Autotaxin, bile acid profile and effect of ileal bile acid transporter inhibition in primary biliary cholangitis patients with pruritus

Liver Int. 2019 May;39(5):967-975. doi: 10.1111/liv.14069. Epub 2019 Feb 25.

Abstract

Background and aims: Pruritus is a common symptom in patients with primary biliary cholangitis (PBC) for which ileal bile acid transporter (IBAT) inhibition is emerging as a potential therapy. We explored the serum metabonome and gut microbiota profile in PBC patients with pruritus and investigated the effect of GSK2330672, an IBAT inhibitor.

Methods: We studied fasting serum bile acids (BAs), autotaxin and faecal microbiota in 22 PBC patients with pruritus at baseline and after 2 weeks of GSK2330672 treatment. Control group included 31 asymptomatic PBC patients and 18 healthy volunteers. BA profiling was done by ultra performance liquid chromatography coupled to a mass spectrometry (UPLC-MS). Faecal microbiomes were analysed by 16S ribosomal RNA gene sequencing.

Results: In PBC patients with pruritus, serum levels of total and glyco-conjugated primary BAs and autotaxin were significantly elevated. Autotaxin activity correlated significantly with tauro- and glyco-conjugated cholic acid (CA) and chenodeoxycholic acid (CDCA), both at baseline and after GSK2330672. GSK2330672 significantly reduced autotaxin and all tauro- and glyco- conjugated BAs and increased faecal levels of CA (P = 0.048) and CDCA (P = 0.027). Gut microbiota of PBC patients with pruritus was similar to control groups. GSK2330672 increased the relative abundance of Firmicutes (P = 0.033) and Clostridia (P = 0.04) and decreased Bacteroidetes (P = 0.033) and Bacteroidia (P = 0.04).

Conclusions: Pruritus in PBC does not show a distinct gut bacterial profile but is associated with elevated serum bile acid and autotaxin levels which decrease after IBAT inhibition. In cholestatic pruritus, a complex interplay between BAs and autotaxin is likely and may be modified by IBAT inhibition.

Keywords: PBC; metabonome; microbiota; pruritus.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Bile Acids and Salts / blood*
  • Biomarkers / blood
  • Carrier Proteins
  • Case-Control Studies
  • Chenodeoxycholic Acid / pharmacology
  • Cholic Acid / pharmacology
  • Chromatography, Liquid
  • Feces / chemistry
  • Feces / microbiology
  • Female
  • Humans
  • Liver Cirrhosis, Biliary / complications*
  • Male
  • Membrane Glycoproteins
  • Methylamines / pharmacology*
  • Middle Aged
  • Phosphoric Diester Hydrolases / blood*
  • Pruritus / blood*
  • Pruritus / drug therapy*
  • Pruritus / etiology
  • RNA, Ribosomal, 16S / genetics
  • Tandem Mass Spectrometry
  • Thiazepines / pharmacology*

Substances

  • 3-((((3R,5R)-3-butyl-3-ethyl-7-(methyloxy)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,4-benzothiazepin-8-yl)methyl)amino)pentanedioic acid
  • Bile Acids and Salts
  • Biomarkers
  • Carrier Proteins
  • Membrane Glycoproteins
  • Methylamines
  • RNA, Ribosomal, 16S
  • Thiazepines
  • bile acid binding proteins
  • Chenodeoxycholic Acid
  • Phosphoric Diester Hydrolases
  • alkylglycerophosphoethanolamine phosphodiesterase
  • Cholic Acid