| [1] |
CHALASANI N, YOUNOSSI Z, LAVINE JE, et al. The diagnosis and management of nonalcoholic fatty liver disease: Practice guidance from the American Association for the Study of Liver Diseases[J]. Hepatology, 2018, 67(1): 328-357. DOI: 10.1002/hep.29367. |
| [2] |
ESLAM M, SANYAL AJ, GEORGE J, et al. MAFLD: A consensus-driven proposed nomenclature for metabolic associated fatty liver disease[J]. Gastroenterology, 2020, 158(7): 1999-2014.e1. DOI: 10.1053/j.gastro.2019.11.312. |
| [3] |
|
| [4] |
CARR RM, REID AE. FXR agonists as therapeutic agents for non-alcoholic fatty liver disease[J]. Curr Atheroscler Rep, 2015, 17(4): 500. DOI: 10.1007/s11883-015-0500-2. |
| [5] |
YOUNOSSI ZM, RATZIU V, LOOMBA R, et al. Obeticholic acid for the treatment of non-alcoholic steatohepatitis: Interim analysis from a multicentre, randomised, placebo-controlled phase 3 trial[J]. Lancet, 2019, 394(10215): 2184-2196. DOI: 10.1016/S0140-6736(19)33041-7. |
| [6] |
SANYAL A, LOPEZ P, LAWITZ E, et al. SAT-357-Tropifexor, a farnesoid X receptor agonist for the treatment of non-alcoholic steatohepatitis: Interim results based on baseline body mass index from first two parts of Phase 2b study FLIGHT-FXR[J]. J Hepatol, 2019, 70(1): e796-e797. DOI: 10.1016/s0618-8278(19)31587-7. |
| [7] |
KLUCHER K, WANG Y, HALCOMB R, et al. FRI-313-A novel farnesoid X receptor agonist, TERN-101, reduces liver steatosis, inflammation, ballooning and fibrosis in a murine model of non-alcoholic steatohepatitis[J]. J Hepatol, 2019, 70(1): e534. DOI: 10.1016/s0618-8278(19)31056-4. |
| [8] |
FORMAN BM, GOODE E, CHEN J, et al. Identification of a nuclear receptor that is activated by farnesol metabolites[J]. Cell, 1995, 81(5): 687-693. DOI: 10.1016/0092-8674(95)90530-8. |
| [9] |
MAKISHIMA M, OKAMOTO AY, REPA JJ, et al. Identification of a nuclear receptor for bile acids[J]. Science, 1999, 284(5418): 1362-1365. DOI: 10.1126/science.284.5418.1362. |
| [10] |
YANG ZX, SHEN W, SUN H. Effects of nuclear receptor FXR on the regulation of liver lipid metabolism in patients with non-alcoholic fatty liver disease[J]. Hepatol Int, 2010, 4(4): 741-748. DOI: 10.1007/s12072-010-9202-6. |
| [11] |
DONG B, YOUNG M, LIU X, et al. Regulation of lipid metabolism by obeticholic acid in hyperlipidemic hamsters[J]. J Lipid Res, 2017, 58(2): 350-363. DOI: 10.1194/jlr.M070888. |
| [12] |
MIYAZAKI T, HONDA A, IKEGAMI T, et al. Human-specific dual regulations of FXR-activation for reduction of fatty liver using in vitro cell culture model[J]. J Clin Biochem Nutr, 2019, 64(2): 112-123. DOI: 10.3164/jcbn.18-80. |
| [13] |
KIR S, BEDDOW SA, SAMUEL VT, et al. FGF19 as a postprandial, insulin-independent activator of hepatic protein and glycogen synthesis[J]. Science, 2011, 331(6024): 1621-1624. DOI: 10.1126/science.1198363. |
| [14] |
WANG Y, NAKAJIMA T, GONZALEZ FJ, et al. PPARs as metabolic regulators in the liver: Lessons from liver-specific PPAR-null mice[J]. Int J Mol Sci, 2020, 21(6): 2061. DOI: 10.3390/ijms21062061. |
| [15] |
PINEDA TORRA I, CLAUDEL T, DUVAL C, et al. Bile acids induce the expression of the human peroxisome proliferator-activated receptor alpha gene via activation of the farnesoid X receptor[J]. Mol Endocrinol, 2003, 17(2): 259-272. DOI: 10.1210/me.2002-0120. |
| [16] |
WANG YD, CHEN WD, WANG M, et al. Farnesoid X receptor antagonizes nuclear factor kappaB in hepatic inflammatory response[J]. Hepatology, 2008, 48(5): 1632-1643. DOI: 10.1002/hep.22519. |
| [17] |
LI L, ZHANG Q, PENG J, et al. Activation of farnesoid X receptor downregulates monocyte chemoattractant protein-1 in murine macrophage[J]. Biochem Biophys Res Commun, 2015, 467(4): 841-846. DOI: 10.1016/j.bbrc.2015.10.056. |
| [18] |
MOURIES J, BRESCIA P, SILVESTRI A, et al. Microbiota-driven gut vascular barrier disruption is a prerequisite for non-alcoholic steatohepatitis development[J]. J Hepatol, 2019, 71(6): 1216-1228. DOI: 10.1016/j.jhep.2019.08.005. |
| [19] |
NEUSCHWANDER-TETRI BA, LOOMBA R, SANYAL AJ, et al. Farnesoid X nuclear receptor ligand obeticholic acid for non-cirrhotic, non-alcoholic steatohepatitis (FLINT): A multicentre, randomised, placebo-controlled trial[J]. Lancet, 2015, 385(9972): 956-965. DOI: 10.1016/S0140-6736(14)61933-4. |
| [20] |
AL-DURY S, WAHLSTRÖM A, PANZITT K, et al. Obeticholic acid may increase the risk of gallstone formation in susceptible patients[J]. J Hepatol, 2019, 71(5): 986-991. DOI: 10.1016/j.jhep.2019.06.011. |
| [21] |
HERNANDEZ ED, ZHENG L, KIM Y, et al. Tropifexor-mediated abrogation of steatohepatitis and fibrosis is associated with the antioxidative gene expression profile in rodents[J]. Hepatol Commun, 2019, 3(8): 1085-1097. DOI: 10.1002/hep4.1368. |
| [22] |
GEGE C, HAMBRUCH E, HAMBRUCH N, et al. Nonsteroidal FXR ligands: Current status and clinical applications[J]. Handb Exp Pharmacol, 2019, 256: 167-205. DOI: 10.1007/164_2019_232. |
| [23] |
PATEL K, HARRISON SA, ELKHASHAB M, et al. Cilofexor, a nonsteroidal FXR agonist, in patients with noncirrhotic NASH: A phase 2 randomized controlled trial[J]. Hepatology, 2020, 72(1): 58-71. DOI: 10.1002/hep.31205. |
| [24] |
LAWITZ E, GANE E, RUANE P, et al. SAT-352-A combination of the ACC inhibitor GS-0976 and the nonsteroidal FXR agonist GS-9674 improves hepatic steatosis, biochemistry, and stiffness in patients with non-alcoholic steatohepatitis[J]. J Hepatol, 2019, 70(1): e794. DOI: 10.1016/S0618-8278(19)31582-8. |
| [25] |
GENIN MJ, BUENO AB, AGEJAS FRANCISCO J, et al. Discovery of 6-(4-{[5-Cyclopropyl-3-(2, 6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic acid: A novel FXR agonist for the treatment of dyslipidemia[J]. J Med Chem, 2015, 58(24): 9768-9772. DOI: 10.1021/acs.jmedchem.5b01161. |
| [26] |
WANG Y, CRITTENDEN DB, ENG C, et al. Safety, pharmacokinetics, pharmacodynamics, and formulation of liver-distributed farnesoid X-receptor agonist TERN-101 in healthy volunteers[J]. Clin Pharmacol Drug Dev, 2021, 10(10): 1198-1208. DOI: 10.1002/cpdd.960. |
| [27] |
CHAU M, LI Y, ROQUETA-RIVERA M, et al. Characterization of EDP-305, a highly potent and selective farnesoid X receptor agonist, for the treatment of non-alcoholic steatohepatitis[J]. Int J Gastroenterol, 2019, 3(1): 4-16. DOI: 10.11648/j.ijg.20190301.12. |
| [28] |
AHMAD A, SANDERSON K, DICKERSON D, et al. Pharmacokinetics, pharmacodynamics, and safety of EDP-305, in healthy and presumptive NAFLD subjects[J]. J Hepatol, 2018, 68: s584. DOI: 10.1016/s0168-8278(18)31427-2. |
| [29] |
AN P, WEI G, HUANG P, et al. A novel non-bile acid FXR agonist EDP-305 potently suppresses liver injury and fibrosis without worsening of ductular reaction[J]. Liver Int, 2020, 40(7): 1655-1669. DOI: 10.1111/liv.14490. |
| [30] |
WAGNER B, GOVEK S, NAGASAWA J, et al. Efficacy of MET409, a potent, novel non-bile acid FXR agonist, in rodents and cynomolgus monkeys[J]. Hepatology, 2017, 66(Suppl): 1049A.
|
| [31] |
WAGNER B, GOVEK S, NAGASAWA J, et al. MET409, a potent, non-bile acid sustained FXR agonist, shows rapid disease reversal in a diet-induced obese mouse model of biopsy-confirmed Nash[J]. Hepatology, 2018, 68(Suppl): 1006A.
|
| [32] |
HARRISON SA, BASHIR MR, SHIM-LOPEZ J, et al. MET409, a sustained FXR agonist, decreased hepatic fat and improved liver function without raising LDL-C after 28 days in NASH patients[J]. Hepatology, 2019, 70(Suppl): 1257A.
|
| [33] |
HARRISON SA, BASHIR MR, LEE KJ, et al. A structurally optimized FXR agonist, MET409, reduced liver fat content over 12 weeks in patients with non-alcoholic steatohepatitis[J]. J Hepatol, 2021, 75(1): 25-33. DOI: 10.1016/j.jhep.2021.01.047. |
| [34] |
RADREAU P, JOLY S, DUBOS C, et al. In vitro and in vivo characterization of EYP001, a novel, potent and selective FXR agonist now in a Phase 2 clinical trial in NASH[J]. Hepatology, 2019, 70(Suppl): 1267A.
|
DownLoad: