in

New Pfizer drug and ivermectin

New Pfizer antiviral and ivermectin, a pharmacodynamic analysis

New Pfizer antiviral, PF-07321332, C₂₃H₃₂F₃N₅O₄

PF-07321332 is designed to block the activity of the SARS-CoV-2-3CL protease,

https://www.pfizer.com/news/press-release/press-release-detail/pfizers-novel-covid-19-oral-antiviral-treatment-candidate

So, what is a protease?

So what is a protease inhibitor?

And, what is 3CL?

Chymotrypsin-like protease (3CL main protease, or 3CL Mpro)

Identification of SARS-CoV‑2 3CL Protease Inhibitors by a Quantitative High-Throughput Screening (3rd September 2020)

https://pubs.acs.org/doi/abs/10.1021/acsptsci.0c00108#

The activity of the anti-SARS-CoV-2 viral infection was confirmed in 7 of 23 compounds

Microscopic interactions between ivermectin and key human and viral proteins involved in SARS-CoV-2 infection

https://pubs.rsc.org/en/content/articlehtml/2021/cp/d1cp02967c

the strength and persistency of the interaction between IVE and the binding site of 3CLpro indicate that a partial inhibition of the catalytic activity could have place as the drug interacts with the main subdomains that define the enzyme binding pocket:

Identification of 3-chymotrypsin like protease (3CLPro) inhibitors as potential anti-SARS-CoV-2 agents

https://www.nature.com/articles/s42003-020-01577-x

as shown in Fig. 4, out of 13 OTDs only ivermectin completely blocked ( more than 80%) the 3CLpro activity at 50 µM concentration.

Development, validation, and approval of COVID-19 specific drugs takes years. Therefore, the idea of drug repositioning, also known as repurposing, is an important strategy to control the sudden outbreak of life-threatening infectious agents that spread rapidly.

Ilimaquinone (marine sponge metabolite) as a novel inhibitor of SARS-CoV-2 key target proteins in comparison with suggested COVID-19 drugs: designing, docking and molecular dynamics simulation study

https://pubs.rsc.org/en/content/articlehtml/2020/ra/d0ra06379g

From the docking analysis, ivermectin showed the highest docking score with an average energy of −8.5 kcal mol−1 among all the compounds. Remdesivir showed the lowest binding energy and highest docking score of −9.9 kcal mol−1

https://bnf.nice.org.uk/medicinal-forms/remdesivir.html

Ritonavir, C37H48N6O5S2

Ivermectin, C48H74O14

Exploring the binding efficacy of ivermectin against the key proteins of SARS-CoV-2 pathogenesis: an in silico approach

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7996102/

We have documented an intense binding of both ivermectin B1a and B1b isomer to the main protease with subsequent energy (ETot-) values of -384.56 and -408.6.

PF-07321332 is designed to block the activity of the SARS-CoV-2-3CL protease,

https://www.pfizer.com/news/press-release/press-release-detail/pfizers-novel-covid-19-oral-antiviral-treatment-candidate

Risk of virus developing resistance to PF-07321332

Molecular Docking Reveals Ivermectin and Remdesivir as Potential Repurposed Drugs Against SARS-CoV-2

https://www.frontiersin.org/articles/10.3389/fmicb.2020.592908/full

With SARS-CoV-2 S Spike protein

Ivermectin showed high binding affinity to the viral S protein as well as the human cell surface receptors ACE-2 and TMPRSS2.

In agreement to our findings, ivermectin was found to be docked between the viral spike and the ACE2 receptor

Binding Interactions of Selected Drugs With Human TMPRSS2 Protein (ACE2 protein)

The docking results revealed that ivermectin showed the highest binding affinity to the active site of the protein (MolDock score −174.971) and protein–ligand interactions

Binding Interactions of Selected Drugs With Human ACE-2 Protein

that ivermectin showed the highest binding affinity to the active site of the protein (MolDock score −159.754) and protein–ligand interactions

With SARS-CoV-2 S Glycoprotein

Ivermectin showed the highest binding affinity to the predicted active site of the protein

With SARS-CoV-2 Nsp14 Protein

ivermectin showed the highest binding affinity (MolDock score −212.265) and protein–ligand interactions

Binding Interactions of Selected Drugs With SARS-CoV-2 PLpro

Ivermectin showed the highest binding affinity to the predicted active site of the protein (MolDock score −180.765) and protein–ligand interactions

A brief message to world leaders

Come on ya all

Written by Dr. John Campbell

Hello Everyone,My name is John Campbell and I am a retired Nurse Teacher and A and E nurse based in England. I also do some teaching in Asia and Africa when time permits. These videos are to help students to learn the background to all forms of health care. My PhD focused on the development of open learning resources for nurses nationally and internationally.

Comments

Leave a Reply
  1. If big pharma can't make money from ivermectin, then MPs can't make money from ivermectin. Go figure. 😬

    I also love Dr John's dry passive aggressive humour.

  2. Dear John, tremendous work you did.
    Proofing that Pfizer just used the no-patented technique of Ivermectin, simplified it and possibly opened a door for future „new generation medication“ launch as soon as new forms of CoV-2 found the way to overcome this only 1 action mechanism. All this to multiply their revenues.

    Of course first the „simple“ and cheap original (Ivermectin) had to be blamed as useless and nonsense to prepare the market for the horribly expensive „new“ breakthrough method in curing Covid patients.
    Shame on the firm and shame on all authorities, politicians and so called scientific experts that follow this strategy.

  3. I notice you never once suggested that anyone should get vaccinated in your report. This discussion has its place, but the way you’ve presented it is contributing to anti-vax idiocy and conspiracy theory mania, it seems to me. Are you working toward public health or click-baiting at everyone’s expense?

  4. It all makes sense now…I knew media was spooking people away from a relatively safe and cheap cure cuz POS big pharma couldn’t make money out of it. I fkn knew it! These folks are beyond abhorrent and repulsive! 🙈😤🤮

  5. The fact that this is clearly available information particularly in the biochemistry community makes the governments opposition to using ivermectin criminal. Somebody needs to go to jail for all the people who died without this drug when it could have saved their life.

  6. I see two groups of doctors. One says no treatment for c so wait at home until deathly ill then go to hospital and die on ventilator since you didn't get jab this is ur punishment. Other doctor,get on ivermectin asap and steroid and zpak. Guess which group recovers. I am a pharmacist and have seen results of both groups. Many deaths in first group.

  7. You are not funny, just a fool, some of the time. BS into computer BS out. Same as climate change, we are all in for a very expensive ride with all these fools ideas at how to SAVE us all from the weather, this is the next BS coming down the tubes.

  8. IVERMECTIN could have saved and can still save how many people yet. Why do you think the virus is low in countries where they take it to stop eye disease. If we had only known! I feel many deaths could have been stopped if we had not listened to all these (fools) experts. Greed is my last word, so sad.

  9. Here's some phrases and words that can be used for people that trust the vaccine and everything the government says but you still want to sound like a critical thinker:
    Studies have shown, double blind, peer reviewed, 97 percent of scientists say, placebo, without vaccines we would still have polio… Try these if you blindly trust the government but wanna sound smart

  10. This is such a sad case of corruption and un-restrained capitalism. It's almost like some kinda virus or demonic possession making the the State work against its citizens. Cancer also fits. Citizens United is one of the nails in our coffins.

  11. Let me get this straight … you people believe that there is a massive conspiracy to stop all information showing that ivermectin works from reaching the public. So they have enough control to stop powerful institutes from talking, but this guy and others can get "the message" out on YT. SMH

  12. I wonder why, as someone with a philosophy degree, pots here to sway the public rather than in legitimate peer review? Is it to avoid the critical views or is it nefarious and you are trying to profit off covid misiniformation?

  13. Monoclonal Antibodies, Nicotinamide Adenine Dinucleotide or NAD, and Ivermectin have been and are proven to be successful in treating the virus without any significant side effects.
    Why do we need to rush in and vax everyone including kids with something that isn't a cure?

  14. Thank you for this, Dr.. I’m still somewhat on the fence here (as a total layman & ignorant of the topic). It is to my understanding that the effective dose for fighting sars-cov2 is toxic/possibly deadly. At least that’s what the study purportedly found in vitro?

Leave a Reply

Your email address will not be published. Required fields are marked *

Loading…

0