Drug intelligence / Profile preview

cyclosporine then everolimus

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

Overview

This entry refers to a sequential immunosuppressive regimen in which cyclosporine is administered first, followed by everolimus. Both drugs are potent immunosuppressants commonly used in organ transplantation, particularly kidney transplantation. Cyclosporine is a calcineurin inhibitor that suppresses T-cell activation by inhibiting the phosphatase activity of calcineurin, thereby preventing the transcription of interleukin-2 and other cytokines essential for T-cell proliferation[6][5]. Everolimus is an mTOR (mammalian target of rapamycin) inhibitor that binds to FK-binding protein 12 (FKBP12), forming a complex that inhibits mTORC1, leading to suppression of cytokine-driven T-cell proliferation and cell cycle progression[5][4]. The sequential use ("then") suggests an initial phase with cyclosporine—often for induction or early maintenance—followed by conversion to everolimus for long-term maintenance therapy. This approach may be employed to reduce nephrotoxicity associated with prolonged cyclosporine exposure while maintaining effective immunosuppression with everolimus[4][3]. Both agents require careful therapeutic drug monitoring due to narrow therapeutic windows and potential drug-drug interactions.

02

Targets

Mechanistic target of rapamycin complex 1CN (Calcineurin)

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