Drug intelligence / Profile preview

ciclosporin + cyclophosphamide + methylprednisolone + mycophenolate mofetil

Development stage
Preclinical
Lead developer
Sandoz
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

This is a combination regimen of four immunosuppressive and cytotoxic drugs—ciclosporin, cyclophosphamide, methylprednisolone, and mycophenolate mofetil. Each drug has a distinct mechanism of action but all are used to suppress the immune system in various autoimmune diseases or to prevent organ transplant rejection. - **Ciclosporin** is a calcineurin inhibitor that suppresses T-cell activation by inhibiting interleukin-2 production. - **Cyclophosphamide** is an alkylating agent that crosslinks DNA, leading to cell death, particularly affecting rapidly dividing immune cells. - **Methylprednisolone** is a synthetic glucocorticoid corticosteroid that reduces inflammation by modulating gene expression and suppressing multiple inflammatory pathways[1][2][3]. - **Mycophenolate mofetil** inhibits inosine monophosphate dehydrogenase (IMPDH), blocking de novo purine synthesis in lymphocytes and thus preventing their proliferation[6][8][10]. This combination may be used for severe or refractory autoimmune conditions (such as lupus nephritis) or as part of aggressive immunosuppression protocols in transplantation.

02

Targets

DNAIMPDH (Inosine-5'-monophosphate dehydrogenase 1)GR (Glucocorticoid receptor)CN (Calcineurin)

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