Drug intelligence / Profile preview

everolimus + cyclosporine + tacrolimus

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

Overview

This is a combination of three immunosuppressive drugs commonly used in organ transplantation to prevent rejection. Everolimus is an mTOR inhibitor that suppresses T-cell activation and proliferation by inhibiting the mammalian target of rapamycin pathway. Cyclosporine and tacrolimus are calcineurin inhibitors that block T-cell activation by inhibiting the phosphatase activity of calcineurin through binding to cyclophilin (cyclosporine) or FK506-binding protein (tacrolimus). These agents are often used together or in various combinations with other immunosuppressants to optimize efficacy while minimizing toxicity. Everolimus is primarily developed by Novartis; cyclosporine was originally developed by Sandoz/Novartis; tacrolimus was developed by Astellas. The combination is mainly indicated for prevention of organ transplant rejection[1][4][5][6].

Other names
everolimuscyclosporinetacrolimusRAD001RAD-001RAD 001FK506FK-506FK 506CsA
02

Targets

PPP3CA (Protein phosphatase 3 catalytic subunit alpha)

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