Immunosuppressive Agents

Question 1

TNF, IL-1, Chemokines function

Answer 1

Inflammation

Question 2

Function of IFN alpha/beta

Answer 2

confers viral resistance

Question 3

IFN-gamma function

Answer 3

Macrophage activation

Question 4

IL-12 function

Answer 4

IFN-gamma production by NK cells and T cells

Question 5

IL-15 function

Answer 5

Proliferation of NK cells

Question 6

IL-10, TGF-beta function

Answer 6

Anti-inflammatory; controls inflammation

Question 7

Short-to-medium acting Corticosteroids

Answer 7

• Hydrocortisone (8-12hrs)
• Cortisone
• Prednisone (12-24hrs)
• Meprednisone
• Prednisolone
• Methylprednisolone

Question 8

Intermediate acting Glucocorticoids

Answer 8

• Triamcinolone (15-24hrs)
• Paramethasone
• Fluprednisolone

Question 9

Long acting Glucocorticoids

Answer 9

• Betamethasone
• Dexamethasone (24-36hrs)

Question 10

Immunophilin Ligands

Answer 10

• Cyclosporine (Cyclophilin)
• Tacrolimus (FK506 immunophilin)
• Sirolimus (FK506 immunophilin)

Question 11

Cyclosporine

Answer 11

Immunophilin Ligands (Cyclophilin)

MOA: Cyclosporine-Cyclophilin complex inhibits Calcineurin –> (-) NF-AT –> (-) IL-2 production

(Organ transplant, Host vs Graft disease)

[HPN, neurotoxicity, hyperglycemia, Drug interaction cyp450]

Question 12

Tacrolimus

Answer 12

Immunophilin Ligands (FK506 Immunophilin)

MOA: Inhibits Calcineurin

(Atopic Dermatitis, Psoriasis, Organ Rejection)

[Drug interaction cyp450, Nephrotoxicity]

Question 13

Sirolimus

Answer 13

mTOR inhibitor

MOA: binds to FK506 immunophilin and inhibits kinase activity of Mammalian Target of Rapamycin

(transplants)

[Myelosuppression, Hepatotoxicity, Hypertriglyceridemia]

Question 14

Mycophenolate mofetil

Answer 14

Purine Antagonist

MOA: Inhibits IMP DH blocking de novo synthesis of Purines (GTP)

(Transplant, Lupus Nephritis, RA, IBD)

[Neutropenia]

Question 15

Thalidomide (Lenalidomide, Pomalidomide)

Answer 15

Immunomodulatory Derivatives of Thalidomide (IMiD’s)

MOA:

1. suppress TNF alpha
2. increase IL-10
3. decrease neutrophil phagocytosis
4. enhanced CMI
5. altered adhesion molecule expression

(Transplants, Multiple Myeloma)

[Teratogenesis, Somnolence, Peripheral Neuropathy, Neutropenia)

Question 16

Muromonab

Answer 16

Immunosuppressant Monoclonal Antibody

MOA: Inhibits Cytotoxic T cells by binding to CD3

Question 17

Abatecept

Answer 17

Immunosuppresant MAb

MOA: CTL4-A domain inhibits T cell stimulation

(RA, Juvenile Idiopathic Arthritis)

Question 18

Alefacept

Answer 18

Immunosuppresant MAb

MOA: inhibits T cell stimulation by binding to CD2 at t cell surface (inhibiting CD2-LFA-3 binding)

(Plaque Psoriasis)

Question 19

Basiliximab & Daclizumab

Answer 19

Immunosuppresant MAb

MOA: inhibits T cell by binding to IL-2 Alpha subunit

Question 20

Anti-TNF alpha MAbs

Answer 20

• Adalimumab
• Certolizumab pegol (coupled to Polyethylene glycol)
• Etanercept (IgG1 fused to TNF receptor)
• Golimumab (binds to soluble and membrane associated TNF-a)
• Infliximab

Question 21

Tocilizumab

Answer 21

Binds to IL-6 receptors

Question 22

Ustekinumab

Answer 22

binds to p40 of IL-12 and IL-23 cytokines

Question 23

Natalizumab

Answer 23

binds to a4 subunit of a4b1 and a4b7 integrins on leukocytes (except neutrophils)

Question 24

Omalizumab

Answer 24

Anti-IgE

Question 25

Anti-Tumor MAbs (7)

(Binds to what??)

Answer 25

• Alemtuzumab (CD-52)
• Bevacizumab (VEGF)
• Cetuximab (EGFR)
• Panitumumab (EGFR)
• Ofatumumab (CD-20)
• Rituximab (CD-20)
• Trastuzumab (Her2/neu)

Question 26

MAb’s used to deliver isotopes to tumors

Answer 26

• Arcitumomab
• Capromab pendetide
• Ibritumomab tiuxetan
• Tositumomab

Question 27

Aldesleukin

Answer 27

Immunomodulating Agent

MOA: activates IL-2 receptors on T,B and NK cells

(Renal Cell CA)