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Use for deferiprone

a deferiprone and prone technology, applied in the field of deferiprone, can solve the problems of dangerous iron overload, widespread iron overload in patients, toxic degenerative changes in liver, endocrine organs, etc., and achieve the effect of reducing iron stores in the hear

Inactive Publication Date: 2006-06-08
APOTEX TECH INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The patent text describes the use of deferiprone as an iron chelating agent to treat heart disease in patients with iron overload. Deferiprone has been found to have a cardio selective effect, meaning it is more effective in treating heart disease than other chelating agents. It has also been found to reduce the risk of heart failure and other iron-induced cardiac complications. The patent text describes the use of deferiprone in a pharmaceutical to prevent, treat, or reverse heart disease in patients with iron overload. The invention provides a novel use of deferiprone for the prevention, treatment, or reversal of heart disease in patients with iron overload."

Problems solved by technology

However, transfusions create a widespread iron overload in the patient.
Iron overload is dangerous since the excessive iron can cause toxic degenerative changes in the heart, liver and endocrine organs.
While blood transfusions constitute the major source of increased iron load, having about 1 mg of iron per ml of transfused red blood cells, increased iron absorption from the gastrointestinal tract can be observed in some diseases and also cause iron overload.
However, only 1 mg of iron is lost each day through sloughing of cells from skin and mucosal surfaces and the body does not have any organ that can perform the role of regulating the iron excretion in conditions of iron overload.
Consequently, increased dietary iron absorption can also lead to iron overload and iron-induced organ toxicity, the most serious of which is heart damage.
Thus, even without blood transfusions, conditions such as thalassemia, or hemochromatosis lead to increased body levels of iron, resulting in iron toxicity and eventually heart damage.
However, because desferrioxamine is not effective when given orally, it has to be given by a parenteral route.
While patient compliance is greater with deferiprone, it is not more effective than desferrioxamine in generally removing iron from the body.
When palliative transfusions are introduced, children live into their late teens, but eventually succumb to heart failure if iron overload is not treated.
However, many still die before 30 years of age, most from heart failure.
The number of patients who are compliant with this therapy is limited since the use of desferrioxamine normally requires the use of an infusion pump for 8 to 12 hours, 5-7 days a week as long as patients continue to receive regular blood transfusions.
This is a rigorous and uncomfortable treatment regime and many patients cannot or will not comply, which results in an increased iron load and iron toxicity in various organs, including the heart.
However, it is apparent that this is not the only reason that thalassemia patients receiving desferrioxamine therapy develop iron-induced heart disease.
The lack of adequate compliance with injectable desferrioxamine leads to a generalized increased iron overload as revealed by increases in iron concentrations assessed by the above methods, and thus also to increased levels of iron in the heart.
It has thus become evident that lowering of the total body iron alone is insufficient to protect against iron-induced heart damage.

Method used

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  • Use for deferiprone

Examples

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Embodiment Construction

[0117] Numerical Reference in this discussion is made to the list of references listed in the background of the invention.

[0118] The efficacy of iron chelation by desferrioxamine therapy, in subjects with thalassemia major is known. Daily subcutaneous infusions of desferrioxamine has been shown to ameliorate hepatic, cardiac and endocrinological dysfunction, improve growth and sexual maturation, and prolong survival in iron-overloaded thalassemia major patients.1,2,3,4,5 However, iron-induced cardiac disease remains a frequent cause of morbidity in patients with thalassemia and is still responsible for 70% of the deaths among those subjects.6 A sustained reduction in iron load, as measured by the proportion of serum ferritin results below 2500 μg / L, and the ability to comply with daily infusions of desferrioxamine have been reported to be the most important factors in the survival among patients with thalassemia major.1,7 The age at the start of chelation therapy and the hepatic ir...

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Abstract

A method of treating iron induced cardiac disease in a patient with iron overload, such as in thalassemia or the like comprising administering to the patient a therapeutically effective amount of deferiprone or a physiologically acceptable salt thereof sufficient to treat induced cardiac disease normally associated with iron overload.

Description

FIELD OF INVENTION [0001] The invention relates to the use of deferiprone for the prevention / stabilization / reduction of the risk of heart disease, such as heart failure, in patients having an iron overload condition such as is found in those suffering from for example, thalassemia, hemochromatosis, and myelodysplasia, and corresponding methods of treatment involving deferiprone therefor. BACKGROUND OF THE INVENTION [0002] Although reference is made in the following discussion to thalassemia specifically, the invention is not intended to be interpreted as limited only to the treatment thereof. Any chronic iron overload condition would benefit from treatment by utilizing the method described herein as well as the other aspects of the invention. For example, those suffering from hemochromatosis and transfused sickle cell anemia would also benefit. [0003] Thalassemia, among other afflictions, must be treated by regular transfusions of red blood cells in order to extend the life of the p...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/198A61K31/44A61K31/4412A61P9/00
CPCA61K31/44A61K31/4412A61K31/16A61K2300/00A61P43/00A61P7/06A61P9/00
Inventor SPINO, MICHAELPIGA, ANTONIO
Owner APOTEX TECH INC
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