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Antibacterial Use of Halogenated Salicylanilides

a technology of halogenated salicylanilides and antibacterial properties, which is applied in the field of halogenated salicylanilides, can solve the problems of ineffective or unsatisfactory treatment of mammal, and achieve the effect of reducing the appearance rate of spontaneous resistant mutants

Inactive Publication Date: 2017-09-14
UNION THERAPEUTICS AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes the discovery of halogenated salicylanilides, specifically closanthel, rafoxanide, oxyclozanide, and niclosamide, which are effective at treating infections caused by Gram-positive bacteria, such as staphylococcus and streptococcus. These compounds are also effective in reducing the development of resistance bacteria. The patent explores the potential use of these compounds in treating various diseases or infections, including those caused by MRSA. The halogenated salicylanilides can be applied topically to the affected area to decolonize the subject and prevent the spread of infection. Overall, the patent provides a valuable resource for developing new treatments for Gram-positive bacterial infections.

Problems solved by technology

Many bacteria are resistant to, or rapidly develop, resistance against antibiotic agents and thus it is undesirable or ineffective to treat a mammal suffering from a topical bacterial disease or infection caused by bacteria that are resistant to the antibiotics.

Method used

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  • Antibacterial Use of Halogenated Salicylanilides
  • Antibacterial Use of Halogenated Salicylanilides
  • Antibacterial Use of Halogenated Salicylanilides

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0147]Experimental tests were conducted to determine the antibacterial activity and the mutation rate conferring resistance for halogenated salicylanilides and reference compounds.

Microorganisms

[0148]Chosen for its relevance regarding bacterial skin infections, the methicillin-resistant S. aureus (MRSA) 01 strain was used as the primary test microorganism. This strain is a community-acquired MRSA clinical isolate of USA 300 type, from a skin abscess.

[0149]Twenty-one other MRSA and methicillin-sensitive S. aureus strains, and 4 Streptococcus pyogenes strains, were also included in the study (Table 1). These covered fusidic acid- and mupirocin-resistant strains, these two types of resistance being of clinical relevance.

[0150]Strains were conserved in Luria Bertani (LB) Broth (S. aureus) or Brain Heart Infusion (BHI) (S. pyogenes) supplemented with glycerol 15% (v / v) at −80° C., and reactivated by isolation on LB (S. aureus) or BHI (S. pyogenes) agar plates. Strains were cultivated in ...

experiment 1

[0167]Sample 5.—Niclosamide (N) 5% modified basis creme with higher lipid content—Lipocreme—according to the description in Danske Laegemiddelsstandarder (DLS).

[0168]2.25 g niclosamide was mixed with 47.75 g créme prepared according to Danske Laegemiddels-standarder (DLS) (see FIG. 3).

Oil phase:Polysorbate 80 10 gCetostearyl alcohol100 gParaffin oil100 gGlycerol monostearate 40-50120 gWater phase:Methyl parabenzoate 1 gGlycerol 85% 40 gSorbitol 70 gWater Milli-Q724 g

Results and Conclusions

Microbiology: MIC & Kill Curves—FIGS. 1&2 and Tables 2 and 3

[0169]

TABLE 2in-vitro susceptibility of S. aureus clinical isolates and S. aureusATCC 29213 reference strain.MIC (μg / ml)S. aureus strainsNewman0.2MRSA 010.4MRSA 020.2MRSA 03*0.4MRSA 040.4MRSA 050.2MRSA 060.4MRSA 070.2MRSA 08*0.4MRSA 090.2MRSA 100.4MRSA 110.1EEFIC 01*0.4EEFIC 02*0.2MRSA 12*0.4MRSA 13*0.4MSSA 01*0.4MSSA 02*0.4MRSA 14*0.4MRSA 15*0.2MRSA 16*0.2MRSA 17*0.2S. pyogenes strains013.2CCUG 255713.2ATCC 196153.2ATCC 123851.6

TABLE 3The...

example 2

[0179]Additional More Extensive Screen of Clinical Isolates Performed with Niclosamide.

Methods

Microorganisms

[0180]Chosen for its relevance regarding bacterial skin infections, the methicillin-resistant S. aureus (MRSA) 01 strain was used as the primary test microorganism. This strain is a community-acquired MRSA clinical isolate of USA 300 type, from a skin abscess.

[0181]Two-hundred-four other MRSA and methicillin-sensitive S. aureus strains, and 4 Streptococcus pyogenes strains, were also included in the study. These covered fusidic acid- and mupirocin-resistant strains, these two types of resistance being of clinical relevance.

[0182]Strains were conserved in Luria Bertani (LB) Broth (S. aureus) or Brain Heart Infusion (BHI) (S. pyogenes) supplemented with glycerol 15% (v / v) at −80° C., and reactivated by isolation on LB (S. aureus) or BHI (S. pyogenes) agar plates. Strains were cultivated in Mueller Hinton (MH) Broth—cation adjusted (S. aureus) or BHI (S. pyogenes). All strains we...

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Abstract

The invention relates to a halogenated salicylanilide selected from closantel, rafoxanide, oxyclozanide and niclosamide and derivatives thereof including salts, hydrates, esters and the like for use in the topical treatment or prevention of infections caused by Gram-positive bacteria such as Staphylococcus, in particular Staphylococcus aureus, and Streptococcus, in particular Streptococcus pyogenes. Gram positive bacteria treated with the halogenated salicylanilides exhibit a very low frequency of appearance of resistant mutants compared to commonly used topical antibiotics.

Description

FIELD OF INVENTION[0001]The invention relates to the halogenated salicylanilides closantel, rafoxanide, oxyclozanide or niclosamide and derivatives thereof including salts, hydrates, esters for use in the topical treatment or prevention of conditions caused by Gram positive bacteria such as Staphylococcus, in particular Staphylococcus aureus, and Streptococcus, in particular Streptococcus pyogenes. The halogenated salicylanilides have a surprisingly low frequency of appearance of resistant mutants in said strains compared to commonly used topical antibiotics. Also provided are topical formulations comprising a halogenated salicylanilide.BACKGROUND OF THE INVENTION[0002]Today, there are many different classes of antibiotics available to medical practitioners. However, many of the bacteria that these antibiotics are designed to treat are quickly developing resistance to drugs in all classes. Unfortunately the large pharmaceutical companies have limited there research in finding new an...

Claims

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Application Information

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IPC IPC(8): A61K31/609
CPCA61K31/609A61K9/0014A61K9/0043A61K9/06A61K47/10A61K47/14A61K47/26A61P17/00A61P31/04
Inventor DELAVENNE, EMILIE FLORA AURORESIMON, DANIEL JEAN JACQUESSOMMER, MORTEN OTTO ALEXANDERTOFT-KEHLER, RASMUS VENDLER
Owner UNION THERAPEUTICS AS
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