Drug intelligence / Profile preview

azathioprine + cyclosporine + methylprednisolone

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

Overview

This is a combination of three immunosuppressive drugs—azathioprine, cyclosporine, and methylprednisolone—used primarily to prevent organ transplant rejection and to treat certain autoimmune diseases. - **Azathioprine** is a purine analogue antimetabolite that acts as an immunosuppressant by inhibiting DNA and RNA synthesis in proliferating cells, particularly lymphocytes[5][6]. - **Cyclosporine** is a calcineurin inhibitor that suppresses T-cell activation by inhibiting the transcription of interleukin-2 (IL-2) and other cytokines[4]. - **Methylprednisolone** is a synthetic glucocorticoid corticosteroid with potent anti-inflammatory and immunosuppressive properties; it modulates gene expression to reduce inflammation and immune responses[1]. This triple-drug regimen is commonly used in solid organ transplantation (such as kidney transplants) to prevent graft rejection by targeting multiple pathways of the immune response. It may also be used for severe autoimmune conditions when monotherapy or dual therapy are insufficient[2][3][4].

02

Targets

GR (Glucocorticoid receptor)CN (Calcineurin)

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