| Identification | Back Directory | [Name]
Spebrutinib | [CAS]
1025216-57-2 | [Synonyms]
LUM002
SHP626
Urea, N-[3-[(3S,4R,5R)-3-butyl-7-(dimethylamino)-3-ethyl-2,3,4,5-tetrahydro-4-hydroxy-1,1-dioxido-1-benzothiepin-5-yl]phenyl]-N'-[3-O-(phenylmethyl)-6-O-sulfo-β-D-glucopyranosyl]- | [Molecular Formula]
C38H51N3O12S2 | [MDL Number]
MFCD30747885 | [MOL File]
1025216-57-2.mol | [Molecular Weight]
805.96 |
| Hazard Information | Back Directory | [Uses]
Volixibat (SHP626) is a highly selective, minimally absorbed, and competitive apical sodium-dependent bile acid transporter (ASBT) inhibitor. Volixibat has potential for treatment for non-alcoholic steatohepatitis (NASH)[1][2]. | [in vivo]
Volixibat (SHP626) (5-30 mg/kg; food intake; daily for 24 weeks) improves metabolic aspects and components of non-alcoholic steatohepatitis in Ldlr-/-.Leiden mice[1]. | Animal Model: | Male Ldlr-/-.Leiden mice (high-fat diet, HFD)[1] | | Dosage: | 5, 15, or 30 mg/kg | | Administration: | Food intake; daily for 24 weeks
| | Result: | Significantly increased the total amount of bile acid in feces. Significantly attenuated the HFD-induced increase in hepatocyte hypertrophy, hepatic triglyceride and cholesteryl ester levels, and mesenteric white adipose tissue deposition at the highest dose. Non-alcoholic fatty liver disease activity score (NAS) was significantly lower in volixibat-treated mice than in the HFD controls.
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| [References]
[1] Salic K, et al. Apical sodium-dependent bile acid transporter inhibition with volixibat improves metabolicaspects and components of non-alcoholic steatohepatitis in Ldlr-/-.Leiden mice. PLoS One. 2019 Jun 24;14(6):e0218459. DOI:10.1371/journal.pone.0218459
[2] Palmer M, et al. A randomised, double-blind, placebo-controlled phase 1 study of the safety, tolerability and pharmacodynamics of volixibat in overweight and obese but otherwise healthy adults: implications for treatment of non-alcoholic steatohepatitis. BMC Pharmacol Toxicol. 2018 Mar 16;19(1):10. DOI:10.1186/s40360-018-0200-y |
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