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Sirolimus

Sirolimus inhibits T-lymphocyte activation and proliferation that occurs secondary to antigenic and cytokine (IL-2, IL-4, and IL-15) stimulation.



Specifically, sirolimus inhibits T-cell proliferation by binding to immunomodulin FK-BP WHICH INHIBITS specific serine-threonine kinase (mTOR), which is necessary for cell cycle progression.

What is speciality of sirolimus when compared to tacrolimus?

Sirolimus is not nephrotoxic

Which are the calcineurin inhibitors?

Tacrolimus


Cyclosporine

Intercalating into DNA

Danarubacin


Doxorubicin



Main side FX : cardiotoxic

Which are the calcineurin inhibitors?

Cyclosporine and Tacrolimus



MOA : Inhibit calcineurin-mediated transcription of the IL-2 gene and subsequently reduce T-cell activation.



Side FX:


nephrotoxicity



sirolimus synergistically enhances cyclosporine-induced nephrotoxicity.

Bortezumib

Used in multiple myeloma



Inhibits proteosome 26s leading to accumulation of pro apoptotic proteins

Rituximab

Chimeric antibody against CD20 .....depletes B cell

Mycophenolate

inhibits purine syn ( IMP dehydrogenase)



Affects b and t cell

Etoposide

Topoisomerase 2 inhibitor



ca


Testicular caSmall cell lung cancer


Small cell lung cancer

Syn podophyllotoxin

Topoisomerase I inhibitor

Topotecan


Irinotecan