Drug intelligence / Profile preview

mycophenolate sodium + tacrolimus

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

Overview

Mycophenolate sodium + tacrolimus is a combination of two immunosuppressive agents commonly used to prevent organ rejection in transplant recipients. Mycophenolate sodium acts as a reversible inhibitor of inosine monophosphate dehydrogenase, thereby inhibiting the de novo synthesis of guanosine nucleotides and suppressing lymphocyte proliferation. Tacrolimus is a calcineurin inhibitor that binds to FK binding protein (FKBP12), forming a complex that inhibits calcineurin phosphatase activity, which blocks T-cell activation by preventing interleukin 2 (IL-2) transcription. This combination regimen is highly effective for maintenance immunosuppression after organ transplantation, particularly kidney transplants, but requires careful monitoring due to risks such as nephrotoxicity (tacrolimus), gastrointestinal and hematologic toxicity (mycophenolate), and increased infection risk[1][2][5][6].

Brand names
Myfortic + PrografMyfortic + Envarsus XRMyfortic + Astagraf XL
Other names
mycophenolate sodium + tacrolimus
02

Targets

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

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