Drug intelligence / Profile preview

tacrolimus extended release + mycophenolate mofetil

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Tacrolimus extended release + mycophenolate mofetil is a combination immunosuppressive regimen mainly used in the prevention of organ transplant rejection, particularly in kidney transplantation. **Tacrolimus extended release** is a calcineurin inhibitor that binds FK506-binding protein, inhibiting calcineurin and consequently blocking the transcription of interleukin-2 (IL-2), a cytokine critical for T-cell activation. **Mycophenolate mofetil** is a prodrug converted to mycophenolic acid, which selectively inhibits inosine monophosphate dehydrogenase, suppressing de novo purine synthesis required for T- and B-lymphocyte proliferation. Together, these agents provide potent immunosuppression by complementary mechanisms, significantly reducing the risk of acute graft rejection but also requiring careful monitoring due to their toxicity profiles, especially nephrotoxicity (tacrolimus) and myelosuppression/gastrointestinal effects (mycophenolate mofetil)[1][2].

Brand names
Envarsus XRCellCeptAdvagrafAstagraf XL
Other names
tacrolimus ER + mycophenolate mofetiltacrolimus XR + mycophenolate mofetil
02

Targets

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

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