Endotoxin and Withdrawn Drug Trovafloxacin
As a Fluorocarbon chemist, I avoid ingesting any drug with a Fluorine atom attached. How do differences in structure affect Lethality and Synergy with Endotoxin?
I came across an interesting paper about Pfizer’s Trovafloxacin which has this structure.
This drug was withdrawn due to many cases of Fatal Liver damage.12
Pfizer owned an expired patent on improved synthesis of this drug and a series of patents on its use.3
Human volunteers took Radioactive Trovafloxacin
I am amazed that people roll up their sleeves to be injected with all manner of things.
Here is the use of radioactive 18F substituted Trovaloxacin in Human volunteers showing the drug reached every organ using PET imaging.4
Endotoxin and Trovafloxacin Liver Damage
Clever work by Shaw and coworkers showed details of epigenetic changes due to Trovafloxacine by itself and in combination with Endotoxin from Eschericia coli serotype O55:B5 (Sigma Chemical Co., Lot 075K4038).5
They measured increased Interleukin (IL)-18, which directly induces IFN-γ production, finding both cytokines were selectively increased by Endotoxin alone and together with Trovafloxacine. Note that Veh = Saline.
The combination also increased Alanine Aminotransferase expression and resulted in 2,156 gene expression changes.
Sadly Shaw and coworkers did not investigate free Fluoride ion liberation from Trivafloxacin, which is a powerful Liver poison.
How much free Fluoride is liberated in the Human body from Trovafloxacin?
The Pfizer patent chemist hints at its light sensitivity, which is likely to lead to photon assisted defluorination.
Now briefly compare the strucure of Trovafloxacin that with Levofloxacin that is on the WHO list of “Essential Medicines” despite its horrendous list of Adverse Reactions.6 Shaw et al. found that Levofloxacin was not as toxic in their experiments. That is to be expected because Levofloxacin is not defluorinated except under forcing conditions.
Ozone Defluorination of Levofloxacin
How much free Fluoride is liberated in the Human body from Levofloxacin?
Fluoride ions liberated by Ozone defluorination of Levofloxacin inhibit E. coli growth.7
February 2024 Update
Peter McCullough still recommends the Fluorinated aromatic drug that is one component of Paxlovid.8
The company Dynamic42 developed a microchip to replace animal testing of Liver toxicity to compare damage to that organ by Trovafloxacin and Levofloxacin.9 Their results were published in August 2023.10
The Pfizer corruption in the Trovafloxacin trials has been covered well in Wikipedia11 and in mainstream media, with just a few selected article links here.
The Washington Post.12
BBC News.13
Forbes.14
The Guardian.15
https://en.wikipedia.org/wiki/Trovafloxacin
Mandell L and Tillotson G. 2002. Safety of fluoroquinolones: An update. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2094848/
Pfizer https://patents.google.com/patent/US5164402
Fischman AJ, et al. 1998. Pharmacokinetics of [18F]Trovafloxacin in Healthy Human Subjects Studied with Positron Emission Tomography. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC105732/
Shaw PJ, et al. 2009. Coexposure of Mice to Trovafloxacin and Lipopolysaccharide, a Model of Idiosyncratic Hepatotoxicity, Results in a Unique Gene Expression Profile and Interferon Gamma–Dependent Liver Injury. https://academic.oup.com/toxsci/article/107/1/270/1660370
https://en.wikipedia.org/wiki/Levofloxacin
Ling W, et al. 2018. Ozonation of norfloxacin and levofloxacin in water: Specific reaction rate constants and defluorination reaction. https://www.sciencedirect.com/science/article/abs/pii/S0045653517320490
Trifluoroacetate from Pfizer Nirmatrelvir
Pfizer say, since their jabs don’t work, take 2 pills to reduce your chances of Covid19 Death. They sell packages of pink and white pills to be taken together. 77.3% of those who take these pills suffer Adverse events.Geoff Pain PhD is a reader-supported publication. To receive new posts and support my work, consider becoming a free or paid subscriber.
https://dynamic42.com/assessment-of-drug-induced-liver-injury/
Tim Kaden, Katja Graf, Knut Rennert, Ruoya Li, Alexander S. Mosig and Martin Raasch. 2023. Evaluation of drug-induced liver toxicity of trovafloxacin and levofloxacin in a human microphysiological liver model. https://www.nature.com/articles/s41598-023-40004-z
https://en.wikipedia.org/wiki/Abdullahi_v._Pfizer,_Inc.
Joe Stephens. 2001. Doctors Say Drug Trial's Approval Was Backdated http://news.bbc.co.uk/2/hi/africa/6768799.stm
Senan Murray. 2007. Anger at deadly Nigerian drug trials. http://news.bbc.co.uk/2/hi/africa/6768799.stm
Nicole Perlroth. 2008. Pfizer's Nigerian Nightmare. https://www.forbes.com/forbes/2008/1208/066.html?sh=6e19c61a23a7
David Smith. 2011. Pfizer pays out to Nigerian families of meningitis drug trial victims. https://www.theguardian.com/world/2011/aug/11/pfizer-nigeria-meningitis-drug-compensation
What The Fluoride? I never knew that one of the quinolone antibiotics had THREE organic Fs in its structure. Seems they bring out a new quinolone every couple of years, saying that the newest ones "have no recognized side effects", this because the drug has not yet been used!!! Just like NSAIDs where Cl has been used instead. Yes the latter works, but the profiles of such NSAIDs are less safe.
Fascinating. Thank you .