In the Nonclassical Biological Activities of Quinolone Derivatives published in Journal of Pharmacy & Pharmaceutical Sciences Vol 15, No 1 2012, it outlines why the quinolones are an excellent platform (scaffold) for modification to create new pharmaceuticals.
The Journal states “Quinolones as “privileged building blocks” with simple and flexible synthetic routes allow the production of large libraries of bioactive molecules. Because of their diversity, drug-like properties and similarities to specific targets they are considered a central scaffold to build chemical libraries with promising bioactivity potential.”(1)
As I have discussed before, the quinolone family of drugs show biological activity in three areas antibacterial, anticancer, and antiviral. Plus its scaffold, or its molecular structure, allows researchers to make structural modifications to transform from an antibacterial into an anticancer agent and/or an antiviral agent.
Since our focus is one of public safety, it behooves us to monitor the research world for the creation, testing, and ultimate release of quinolone derivatives into the marketplace. It is this author’s opinion, that anything based on the quinoline pharmacophore synthetic or not, whose history can be traced all the way back to the cinchona tree, has a unique propensity for toxic damage in the human body. A propensity not full realized or understood by researchers.
As of May, 2016 the Pew Charitable Trusts listed 37 antibiotics in clinical development. Of the 37 new antibiotics listed 6 were either fluoroquinolone or quinolone based.
Currently in Phase 1 Development
WCK2349 a novel sub-class of the quinolone benzoquinolizine fluoroquinolone levonadifloxacin
WCK771 a novel sub-class of the quinolone benzoquinolizine fluoroquinolone levonadifloxacin
Currently in Phase 2 Development
Finafloxacin a novel member of the fluoroquinolone class
Nemonoxacin a novel nonfluorinated quinolone
Currently in Phase 3 Development
Zabofloxacin a novel member of the fluoroquinolone class
Baxdela (delafloxacin) a novel member of the fluoroquinolone class
Again, it is this author’s opinion that researchers start from a flawed premise when developing quinolones. That flawed premise is that the quinolones have a good safety profile. They generally do not take into consideration factors such as delayed toxicity and mitochondrial toxicity. According to mitochondrial researchers most of the frequently prescribed fluoroquinolones are mito toxic.(2)
It is interesting to note that some of these newer quinolones are using some novel modifications to manipulate efflux pumps that are associated with bacterial resistance. It has been speculated in the past that eukaryotic efflux pumps (as opposed to bacterial efflux pumps) may play a role in adverse events.
As we know many of the supposedly safe quinolones have been removed due to toxicity issues. In addition, the ones that currently remain on the market, that are deemed safe by the FDA and the medical community, have serious safety concerns. For this reason we must stay vigilant to the release of new quinolones that have the propensity to affect public safety.
I will continue to write about these quinolones as research data becomes available.
Stayed tuned to My Quin story for updates on community related research information.
© 2009-2016 My Quin Story
These researchers have to try these medication on themselves. This is totally waste of time and resources… I find myself not taking this medication never in my life
Excellent write up. I agree this is a serious concern. Until we change the general understanding the fQA and Quinolones are generally safe, which is beginning to change slowly with the new FDA warnings, we will not have quality and effective research into new antibiotics. I believe that the toll on human health from FQA is great and currently under-recognized.
Thank you for your research on this topic.
can we get together on this. I have wasted my time on another website only to be told that I must pay to get help from the owner and her side kick. IMHO this is despicable.
Can we pool resources to help each other. I am badly affected with peripheral neuropathy following floxing. Does anyone know te triggers plese to prevent relapses.
Thank you for your awareness. I would like to see more physicians recognizing and voicing the awareness and seriousness of Fluoroquinolone toxicity and the standard of care be based on FDA warnings. That accountability for not following FDA warnings fall on both doctors & pharmacist.
Your story is similar to mine and the same year it happened and our age at the time, all the same. I feel like Big Pharma tried to take my life because of the damage done when floxed and the subsequent damage done by the drugs given to “help” with my varied symptoms. All I can do is thank God that I was able to overcome what they did and I now lead a fairly normal life, but I fought for my life for 12 years. I have permanent damage but I try not to dwell on it and make the best of what years I have left on this beautiful planet called earth.