Immuno

Question 1

Cyclosporine

[MOA, clinical use, Toxicity]

Answer 1

Calcineurin inhibitor (calcineurin activated by TCR of Th cells).
>Binds cyclophilin on Calcineurin – prevents IL-2 transcription – blocks T cell activation.
>For transplant rejection prophylaxis, psoriasis, RA.
>Nephrotoxic, neurotoxic

Question 2

Tacrolimus (FK506)

[MOA, clinical use, toxicity]

Answer 2

Calcineurin inhibitor (calcineurin activated by TCR of Th cells).
>Binds FKBP on calcineurin – prevents IL-2 transcription – blocks T cell activation.
>For transplant rejection prophylaxis.
>Nephrotoxic, neurotoxic; Inc. risk of diabetes.

Question 3

Sirolimus (Rapamycin)

[MOA, clinical use, toxicity]

Answer 3

mTOR inhibitor (mTOR activated by IL-2R).
>Binds FKBP on mTOR – prevents RESPONSE to IL-2 – blocks T cell activation, B cell differentiation.
>For kidney transplant rejection prophylaxis.
>Toxicity: Pancytopenia, insulin resistance.
*Synergistic w/ cyclosporine

Question 4

Daclizumab, Basiliximab

[MOA, clinical use]

Answer 4

Monoclonal antibodies.
Block IL-2R – prevents T cell proliferation.
For kidney transplant rejection prophylaxis

Question 5

Azathioprine (6-MP metabolite)

[MOA, clinical use, toxicity]

Answer 5

> Blocks nucleotide synth (PRPP amidotransferase) – inhibits lymphocyte proliferation.
For transplant rejection prophylaxis, GN, Crohn dse, RA.
Toxicity: Leukopenia, anemia, thrombocytopenia (6-MP degraded by xanthine oxidase, so toxicity inc. by allopurinol)

Question 6

Glucocorticoids

[MOA, clinical use, toxicity]

Answer 6

> Inhibits NF-kB – dec. cytokine transcription – suppresses B/T cell function.
For transplant rejection prophylaxis, autoimmune d/o, inflammation.
Toxicity: hyperglycemia, obesity, osteoporosis; iatrogenic Cushing syndrome

Question 7

IFN-alpha

Answer 7

Chronic hep B/C, Kaposi sarcoma, malignant melanoma

Question 8

IFN-beta

Answer 8

Multiple sclerosis

Question 9

IFN-gamma

Answer 9

Chronic granulomatous dse

Question 10

Aldesleukin (IL-2)

Answer 10

Renal cell carcinoma, metastatic melanoma

Question 11

Epoetin alfa

Answer 11

Anemias (esp. in renal failure)

Question 12

Oprelvekin (IL-11)

Answer 12

Thrombocytopenia

*IL-11 induces megakaryocyte maturation – platelet formation

Question 13

Filgrastim (G-CSF)

Answer 13

Recovery of bone marrow

Question 14

Alemtuzumab

[Target, clinical use]

Answer 14

Targets CD52 (all lymphocytes, monocytes).
For CLL

Question 15

Bevacizumab

[Target, clinical use]

Answer 15

Targets VEGF.

Colorectal cancer, renal cell carcinoma

Question 16

Cetuximab

[Target, clinical use]

Answer 16

Targets EGFR
Stage IV colorectal cancer
Head and neck cancer

Question 17

Rituximab

[Target, clinical use]

Answer 17

Targets CD20 (B cells)
B cell NHL, CLL
Rheumatoid arthritis
ITP

Question 18

Trastuzumab

[Target, clinical use]

Answer 18

Targets HER2/neu

Breast cancer

Question 19

Eculizumab

[Target, clinical use]

Answer 19

Targets complement C5.

Paroxysmal nocturnal hemoglobinuria

Question 20

Natalizumab

[Target, clinical use]

Answer 20

Targets alpha4-integrin (WBC adhesion).

Multiple sclerosis, Crohn dse

Question 21

Adalimumab, Infliximab

[Target, clinical use]

Answer 21

Targets soluble TNF-alpha (monocloncal antibodies vs Etanercept decoy receptor).
IBD, psoriasis, Rheumatoid arthritis, ankylosing spondylitis.

Question 22

Denosumab

[Target, clinical use]

Answer 22

Targets RANKL

Osteoporosis (inhibits osteoclast maturation; mimics osteoprotegrin)

Question 23

Omalizumab

[Target, clinical use]

Answer 23

Targets IgE

Allergic asthma

Question 24

Abciximab

[Target, clinical use]

Answer 24

Targets gpIIB/IIIa on platelets – links platelets together for aggregation.
Antiplatelet agent to prevent ischemic cx in patients undergoing PCI.