Most sold drugs (EXAM 3) Flashcards
What is the type of drug is ADALIMUMAB (HUMIRA)
-First fully-human mAb, derived from phage display - Anti-TN
-TNF causes ADALIMUMABinflammatory signals -> blocked by mAb
-for immunosuppressant for rheumatoid arthritis, Crohn’s and psoriasis
Where is it derived from and what is the benefit?
derived from phage display
-screening of many antigen-binding fragments (antigenic) at one time (expressed on viral coat)
-faster than with Hybridoma-technique
Which drug is used with HUMIRA?
disease-modifying anti-rheumatic drugs (DMARs; e.g. methotrexate)
-because DMARS reduces the possibility of developing an antigen-Ab response against the biological mAb (HUMIRA)
-prolongs duration time of HUMIRA
Which risks come with HUMIRA?
Increased risk for infections (bacterial/fungal/viral/parasitic
infections, cancer cells)
-patients may develop infections they were aware of, bc of neutralizing TNF
What else is damaged by Rheumatoid arthritis?
-besides joints (bend joints) skin, eyes, lungs, heart and blood vessels
What are the two types of Inflammatory Bowel Disease (BWL)?
Ulcerative Colitis (UC)
Crohn’s Disease (CD)
What is Psioris?
-skin condition that speeds up the life cycle of skin cells
-itchy scales and red patches
What is Etanercept?
A fusion protein against TNF (Enbrel)
-Fc of a human IgG1 combined with extracellular human TNFR2 (antigen-binding site)
How is Etanercept different from Adalimumab?
Indication is similar: Anti-TNF
but named in a different manner
What is Infliximab (Remicabe)?
-Anti-TNF Antibody
Origin: 60% human 40% mouse
What are the complications with Infliximab and how to treat those?
-immediate-type Hypersensitivity
-Antihistaminic drugs (e.g. diphenhydramine/Benadryl - H1 Antagonist) (H2 Antagonist doesn’t work, duodenal ulcer) plus acetaminophen as prophylaxis against IgE reactions
-slow infusion rate
What is Ustekinumab (STELARA)?
-100% human
-Anti-IL-12/23 Ab
-Macrophages secrete IL-12/23 -> help Th develop into specific T helper cells
Rituximab (Rituxan)
-Anti CD20 Ab
-mouse chimeric
-binds to CD20 on B-lymphocyte
-CD20 is involved in the differentiation of B-cell
What is Rituximab (Rituxan) used for?
-leukemia and lymphomas (B-cell cancer)
-rheumatoid arthritis (RA) and managing organ transplants
-First infusion may elicit toxicity due to interleukin release and hypersensitivity -> Antihistamine + Acetaminophen
Why can chimeric and fully mouse mAb be used for organ transplants?
Because patients are on immunosuppressants prior transplantation
Keytruda - Checkpoint Inhibition (PD1)
-Checkpoint receptors (PD1) are recognized by T-cells that a cell is “SELF” -> so as not to kill
-cancer cells used these receptors to hide from T-cells
-The company MERCK used a biomarker specific for breast cancer (HER2) -> promising clinical trials -> breakthrough status by FDA
Trastuzumab (Herceptin) - Anti HER2
-90% human
-HER-2 is a type of EGF (TK) receptor involved in cell proliferation
-ligand (EGF) stimulates dimerization of HER-2
-Herceptin prevents TK-dimerization and VEGF production
HER-2 dimerizes with different HER subtypes - one of the two receptor monomers must be HER2
What is the hazard ratio in cancer patients?
-the ratio of mortality compared to different patients (different conditions, with or without medication)
-patients treated with a drug compared to placebo -> both have the same risk of death -> ratio would be 1
-with Trastuzumab the ratio is 0.6 -> 40% protection compared to those who do not get the drug
-but an increase in heart failure of 20% with the drug
Bevacizuman
-90% human
-tumor cells secrete VEGF (stimulates angiogenesis - new blood vessels) due to hypoxia (not enough O2)
-leaky blood vessels and damage to macula -> loss of central/foveal vision)
-Anti-VEGF Ab
PEG-Filgrastim (NEULASTA)
Neutropenia (low count of neutrophils) often in HIV, chemotherapy, radiation poisoning
-Granulocyte Colony-stimulating factor (growth factor that stimulates bone marrow) - Neutrophile, Basophile, Eosinophile
-rGCSF is an endogenous growth factor that stimulates the bone marrow to make more neutrophils (normally secreted by monocytes and endothelial cells)
Why is PEG-Filgrastim more convenient for patients compared to Filgrastim?
Because it is PEGlytaed and increases the half-life -> has to be injected once
What is AVONEX (INF beta-1a) used for?
-it is recombinant INF beta1-a used in multiple sclerosis (Myelin gets destroyed by auto-immune response)
-IFN balances the expression of pro and anti-inflammatory agents in the brain
-> reduces the number of inflammatory cells crossing the BBB
- increase of nerve growth factor -> improve neuronal survival
Pneumococcal Vaccine (Prevnar13)
-13-valent anti-pneumococcal vaccine (Streptococcus pneumonia)
-Contains purified capsular polysaccharide from 13 strains
Dulagltuide: Glucagol-like-Peptide 1 (GLP) agonist (TRULICITY)
-stimulate Insulin release and slow gastric emptying (glucose level will rise slowlier)
-decrease in glucagon
-for Type2 diabetes: as an adjunct to diet and exercise to improve glycemic control
