- Coats B cell by targeting CD20
- Attacks B cell by NK cells with ADCC mechanism
daratumumab
Indication: multiple myeloma
MOA
- CD38 Ab, which is expressed in myeloma cells
- Triggers complement pathway in addition to ADCC and ADCP
- Recruits C1 complement protein
- MAC made
- Ab also capable of ADCC, ADCP, apoptosis
7 kinds of vaccines
attenuated/ killed bacteria
live attenuated viruses
subunit vaccines
conjugate vaccines
synthetic vaccines
viral and DNA vectors
methotrexate
Indication: autoimmune disorders
MOA
- Inhibitor of folate metabolism
- Decreases proliferation of immune cells
- Immunosuppression
cyclosporine
Indication: organ transplant rejection
MOA
- Inhibits calcineurin, which is critical to transcription of IL-2 and T cell response
- Blocking T cell response causes immunosuppression
natalizumab
Indication: MS
MOA
- Monoclonal antibody targeting CD49d
- CD49 is an integrin which is required for T cell migration into affected organs
- Prevents infiltration of immune cells into brain
mycophenolic acid
Indication: kidney transplant
MOA
- Inhibitor of inosine-5’-monophosphate dehydrogenase
- Prevents de novo GMP synthesis, which is required for lymphocyte proliferation
- Good localization to kidney
cancer vaccines
2 vaccines (HBV, HPV) prevent liver cancer and cervical cancer, but these work through inhibiting the virus that causes these cancers
Unlike vaccines for infectious diseases, cancer vaccines are therapeutic not prophylactic
Not yet used in humans, but Torigen markets this product for dogs
- Founder is a UConn grad
- Tumor is taken out of dog, isolated into tumor cells, combined with adjuvant, and then can be injected into dog for anything residual remaining
