Pharmacogenetics of the effects of colesevelam on colonic transit in irritable bowel syndrome with diarrhea

Dig Dis Sci. 2012 May;57(5):1222-6. doi: 10.1007/s10620-012-2035-5. Epub 2012 Jan 21.

Abstract

Background: Protein products of klothoβ (KLB) and fibroblast growth factor receptor 4 (FGFR4) impact fibroblast growth factor 19-mediated feedback inhibition of hepatic bile acid (BA) synthesis. Variants of KLB and FGFR4 influence colonic transit (CT) in diarrhea-predominant irritable bowel syndrome (IBS-D).

Aim: The purpose of this study was to test the hypothesis that colesevelam's slowing effects on CT in IBS-D patients is influenced by genetic variants in KLB and FGFR4.

Methods: We examined pharmacogenetic effects of KLB and FGFR4 coding variants (SNPs) on scintigraphic CT response to the BA sequestrant, colesevelam 1.875 g b.i.d. versus placebo (PLA) for 14 days in 24 female IBS-D patients.

Results: FGFR4 rs351855 and KLB rs497501 were associated with differential colesevelam effects on ascending colon (AC) half-emptying time (t(1/2), P = 0.046 and P = 0.085 respectively) and on overall CT at 24 h (geometric center, GC24: P = 0.073 and P = 0.042, respectively), with slower transit for rs351855 GA/AA (but not for GG) and rs497501 CA/AA (but not CC) genotypes.

Conclusion: FGFR4 rs351855 and KLB rs4975017 SNPs may identify a subset of IBS-D patients with beneficial response to colesevelam.

Publication types

  • Randomized Controlled Trial
  • Research Support, N.I.H., Extramural

MeSH terms

  • Adult
  • Allylamine / administration & dosage
  • Allylamine / analogs & derivatives*
  • Allylamine / pharmacokinetics
  • Anticholesteremic Agents / administration & dosage
  • Anticholesteremic Agents / pharmacokinetics
  • Bile Acids and Salts* / biosynthesis
  • Bile Acids and Salts* / genetics
  • Biotransformation
  • Colesevelam Hydrochloride
  • Colon / metabolism
  • Colon / physiopathology
  • Diarrhea* / drug therapy
  • Diarrhea* / etiology
  • Diarrhea* / genetics
  • Diarrhea* / physiopathology
  • Feedback, Physiological / drug effects
  • Female
  • Fibroblast Growth Factors / metabolism
  • Gastrointestinal Transit / genetics*
  • Humans
  • Irritable Bowel Syndrome* / complications
  • Irritable Bowel Syndrome* / drug therapy
  • Irritable Bowel Syndrome* / genetics
  • Irritable Bowel Syndrome* / physiopathology
  • Klotho Proteins
  • Membrane Proteins / genetics*
  • Pharmacogenetics
  • Polymorphism, Single Nucleotide
  • Receptor, Fibroblast Growth Factor, Type 4 / genetics*

Substances

  • Anticholesteremic Agents
  • Bile Acids and Salts
  • FGF19 protein, human
  • KLB protein, human
  • Membrane Proteins
  • Allylamine
  • Fibroblast Growth Factors
  • Receptor, Fibroblast Growth Factor, Type 4
  • Klotho Proteins
  • Colesevelam Hydrochloride