PolyMedix's defensin-mimetic antimicrobial compounds show both anti-inflammatory and antimicrobial activity against bacteria which cause oral infections.
PolyMedix, Inc. (OTC BB: PYMX), an emerging biotechnology company focused on developing new therapeutic drugs to treat infectious diseases and acute cardiovascular disorders, announced that data from two separate pre-clinical research studies were published in the December issue of Molecular Oral Microbiology. The data demonstrated that PolyMedix's investigational defensin-mimetic compounds exhibited both anti-inflammatory and antimicrobial activity against microbial biofilms that cause infections of the oral cavity. This is the first scientific publication of the discovery of anti-inflammatory activity with PolyMedix's defensin-mimetic compounds.
Inflammation and formation of biofilms are believed to be important components of many oral infections. PolyMedix believes that its defensin-mimetic compounds, which combine anti-inflammatory as well as anti-biofilm properties together with antimicrobial effects, could potentially provide important benefits, that other antibiotic agents may not possess, for the treatment of oral infections.
"Several of our defensin-mimetic antimicrobial compounds have demonstrated, in pre-clinical research studies, promising activity against fungi such as Candida that can cause infections of the oral cavity," commented Dr. Richard Scott, Vice President of Research at PolyMedix. "Resistance has developed to current treatments used for these infections, creating an important need for a new treatment where resistance is less likely to develop. We believe our small molecule defensin- mimetic compounds represent a novel approach to developing new agents to treat these painful infections which sometimes can be life-threatening, with the important potential advantage of limited opportunity for the development of resistance."
PolyMedix's small molecule defensin-mimetic antimicrobial compounds are designed to mimic human host defense proteins, the body's natural defense against bacterial infections. Human host defense proteins use a simple but effective method for killing bacteria and other microbes by directly targeting the microbial membranes and disrupting them. This mechanism of action makes it difficult for resistance to develop.
The following research studies were published:
Hua, J., Yamarthy, R., Felsenstein, S., Scott, R.W., Markowitz, K., and Diamond, G. "Activity of Antimicrobial Peptide Mimetics in the Oral Cavity: I. Activity against Biofilms of Candida Albicans." Molecular Oral Microbiology 25 (2010): 418-425.
In this study, several series of PolyMedix's antimicrobial defensin-mimetics were screened against oral Candida strains as proof-of-principle test of their antifungal properties. Candida is a yeast fungus that grows as a biofilm on the bioprosthetic materials used to make dentures. Candida also causes oral candidiasis, a common infection of the oral cavity. The results demonstrated that several of PolyMedix's defensin-mimetic compounds exhibited potent antifungal activity against Candida species, in both biofilms formed on denture material, and in the presence of saliva.
Hua, J., Scott, R.W., and Diamond, G. "Activity of Antimicrobial Peptide Mimetics in the Oral Cavity: II. Activity against Periopathogenic Biofilms and Anti-inflammatory Activity." Molecular Oral Microbiology 25 (2010): 426-432.
In this study, PolyMedix's antimicrobial defensin-mimetics were screened against the microbial pathogens associated with periodontal diseases. Periodontal disease is caused by colonization of pathogenic bacteria such as Porphyromonas gingivalis and Aggregatibacter actinomycetemcomitans, which results in an inflammation that occurs in response to this colonization and invasion. Metabolic assays as well as culture and biomass measurement assays were used to determine if PolyMedix's defensin-mimetics were active against these two bacterial species associated with periodontitis. The results demonstrated that PolyMedix's defensin-mimetics exhibited potent activity against biofilm cultures of both Porphyromonas gingivalis and Aggregatibacter actinomycetemcomitan. In addition, for the first time, an anti-inflammatory response was seen through a reduction in activation of nuclear factor-ÎºB.
The research described above was supported by Grant Award Number R44DE018371 from the National Institute of Dental & Craniofacial Research. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institute of Dental & Craniofacial Research or the National Institutes of Health.
About Molecular Oral Microbiology
Molecular Oral Microbiology publishes high quality research papers and reviews on fundamental or applied molecular studies of microorganisms of the oral cavity and respiratory tract, host-microbe interactions, cellular microbiology, molecular ecology, and immunological studies of oral and respiratory tract infections.
About PolyMedix, Inc.
PolyMedix is a publicly traded biotechnology company focused on the development of novel drugs for the treatment of serious infectious diseases and acute cardiovascular disorders. PolyMedix uses a rational drug design approach to create non-peptide small molecule drug candidates. PolyMedix's lead antibiotic compound, PMX-30063, is currently in Phase 2 clinical trials. PMX-30063 is a small molecule that mimics the mechanism of action of human host defense proteins, a mechanism that is distinct from currently approved antibiotic drugs and is intended to make bacterial resistance unlikely to develop. PolyMedix plans to develop this compound for serious systemic Staphylococcal infections, including methicillin resistant Staphylococcus aureus (MRSA). PolyMedix's lead heptagonist compound, PMX-60056, has completed Phase 1 testing and is being developed to reverse the anticoagulant activity of both heparin and low molecular weight heparins (LMWH). PolyMedix believes that PMX-60056 could potentially be a safer and easier to use anticoagulant reversing agent, with broader activity, than the currently approved therapy for reversing heparin and LMWH. In addition to its small molecule therapeutics, PolyMedix has polymeric formulations with the same mechanism of action as PMX-30063, PolyCides™, which are intended for use in antimicrobial biomaterials applications such as additives to paints, plastics, and textiles to create self-sterilizing products and surfaces. For more information, please visit our website at www.polymedix.com.