Target intelligence / Profile preview

Apical sodium-dependent bile acid transporter (SLC10A2) (ASBT)

Target
ASBT
Molecular classification
Transporter, Solute carrier family
01

Overview

The Apical sodium-dependent bile acid transporter (ASBT), also known as the ileal bile acid transporter (IBAT), is a transmembrane protein encoded by the SLC10A2 gene that is essential for the enterohepatic circulation of bile acids [9, 10]. Located on the apical membrane of enterocytes in the terminal ileum, ASBT mediates the sodium-dependent reabsorption of bile acids from the intestinal lumen, returning them to the liver via the portal vein [9]. This process is crucial for maintaining the bile acid pool and regulating cholesterol levels, as bile acids are the primary catabolic product of cholesterol [10]. Pharmacological modulation of this system, either through direct binding of bile acids by sequestrants or through the inhibition of ASBT, is used to treat conditions such as hypercholesterolemia, chronic constipation, and cholestatic liver diseases [6, 7, 8]. By increasing the fecal excretion of bile acids, these therapies reduce the systemic bile acid burden and stimulate the liver to convert more cholesterol into new bile acids, thereby lowering LDL cholesterol levels [10]. Recent clinical advances have focused on ASBT inhibitors like odevixibat and maralixibat for the treatment of severe pruritus associated with rare cholestatic disorders such as Alagille syndrome and progressive familial intrahepatic cholestasis [1, 2].

Other names
Ileal bile acid transporterIBATSLC10A2Sodium/bile acid cotransporterISBTIleal bile acid-binding proteinFABP6
02

Mechanism of action

Inhibition of the apical sodium-dependent bile acid transporter (ASBT) or direct sequestration of bile acids in the gut to prevent reabsorption and promote fecal excretion.

03

Biological functions

Bile acid recyclingLipid metabolismCholesterol homeostasisEnterohepatic circulation
04

Disease associations

CholestasisHypercholesterolemiaPruritusChronic constipationAlagille syndromeProgressive familial intrahepatic cholestasis
05

Safety considerations

DiarrheaAbdominal painFat-soluble vitamin malabsorptionPotential for increased liver enzymes
06

Interacting drugs

Odevixibat

7 more in the full profile.

07

Biomarkers

Serum bile acids7α-hydroxy-4-cholesten-3-one (C4)Fibroblast growth factor 19 (FGF19)Fecal bile acid excretion

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