Abstract: Saturated aliphatic straight chain dicarboxylic acids having a total number of carbon atoms which are divisible by four, are selectively toxic to certain tumor cells while non-toxic to normal cells of the same origin. Octacosanedioic acid is particularly preferred as it is a component of normal blood serum. Compositions containing these compounds may be used in the treatment of certain malignancies.
Type:
Grant
Filed:
March 1, 1984
Date of Patent:
January 23, 1990
Assignees:
David Rubin, Ely J. Rubin, Adolf W. Schwimmer, Irwin S. Schwartz, Century Laboratories, Inc.
Abstract: Hyperacidified tumors having high .beta.-glucuronidase activity can be treated with glucuronides with aglycones toxic to the tumor cells with great safety toward the rest of the body by first administering an alkalinizing agent in an amount sufficient to maintain the pH level of non-tumor tissues at approximately 7.4 during the glucuronide treatment. This will cause inactivation of .beta.-glucuronidase activity in the rest of the body. Novel glucuronides are disclosed the aglycones of which exert a higher toxic effect in an acid environment or is water-soluble only in an alkaline environment. Such compounds have particular utility with the above process. By substituting radioisotopes into the aglycone, diagnosis and in situ radiation therapy may be accomplished. Bacterial cells having .beta.-glucuronidase activity may also be diagnosed and treated in accordance with the present invention.
Type:
Grant
Filed:
October 13, 1978
Date of Patent:
April 22, 1986
Assignees:
Adolf W. Schwimmer, Irwin S. Schwartz, David Rubin
Abstract: Hyperacidified tumors having high .beta.-glucuronidase activity can be treated with glucuronides with aglycones toxic to the tumor cells with great safety toward the rest of the body by first administering an alkalinizing agent in an amount sufficient to maintain the pH level of non-tumor tissues at approximately 7.4 during the glucuronide treatment. This will cause inactivation of .beta.-glucuronidase activity in the rest of the body. When nitrile-containing aglycones are used sodium thiosulfate is also administered to avoid cyanide poisoning. A loading dose of glucuronide greater than 2 mMoles per kilogram body weight is first administered with additional administration of one third the initial dose each hour as long as .beta.-glucuronidase activity remains at the tumor site. Bacterial cells having .beta.-glucuronidase activity may also be diagnosed and treated in accordance with the present invention.
Type:
Grant
Filed:
October 13, 1981
Date of Patent:
November 6, 1984
Assignees:
Adolf Schwimmer, Irwin S. Schwartz, David Rubin, Century Science Corp.
Abstract: A method of diagnosing the presence of tumors having .beta.-glucuronidase activity comprises administering a glucuronide which differs in color or color intensity from the aglycone thereof to a patient. The preferred glucuronide is phenolphthalein glucuronide. The urine is then collecting for a twenty four hour period and the amount of phenolphthalein glucuronides present in the urine is determined. If substantially all of the phenolphthalein glucuronide is expelled then it is apparent that the body has no tumors or bacterial infections exhibiting .beta.-glucuronidase activity. If however substantial amounts of phenolphthalein is retained, then this is an indication of the presence of tumors having .beta.-glucuronidase activity or a bacterial infection having .beta.-glucuronidase activity.
Type:
Grant
Filed:
July 18, 1980
Date of Patent:
September 28, 1982
Assignees:
Adolf W. Schwimmer, Irwin S. Schwartz, David Rubin