Drug intelligence / Profile preview

tacrolimus + mycophenolate mofetil + corticosteroids

Development stage
Phase 4
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This combination regimen consists of tacrolimus, mycophenolate mofetil, and corticosteroids, and is widely used as a maintenance immunosuppressive therapy in organ transplantation, particularly kidney transplantation. Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by inhibiting the phosphatase activity of calcineurin, thereby reducing interleukin-2 (IL-2) production. Mycophenolate mofetil is an ester prodrug of mycophenolic acid that inhibits inosine monophosphate dehydrogenase (IMPDH), blocking de novo purine synthesis required for lymphocyte proliferation. Corticosteroids act through glucocorticoid receptors to broadly suppress immune responses and inflammation. Together, these agents synergistically reduce the risk of acute transplant rejection by targeting multiple pathways in the immune response[1][2][6]. This triple therapy has been shown to be more effective at preventing early acute rejection than regimens omitting one component[2].

Other names
FK506 + MMF + steroidstacrolimus triple therapy
02

Targets

CN (Calcineurin)FKBP1AGR (Glucocorticoid receptor)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)

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