An antimicrobial peptide, its pharmaceutical composition, and its application

The novel antimicrobial peptides modified with deuteration enhance their binding affinity to β-1,3-D-glucan synthase, overcoming the limitations of existing antifungal drugs in terms of target availability and safety. This enables highly effective inhibition and safe treatment of drug-resistant Candida, making it suitable for the prevention and treatment of various infections.

CN121627830BActive Publication Date: 2026-05-26CHINA PHARM UNIV
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Patent Information

Application Number
CN202610163719.X
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2026-02-05
Publication Date
2026-05-26
Estimated Expiration
2046-02-05

AI Technical Summary

Technical Problem

Existing antifungal drugs are ineffective against fluconazole-resistant Candida, have insufficient target binding specificity, and exhibit poor in vivo stability and safety, leading to clinical treatment difficulties and an inability to effectively address the high incidence and mortality of invasive candidiasis.

Method used

Novel antimicrobial peptides were developed through deuteration modification to enhance their binding affinity to β-1,3-D-glucan synthase, improve their stability and water solubility, and design them into multiple dosage forms to cover drug-resistant strains, providing a highly effective, long-acting, and safe treatment option.

Benefits of technology

It achieves highly efficient inhibition of drug-resistant Candida, significantly broadens the therapeutic window, reduces host cell toxicity, and has the advantages of good biocompatibility, high stability, simple synthesis process, and controllable cost, making it suitable for the prevention and treatment of various infections.

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Abstract

This invention discloses an antimicrobial peptide, its pharmaceutical composition, and its applications. The invention optimizes the structure of the antimicrobial peptide through deuteration modification technology, significantly enhancing its targeted binding ability to β-1,3-D-glucan synthase. The affinity of this antimicrobial peptide for the aforementioned target is 9-27 times that of the control peptide. In vitro assays show that its minimum inhibitory concentration (MIC) against nine standard Candida strains is consistently 0.002 μg / mL, exhibiting significantly superior activity compared to fluconazole, anidoxurine, and the control peptide. It also exhibits extremely low cytotoxicity against L02 human normal hepatocytes. In in vivo experiments, in a neutropenic mouse model of Candida albicans infection, the antimicrobial peptide at all doses showed superior reduction in renal fungal load compared to anidoxurine and the control peptide. The antimicrobial peptide of this invention combines highly efficient anti-Candida activity, low cytotoxicity, and excellent in vivo efficacy, providing a safe and effective candidate drug for the treatment of drug-resistant candidiasis and possessing good clinical translational value.
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