Drug intelligence / Profile preview

azathioprine

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

Overview

Azathioprine is an immunosuppressive small molecule drug used primarily to prevent organ transplant rejection (especially kidney transplants) and to treat autoimmune diseases such as rheumatoid arthritis, Crohn's disease, ulcerative colitis, systemic lupus erythematosus, and others. It is a prodrug of 6-mercaptopurine and was first synthesized in 1956 by Gertrude Elion, William Lange, and George Hitchings. Azathioprine works by decreasing the activity of the immune system through multiple mechanisms. Its main mechanism involves inhibition of purine synthesis—thereby blocking DNA replication in rapidly dividing cells like lymphocytes—and modulation of T cell apoptosis via rac1 inhibition. This results in reduced proliferation and function of B and T lymphocytes[1][5][6][8].

Brand names
AzasanImuran
Other names
azathioprin
02

Targets

RAC1 (Rac family small GTPase 1)

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