Drug intelligence / Profile preview

steroids + azathioprine + tacrolimus + mycophenolate mofetil

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

Overview

This is a combination immunosuppressive regimen consisting of corticosteroids, azathioprine, tacrolimus, and mycophenolate mofetil. These agents are used together primarily to prevent organ transplant rejection (such as kidney, heart, or liver transplants) and to treat severe autoimmune diseases. - **Corticosteroids** act as broad-spectrum anti-inflammatory and immunosuppressive agents by modulating gene expression through the glucocorticoid receptor, suppressing multiple inflammatory pathways. - **Azathioprine** is a purine analog antimetabolite that inhibits DNA synthesis in proliferating cells (especially lymphocytes), thereby reducing immune cell proliferation[5][3]. - **Tacrolimus** is a calcineurin inhibitor that blocks T-cell activation by inhibiting interleukin-2 transcription[1][2][8]. - **Mycophenolate mofetil** is an ester prodrug of mycophenolic acid; it selectively inhibits inosine monophosphate dehydrogenase in lymphocytes, blocking de novo guanosine nucleotide synthesis required for T and B cell proliferation[7][10]. This multi-drug protocol provides potent immunosuppression with complementary mechanisms to reduce the risk of acute rejection after transplantation or control severe autoimmune inflammation.

02

Targets

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

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