Hepatotoxicity associated with 6-methyl mercaptopurine formation during azathioprine and 6-mercaptopurine therapy does not occur on the short-term during 6-thioguanine therapy in IBD treatment

J Crohns Colitis. 2012 Feb;6(1):95-101. doi: 10.1016/j.crohns.2011.07.009.

Abstract

Background and aims: High concentrations of methylated thiopurine metabolites, such as 6-methyl mercaptopurine, are associated with hepatotoxicity during administration of the conventional thiopurines azathioprine or 6-mercaptopurine in IBD patients. Metabolization of the non-conventional thiopurine 6-thioguanine does not generate 6-methyl mercaptopurine. Hence, the aim of our study was to evaluate hepatotoxicity during 6-thioguanine in IBD patients who previously failed conventional thiopurines due to 6-methyl mercaptopurine associated hepatotoxicity.

Methods: A retrospective single center intercept cohort study was performed of IBD patients using 6-thioguanine between January 2006 and July 2010 after failing conventional thiopurine therapy due to 6-methyl mercaptopurine associated hepatotoxicity. The primary outcome was the occurrence of 6-thioguanine induced hepatotoxicity, scaled according to the Common Terminology Criteria for Adverse Events.

Results: Nineteen patients were included. Median duration of 6-thioguanine therapy (median daily dosage 21 mg (9-24)) was 23 weeks (6-96). Hepatotoxicity did not reoccur in 15 out of 19, whereas grade 1 toxicity persisted in 4 patients (p<0.001). Median aspartate aminotransferase and alanine aminotransferase concentrations decreased from 34 U/l (20-59) and 64 U/l (15-175) to 23 U/l (18-40; p=0.003) and 20 U/l (14-48; p=0.019), respectively.

Conclusion: Hepatotoxicity does not reoccur during 6-thioguanine treatment in most IBD patients who failed conventional thiopurines due to 6-methyl mercaptopurine associated hepatotoxicity. Hence, at least at short-term, 6-thioguanine appears a justifiable alternative thiopurine for these IBD patients.

MeSH terms

  • Antimetabolites, Antineoplastic / adverse effects*
  • Antimetabolites, Antineoplastic / metabolism
  • Antimetabolites, Antineoplastic / therapeutic use
  • Azathioprine / adverse effects
  • Azathioprine / metabolism
  • Chemical and Drug Induced Liver Injury / etiology*
  • Female
  • Humans
  • Inflammatory Bowel Diseases / drug therapy*
  • Male
  • Mercaptopurine / adverse effects
  • Mercaptopurine / analogs & derivatives*
  • Mercaptopurine / metabolism
  • Retrospective Studies
  • Thioguanine / adverse effects*
  • Thioguanine / therapeutic use
  • Treatment Outcome

Substances

  • Antimetabolites, Antineoplastic
  • 6-methylthiopurine
  • Mercaptopurine
  • Thioguanine
  • Azathioprine