Drug intelligence / Profile preview

everolimus + calcineurin inhibitor

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Everolimus + calcineurin inhibitor is a combination immunosuppressive therapy used primarily in kidney and other solid organ transplantation. Everolimus is a mammalian target of rapamycin (mTOR) inhibitor that suppresses T-cell and B-cell proliferation by inhibiting the mTOR pathway, which is critical for cell cycle progression in lymphocytes. Calcineurin inhibitors (CNIs), such as cyclosporine and tacrolimus, inhibit calcineurin phosphatase activity, thereby blocking T-cell activation and interleukin-2 production. The combination takes advantage of their complementary mechanisms: everolimus allows for a reduction in CNI dosing, which can minimize nephrotoxicity while maintaining effective immunosuppression. This strategy has shown efficacy in reducing the incidence of acute rejection, preserving renal function, and lowering the risk of infection and certain malignancies compared to full-dose CNI regimens[1][2][3][4].

Other names
everolimus plus calcineurin inhibitoreverolimus plus cyclosporineeverolimus plus tacrolimus
02

Targets

mTOR (Mammalian target of rapamycin kinase)Cyp (Cyclophilin family)FKBP (FK506-binding protein family)FKBP1ACN (Calcineurin)

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