Mitochondrially targeted antioxidants in the treatment of liver diseases and epithelial cancers

An antioxidant and mitochondrial technology, which can be used in medical preparations with non-active ingredients, digestive system, antitumor drugs, etc., and can solve problems such as inability to improve efficacy.

Inactive Publication Date: 2007-07-11
奥里迪斯生物医学研究及开发有限责任公司
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Problems solved by technology

[0026] In addition, oral supplementation with N-acetylcysteine ​​was administered orally in a multicenter study of 120 consecutive patients with biopsy-proven chronic hepatitis C infection unresponsive to a previous course of interferon-alpha. Amino acid (1200mg / day) and vitamin E (600mg / day) can not improve the efficacy of retreatment with α-interferon alone is poor (Ideo, G. et al., 1999, Eur.J.Gastroenterol.Hepatol., 11( 11): 1203-7)

Method used

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  • Mitochondrially targeted antioxidants in the treatment of liver diseases and epithelial cancers
  • Mitochondrially targeted antioxidants in the treatment of liver diseases and epithelial cancers
  • Mitochondrially targeted antioxidants in the treatment of liver diseases and epithelial cancers

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[0028] Mitochondria-targeted antioxidants such as vitamin E derivatives, coenzyme Q 10 or glutathione peroxide mimetics for the treatment and prevention of liver disease and / or epithelial cancer.

[0029] In its broadest aspect, the present invention provides a mitochondria-targeted antioxidant comprising a lipophilic cation covalently coupled to an antioxidant moiety for use in the treatment and prevention of liver disease and / or epithelial cancer , wherein the antioxidant moiety is capable of being transported across the mitochondrial membrane and accumulated within the mitochondria of intact cells. In particular, the compounds of the invention prevent cellular damage caused by oxidative stress (or free radicals) in the mitochondria.

[0030] The term "liver disease" as used in the present invention is meant to include global or partial, transient, temporary, chronic or permanent pathological effects on the anatomy, physiology, metabolism and / or genetic activity of the live...

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Abstract

The present invention relates to the use of a mitochondrially targeted antioxidant, e.g. derivatives of vitamin E, coenzyme Q10 or a glutathione peroxidase mimetic, in the treatment and prevention of liver diseases and / or epithelial cancers. The present invention also relates to pharmaceutical compositions containing the antioxidant(s) intended for such use. Furthermore the invention relates to the manufacture of medicaments containing the antioxidant(s) useful for such prevention and treatment.

Description

technical field [0001] The present invention relates to an antioxidant targeting mitochondria such as vitamin E derivatives, coenzyme Q 10 Or the use of glutathione peroxidase mimetic in the treatment and prevention of liver disease and / or epithelial cancer. Background technique [0002] Liver disease ranges from reversible mild fatty liver disease to progressive chronic liver disease, eventually leading to the development of life-threatening diseases such as cirrhosis, liver failure and liver cancer. [0003] The main causes of chronic liver disease are infection with hepatitis B virus or hepatitis C virus, excessive alcohol consumption, and nonalcoholic fatty liver disease (NAFLD). [0004] Hepatitis B virus (HBV) infection is a global public health problem. It is a major cause of cirrhosis and hepatocellular carcinoma (HCC) worldwide (Conjeevaram H.S. et al., 2003, Journal of Hepatology, 38:90-103). Hepatitis C virus (HCV) is one of the leading causes of liver-related ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61P35/00A61P5/00
CPCA61K47/48023A61K47/54A61P1/16A61P35/00A61P5/00
Inventor E·弗罗利克I·克维蒂科瓦K·扎特劳卡尔G·沙茨H·邓克C·斯图姆普特纳C·布克
Owner 奥里迪斯生物医学研究及开发有限责任公司
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