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sirolimus + mycophenolate mofetil + mycophenolic acid + azathioprine + steroid

Development stage
Unknown
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

This combination represents a multi-agent **immunosuppressive regimen** typically used in **solid organ transplantation**, especially kidney transplants, to prevent graft rejection. Each agent has a distinct mechanism: - **Sirolimus** (also known as rapamycin) inhibits the mammalian target of rapamycin (mTOR), leading to suppression of T-cell activation and proliferation. - **Mycophenolate mofetil** (MMF) is a prodrug of mycophenolic acid which preferentially inhibits inosine monophosphate dehydrogenase II, impeding de novo purine synthesis, and thus T- and B-lymphocyte proliferation. - **Mycophenolic acid** is the active metabolite of MMF and has similar effects. - **Azathioprine** is a purine analog that interferes with DNA synthesis, inhibiting the proliferation of immune cells, especially lymphocytes. - **Steroids** (i.e., corticosteroids such as prednisone or prednisolone) modulate gene transcription to suppress numerous pathways in inflammation and immunity, including T-cell activation. The combination of these drugs increases immunosuppression and reduces the risk of acute rejection, but also increases risk of toxicity and infection, thus requiring careful monitoring[2][3][4].

Brand names
RapamuneCellCept
Other names
sirolimus + MMF or MPS or AZA + steroid
02

Targets

DNA polymerase familyMechanistic target of rapamycin complex 1GR (Glucocorticoid receptor)

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