Drug intelligence / Profile preview

cyclosporine + tacrolimus + mycophenolate mofetil + everolimus

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

Overview

This is a combination immunosuppressive regimen consisting of four agents commonly used in organ transplantation: - **Cyclosporine** and **tacrolimus** are calcineurin inhibitors that suppress T-cell activation by inhibiting the phosphatase activity of calcineurin, thereby blocking the transcription of interleukin-2 (IL-2) and other cytokines essential for T-cell proliferation[4][6]. - **Mycophenolate mofetil** is an antimetabolite that inhibits inosine monophosphate dehydrogenase (IMPDH), a key enzyme in de novo purine synthesis, leading to suppression of both T-cell and B-cell proliferation[8]. - **Everolimus** is an mTOR inhibitor that blocks the mammalian target of rapamycin pathway, inhibiting cell cycle progression and lymphocyte proliferation[8]. This multi-drug regimen provides potent immunosuppression by targeting multiple pathways involved in immune activation. It may be considered for use in solid organ transplantation (such as kidney or heart transplant) to prevent rejection, especially when tailored regimens are needed due to patient-specific factors or prior intolerance/failure with standard dual or triple therapy. The combination increases efficacy but also raises the risk for adverse effects such as nephrotoxicity, infections, metabolic disturbances, and hematologic toxicity.

02

Targets

IMPDH (Inosine-5'-monophosphate dehydrogenase 1)Mechanistic target of rapamycin complex 1CN (Calcineurin)

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