Drug intelligence / Profile preview

prednisone + ciclosporin + mycophenolate mofetil

Development stage
Unknown
Lead developer
Bayer HealthCare Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination immunosuppressive regimen consisting of three agents—prednisone, ciclosporin (also known as cyclosporine), and mycophenolate mofetil. This triple therapy is widely used in the management of autoimmune diseases and to prevent organ transplant rejection. - **Prednisone** is a synthetic glucocorticoid corticosteroid that suppresses inflammation and modulates immune responses by binding to the glucocorticoid receptor, affecting gene transcription. - **Ciclosporin** is a calcineurin inhibitor that blocks T-cell activation by inhibiting the phosphatase activity of calcineurin, thereby reducing interleukin-2 production. - **Mycophenolate mofetil** is an antimetabolite immunosuppressant; it acts as a prodrug for mycophenolic acid, which inhibits inosine monophosphate dehydrogenase (IMPDH) in lymphocytes, blocking de novo purine synthesis essential for T and B cell proliferation. The combination provides synergistic immunosuppression through distinct mechanisms targeting multiple steps in immune activation. It has been studied and used primarily for preventing acute rejection after solid organ transplantation (such as kidney transplants) and for treating certain autoimmune conditions like idiopathic membranous nephropathy[3][4][1]. The regimen may be adjusted based on patient tolerance or specific clinical scenarios.

Brand names
CellCeptMyfenaxMyhibbin
Other names
mycophenolic acid morpholinoethyl ester
02

Targets

GR (Glucocorticoid receptor)PPP3CA (Protein phosphatase 3 catalytic subunit alpha)

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