Drug intelligence / Profile preview

dehydrolithocholic acid

Development stage: Preclinical
Modality: Small Molecules
Administration: Oral

Overview

Dehydrolithocholic acid (also known as 3-oxolithocholic acid or DHLCA) is a naturally occurring secondary bile acid metabolite derived from the bacterial or enzymatic oxidation of lithocholic acid (LCA). It acts as a multi-receptor modulator, functioning as an agonist of G-protein coupled bile acid receptor 1 (GPBAR1/TGR5), farnesoid X receptor (FXR), vitamin D receptor (VDR), and pregnane X receptor (PXR), while also acting as a direct inhibitor/inverse agonist of retinoic acid receptor-related orphan receptor-gamma t (RORγt). Through these pathways, dehydrolithocholic acid regulates adaptive immunity by suppressing T helper 17 (Th17) cell differentiation and has demonstrated protective, anti-inflammatory, and metabolic benefits in preclinical models of diabetic kidney disease (DKD) and inflammatory bowel disease (IBD).

Other names: (5β)-3-oxo-cholan-24-oic acid3-dehydrolithocholic acid3-keto LCA3-keto Lithocholate3-keto Lithocholic Acid3-keto-lithocholic acid3-ketolithocholic acid3-KLCA3-oxo LCA3-oxo Lithocholate3-oxo Lithocholic Acid3-oxo-5β-cholanoic acid3-oxo-5beta-cholanoic acid3-oxo-lithocholic acid3-oxolithocholic acid3-oxoLCADHLCADLADLCA

Targets

FXR (Farnesoid x-activated receptor)GPBAR1RORγt

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