Drug – bio-affecting and body treating compositions – Lymphokine – Interferon
Patent
1993-02-04
1994-09-13
Wityshyn, Michael G.
Drug, bio-affecting and body treating compositions
Lymphokine
Interferon
424 856, 424 857, 530351, 530395, 435 681, A61K 3766
Patent
active
053466969
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a novel conjugated medicinal agent prepared by combining asialoglycoprotein(ASGP) with a medicinal component which acts specifically on the liver and includes a novel conjugated interferon antiviral agent prepared by combining asialoglycoprotein with recombinant interferon(INF). More specifically, the present invention relates to a novel conjugated interferon which is effective in treating viral hepatitis. The conjugated interferon of the present invention is selectively distributed and absorbed only in the liver, the main site of hepatitis virus replication, and demonstrates potential usefulness as a therapeutic agent for the treatment of B-type and C-type hepatitis. The present invention further relates to a process for preparing the conjugated medicinal agent, a pharmaceutical composition and use thereof.
BACKGROUND ART
Chronic viral hepatitis is a very common disease in the world. It is estimated that approximately 5% of the world population and about 10% of the population in Korea suffer from chronic viral hepatitis. In addition, chronic viral hepatitis arouses medical and social interest since the disease adversely impacts the life, especially the quality and productive aspects of life. Chronic hepatitis generally progresses to liver cirrhosis and possibly primary hepatoma which leads to death. Chronic hepatitis viral infection is the major cause of hepatoma and is considered a highly morbid disease. Therefore, the development of an effective antiviral agent is urgently needed. At present, reliable antiviral therapy for chronic viral hepatitis has yet to be developed. Although some agents have been proven partially effective in the treatment of chronic viral hepatitis, they have many disadvantages, including adverse side effects, which remain to be solved.
As one of the anti-viral agents commonly used in the past adenosine arabinoside monophosphate (Ara-AMP) is a purine-based preparation which exerts strong antiviral activity by inhibiting the activity of DNA polymerase. Early in the 1980's it was reported that Ara-AMP has a therapeutic response of 10 to 17% in the treatment of chronic hepatitis B. However, in 1987 Garcia et al. (Garcia G., Smith C. L., Weissberg J. I., et al.: Adenine arabinoside monophosphate in combination with human leukocyte interferon in the treatment of chronic hepatitis B: A randomized, double-blind, placebo-controlled trial. Ann Intern Med 107:278-285, 1987) reported that the Ara-AMP treatment group did not show any significantly greater effect as compared to the control group. Further, the administration of Ara-AMP sometimes develops very serious adverse effects, such as bone marrow suppression and irreversible neuromuscular pain. Accordingly, Ara-AMP is no longer used in the treatment of chronic viral hepatitis B.
It is generally known that interferon produced by animal cells, i.e. naturally occurring, is effective in the treatment of chronic vital hepatitis B. Natural interferon is a glycoprotein, i.e. a conjugated protein in which the nonprotein group is a carbohydrate of a low molecular weight. It was disclosed as a substance having antiviral activity in 1957. Numerous studies on its action, effect, mechanism of action, method for separation into a purified state, mass production, and the like, have been done in both the industrial and academic fields because of the interest in interferon as an antiviral agent and an anticancer agent. At present, the following kinds of interferon are known: the leucocytes, has antiviral activity and a natural killer cell-activating effect; especially double-strand RNA virus infection, of the fibroblasts, and has antiviral activity; and stimulation of lymphocytes with mitogen or antigen, and has an immunemodulating activity. activity as compared to the alpha and beta interferons.
Today genetic recombination methods produce recombinant interferon on an industrial scale such that it is widely used for its antiviral and immunomodulator activities.
The therapeutic effect of recombinant int
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Kim Chung Y.
Lee Hyo S.
Korea Green Cross Corporation
Sayala C.
Wityshyn Michael G.
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