Immunosuppressants

Question 1

Cyclosporine

Answer 1

Calcineurin inhibitor that binds cyclophilin. Blocks dephosphorylation of NFAT-P. Without this, no NFAT binding and transcription of IL-2. No T-cell activation

Use for transplant rejection prophylaxis, psoriasis, and RA

Question 2

Cyclosporine Toxicity

Answer 2

VERY nephrotoxic.

Also can cause HTN, tremor, gingival hyperplasia.

Question 3

Tacrolimus

Answer 3

Calcineurin Inhibitor that binds FKBP. Prevents NFAT from transcribing IL-2. No T cell activation.

Used to prevent organ transplant rejction

Question 4

Tacrolimus toxicity

Answer 4

NEPHROTOXIC.

Increased risk of diabetes and neurotoxicity. No gingival hyperplasia.

Question 5

Sirolimus/rapamycin

Answer 5

Blocks M-TOR which transduces signal of IL2 activation. Prevents T cell activation and B-cell differentiation.

Question 6

Sirolimus/rapamycin

Answer 6

Blocks M-TOR by binding FKBP which transduces signal of IL2 activation. Prevents T cell activation and B-cell differentiation.

Used for prevention of kidney transplant rejection

Question 7

Sirolimus toxicity

Answer 7

NOT nephrotoxic, but can cause pancytopenia.

Question 8

Basiliximab

Answer 8

Monoclonal antibody that blocks IL2R.

Used in kidney transplant rejection prophylaxis.

Question 9

Basiliximab toxicity

Answer 9

Edema, hypertension, tremor

Question 10

Azathioprine

Answer 10

Precursor to 6MP. Purine analog that prevents de novo purine synthesis.

Use in transplant rejection, RA, Crohns. Don’t use with allopurinol.

Question 11

Glucocorticoids

Answer 11

Block NFkB which decreases B and T cell function.

Used to prevent transplant rejection.

Question 12

Oprelvekin

Answer 12

Recombinant IL11 used in thrombocytopenia.

Question 13

Alemtuzumab

Answer 13

CD52 MAb used for CLL.

Question 14

Bevacizumab

Answer 14

VEGF MAb used for colorectal cancer and renal cell carcinoma

Question 15

Cetuximab

Answer 15

EGFR monoclonal antibody. Stage IV colorectal cancer

Question 16

Rituximab

Answer 16

CD20 MAb used in B-cell NHL, RA, ITP

Question 17

Rituximab

Answer 17

CD20 MAb used in B-cell NHL, RA, ITP

Question 18

Trastuzumab

Answer 18

AntiHer2 used in breast cancer/ gastric cancer

Question 19

Infliximab/adalimumab

Answer 19

TNFalpha MAb

Question 20

Natalizumab

Answer 20

Alpha 4 integrin MAb used for MS. Can cause PML with JC virus.

Question 21

Denosumab

Answer 21

RANK L antibody. Prevents osteoblast maturation. Mimics osteoprotegerin.

Question 22

Omalizumab

Answer 22

Binds IgE prevents asthma

Question 23

Palivizumab

Answer 23

RSV F protein monoclonal antibody. Prophylaxis in high risk infants.