Drug intelligence / Profile preview

mycophenolate mofetil + tacrolimus + methylprednisolone + prednisolone + basiliximab

Development stage
Unknown
Lead developer
Roche
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Oral, Intravenous, Intramuscular
01

Overview

This is a **combination immunosuppressive regimen** commonly used in renal transplantation. The regimen consists of: - **mycophenolate mofetil**: an antimetabolite immunosuppressant that inhibits inosine monophosphate dehydrogenase, suppressing de novo guanosine nucleotide synthesis and thus T and B lymphocyte proliferation. - **tacrolimus**: a calcineurin inhibitor that suppresses T cell activation by inhibiting interleukin-2 (IL-2) transcription. - **methylprednisolone and prednisolone**: synthetic corticosteroids with anti-inflammatory and immunosuppressive effects, acting via glucocorticoid receptor agonism to inhibit multiple inflammatory mediators. - **basiliximab**: a monoclonal antibody that selectively binds the interleukin-2 receptor alpha chain (CD25) on activated T lymphocytes, blocking IL-2 mediated activation. This combination is frequently used for **induction and maintenance immunosuppression after kidney transplantation** to prevent acute organ rejection, with basiliximab often employed for induction and the others for maintenance. The regimen exploits complementary mechanisms to maximize prevention of allograft rejection while allowing dose reduction of individual agents and minimizing toxicity. It does not have a marketed fixed-dose combination or single brand name formulation.

Other names
mycophenolate mofetil + tacrolimus + methylprednisolone + prednisolone + basiliximab
02

Targets

GR (Glucocorticoid receptor)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)IL2RA (Interleukin-2 receptor alpha subunit)CN (Calcineurin)

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