Thank you @LauermanJohn for revealing the untold origin story for Pfizer's Paxlovid COVID-19 pill.
The interesting part: Merck's drug boceprevir provided an essential backbone structure for Paxlovid, and boceprevir is still under patent.
bloomberg.com/news/articles/…
The interesting part: Merck's drug boceprevir provided an essential backbone structure for Paxlovid, and boceprevir is still under patent.
bloomberg.com/news/articles/…
The article reveals many things not publicly known earlier.
First, Merck had (like my own lab and others) found boceprevir to have some activity against SARSCoV2. Not too surprising, as boceprevir is a HCV protease inhibitor, and SARSCoV2 protease is homologous to HCV protease.
First, Merck had (like my own lab and others) found boceprevir to have some activity against SARSCoV2. Not too surprising, as boceprevir is a HCV protease inhibitor, and SARSCoV2 protease is homologous to HCV protease.
I had emailed Merck to let them know in case they didn't already. But I expected the to know, and this confirms it. They determined that is was unlikely to work well for COVID19 on its own, but Merck was in a good position to modify it to work better, but they didn't.
There's an interesting quote from George Njoroge, the developer of boceprevir, regarding Merck's inaction: "I thought they would jump into it... I was a bit surprised"
Instead Pfizer took the ball and ran with it. Paxlovid (L) copied the crucial central portion of boceprevir (R) bond by bond over 22 atoms. The ends are also altered to work better on SARSCoV2, which is also crucial. But Pfizer papers and documents never mention boceprevir. 
I'm quoted in the article pointing out that the idea for this structure in Paxlovid clearly came from boceprevir (it does not resemble anything from Pfizer's previous work in any way).
Anyway so now I probably have 2 big pharmas annoyed at me.
Anyway so now I probably have 2 big pharmas annoyed at me.
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