Drug intelligence / Profile preview

ciclosporin + methotrexate + prednisolone

Development stage
Unknown
Lead developer
Sanofi
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Intramuscular, Subcutaneous
01

Overview

This is a combination therapy consisting of three immunosuppressive and anti-inflammatory agents: - **Ciclosporin (also known as cyclosporine or cyclosporine A)** is a calcineurin inhibitor that suppresses T-cell activation by inhibiting the transcription of interleukin-2 and other cytokines. - **Methotrexate** is an antimetabolite and antifolate agent that inhibits dihydrofolate reductase, leading to suppression of DNA synthesis in rapidly dividing cells, including immune cells. It acts as a disease-modifying antirheumatic drug (DMARD). - **Prednisolone** is a synthetic glucocorticoid corticosteroid with potent anti-inflammatory and immunosuppressive properties. It modulates gene expression to reduce the production of pro-inflammatory cytokines. This triple-drug regimen has been studied for the prevention of acute graft-versus-host disease (GVHD) following allogeneic bone marrow transplantation[1], as well as for early aggressive treatment in rheumatoid arthritis[2][3]. The combination leverages complementary mechanisms to more effectively suppress immune responses than dual or monotherapy regimens.

Other names
cyclosporine + methotrexate + prednisonecyclosporine A + methotrexate + prednisolone
02

Targets

GR (Glucocorticoid receptor)CN (Calcineurin)DHFR (Dihydrofolate reductase)

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