Drug intelligence / Profile preview

mycophenolate mofetil + tacrolimus + steroids

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**mycophenolate mofetil + tacrolimus + steroids** is a triple immunosuppressive regimen frequently used as maintenance therapy in organ transplantation (especially kidney and heart) and in autoimmune diseases such as lupus nephritis[1][2][3][4]. Mycophenolate mofetil is a selective, noncompetitive inhibitor of inosine monophosphate dehydrogenase, which inhibits lymphocyte proliferation. Tacrolimus is a macrolide calcineurin inhibitor that suppresses T-cell activation through inhibition of interleukin-2 transcription. Steroids (typically glucocorticoids such as prednisone or methylprednisolone) provide broad immunosuppressive and anti-inflammatory effects via glucocorticoid receptor agonism. The combination is used for its synergistic immunosuppressive activity, with the aim of preventing transplant rejection or inducing/remission maintenance in severe autoimmune diseases. Drug-drug interactions exist, particularly affecting the pharmacokinetic profiles, and therapeutic drug monitoring is frequently employed[3][4].

02

Targets

ABCB1 (P-glycoprotein)FKBP (FK506-binding protein family)GR (Glucocorticoid receptor)CYP3A5 (Cytochrome P450 family 3 subfamily A member 5)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)CN (Calcineurin)

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