Drug intelligence / Profile preview

cyclosporine A + methylprednisolone + mycophenolate mofetil

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

Overview

This is a combination immunosuppressive regimen consisting of three agents: - **Cyclosporine A** is a calcineurin inhibitor that suppresses T-cell activation by inhibiting the transcription of interleukin-2 and other cytokines, thereby reducing immune responses[6][9]. - **Methylprednisolone** is a synthetic glucocorticoid corticosteroid with potent anti-inflammatory and immunosuppressive properties. It acts primarily by modulating gene expression to suppress pro-inflammatory cytokines and immune cell activity. - **Mycophenolate mofetil** is an antimetabolite immunosuppressant that inhibits inosine monophosphate dehydrogenase, blocking de novo purine synthesis in lymphocytes, leading to reduced proliferation of T and B cells[2][7]. This triple-drug regimen is commonly used for the prevention of organ transplant rejection (renal, cardiac, hepatic) and for treatment or maintenance therapy in certain autoimmune diseases such as steroid-resistant nephrotic syndrome. The combination leverages different mechanisms to achieve synergistic immunosuppression while minimizing toxicity from any single agent[4][5][1].

02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)CN (Calcineurin)UGT2B7 (UDP-glucuronosyltransferase 2B7)GR (Glucocorticoid receptor)UGT1A9 (UDP-glucuronosyltransferase 1A9)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)ABCB1 (P-glycoprotein)SLCO1B3 (Organic anion transporting polypeptide 1B3)ABCC2 (ATP-binding cassette sub-family C member 2)

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