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New type of flu drug now available - takes one day to work

JacksinPA

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https://www.nejm.org/doi/full/10.1056/NEJMoa1716197

Baloxavir Marboxil for Uncomplicated Influenza in Adults and Adolescents

Abstract
BACKGROUND

Baloxavir marboxil is a selective inhibitor of influenza cap-dependent endonuclease. It has shown therapeutic activity in preclinical models of influenza A and B virus infections, including strains resistant to current antiviral agents.
==============================================
This new drug from a Japanese pharma company works differently than current flu drugs. It inhibits the enzyme in the flu virus that it needs to replicate. Knocks down the flu in a couple of days rather than a week with current drugs. Even works on flu strains that have developed resistance to current anti-flu drugs.

As shown on a map on TV last night, the flu is here & is spreading.

The molecule is shown in the graphic. As shown, it is called a prodrug. The part shown in red is clipped off once inside a cell to produce the active drug.

Baloxavir marboxil.jpg

https://www.xofluza.com/hcp/why-xof...ZtMfO6Ma_If_A5gmy4RoC_gwQAvD_BwE&gclsrc=aw.ds
 
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haymarket

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My wife and I never get flu shots and are both over 65. And the last time either one of us got the flu is at least a decade ago. We have friends who always get a flu shot and are fanatics about it. Both recently had the flu - one a pretty severe case.
 

JacksinPA

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My wife and I never get flu shots and are both over 65. And the last time either one of us got the flu is at least a decade ago. We have friends who always get a flu shot and are fanatics about it. Both recently had the flu - one a pretty severe case.

As an adult I have only had the flu once. My wife at the time got it also. We could not get out of bed for several days. Bad. But that was many years ago & I did not think of getting vaccinated.

This new drug treats the flu once you've come down with it. It is not prophylactic like the vaccine.
 

haymarket

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As an adult I have only had the flu once. My wife at the time got it also. We could not get out of bed for several days. Bad. But that was many years ago & I did not think of getting vaccinated.

This new drug treats the flu once you've come down with it. It is not prophylactic like the vaccine.

Thanks for explaining that. I saw the diagram and immediately just did the usual "flu shot" post.
 

Hawkeye10

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In the phase III trial, median time to alleviation of symptoms was 53.7 hours (95% CI 49.5-58.5) for patients on baloxavir versus 80.2 hours (95% CI 72.6-80.1, P<0.001) for patients on placebo, reported Frederick G. Hayden, MD, of the University of Virginia School of Medicine in Charlottesville, and colleagues
https://www.medpagetoday.com/infectiousdisease/uritheflu/74940

Is this worth $180 to you?

Not to me.
 

JacksinPA

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Thanks for explaining that. I saw the diagram and immediately just did the usual "flu shot" post.

Only one dose needed. A pill, not an injection.

Complicated molecule. Expensive to produce. But still a lot cheaper than current drug from Roche.
 

Keridan

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JacksinPA

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Thanks for explaining that. I saw the diagram and immediately just did the usual "flu shot" post.

I had to go through hundreds of molecules illustrated in the Shionogi patent to verify the structure of the drug, then drew it using my ChemDraw organic chemical CAD program.
 

JacksinPA

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If I will miss more than one day of work (Worth roughly $250), it is well worth it to me. To some others, it may not be. Seems to me the ones who spent (b/m)illions in research get to decide what they price it at. Then the public decides what is worth it to them.

It's still a lot cheaper than the current Roche drug (now a generic) & works a lot quicker. One dose & you're right as rain in a few days compared to a week with the old drug.
 

Hawkeye10

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If I will miss more than one day of work (Worth roughly $250), it is well worth it to me. To some others, it may not be. Seems to me the ones who spent (b/m)illions in research get to decide what they price it at. Then the public decides what is worth it to them.

Denying people the good works of civilization by the practice of ripping people off is one that you should reconsider your support for.

This is bad for us all the way around, both individually and collectively.
 

Keridan

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Denying people the good works of civilization by the practice of ripping people off is one that you should reconsider your support for.

This is bad for us all the way around, both individually and collectively.

Denying a company the results of taking risks on innovations that change the world is something you should consider, both individually and collectively.
 

Hawkeye10

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Denying a company the results of taking risks on innovations that change the world is something you should consider, both individually and collectively.

If they are not willing to do things on a reasonable cost basis I say **** them, privatize their asses.....then hand off the operation to a newly formed non profit NGO.
 

Keridan

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If they are not willing to do things on a reasonable cost basis I say **** them, privatize their asses.....then hand off the operation to a newly formed non profit NGO.

Reasonable is relative. Sure, pill #2 costs $.50 but pill #1 costs 30 million. Not to mention any future ventures they plan to take to help the world. Let's take that risk and reward away and see how quickly we advance.
 

sangha

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My wife and I never get flu shots and are both over 65. And the last time either one of us got the flu is at least a decade ago. We have friends who always get a flu shot and are fanatics about it. Both recently had the flu - one a pretty severe case.

I havent had a flu shot in decades. However, now that I am getting older, and not in the best health, I am wondering if I should reconsider. The one thing that concerns me though is the possibility that having virii injected into me might cause me to come down with the flu. This new discovery sounds promising because it does not involve injecting any virus.
 

JacksinPA

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My wife and I never get flu shots and are both over 65. And the last time either one of us got the flu is at least a decade ago. We have friends who always get a flu shot and are fanatics about it. Both recently had the flu - one a pretty severe case.

Flu shots are based on the best guess as to what strains of the virus are going to be prevalent in the coming season. Being a guess means it's never going to be 100% effective. You could be infected by a strain not covered by the vaccine. This new drug stops any flu virus dead with one pill because it cripples the virus particles from multiplying.

The part of the virus that the immune system recognizes & attacks is the outer shell of proteins called the capsid. These proteins keep mutating, giving rise to new strains that your immune system won't reciognize. The enzyme that this new drug deactivates is called an endonuclease. It's amino acid sequence looks to be conserved by evolution so it will always react with the new drug, deactivating it, so the flu virus can't spread further.
 

Hawkeye10

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Flu shots are based on the best guess as to what strains of the virus are going to be prevalent in the coming season. Being a guess means it's never going to be 100% effective. You could be infected by a strain not covered by the vaccine. This new drug stops any flu virus dead with one pill because it cripples the virus particles from multiplying.

The part of the virus that the immune system recognizes & attacks is the outer shell of proteins called the capsid. These proteins keep mutating, giving rise to new strains that your immune system won't reciognize. The enzyme that this new drug deactivates is called an endonuclease. It's amino acid sequence looks to be conserved by evolution so it will always react with the new drug, deactivating it, so the flu virus can't spread further.

Food for thought:

Danuta Skowronski, an epidemiologist at the BC Centre for Disease Control in Vancouver, Canada, instead blames mutations in the vaccine strain itself. The most common influenza vaccine contains an "inactivated" virus, which manufacturers grow in chicken eggs. As Skowronski's team first reported in 2014, the virus can mutate while it is growing in the eggs, resulting in a vaccine unable to block circulating strains.

"I think [these mutations] play an enormous role," says viral immunologist Scott Hensley of the University of Pennsylvania. He has preliminary evidence that egg-adapted mutations were behind the weak protection seen with the vaccine used in the 2016–17 season, he says. He also points to a recent study by another group that compared an egg-grown vaccine with one that contained genetically engineered HA, which sidesteps the mutation issue. The engineered vaccine offered more solid protection. That suggests a way to improve current vaccines, Hensley says. "I'd be shocked in 15 years if any of our flu vaccines are grown in eggs.
https://www.sciencemag.org/news/2017/09/why-flu-vaccines-so-often-fail

Thing is I was hearing about how we needed up upgrade vaccine production many many years ago, but nothing has been done.

Great piece at the link.
 
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