Drug intelligence / Profile preview

azathioprine + tacrolimus

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

Overview

Azathioprine + tacrolimus is a combination of two immunosuppressive drugs used primarily to prevent organ transplant rejection and as an induction therapy in certain autoimmune diseases such as lupus nephritis. Azathioprine is a purine synthesis inhibitor that suppresses the proliferation of T and B lymphocytes by interfering with DNA and RNA synthesis, leading to reduced immune cell activity. Tacrolimus is a calcineurin inhibitor that binds to FKBP-12, inhibiting calcineurin phosphatase activity, which blocks T-lymphocyte activation and interleukin-2 transcription. The combination provides potent immunosuppression by targeting different pathways in the immune response[1][5][6][10].

02

Targets

PPAT (Amidophosphoribosyltransferase)RAC1 (Rac family small GTPase 1)CN (Calcineurin)

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