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Antibacterial drug composition for treating Gram-negative bacterial infections

A technology of gram-negative bacteria and antibacterial drugs, applied in the field of medicinal chemical pharmaceutical compositions

Inactive Publication Date: 2016-08-24
TENNOR THERAPEUTICS (SUZHOU) LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Treatment of Gram-negative bacterial infections is facing enormous challenges due to the emergence of antimicrobial resistance

Method used

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  • Antibacterial drug composition for treating Gram-negative bacterial infections
  • Antibacterial drug composition for treating Gram-negative bacterial infections
  • Antibacterial drug composition for treating Gram-negative bacterial infections

Examples

Experimental program
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Embodiment

[0029] The MIC and MBC endpoints were determined in parallel using a two-drug combination checkerboard test. TNP-2092, polymyxin B and polymyxin E had certain antibacterial activity against E. coli ATCC 25922 when tested individually (see Table 1). When using the checkerboard method to test the drug combination of different ratios of TNP-2092 and polymyxin B or polymyxin E, if the MIC is used as the test endpoint, TNP-2092 and polymyxin B or polymyxin E It has additive and synergistic effects. If MBC is used as the test endpoint, TNP-2092 has obvious synergistic effects with polymyxin B or polymyxin E (see Table 2 and figure 1 , figure 2 ). Depend on figure 1 It can be seen that the test concentration range of TNP-2092 is 0.03-2 μg / mL, the test range of polymyxin B is 0.008-8 μg / mL, and the weight ratio of TNP-2092 and polymyxin B is 0.25:0.008 to 0.03: The superimposed or synergistic effects of the two were observed in all four. Depend on figure 2It can be seen that t...

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Abstract

The invention discloses an antibacterial drug composition for treating Gram-negative bacterial infections. The composition is prepared from TNP-2092 and a cell membrane penetrant, wherein the cell membrane penetrant is polymyxin B or polymyxin E. According to the antibacterial drug composition for treating Gram-negative bacterial infections, the Gram-negative bacterial infections are treated through the combined use of TNP-2092 and the cell membrane penetrant, the antibacterial activity of the composition is enhanced compared with the use of TNP-2092 or the cell membrane penetrant alone, and the composition has an antibacterial synergistic effect and can be used for treating the Gram-negative bacterial infections, including drug-resistance bacterial infections.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical chemical pharmaceutical compositions, and in particular relates to an antibacterial pharmaceutical composition for treating Gram-negative bacterial infections. Background technique [0002] The treatment of Gram-negative bacterial infections is facing great challenges due to the emergence of antimicrobial resistance. The main clinically pathogenic Gram-negative bacteria include: Escherichia coli (E.coli), Klebsiella pneumoniae (Klebsiellapneumonia), Acinetobacter baumannii (Acinetobacter baumannii), Pseudomonas aeruginosa ), Stenotrophomonas maltophilia (S.maltophilia), Salmonella Typhi, non-typhoidal Salmonella and Shigella, etc. In common hospital-acquired infections, Klebsiella pneumoniae is a major pathogen, and carbapenem antibiotics used to be the last line of defense in the treatment of this bacterial infection. However, in some areas, more than half of Klebsiella pneumoniae infecti...

Claims

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Application Information

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IPC IPC(8): A61K38/12A61P31/04A61K31/4545
CPCA61K31/4545A61K38/12A61K2300/00A61P31/04Y02A50/30A61K31/4375
Inventor 马振坤格雷戈瑞·罗伯森王晓梅
Owner TENNOR THERAPEUTICS (SUZHOU) LTD
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