Target intelligence / Profile preview

Bile acids and bile salts (BA) (BA)

Target
BA
Molecular classification
Steroid derivatives, Metabolites, Amphipathic molecules, Other
01

Overview

Bile acids and bile salts are amphipathic steroid molecules synthesized from cholesterol in the liver and secreted into the intestinal lumen [NIH, 2022]. Their primary biological function is to facilitate the emulsification and absorption of dietary lipids and fat-soluble vitamins by forming mixed micelles [StatPearls, 2023]. Beyond digestion, they act as potent signaling molecules that regulate glucose and lipid metabolism through receptors like the Farnesoid X Receptor (FXR) and TGR5 [Nature Reviews, 2017]. In the context of pharmacology, luminal bile acids are the direct target of bile acid sequestrants, which are non-absorbable polymers that bind these molecules in the gut [PubChem, 2023]. This binding prevents their reabsorption in the terminal ileum, interrupting the enterohepatic circulation and forcing the liver to convert more cholesterol into bile acids, thereby lowering systemic LDL cholesterol levels [StatPearls, 2023]. Additionally, modulating the bile acid pool in the lumen is a therapeutic strategy for treating bile acid malabsorption, chronic diarrhea, and cholestatic pruritus [Mayo Clinic, 2023]. Recent research also highlights their role in modulating the gut microbiome and metabolic health in conditions like type 2 diabetes [Journal of Lipid Research, 2021].

Other names
Bile saltsIntestinal bile acidsLuminal bile acidsBile acid micellesPrimary and secondary bile acids
02

Mechanism of action

Bile acid sequestration, interruption of enterohepatic circulation, and induction of hepatic cholesterol-7-alpha-hydroxylase.

03

Biological functions

Lipid emulsificationCholesterol homeostasisSignal transductionAntimicrobial activityVitamin absorption
04

Disease associations

HypercholesterolemiaBile acid malabsorptionCholestatic pruritusType 2 diabetesNonalcoholic steatohepatitis (NASH)
05

Safety considerations

Malabsorption of fat-soluble vitamins (A, D, E, K)Gastrointestinal distress (constipation, bloating)Interference with absorption of other oral medications
06

Interacting drugs

Cholestyramine

2 more in the full profile.

07

Biomarkers

7α-hydroxy-4-cholesten-3-one (C4)Fecal bile acid excretionFibroblast growth factor 19 (FGF19)

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