Drug intelligence / Profile preview

Everolimus + cyclosporine

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

Overview

Everolimus + cyclosporine is a combination of two immunosuppressive agents used primarily to prevent organ transplant rejection. Everolimus is an mTOR (mammalian target of rapamycin) inhibitor that blocks T cell proliferation by inhibiting the progression from the G1 to S phase of the cell cycle in response to growth factors. Cyclosporine is a calcineurin inhibitor that suppresses immune responses by inhibiting T cell activation through blocking transcriptional activation of cytokines such as IL-2. The combination leverages their complementary mechanisms for synergistic immunosuppression and allows for dose reduction of each agent while maintaining efficacy in preventing acute rejection after transplantation[4][6][5]. Everolimus also has antiproliferative effects beyond the immune system and is used in certain cancers and noncancerous tumors[1][3].

Brand names
NeoralSandimmuneGengrafZortressAfinitor
Other names
everolimuscyclosporine
02

Targets

PPIA (Peptidyl-prolyl cis-trans isomerase A)Mechanistic target of rapamycin complex 1CN (Calcineurin)

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