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Potentiation of antibiotic activity by a novel cationic peptide, spr741

An antibiotic, effective dose technology, applied in the direction of organic active ingredients, resistance to vector-borne diseases, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2019-02-05
我希望增效剂公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, their systemic (i.e., nontopical) use is largely limited to the treatment of life-threatening diseases caused by multidrug-resistant strains of Pseudomonas aeruginosa and Acinetobacter baumannii and carbapenem-resistant Enterobacteriaceae. Infect

Method used

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  • Potentiation of antibiotic activity by a novel cationic peptide, spr741

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Experimental program
Comparison scheme
Effect test

Embodiment approach

[0018] The present disclosure includes a method of treating a bacterial infection in a subject comprising administering to the subject a therapeutically effective amount of SPR741 in combination with an antibiotic selected from the group consisting of retapalene, telithromycin, aztreonam, and combinations thereof.

[0019] In certain embodiments, the bacterial infection is an E. coli infection, a Klebsiella pneumoniae infection, or an Acinetobacter baumannii infection.

[0020] The present disclosure includes the following embodiments, in which:

[0021] (1) The antibiotic is retapalene.

[0022] (2) The antibiotic is telithromycin.

[0023] (3) The antibiotic is aztreonam.

[0024] (4) The subject is a mammal.

[0025] (5) The subject is a human patient.

[0026] (6) Retapalene is administered as a topical formulation containing SPR741 and less than 1 mg of retapalene per gram of formulation.

[0027] (7) Oral administration of telithromycin, 10 mg to 300 mg, or 10 mg to...

Embodiment 1

[0035] Example 1. Efficacy Evaluation of Combinations of SPR741 and Certain Antibiotics

[0036] SPR741 and azithromycin (AZ), aztreonam (AZT), clarithromycin (CLR), fusidic acid (FA), meropenem (MEM), mupirocin (MUP), rifampicin (RIF) and The efficacy of the combination of retapalene (RET) was assessed using a susceptibility testing method based on CLSI guideline M7-A10. Test against 25 Escherichia coli (Ec), 25 Klebsiella pneumoniae (Kp) and 17 Baumannii Acinetobacter (Ab) MDR and clinical isolates were performed. The minimum inhibitory concentration (MIC) is defined as the lowest concentration of antibiotic required to inhibit visible bacterial growth. MIC values ​​were determined for each antibiotic / SPR741 combination and the greatest reduction in MIC of the antibiotic in the combination was determined.

[0037] Combination with SPR741 resulted in potentiation of test antibiotics against isolates of Ab, Ec and Kp. For Ab, synergy follows the order FA>RIF>CLR>RET>MEM>AZ...

Embodiment 2

[0038] Example 2. Evaluation of the efficacy of SPR741 in combination with certain antibiotics in a checkerboard assay

[0039] Evaluate power in a checkerboard test. The minimum inhibitory concentration (MIC) of SPR741, antibiotics and their combination was defined as the lowest concentration that inhibited the growth of Ec ATCC 25922, Ab NCTC 12156 and Kp ATCC 43816. Ec BW25113, ΔtolC and ΔacrA were used to evaluate the contribution of the multi-drug efflux pump AcrAB-TolC to the drug susceptibility of the combination. For each combination in which the MIC differs from the compounds in the isolate, the interaction is assessed by calculating the Fractional Inhibitory Concentration Index (FICI). Interactions were defined as: FICI >4, antagonism; 0.5 to 4, no interaction; <0.5, synergy. The minimum bactericidal concentration of each combination in the presence of 5% surfactant (Survanta) was also determined.

[0040] Of the 22 antibiotics tested, 7 antibiotics, azithromycin, c...

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Abstract

This disclosure provides a method of potentiating the efficacy of certain antibiotics by administering a therapeutically effect amount of the antibiotic in combination with SPR741. In certain embodiments the antibiotic is retapamulin, telithromycin, or aztreonam. The disclosure also provides a method of treating a bacterial infection by administering SPR741 in combination with a second antibioticand pharmaceutical compositions comprising SPR741 and a second antibiotic.

Description

[0001] Citations to related applications [0002] This application claims priority to US Provisional Application No. 62 / 336,177, filed May 13, 2016, the entire contents of which are incorporated herein by reference. Background technique [0003] Gram-negative bacteria cause greater than 40% of all septic infections, and many Gram-negative bacteria are resistant to multiple antibiotics. Gram-negative bacteria have lipopolysaccharide as a component of the outer membrane, which inhibits the diffusion of many antimicrobial agents deeper into the cell where their ultimate target is located. Many antibacterial agents that are effective against Gram-positive bacteria lack activity against Gram-negative bacteria. [0004] Polymyxins are a group of closely related antibiotic substances produced by strains of Paenibacillus polymyxa and related organisms. These cationic drugs are relatively simple peptides with a molecular weight of about 1000. Polymyxins, such as polymyxin B, are dec...

Claims

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Application Information

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IPC IPC(8): A61K38/12A61K31/427A61K31/46A61K31/7048A61P31/04
CPCA61K31/427A61K31/46A61K31/7048A61K38/12A61P31/04A61K31/439Y02A50/30A61K2300/00A61K9/0014A61K9/0019
Inventor 特罗伊·利斯特
Owner 我希望增效剂公司
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