Drug intelligence / Profile preview

everolimus + tacrolimus + prednisone

Development stage
Unknown
Lead developer
Novartis
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

This is a combination immunosuppressive regimen consisting of three drugs—everolimus, tacrolimus, and prednisone—used primarily in organ transplantation (notably kidney and liver) to prevent graft rejection. - **Everolimus** is an mTOR inhibitor that suppresses T-cell activation and proliferation by inhibiting the mammalian target of rapamycin pathway. - **Tacrolimus** is a calcineurin inhibitor that blocks T-cell activation by inhibiting calcineurin phosphatase activity, thereby reducing interleukin-2 production. - **Prednisone** is a synthetic glucocorticoid corticosteroid with anti-inflammatory and immunosuppressive properties; it modulates gene expression to broadly suppress immune responses. The combination leverages complementary mechanisms to provide potent immunosuppression while allowing for dose minimization of individual agents, potentially reducing toxicity (e.g., nephrotoxicity from high-dose calcineurin inhibitors). This regimen has been shown effective in preventing acute rejection episodes in renal and liver transplant recipients, especially when mycophenolate-based regimens are not tolerated[1][2][3][4]. Everolimus plus low-dose tacrolimus with prednisone can maintain stable graft function with acceptable safety profiles.

02

Targets

GR (Glucocorticoid receptor)Mechanistic target of rapamycin complex 1CN (Calcineurin)

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