Pharmaceutical composition for treatment of the pulmonary form of altitude sickness caused by lack of oxygen and reduced air pressure

a technology of altitude sickness and pharmaceutical compositions, applied in the direction of drug compositions, peptides, peptides/protein ingredients, etc., can solve the problems of arterial pressure, high blood pressure, and individual life-threatening altitude sickness clinical condition,

Inactive Publication Date: 2019-07-11
APEPTICO FORSCHUNG & ENTWICKLUNG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The invention relates to certain peptides that have been found to have certain beneficial effects. These peptides are cyclic peptides that have a specific sequence. The patent text describes how these peptides can be made and their potential uses. The technical effect of this invention is the creation of new peptides that can be used for various purposes such as medication or skincare products.

Problems solved by technology

At least four members of the expedition suffered from altitude sickness, with one member dying on 2 Sep. 1891 at a height of 4000 m. Since these cases, altitude sickness is deemed to be an individual life-threatening clinical condition.
If untreated, the pulmonary form of altitude sickness can lead to death in less than 24 hours, with death frequently occurring through a secondary pulmonary embolism.
However, in mountainous regions, a rapid descent is often not possible.
Oxygen ventilation by e.g. bottled oxygen does indeed reduce the increased pulmonary arterial pressure, but does not normalize it.
Also, in the case of a portable hyperbaric chamber, the positive effect is only temporary.
A medicinal treatment for altitude sickness is currently only limited and controversial: Thus, dexamethasone is suggested in severe acute altitude sickness and also specifically in the cerebral form of altitude sickness.
However, it is to be noted that currently the possibility for medicinal treatment of the pulmonary form of altitude sickness is still very limited.
Furthermore, it is known that organized rescue operations can only be counted upon in the European alpine region and partly also in the North American region.
In remote high mountains of the world and in extreme altitudes, rescue operations and medical aid in emergencies (with the use of bottled oxygen or portable hyperbaric chamber) are scarcely possible.

Method used

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  • Pharmaceutical composition for treatment of the pulmonary form of altitude sickness caused by lack of oxygen and reduced air pressure
  • Pharmaceutical composition for treatment of the pulmonary form of altitude sickness caused by lack of oxygen and reduced air pressure
  • Pharmaceutical composition for treatment of the pulmonary form of altitude sickness caused by lack of oxygen and reduced air pressure

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0081]Use of the peptide with SEQ NO: 1 according to the invention for the treatment of the pulmonary form of altitude sickness.

[0082]With the present example, in an experimental rat model of altitude sickness it is shown that the aim according to the invention was achieved by the synthetic peptide according to the invention (SEQ ID NO: 1) being administered to rats suffering from the pulmonary form of altitude sickness. Physical exertion under conditions of reduced oxygen and air pressure, such as occur at high altitudes, are the 2 main factors which lead to the development of the pulmonary form of altitude sickness. Therefore, the selected rat model, in which the rats carried out physical activity under conditions of reduced oxygen and reduced air pressure, simulates a physically strenuous ascent to high altitudes. This takes place without carrying out a prior acclimatization. This corresponds to the scenario such as is to be found in the case of mountaineers who suffer from the p...

example 2

[0089]Ex vivo assessment of the pro-inflammatory characteristics of the peptide according to the invention with SEQ ID NO: 1 in human whole blood.

[0090]A pharmacological ex vivo safety study was carried out with regard to the peptide SEQ ID NO: 1 according to the invention in human full blood, in order to establish whether the peptide SEQ ID NO: 1 leads to the release of the pro-inflammatory marker interleukin-6 (IL-6) from fresh full blood (i.e. whether or not peptide SEQ ID NO: 1 shows TNF-specific inflammatory activity (i.e. TNF receptor binding activity)). In this study, fresh full blood was used; this is a recognized prediction model for the assessment of the inflammatory reaction in vivo.

[0091]Summary of the Methodology

[0092]The aim of this study was to determine the pro-inflammatory signal capacity of the peptide SEQ ID NO: 1. Here, full blood cultures were used and the secretion of interleukin-6 (IL-6), a very sensitive marker for pro-inflammatory stimulation, was quantified...

example 3

[0111]Assessment of the bioactivity of the peptide according to the invention compared with the non-cyclized (and therefore not according to the invention) form of the peptide and other synthetic peptides which have been proposed in the prior art for the treatment of oedemas, in a patch clamp assay with A549 cells.

[0112]Summary

[0113]In this example, the biological activity of the peptide according to the invention was assessed with three other synthetic peptides with regard to the capability for induction of the sodium flow. The synthetic comparative peptides were also proposed in European Patent Application EP 2 009 023 A1 as peptides for the treatment of oedemas. For these peptides, it was assumed in EP 2 009 023 A1 that they would be able to inhibit or reduce the accumulation of excess fluid in tissues. In EP 2 009 023 A1 this characteristic was investigated by means of the TEER test; within the present example, this biological activity is investigated in a whole cell patch clamp...

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Abstract

The present invention provides a method of treating and preventing altitude sickness, comprising the steps of: obtaining a peptide, wherein the peptide is 7-20 adjacent amino acids in length and comprises an amino acid sequence having a hexamer TX1EX2X3E, wherein X1, X2 and X3 can be any natural or unnatural amino acid, and wherein the peptide does not have tumor necrosis factor receptor binding activity, and wherein the peptide is cyclized; and administering to a patient having the pulmonary form of altitude sickness or being at risk of developing the pulmonary form of altitude sickness an effective amount of the peptide.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application is a continuation of U.S. patent application Ser. No. 14 / 410,642 filed on Dec. 23, 2014, which is a national stage application under 35 U.S.C. 371 of PCT / EP2013 / 062777 filed on Jun. 19, 2013 and claims foreign priority to European Patent Office (EPO) Application No. 12173983.3 filed on Jun. 28, 2012.TECHNICAL FIELD OF THE INVENTION[0002]The present invention relates to the treatment of the pulmonary form of altitude sickness caused by lack of oxygen and reduced air pressure.STATEMENT OF FEDERALLY FUNDED RESEARCH[0003]None.INCORPORATION-BY-REFERENCE OF MATERIALS FILED ON COMPACT DISC[0004]None.BACKGROUND OF THE INVENTION[0005]Altitude sickness can occur in humans from a height of over 2500 m above sea level. At a height of over 2500 metres, the oxygen concentration and the air pressure decrease considerably. A differentiation is made between cerebral and pulmonary forms of acute altitude sickness. Acute altitude sickness t...

Claims

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Application Information

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Patent Type & AuthorityApplications(United States)
IPC IPC(8): C07K7/64A61K38/19
CPCC07K7/64A61K38/191A61P11/00C07K7/08
InventorFISCHER, BERNHARDLUCAS, RUDOLFFISCHER, HENDRIK
OwnerAPEPTICO FORSCHUNG & ENTWICKLUNG