Drug intelligence / Profile preview

everolimus + reduced-dose calcineurin inhibitor

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

Overview

Everolimus + reduced-dose calcineurin inhibitor is a combination immunosuppressive regimen used primarily in solid organ transplantation, such as kidney, heart, and liver transplants. Everolimus is a mammalian target of rapamycin (mTOR) inhibitor that suppresses T-cell activation and proliferation by inhibiting the mTOR pathway. Calcineurin inhibitors (CNIs), such as tacrolimus or cyclosporine, inhibit the phosphatase activity of calcineurin, thereby blocking T-cell activation via inhibition of interleukin-2 transcription. The combination allows for synergistic immunosuppression while enabling reduction in CNI dosage to minimize nephrotoxicity and other adverse effects associated with standard CNI exposure. This regimen has been shown to be effective for prophylaxis against organ rejection and may improve renal function outcomes compared to standard-dose CNI regimens[2][4][5][8].

02

Targets

CN (Calcineurin)FKBP1AMechanistic target of rapamycin complex 1

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