Lakewood-Amedex Inc., a leading developer of novel anti-infective pharmaceuticals, this week announced that a recent series of in vitro studies conducted by ImQuest BioSciences of Fredrick, MD, have demonstrated that its novel class of antimicrobials, named bisphosphocins, have proven effective at killing bacterial strains carrying the NDM-1 plasmid.
These studies expand on previously published experiments demonstrating Nu-3 to be effective in killing multi-drug resistant bacteria and highlight the potential of this important new class of antimicrobials.
Specifically, the studies revealed that Nu-3 was rapidly bactericidal to NDM-1 positive Klebsiella pneumonia BAA2146 and Escherichia coli BAA2469, both of which are resistant to more than 5 classes of antibiotics, generating a greater than 5 log reduction in bacterial counts or 100% kill with a fifteen minute incubation at room temperature, which is less time than these bacteria take to replicate.
This result is significant because the unique bisphosphocin mechanism of action eliminates many of the current problems in the treatment of bacterial or fungal diseases, namely the development of microbial resistance, and can eradicate slow growing or stationary bacteria and bacterial biofilms, constantly a major problem for the medical community.
Traditional antibiotics only inhibit bacterial growth, typically through a single target molecule, thus requiring a prolonged exposure and that provides an opportunity for the bacteria to mutate and become resistant or dormant to avoid the antibiotic affecting them. In the case of bisphosphocins, the effect is directly bactericidal and does not depend on the bacteria being in a growth cycle, eliminating any opportunity for the development of resistance and increasing their potency when bacteria become dormant or form a biofilm.
The company is fast-tracking the development of a topical bisphosphocin formulation specifically because its rapid bactericidal activity makes it an excellent therapeutic candidate to address several unmet medical needs for clinical indications such as acute bacterial skin infection, infected diabetic foot ulcer, ophthalmic infections, and fungal infections such as onychomycosis. In addition, bisphosphocins exhibit an extremely broad spectrum of activity that is critical when addressing clinical indications where the infection may be polymicrobial, or with eye infections where there is no time to identify the infecting organism.
The compounds possess an excellent safety profile and are well tolerated in vivo due to their highly specific mechanism of action that exploits a critical difference between the membranes of bacteria/fungi and the membranes of mammals, including humans.