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Pilot study with IBAT inhibitor A4250 for the treatment of cholestatic pruritus in primary biliary cholangitis.
Al-Dury S, Wahlström A, Wahlin S, Langedijk J, Elferink RO, Ståhlman M, Marschall HU. Al-Dury S, et al. Sci Rep. 2018 Apr 27;8(1):6658. doi: 10.1038/s41598-018-25214-0. Sci Rep. 2018. PMID: 29704003 Free PMC article. Clinical Trial.
Our aim was to assess tolerability and effect on pruritus of the selective IBAT inhibitor A4250 in patients with primary biliary cholangitis (PBC). Ten patients with PBC and bile acid sequestrant treatment of cholestatic pruritus were after a two-week wash out of the bile …
Our aim was to assess tolerability and effect on pruritus of the selective IBAT inhibitor A4250 in patients with primary biliary chol …
Loss of SLC27A5 Activates Hepatic Stellate Cells and Promotes Liver Fibrosis via Unconjugated Cholic Acid.
Wu K, Liu Y, Xia J, Liu J, Wang K, Liang H, Xu F, Liu D, Nie D, Tang X, Huang A, Chen C, Tang N. Wu K, et al. Adv Sci (Weinh). 2024 Jan;11(2):e2304408. doi: 10.1002/advs.202304408. Epub 2023 Nov 13. Adv Sci (Weinh). 2024. PMID: 37957540 Free PMC article.
The re-expression of hepatic SLC27A5 by an adeno-associated virus or the reduction of CA levels in the liver using A4250, an apical sodium-dependent bile acid transporter (ASBT) inhibitor, ameliorates liver fibrosis in Slc27a5(-/-) mice. ...
The re-expression of hepatic SLC27A5 by an adeno-associated virus or the reduction of CA levels in the liver using A4250, an apical s …
The ileal bile acid transporter inhibitor A4250 decreases serum bile acids by interrupting the enterohepatic circulation.
Graffner H, Gillberg PG, Rikner L, Marschall HU. Graffner H, et al. Aliment Pharmacol Ther. 2016 Jan;43(2):303-10. doi: 10.1111/apt.13457. Epub 2015 Nov 2. Aliment Pharmacol Ther. 2016. PMID: 26527417 Free article. Clinical Trial.
AIM: To assess tolerability and study, bile acid metabolism in a phase 1 trial with the selective ileal bile acid transporter inhibitor A4250. METHODS: A randomised double-blind, single-ascending dose (SAD) and multiple-ascending-dose study consisting of five cohorts compr …
AIM: To assess tolerability and study, bile acid metabolism in a phase 1 trial with the selective ileal bile acid transporter inhibitor A …
[The inhibitors of the apical sodium-dependent bile acid transporter (ASBT) as promising drugs].
Saveleva EE, Tyutrina ES, Nakanishi T, Tamai I, Salmina AB. Saveleva EE, et al. Biomed Khim. 2020 May;66(3):185-195. doi: 10.18097/PBMC20206603185. Biomed Khim. 2020. PMID: 32588824 Review. Russian.
To date the most known chemically synthesized inhibitors are: A3309, SHP626, A4250, 264W94, GSK2330672, SC-435. All of them are at different stages of clinical trials, which confirm the high efficacy and good tolerance of these inhibitors. ...
To date the most known chemically synthesized inhibitors are: A3309, SHP626, A4250, 264W94, GSK2330672, SC-435. All of them are at di …
Inhibition of intestinal bile acid absorption improves cholestatic liver and bile duct injury in a mouse model of sclerosing cholangitis.
Baghdasaryan A, Fuchs CD, Österreicher CH, Lemberger UJ, Halilbasic E, Påhlman I, Graffner H, Krones E, Fickert P, Wahlström A, Ståhlman M, Paumgartner G, Marschall HU, Trauner M. Baghdasaryan A, et al. J Hepatol. 2016 Mar;64(3):674-81. doi: 10.1016/j.jhep.2015.10.024. Epub 2015 Oct 31. J Hepatol. 2016. PMID: 26529078 Free article.
Furthermore, A4250 significantly reduced bile flow and biliary BA output, which correlated with reduced Bsep transcription, while Ntcp and Cyp7a1 were induced. Importantly A4250 significantly reduced biliary BA secretion but preserved HCO3(-) and biliary phospholipi …
Furthermore, A4250 significantly reduced bile flow and biliary BA output, which correlated with reduced Bsep transcription, while Ntc …