Simultaneously, MP is methylated by thiopurine methyltransferase to 6-methylmercaptopurine. Briefly, AZA is converted to MP and eventually converted into the pharmacologically active metabolites 6-tioguanine nucleotides. The relatively high number of AE due to conventional thiopurines can partially be explained by thiopurine metabolism. 4, 5 However, subsequent incidence of failure of conventional thiopurine monotherapy due to adverse events is as high as 43%, resulting in the use of alternative immunosuppressive therapies including MTX and tioguanine. 3 Current international guidelines recommend a conventional thiopurine, such as azathioprine or mercaptopurine, as the first-choice drug in regular step-up therapy for CD. 1, 2 Up to 71% of CD patients are exposed to an immunomodulator in the first 5 years of disease.

Thiopurines and methotrexate are immunosuppressants that are widely used to maintain remission in patients with Crohn’s disease, with over three decades of experience for each therapy. Inflammatory bowel diseases, immunosuppressives, side effects 1.

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