Therapeutic agent for hyperlipidemia
OwnerShinichiro Tojo, Masahiro Nita +2inventors
InventorsShinichiro Tojo, Masahiro Nita, Takeshi Nishimura, Bei Shan
Life of this patent
Estimating the term…
Abstract
The present invention provides a therapeutic agent for hyperlipidemia, which has a novel action mechanism and which contains a farnesoid X receptor (FXR) antagonist as an active ingredient, and a screening method of the antagonist.
Claims16
A method for treating hyperlipidemia, which comprises administering a pharmaceutically effective amount of a farnesoid X receptor antagonist to a patient.
A method for treating hyperlipidemia, which comprises repressing a ligand dependent action of farnesoid X receptor.
A method for promoting biosynthesis of bile acid, which comprises increasing an expression of a cholesterol 7α-hydroxylase (CYP7A) gene or protein.
A method for inhibiting re-absorption of bile acid, which comprises repressing an expression of an intestinal bile acid-binding protein (I-BABP) gene or protein.
A method for promoting bile acid secretion, which comprises prohibiting decrease of an expression of a bile salt export pump (Bsep) gene or protein.
A method for screening a farnesoid X receptor antagonist, which comprises the following steps:
- (1) forming, in the presence of bile acid, a complex of farnesoid X receptor or its operable fragment labeled with a first fluorescent dye and a farnesoid X receptor coactivator labeled with a second fluorescent dye,
- (2) adding a test compound and incubating the compound, and
- (3) measuring an amount of a free coactivator by a fluorescence resonance energy transfer assay method.
A method for treating hyperlipidemia, which comprises administering a pharmaceutically effective amount of a farnesoid X receptor antagonist to a patient.
Dependencies are inferred from the claim text.