Immunosuppressants

Question 1

What is the MOA for mycophenolate & Azathioprine?

Answer 1

-These drugs block nucleotide synthesis
-Inhibiting cell growth & proliferation of T cells

Question 2

What is the MOA for Cyclosporine & Tacrolimus?

Answer 2

-These drugs bind cyclophilin or FKBP which will inhibit calcineurin

-When the antigen presenting cell (MHC) presents the antigen to the T cell receptor = activation of calcineurin
-This results in IL-2 gene transcription
-IL-2 = autocrine signal
-The T-cell becomes a cytotoxic T-cell (CD8+)

-Important in transplant patients

Question 3

What is the MOA of Sirolimus?

Answer 3

-The drug will bind FKBP and inhibit mTOR

-The autocrine IL-2 signal has bound to its receptor and starts the downstream signal
-mTOR would continue into the nucleus for T-cell growth & proliferation into CD8+ cell