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Novel treatment for hot flushes

a hot flush and treatment technology, applied in the field of medical and biomedical, can solve the problems of hot flushes, estrogen therapy is not selective for hot flushes, has several dangerous side effects, and its development has been aborted

Inactive Publication Date: 2020-05-14
DIGNITY HEALTH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes a method for treating hot flushes in a subject by administering a composition containing a transient receptor potential channel blocker, or a pharmaceutical equivalent, analog, derivative, or salt thereof. The blocker can specifically target a specific channel, such as TRPV1, which is involved in the pathophysiology of hot flushes. The composition can be administered in various ways, such as through a patch, plaster, or spray, and can be formulated as a gel, cream, or solution for topical application. The method can help to reduce the risk of thermal discomfort associated with hot flushes.

Problems solved by technology

Hot flushes are a major medical problem, which currently does not have a solution.
Estrogen therapy is not selective for hot flushes and has several dangerous side effects.
Recently, a neurokinin-3 receptor antagonist has been tested in a clinical trial for treating menopausal hot flushes in a more specific manner, but its development has since been aborted due to hepatotoxicity.

Method used

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  • Novel treatment for hot flushes
  • Novel treatment for hot flushes
  • Novel treatment for hot flushes

Examples

Experimental program
Comparison scheme
Effect test

example 1

Generally

[0065]Hot flushes (or hot flashes) constitute the most frequent complaint of postmenopausal women. There are no treatments for hot flushes other than the estrogen treatment, which treats the entire postmenopausal syndrome. Contrary to current beliefs, the inventors have disclosed that abnormal thermal discomfort is involved in this disorder.

[0066]Many TRPV1 antagonists have been synthesized and tested by multiple pharmaceutical companies as potential painkillers, but they have not been developed further due to the dangerous side effect—hyperthermia. The TRPV1 antagonist compounds that do not cause hyperthermia have reduced analgesic efficacy, as they do not block the proton mode of TRPV1 activation. Hence for inflammatory pain, these compounds would not work. In one embodiment, the inventors have disclosed that they do, however, block the heat mode. As such, TRPV1 antagonists are potential drugs to treat the abnormal heat discomfort, which takes place in hot flushes. Many s...

example 2

The TRPV1 Antagonists “Paradox”—Further Explained

[0068]As noted above and known to those of skill in the art, those TRPV1 antagonists that potently block the proton mode of activation of the TRPV1 channel (most antagonists), cause hyperthermia. Because hyperthermia by itself is likely to provoke hot flushes, these antagonists have not been the preferred compounds of choice. However, in accordance with various embodiments herein, one may still be able use them if one can decrease or prevent the hyperthermic effect (e.g., by desensitization), or for example, by administering them in such a way that they do not cause hyperthermia (e.g., applying them topically to the skin), or for example, if their desired thermal discomfort-preventing effect compensates for the adverse hyperthermic effect. These antagonists could be referred to herein as “group A.”

[0069]Further, those antagonists that do not cause hyperthermia (they do not affect the protons mode of activation) can still be effective ...

example 3

Experiments

[0072]Hot flushes are currently viewed as a normal reaction of abnormal(readily occurring) skin vasodilation. However, similar vasodilation often develops in non-estrogen-deficient individuals, both men and women, under many circumstances, such as, in a warm environment, after cold exposure, after eating spicy food, during heavy lifting, during sexual intercourse, when a person is ashamed or angry, and myriad other conditions. In some embodiments, the unpleasant general feeling of being hot (thermal discomfort) may be associated with hot flushes.

[0073]Thermal sensations are mediated by Thermo-TRP channels. There are six main warmth-sensitive channels in the skin and neurons that innervate the skin: TRPV1, TRPV2, TRPV3, and TRPV4, TRPM2, and TRPM3. TRPV1 channel is abundant on pain fibers and has a temperature threshold around 41° C. in vitro, but there is strong evidence that in vivo the threshold is lower, and that many biologically active substances can affect this thre...

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Abstract

Disclosed herein are methods for treating hot flushes in a subject. In one embodiment, treating hot flushes includes administering to a subject in need of such treatment, a therapeutically effective amount of a transient receptor potential channel (TRP channel) blocker or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods for amelioration, alleviation, or prevention of the thermal discomfort in hot flushes, comprising: selecting a subject in need of treatment for hot flushes, administering to the subject a therapeutically effective amount of a TRP channel blocker, such as a TRPV1 blocker, or a pharmaceutically acceptable salt thereof.

Description

FIELD OF THE INVENTION[0001]The present disclosure is in the medical and biomedical field.BACKGROUND OF THE DISCLOSURE[0002]All publications herein are incorporated by reference to the same extent as if each individual publication or patent application was specifically and individually indicated to he incorporated by reference. The following description includes information that may be useful in understanding the present invention. It is not an admission that any of the information provided herein is prior art or relevant to the presently claimed invention, or that any publication specifically or implicitly referenced is prior art.[0003]Hot flushes are a major medical problem, which currently does not have a solution. Current treatments target skin vasodilation, as a part of the menopausal syndrome. Estrogen therapy is currently used to treat the entire menopausal syndrome in women. Estrogen therapy is not selective for hot flushes and has several dangerous side effects. Recently, a...

Claims

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Application Information

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IPC IPC(8): A61K31/17A61K31/167A61K31/55A61K31/4725A61K9/00
CPCA61K31/4725A61K9/0014A61K31/167A61K45/06A61K31/17A61K31/55A61K31/18A61P15/12
Inventor ROMANOVSKY, ANDREJ A
Owner DIGNITY HEALTH
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