Drug intelligence / Profile preview

tacrolimus + everolimus + methylprednisolone

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination immunosuppressive regimen consisting of tacrolimus, everolimus, and methylprednisolone. It is primarily used in the prevention of organ transplant rejection, especially in kidney and liver transplantation. Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by inhibiting interleukin-2 transcription. Everolimus is an mTOR inhibitor that blocks T-cell proliferation by inhibiting the mammalian target of rapamycin pathway. Methylprednisolone is a synthetic glucocorticoid corticosteroid with potent anti-inflammatory and immunosuppressive effects, acting through glucocorticoid receptor agonism to modulate gene expression and suppress immune responses. The combination allows for minimization of calcineurin inhibitor exposure (tacrolimus) while maintaining effective immunosuppression with everolimus and steroids (methylprednisolone). This approach can reduce nephrotoxicity associated with higher doses of calcineurin inhibitors while preserving graft function and preventing acute rejection episodes[1][2][3]. The regimen has been shown to be safe and effective in clinical studies for de novo kidney transplant recipients as well as in conversion protocols for patients intolerant to other antimetabolites[1][2][3].

02

Targets

GR (Glucocorticoid receptor)CN (Calcineurin)mTOR (Mammalian target of rapamycin kinase)

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