Glutamine-high z element compounds for treating cancer

a high z element, glutamine technology, applied in the direction of antineoplastic agents, medical preparations, energy modified materials, etc., can solve the problems of not being effective against the target tissue, damage to surrounding healthy tissue, limitations of radiation therapy,

Active Publication Date: 2019-03-14
SERBIG PHARMA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0027]The present invention helps to overcome the limitations of radiation therapy as disclosed above, by providing a radiosensitizing glutamine non-radioisotope high Z element compounds, which when exposed to x-rays or other ionizing or high energy radiation such as gamma rays, alpha particles, protons, neutrons, or fast ions, causes the destruction of mitochondrial and other structures of targeted tissue and cells.
[0028]These compounds can be used to destroy mitochondria, which effectively denies energy and substrates necessary for proliferation for cancerous cells.

Problems solved by technology

Radiation therapy, however, has its limitations.
The ionizing radiation used to ablate unwanted tissue can cause damage to surrounding healthy tissue, or may not be effective against the target tissue due to conditions such as hypoxia which makes the targeted cells radioresistent or cells being in a part of the mitotic cycle where they are not as sensitive to the effects of such radiation.
This substitution weakens the DNA chain and makes cells more susceptible to radiation and ultraviolet light.
It has also been theorized that the drug cisplatin, a chemotherapeutic drug that is known to have radiosensitizing properties, may cause damage to mitochondrial structures.
However, under such hypoxic conditions, the resulting pyruvate is not transported into the mitochondria for further processing, but rather remains in the cytoplasm where it is converted to lactate by lactic acid fermentation and expelled from the cell.
Interestingly, it has been observed for some time that even in the presence of oxygen, rapidly proliferating tumorigenic cells have a preference for inefficient anaerobic respiration and therefore utilize an abnormally high amount of glucose.
However, their usefulness as therapies for humans has been limited due to their high toxicity.
To date, there has been no drug specifically designed as a radiosensitizer that targets the mitochondria of tumorigenic tissue and cells for destruction.

Method used

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  • Glutamine-high z element compounds for treating cancer
  • Glutamine-high z element compounds for treating cancer
  • Glutamine-high z element compounds for treating cancer

Examples

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examples

[0082]Glioblastoma multiforme (GBM) tissue culture cells are tested using glutamine-linker-high Z element compounds. Various controls include: Control GBM culture cells that will receive no treatment and that will not be exposed to CST; control GBM culture cells that will receive no treatment but that will be exposed to CST; control GBM culture cells that will receive radiation without exposure to the medication and GBM culture cells that will receive radiation and will be exposed to the medication. The next step is to move to animal models with GBM and treat using the above protocol and at the same time to measure normal tissue toxicity. If permissible then the next step is to start a pilot compassionate study for patients with GBM and from there move forward to more formal studies.

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Abstract

The present invention is a glutamine compound having a non-radioisotope high Z element attached via a linker, which enters the mitochondrion and is subsequently exposed to ionizing radiation. When exposed to ionizing radiation, the present invention damages mitochondrial (as well as other) substructures such as mtDNA, the outer membrane, the inner membrane, cristae, ribosomes, etc., and causes the effective destruction of such mitochondrion. Tumorigenic cells without mitochondria cannot produce the energy they need to subsist and replicate, effectively starving them of energy and causing their destruction.

Description

[0001]This application is a by-pass, continuation-in-part application of PCT / US16 / 52603, filed on Sep. 20, 2016, which designated the U.S. This application claims priority to PCT / US16 / 52603 filed on Sep. 20, 2016, which claims priority to U.S. provisional application 62 / 221,448, filed on Sep. 21, 2015.FIELD OF THE INVENTION[0002]The present invention describes a method for the ablation of targeted tissue or cells via the administration of non-radioisotope glutamine-high Z element compounds and subsequently exposing such tissue or cells to high energy radiation, including, but not limited to, x-rays, gamma rays, microwaves, alpha particles, protons, and neutrons. More specifically, the present invention describes a method for targeting the mitochondria of the aforementioned tissue or cells for destruction, thereby starving such cells of the energy they require to proliferate.BACKGROUND[0003]Radiation therapy is usually defined as the use of high-energy radiation from x-rays, gamma ra...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K41/00A61K31/165
CPCA61K41/0038A61K31/165A61K47/542A61P35/00
Inventor SERRANO-OJEDA, PEDRO ANASTACIO
Owner SERBIG PHARMA CORP
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