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Use of non-peptide nk1 antagonists in a predetermined dose for the treatment of cancer

a non-peptide nk1 receptor and predetermined dose technology, applied in the field of molecular biology applied to medicine, pharmacology and oncology, to achieve the effects of reducing tumour size, preventing their development, and facilitating their disappearan

Inactive Publication Date: 2016-11-03
SERVICIO ANDALUZ DE SALUD (SAS)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention indicates that larger doses of NK1 agonists are needed to have a significant anti-tumor effect. This information is important for researchers working on developing these compounds for treatment of cancer.

Problems solved by technology

However, the known precedents, which include the use of non-peptide NK1 receptor antagonists to cause death (apoptosis) in tumour cells and the modification of the peritumoral environment by means of the induction of changes in the cells forming said environment and in the substances secreted by them, with the aim of preventing or hindering the genesis, development or progression of tumours, at present, there is controversy about the effect of the in vivo use of NK1 receptor antagonists for the treatment of cancerous tumour disease (Harford-Wrigth et al., Drug Discovery, 2013, 8, 13-23).

Method used

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  • Use of non-peptide nk1 antagonists in a predetermined dose for the treatment of cancer
  • Use of non-peptide nk1 antagonists in a predetermined dose for the treatment of cancer
  • Use of non-peptide nk1 antagonists in a predetermined dose for the treatment of cancer

Examples

Experimental program
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Effect test

example 1

Treatment with Non-Peptide NK1 Receptor Antagonists, at Doses Between 10 and 80 mg Per Kilogram of Weight and Day, Reduces the Size of Cancerous Tumours of Epithelial Cell Line (Cancers) in Mammals

[0072]To verify that the administration of the antagonists not of the NK1 receptors, at doses between 10 and 80 mg per kilogram of weight and day, reduces the sizes of epithelial cell line tumours (cancers) in mammals, tumour cells were implanted in mice and were later treated with non-peptide NK1 receptor antagonists.

[0073]Immunocompromised female mice, 5-6 weeks of age were used, nu / nu Balb / c nude mice, provided by Harlan Iberica Barcelona (Spain). They were kept at 24° C. and in sterile conditions with food and water “ad libitum”. They were injected with 2×107 tumour cells, corresponding to cancer (human lung cancer, reference HCC-44 supplied by DSMZ) in 200 μl of PBS subcutaneous route. The tumour size was measured and the mice were evaluated for their state of health and weight daily....

example 2

Treatment with Non-Peptide NK1 Receptor Antagonists, at Doses Between 10 and 80 mg Per Kilogram of Weight and Day, Reduces the Size of Cancerous Tumours of Glial Cell Line (e.g. Astrocytomas) of the Central Nervous System in Mammals

[0074]To verify that the administration of the antagonists not of the NK1 receptors, at doses between 10 and 80 mg per kilogram of weight and day, reduces the sizes of glial cell line tumours of the nervous system in mammals, tumour cells were implanted in mice and were later treated with non-peptide NK1 receptor antagonists.

[0075]Immunocompromised female mice, 5-6 weeks of age were used, in the same conditions as explained in example 1. They were injected with 2×107 tumour cells, corresponding to a glial cell line tumour of the central nervous system human (human glioma; reference GAMG; supplied by DSMZ) in 200 μl of PBS by subcutaneous route. The tumour size was measured and the mice were evaluated for their state of health and weight daily. The mice we...

example 3

Treatment with Non-Peptide NK1 Receptor Antagonists, at Doses Between 10 and 80 mg Per Kilogram of Weight and Day, Reduces the Size of Cancerous Tumours of Mesenchymal Cell Line (Sarcomas) in Mammals

[0076]To verify that the administration of the antagonists not of the NK1 receptors, at doses between 10 and 80 mg per kilogram of weight and day, reduces the sizes of glial cell line tumours of the nervous system in mammals, tumour cells were implanted in mice and were later treated with non-peptide NK1 receptor antagonists.

[0077]Immunocompromised female mice, 5-6 weeks of age were used, in the same conditions as explained in example 1. They were injected with 2×107 tumour cells, corresponding to a mesenchymal cell line tumour (human fibrosarcoma; reference HT-1080; supplied by DSMZ) in 200 μl of PBS by subcutaneous route. The tumour size was measured and the mice were evaluated for their state of health and weight daily. The mice were randomized in nine groups when the tumours reached ...

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Abstract

Use of the non-peptide NK1 receptor antagonist, preferably Aprepitant, for the treatment of cancer in predetermined doses. The present invention also describes pharmaceutical compositions comprising said agents, alone or in combination with at least one other active principle, for the treatment of cancer

Description

FIELD OF THE INVENTION[0001]The present invention is within the field of molecular biology applied to medicine, pharmacology and oncology. Specifically, it is related to the use of anti-tumour agents, more specifically non-peptide NK1 receptor antagonists, in predetermined doses, for the manufacturing of medicaments of use in the treatment of cancer in mammals and, more preferably, in humans.BACKGROUNDS OF THE INVENTION[0002]NK1 receptors (neuropeptide receptors of Substance P and tachykinins), are widely distributed in the organism's cells. Their presence has been verified in the central and peripheral nervous system of mammals, in the digestive apparatus, in the circulatory system, in haematopoietic and inflammatory and / or immune response cell lines cells, as well as in soft tissues and especially in vascular endothelium. Numerous biological processes are currently known in which regulation NK1 receptors are involved.[0003]Substance P (SP), is the preferred agonist of the NK1 rece...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/5377A61K33/24A61K33/243
CPCA61K33/24A61K31/5377A61K45/06A61P35/00A61K33/243A61K2300/00
Inventor SALINAS MARTIN, MANUEL VICENTE
Owner SERVICIO ANDALUZ DE SALUD (SAS)
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