The utility of 6-thioguanine metabolite levels in managing patients with inflammatory bowel disease

Am J Gastroenterol. 2004 Sep;99(9):1744-8. doi: 10.1111/j.1572-0241.2004.30415.x.

Abstract

Objectives: We aimed at determining the utility of measuring 6-thioguanine (6-TG) and 6-methylmercaptopurine (6-MMP) in inflammatory bowel disease (IBD) patients on azathioprine (AZA) or 6-mercaptopurine (6-MP), whether the described therapeutic range for 6-TG (235-400 pmol/8 x 10(8) red blood cells, RBC) correlated with clinical remission or leukopenia, and if 6-MMP level was a marker for hepatotoxicity (>5,700 pmol/8 x 10(8) RBC).

Methods: Study eligibility included an IBD diagnosis of >6 months and either active disease or disease remission of <6 months and the use of AZA/6-MP for >10 wk consecutively. Metabolite levels were evaluated against clinical status, CBC, and hepatic parameters.

Results: Seventy-four of 166 AZA/6-MP users were eligible. 6-TG levels >235 pmol/8 x 10(8) RBC were found in 22/59 (38%) with active disease and in 7/15 with remission (47%, p= 0.16). There was a trend of higher 6-TG levels among those in remission versus those with active disease (mean 325 +/- 284 vs 223 +/- 159 pmol/8 x 10(8) RBC, p= 0.2). No hepatotoxicity was observed, although 12.2% had 6-MMP levels > 5,700 pmol/8 x 10(8) RBC. The correlation between 6-MP dose and 6-TG levels was weak (r = 0.22, p= 0.08). The 6-TG level did not correlate with WBC. There were five instances, each of markedly low levels of both 6-TG and 6-MMP, suggesting noncompliance and of marked 6-MMP levels versus 6-TG.

Conclusions: There was a poor correlation between 6-TG levels and remission. Nonetheless, the measurements of these levels are helpful when patients are on high doses but not achieving remission since noncompliance or metabolism favoring 6-MMP can be established.

Publication types

  • Comparative Study

MeSH terms

  • Adult
  • Azathioprine / administration & dosage
  • Azathioprine / pharmacokinetics*
  • Biomarkers / blood
  • Cohort Studies
  • Colitis, Ulcerative / blood
  • Colitis, Ulcerative / diagnosis
  • Colitis, Ulcerative / drug therapy*
  • Crohn Disease / blood
  • Crohn Disease / diagnosis
  • Crohn Disease / drug therapy*
  • Dose-Response Relationship, Drug
  • Drug Administration Schedule
  • Female
  • Humans
  • Inflammatory Bowel Diseases / blood
  • Inflammatory Bowel Diseases / diagnosis
  • Inflammatory Bowel Diseases / drug therapy
  • Male
  • Maximum Tolerated Dose
  • Mercaptopurine / administration & dosage
  • Mercaptopurine / analogs & derivatives*
  • Mercaptopurine / pharmacokinetics*
  • Middle Aged
  • Predictive Value of Tests
  • Prognosis
  • Prospective Studies
  • Risk Assessment
  • Severity of Illness Index
  • Thioguanine / blood*
  • Treatment Outcome

Substances

  • Biomarkers
  • 6-methylthiopurine
  • Mercaptopurine
  • Thioguanine
  • Azathioprine