Anticytokine Drugs

Question 1

Etanercept (ENBREL^TM) 1.) Structure 2.) Target 3.) Disease 4.) Administration

Answer 1

1. ) Recombinant fusion protein of 2 soluble TNF receptor moieties linked to Fc portion of human IgG
2. ) Binds TNF-alpha w/ high affinity and neutralizes its biological activity
3. )RA
4. ) SubQ

Question 2

Infliximab 1.) Structure 2.) Target 3.) Disease 4.) Administration

Answer 2

1. ) Chimeric monoclonal Ab to TNF-alpha
2. ) Reduces blood level of TNF-alpha; may dislodge TNF-alpha bound to cells
3. ) Crohn’s disease or RA
4. ) IV infusion

Question 3

Adalimumab (HUMIRA) 1.) Structure 2.) Target 3.) Disease 4.) Administration

Answer 3

1. ) Recombinant human monoclonal Ab to TNF-alpha
2. ) Complexes with soluble TNF-alpha and prevents interaction with p55 and p75 cell surface receptors
3. ) RA
4. ) SubQ

Question 4

Anakinra 1.) Structure 2.) Target 3.) Disease 4.) Administration

Answer 4

1. ) Recombinant non-glycosylated IL-1Ra (antagonist)
2. ) Blocks effects of IL-1
3. ) RA
4. ) SubQ

Question 5

Abatacept (CTLA-4-IG) 1.) Structure 2.) Target 3.) Disease 4.) Administration

Answer 5

1. ) Fusion protein of cytotoxic T lymphocyte- associated CTLA-4 linked to IgG1
2. ) Binds to B7 on APC -> prevents interaction with CD28 on T cell-> no T cell activation (costimulatory blockade)
3. ) RA
4. ) IV

Question 6

Certolizumab 1.) Structure 2.) Target 3.) Disease 4.) Administration

Answer 6

1. ) PEGylated Fab fragment of human TNF-alpha Ab; heavy and light chain of IgG fused to PEG
2. ) Binds soluble and membrane bound TNF-alpha
3. ) Crohn’s disease (more for this) and RA
4. ) SubQ * PEG extends half-life

Question 7

Benlysta 1.) Structure 2.) Target 3.) Disease 4.) Administration

Answer 7

1. ) Monoclonal Ab
2. ) BAFF/BLys- key determinants of B cell survival during development of tolerance
3. ) Lupus
4. ) Atypical Route

Question 8

Secukinumab 1.) Structure 2.) Target 3.) Disease 4.) Administration

Answer 8

1. ) N/A
2. ) Human IL-17 Antagonist
3. ) Psorasis and Asthma
4. ) Injection

Question 9

Omalizumab 1.) Structure 2.) Target 3.) Disease 4.) Administration

Answer 9

1. ) IgE-specific Ab
2. ) Binds up IgE
3. ) Asthma/Allergens
4. ) Atypical route

Question 10

DMARD (leflunomide/methotrexate)-1.) Structure 2.) Target 3.) Disease 4.) Administration

Answer 10

1. ) Small molecule
2. ) Prevents proliferation of lymphocytes-> reduce inflammatory process
3. ) Rheumatoid arthritis
4. ) Any