Drug intelligence / Profile preview

cyclosporine + mycophenolate mofetil + prednisolone

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

Overview

A combination immunosuppressive therapy consisting of cyclosporine, mycophenolate mofetil, and prednisolone. This triple therapy combines different mechanisms of action to provide synergistic immunosuppressive effects. Cyclosporine works by inhibiting calcineurin in T-cells, preventing the activation and proliferation of T-lymphocytes by blocking the production of interleukin-2 and other cytokines. It forms a complex with cyclophilin that inhibits calcineurin, preventing the dephosphorylation of the transcription factor NF-AT, which is necessary for cytokine gene transcription. Mycophenolate mofetil is a prodrug that is rapidly converted to its active form, mycophenolic acid (MPA). MPA inhibits inosine monophosphate dehydrogenase, an enzyme critical for the de novo synthesis of guanosine nucleotides, which are essential for lymphocyte proliferation. Prednisolone/prednisone is a corticosteroid that has broad anti-inflammatory and immunosuppressive effects, acting on multiple immune cell types and inflammatory pathways. The combination of these three medications has been studied in various conditions, including focal segmental glomerulosclerosis (FSGS) and organ transplantation. In patients with cyclosporin-resistant FSGS, a 12-month treatment with combined CsA and MMF did not significantly alter kidney function evolution but induced partial reductions in proteinuria in some patients. In transplantation, this triple therapy has been used to prevent organ rejection.

02

Targets

IMPDH (Inosine-5'-monophosphate dehydrogenase 1)Cyp (Cyclophilin family)GR (Glucocorticoid receptor)CN (Calcineurin)

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