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Publication Number
US-10220011-B2
Publication Date
2019-03-05
Expiration Date
Abstract
Treatment of intrahepatic cholestatic diseases by therapy with MBX-8025 or an MBX-8025 salt.
Core Innovation
The invention relates to a method of treating intrahepatic cholestatic diseases, including progressive familial intrahepatic cholestasis, by administering MBX-8025 or a pharmaceutically acceptable salt to a subject in need thereof. The approach is premised on reducing cholestasis in intrahepatic cholestatic diseases by lowering alkaline phosphatase (ALP) and γ-glutamyl transpeptidase (GGT). MBX-8025 is described as an orally active potent PPARδ agonist.
The document further describes the role of key biomarkers ALP and GGT in the context of cholestatic diseases and reports studies in which reductions in ALP and GGT are summarized. It states that lowering ALP and GGT reduces cholestasis in intrahepatic cholestatic diseases. Example adult treatment assessments are described to show dose-related decreases in ALP and GGT.
Administration is described in terms of therapeutically effective amounts, with oral routes and pharmaceutical formulations, and an oral dosing range of 20–200 mg/day. A preferred adult range of 50–100 mg/day is described, along with an example once daily dosing concept. The compound is specified as (R)-2-(4-((2-ethoxy-3-(4-(trifluoromethyl)phenoxy)propyl)thio)-2-methylphenoxy)acetic acid and also as MBX-8025 L-lysine dihydrate salt.
Claims Coverage
The provided portion contains two independent claims, both directed to treating progressive familial intrahepatic cholestasis by administering a therapeutically effective amount of a specified MBX-8025 compound or salt, with oral administration and daily dosing constraints reflected in dependent features. The inventive features focus on the specific compound or salt identity combined with an oral treatment method and defined daily dose ranges and dosing frequency.
Treating progressive familial intrahepatic cholestasis with specified MBX-8025 compound or salt
Administering to a subject in need thereof a therapeutically effective amount of (R)-2-(4-((2-ethoxy-3-(4-(trifluoromethyl)phenoxy)propyl)thio)-2-methylphenoxy)acetic acid or a salt thereof for treatment of progressive familial intrahepatic cholestasis.
Orally administering MBX-8025 L-lysine dihydrate salt
Orally administering to a subject in need thereof a therapeutically effective amount of (R)-2-(4-((2-ethoxy-3-(4-(trifluoromethyl)phenoxy)propyl)thio)-2-methylphenoxy)acetic acid L-lysine dihydrate salt for treatment of progressive familial intrahepatic cholestasis.
Across the independent claims, the core coverage is the use of MBX-8025 ((R)-2-(4-((2-ethoxy-3-(4-(trifluoromethyl)phenoxy)propyl)thio)-2-methylphenoxy)acetic acid) and/or a salt, including the specifically identified L-lysine dihydrate salt, administered as a therapeutically effective amount to treat progressive familial intrahepatic cholestasis. Dependent features in the provided claim set further specify oral administration and define daily dose ranges and once-per-day dosing.
Stated Advantages
Reduces cholestasis in intrahepatic cholestatic diseases by lowering ALP and GGT.
Example adult treatment assessments show dose-related decreases in ALP and GGT.
Documented Applications
Treatment of progressive familial intrahepatic cholestasis using MBX-8025 or a pharmaceutically acceptable salt, including the L-lysine dihydrate salt.
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