Drug intelligence / Profile preview

azathioprine + glucocorticoids

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

Overview

Azathioprine + glucocorticoids is a combination immunosuppressive therapy widely used to treat a range of autoimmune and inflammatory diseases, such as steroid-dependent ulcerative colitis, vasculitis associated with rheumatoid arthritis, serpiginous choroiditis, and IgA nephropathy. - **Azathioprine** is a purine analogue prodrug that is metabolized to 6-mercaptopurine, inhibiting purine synthesis, which in turn suppresses the proliferation of B and T lymphocytes by interfering with DNA and RNA synthesis and inducing apoptosis in activated mononuclear cells. - **Glucocorticoids** are synthetic analogs of endogenous steroids. They bind to glucocorticoid receptors, modulate gene transcription, and broadly inhibit immune and inflammatory responses, including the suppression of pro-inflammatory cytokine production, inhibition of immune cell proliferation, and reduction in leukocyte recruitment. The combination aims to achieve rapid and sustained immunosuppression: glucocorticoids provide fast anti-inflammatory action, while azathioprine acts as a steroid-sparing agent for long-term immunosuppression. This combination is considered especially when monotherapy is insufficient or to reduce steroid dependency in chronic diseases. Typical indications include autoimmune hepatitis, inflammatory bowel disease (notably ulcerative colitis), certain forms of glomerulonephritis (such as IgA nephropathy), and systemic vasculitides[1][3][5][7]. Both medications require careful dose individualization and monitoring for toxicity, including myelosuppression (with azathioprine) and infection risk (with both agents), and pharmacogenetic testing (e.g., for TPMT deficiency) is recommended before azathioprine use[2].

Other names
prednisolone + azathioprineprednisone + azathioprinecorticosteroids + azathioprine
02

Targets

PPAT (Amidophosphoribosyltransferase)GR (Glucocorticoid receptor)RAC1 (Rac family small GTPase 1)

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