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Methods of treatment for cholestatic and fibrotic diseases

A technique for cholestasis, fibrosis, applied in the medical field, capable of addressing issues such as chemical structure, potency tissue penetration and residence, half-life metabolism and elimination of drug-drug interactions and safety differences

Active Publication Date: 2019-01-04
GENFIT SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although all statins contain a dihydroxyheptanoate HMG-CoA-like moiety that competes for binding to HMG-CoA reductase, each statin is unique and differs in chemical structure, potency (e.g., for HMG-CoA IC for reductase inhibition 50 ), tissue penetration and residence, half-life, metabolism and elimination, drug-drug interactions and safety

Method used

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  • Methods of treatment for cholestatic and fibrotic diseases
  • Methods of treatment for cholestatic and fibrotic diseases
  • Methods of treatment for cholestatic and fibrotic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0186] Materials and methods

[0187] Compounds were dissolved in dimethylsulfoxide (DMSO, Fluka cat#41640). Nitazoxanide (INTERCHIM cat#RQ550U), tizoxanide (INTERCHIM cat#RP253) and pitavastatin (INTERCHIM cat#15414), simvastatin (Sigma Aldrich cat#S6196), fluvastatin (Sigma Aldrich cat# Y0001090), Pravastatin (Selleckchem cat#S3036), Rosuvastatin (Selleckchem cat#S2169), Lovastatin (Selleckchem cat#S4223), Atorvastatin (Sigma Aldrich cat#PZ0001) are commercially available.

[0188] hHSC culture

[0189] Human primary hepatic stellate cells (hHSC) (Innoprot) were cultured in a culture medium supplemented with 2% fetal bovine serum (FBS, ScienCellcat#0010), 1% penicillin / streptomycin (ScienCell cat#0503) and stellate cell growth supplement (SteCGS; ScienCell cat#5352) in STeCM medium (ScienCell cat#5301). Cell culture flasks were coated with poly-L-lysine (Sigma cat#P4707) for better adhesion.

[0190] Preparation of the composition

[0191] 2-component combination ma...

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Abstract

The present invention relates to a synergistic combination of active ingredients for use in the treatment of fibrotic diseases.

Description

technical field [0001] The present invention relates to the field of medicine, in particular to the treatment of cholestatic or fibrotic diseases. Background technique [0002] Abnormal and exaggerated deposition of extracellular matrix is ​​a hallmark of all fibrotic diseases including liver, lung, kidney or cardiac fibrosis. The extent of organs affected, the progressive nature of the fibrotic process, the large number of affected populations, and the lack of effective treatments pose formidable challenges when treating fibrotic diseases. [0003] In an attempt to propose new therapeutic strategies for the treatment of fibrotic diseases, the inventors found that 2-[(5-nitro-1,3-thiazol-2-yl)carbamoyl]phenyl]acetate ( Nitazoxanide - NTZ), a synthetic antiprotozoal agent or its deuterated derivatives or its active metabolite 2-hydroxy-N-(5-nitro-2-thiazolyl)benzamide (thiazole nit, known as TZ) in combination with statins showed synergistic anti-fibrotic activity. Further...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/22A61K31/366A61K45/06A61K31/40A61K31/405A61K31/426A61K31/47A61K31/505A61P11/00A61P1/16
CPCA61K31/22A61K31/222A61K31/366A61K31/40A61K31/405A61K31/426A61K31/47A61K31/505A61K45/06A61P1/04A61P1/16A61P1/18A61P11/00A61P13/12A61P15/00A61P17/00A61P19/00A61P19/02A61P21/00A61P27/02A61P9/00Y02A50/30A61K2300/00A61K31/4418A61K31/573
Inventor 罗伯特·瓦尔恰克克林内·富卡尔菲利普·达勒泰勒
Owner GENFIT SA