Most sold drugs (EXAM 3)

Question 1

What is the type of drug is ADALIMUMAB (HUMIRA)

Answer 1

-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

Question 2

Where is it derived from and what is the benefit?

Answer 2

derived from phage display
-screening of many antigen-binding fragments (antigenic) at one time (expressed on viral coat)
-faster than with Hybridoma-technique

Question 3

Which drug is used with HUMIRA?

Answer 3

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

Question 4

Which risks come with HUMIRA?

Answer 4

Increased risk for infections (bacterial/fungal/viral/parasitic
infections, cancer cells)
-patients may develop infections they were aware of, bc of neutralizing TNF

Question 5

What else is damaged by Rheumatoid arthritis?

Answer 5

-besides joints (bend joints) skin, eyes, lungs, heart and blood vessels

Question 6

What are the two types of Inflammatory Bowel Disease (BWL)?

Answer 6

Ulcerative Colitis (UC)
Crohn’s Disease (CD)

Question 7

What is Psioris?

Answer 7

-skin condition that speeds up the life cycle of skin cells
-itchy scales and red patches

Question 8

What is Etanercept?

Answer 8

A fusion protein against TNF (Enbrel)
-Fc of a human IgG1 combined with extracellular human TNFR2 (antigen-binding site)

Question 9

How is Etanercept different from Adalimumab?

Answer 9

Indication is similar: Anti-TNF
but named in a different manner

Question 10

What is Infliximab (Remicabe)?

Answer 10

-Anti-TNF Antibody
Origin: 60% human 40% mouse

Question 11

What are the complications with Infliximab and how to treat those?

Answer 11

-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

Question 12

What is Ustekinumab (STELARA)?

Answer 12

-100% human
-Anti-IL-12/23 Ab
-Macrophages secrete IL-12/23 -> help Th develop into specific T helper cells

Question 13

Rituximab (Rituxan)

Answer 13

-Anti CD20 Ab
-mouse chimeric
-binds to CD20 on B-lymphocyte

-CD20 is involved in the differentiation of B-cell

Question 14

What is Rituximab (Rituxan) used for?

Answer 14

-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

Question 15

Why can chimeric and fully mouse mAb be used for organ transplants?

Answer 15

Because patients are on immunosuppressants prior transplantation

Question 16

Keytruda - Checkpoint Inhibition (PD1)

Answer 16

-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

Question 17

Trastuzumab (Herceptin) - Anti HER2

Answer 17

-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

Question 18

What is the hazard ratio in cancer patients?

Answer 18

-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

Question 19

Bevacizuman

Answer 19

-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

Question 20

PEG-Filgrastim (NEULASTA)

Answer 20

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)

Question 21

Why is PEG-Filgrastim more convenient for patients compared to Filgrastim?

Answer 21

Because it is PEGlytaed and increases the half-life -> has to be injected once

Question 22

What is AVONEX (INF beta-1a) used for?

Answer 22

-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

Question 23

Pneumococcal Vaccine (Prevnar13)

Answer 23

-13-valent anti-pneumococcal vaccine (Streptococcus pneumonia)
-Contains purified capsular polysaccharide from 13 strains

Question 24

Dulagltuide: Glucagol-like-Peptide 1 (GLP) agonist (TRULICITY)

Answer 24

-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