Bile acids transporter modulation

Bile acid transporter modulation is a pharmacological strategy that targets key proteins responsible for the absorption, export, and overall regulation of bile acids in the enterohepatic circulation. Major transporters include NTCP (liver uptake), ASBT/IBAT (intestinal reuptake), BSEP (canalicular export from hepatocytes), and OSTα/β (facilitated diffusion across basolateral membranes). Modulation of these transporters is clinically valuable for the treatment of cholestatic pruritus, genetic cholestatic disorders, metabolic liver diseases, and has notable implications for drug safety as inhibition can lead to cholestasis and liver injury. Specific transporter inhibitors are approved or in development, and transporter function is central to bile acid-related physiology and pathophysiology.

Other names

Sodium taurocholate cotransporting polypeptide (NTCP)Apical sodium-dependent bile acid transporter (ASBT)Apical sodium-dependent bile acid transporter (IBAT)Bile salt export pump (BSEP)Organic solute transporter alpha/beta (OSTα/β)

Inhibition of bile acid uptake (ASBT/IBAT, NTCP); Restoration or enhancement of bile acid export (BSEP activators—not commercially available); Indirect modulation by FXR agonists; Competitive inhibition of transporter function (reducing bile acid pool, altering composition, increasing fecal excretion)