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. Author manuscript; available in PMC: 2018 May 1.
Published in final edited form as: Curr Opin Gastroenterol. 2017 May;33(3):149–157. doi: 10.1097/MOG.0000000000000352

Table 1. Potential therapeutics for primary sclerosing cholangitis that modulate bile acids.

Process Targets Drug

UDCA norUDCA OCA Fibrates ASBT–
BA synthesis FXR graphic file with name nihms879869t1.jpg
RXR graphic file with name nihms879869t1.jpg
CYP7A1 graphic file with name nihms879869t1.jpg graphic file with name nihms879869t1.jpg
CYP27A1 graphic file with name nihms879869t1.jpg graphic file with name nihms879869t1.jpg

BA detoxification SULT2A1 graphic file with name nihms879869t1.jpg graphic file with name nihms879869t1.jpg graphic file with name nihms879869t1.jpg
UGT1A1 graphic file with name nihms879869t1.jpg graphic file with name nihms879869t1.jpg graphic file with name nihms879869t1.jpg

BA secretion BSEP graphic file with name nihms879869t1.jpg graphic file with name nihms879869t1.jpg

MRP2 graphic file with name nihms879869t1.jpg graphic file with name nihms879869t1.jpg
MDR2/3 graphic file with name nihms879869t1.jpg graphic file with name nihms879869t1.jpg

Alternative BA export OSTα/β graphic file with name nihms879869t1.jpg
MRP4 graphic file with name nihms879869t1.jpg graphic file with name nihms879869t1.jpg
MRP3 graphic file with name nihms879869t1.jpg graphic file with name nihms879869t1.jpg

Bicarbonate umbrella CFTR graphic file with name nihms879869t1.jpg graphic file with name nihms879869t1.jpg
AE2 graphic file with name nihms879869t1.jpg graphic file with name nihms879869t1.jpg
CaCl graphic file with name nihms879869t1.jpg graphic file with name nihms879869t1.jpg

Cholehepatic shunting ASBT graphic file with name nihms879869t1.jpg

Enterohepatic circulation ASBT graphic file with name nihms879869t1.jpg
FXR graphic file with name nihms879869t1.jpg
OSTα/β (ileal) graphic file with name nihms879869t1.jpg
FGF19 graphic file with name nihms879869t1.jpg

Checkboxes indicate where each drug acts on individual targets. ASBT, apical sodium-bile acid transporter; ASBT–, apical sodium-bile acid transporter inhibitor; BA, bile acids; BSEP, bile salt export pump; CaCl, Ca2+-dependent chloride channel; CFTR, cystic fibrosis transmembrane conductance regulator; FXR, farsenoid X receptor; MDR2/3, multidrug resistance 2/3; MRP2, multidrug resistance-associated protein 2; MRP3, multidrug resistance-associated protein 3; MRP4, multidrug resistance-associated protein 4; norUDCA, 24-norursodeoxycholic acid; OCA, obetichoic acid; OSTα/β, organic solute transporter α/β; PSC, primary sclerosing cholangitis; RXR, retinoid X receptor; SULT2A1, sulfotransferase family 2A member 1; UDCA, ursodeoxycholic acid; UGT1A1, uridine diphosphate-glucoronosyltransferase family 1 member A1.