6‐thioguanine: a new old drug to procure remission in inflammatory bowel disease

The thiopurine analogues, azathioprine (AZA) and 6-mercaptopurine (6-MP), have become the standard immunomodulating therapies for retaining remission in inflammatory bowel diseases (IBD).1,2 Both AZA and 6-MP are prodrugs. AZA is metabolized to 6-MP in the liver and subsequently to the putative active metabolites, 6-thioguanine nucleotides (6-TGN), which impair biosynthesis of purines and inhibit cellular proliferation. Another metabolite, 6-methylmercaptopurine ribonucleotide (6-MMPR), is believed to account for the dose-dependent hepatotoxicity.3–5