Drug intelligence / Profile preview

chenodeoxycholic acid + colesevelam

Development stage
Phase 4
Lead developer
Travere Therapeutics
Modality
Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems, Non-biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems, Injectable Hydrogels → Hydrogel Systems → Drug Delivery Systems, Implantable Hydrogels → Hydrogel Systems → Drug Delivery Systems
Administration
Oral
01

Overview

Chenodeoxycholic acid + colesevelam is a combination of two agents with complementary actions on bile acids and cholesterol metabolism. Chenodeoxycholic acid (CDCA) is a primary bile acid that acts by reducing cholesterol levels in the bile, suppressing hepatic synthesis of both cholesterol and cholic acid, and promoting the dissolution of radiolucent cholesterol gallstones. It also activates the bile acid receptor (FXR) and may influence GLP-1 secretion via TGR5 activation[1][2]. Colesevelam is a non-absorbed polymeric bile acid sequestrant that binds intestinal bile acids, preventing their reabsorption, which leads to increased conversion of cholesterol to bile acids in the liver and upregulation of LDL receptors, thereby lowering LDL-cholesterol[3][8]. Colesevelam also has modest effects on glycemic control in type 2 diabetes[5][6]. When used together, colesevelam can reduce absorption or activity of chenodeoxycholic acid by sequestering it in the gut[1][2].

02

Targets

FXR (Farnesoid x-activated receptor)GPBAR1BAR (Bile acid receptor)PXR (Pregnane X receptor)

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