Drug intelligence / Profile preview

azathioprine + 6-mercaptopurine

Development stage
Unknown
Lead developer
PIBD-Net
Modality
Small Molecules
Administration
Oral
01

Overview

Azathioprine and 6-mercaptopurine are thiopurine immunomodulators used primarily for the maintenance of remission in inflammatory bowel diseases, including Crohn's disease. Azathioprine acts as a prodrug that is non-enzymatically cleaved to 6-mercaptopurine, which is then further metabolized into active thioguanine nucleotides. These metabolites incorporate into DNA and inhibit de novo purine synthesis, leading to the suppression of T- and B-lymphocyte proliferation and a reduction in immune-mediated inflammation. In clinical practice and trials like the PIBD-Net study (NCT02852694), they are often used interchangeably or as a treatment arm to maintain steroid-free remission in pediatric patients.

Brand names
ImuranPurinethol
Other names
AZA6-MPthiopurinesazathioprine/6-mercaptopurine
02

Targets

RAC1 (Rac family small GTPase 1)GMPS (Guanosine Monophosphate Synthetase)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)PPAT (Amidophosphoribosyltransferase)DNA

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