Treatment with the natural FXR agonist chenodeoxycholic acid reduces clearance of plasma LDL whilst decreasing circulating PCSK9, lipoprotein(a) and apolipoprotein C‐III

• Published in: Journal of internal medicine Vol. 281; no. 6; pp. 575 - 585
• Main Authors: Ghosh Laskar, M., Eriksson, M., Rudling, M., Angelin, B.
• Format: Journal Article
• Language: English
• Published: England Blackwell Publishing Ltd 01.06.2017
• Subjects: Acids; apolipoprotein; Apolipoprotein C-III; Apolipoprotein C-III - blood; Apolipoprotein C-III - drug effects; Apolipoproteins; Bile; Bile acids; Binding; Chenodeoxycholic acid; Chenodeoxycholic Acid - pharmacology; Chenodeoxycholic Acid - therapeutic use; Cholecystectomy; Cholesterol; Cholesterol, LDL - blood; Cholesterol, LDL - drug effects; Diabetes mellitus; Fibroblast growth factors; Gallstones; Gallstones - drug therapy; Humans; Hydroxylase; Hydroxymethylglutaryl-CoA reductase; Insulin; Kexin; Kinetics; LDL cholesterol; LDL receptors; Lipid metabolism; lipoprotein(a); Lipoprotein(a) - drug effects; Lipoproteins; Liver; Liver - enzymology; Liver diseases; Low density lipoprotein; Low density lipoprotein receptors; Male; Markers; Metabolism; Patients; PCSK9; Plasma; Proprotein Convertase 9 - blood; Proprotein Convertase 9 - drug effects; Proprotein convertases; Receptors; Receptors, Cytoplasmic and Nuclear - agonists; Receptors, LDL - metabolism; Reduction; Secretion; Serum levels; Subtilisin; Surgery; Triglycerides; PCSK9; apolipoprotein; LDL cholesterol; lipoprotein(a); chenodeoxycholic acid; LDL receptors

Background The natural farnesoid X receptor (FXR) agonist chenodeoxycholic acid (CDCA) suppresses hepatic cholesterol and bile acid synthesis and reduces biliary cholesterol secretion and triglyceride production. Animal studies have shown that bile acids downregulate hepatic LDL receptors (LDLRs); h...