everolimus + tacrolimus

Everolimus + tacrolimus is a combination of two immunosuppressive agents commonly used to prevent organ transplant rejection, particularly in kidney and liver transplantation. Everolimus is a mammalian target of rapamycin (mTOR) inhibitor that binds to FKBP12, forming a complex that inhibits mTORC1, leading to reduced cell proliferation, angiogenesis, and immune cell activation. Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by inhibiting the phosphatase activity of calcineurin after binding to FKBP12. The combination allows for minimization of individual drug doses while maintaining efficacy in preventing acute rejection; however, it may increase the risk of nephrotoxicity and other adverse effects due to pharmacological interactions[3][4][6]. Everolimus was developed by Novartis and approved for use in 2009[8]. Tacrolimus was originally developed by Fujisawa (now Astellas Pharma).

Brand names

PrografAdvagrafEnvarsusCerticanAfinitor

Other names

FK506 + RAD001