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Amid a worldwide pandemic, it is perhaps no surprise that a drug which significantly reduces hospitalization and death due to COVID-19 would rise to the top of any drug hunter’s “best of” list. Yet Pfizer’s nirmatrelvir (Paxlovid) proved to be in a class by itself. Developed and advanced to market with unprecedented speed, this small molecule has the potential to save millions of lives. That’s why the global drug discovery community has selected nirmatrelvir as Drug Hunter’s 2021 Small Molecule of the Year.

While vaccines and antibody treatments have also been developed at a record pace, both have been challenged by the emerging variants springing from COVID-19’s rapidly mutating spike protein.  An easy-to-administer oral treatment that doesn’t target the spike protein thus presents several advantages, including effectiveness against new mutations, better time-to-treatment, and improved worldwide accessibility.
The story behind Paxlovid’s discovery and development is fascinating. Target identification had a head start, thanks to early genomic sequencing of the SARS-CoV-2 virus and previous experience with SARS-CoV, which caused SARS in the early 2000s. The challenge then became finding a molecule that was orally bioavailable, a mystery unlocked as Pfizer’s team turned its attention to the hydrogen bonds that normally keep such a molecule trapped in the gut.
Drug Hunter follows Paxlovid’s whole breathtaking arc, from genome analysis through Phase I trials and beyond, a design and development triumph that Drug Hunter reviewer Mike Koehler says “sets a speed record that may never be broken.” It’s a story you won’t want to miss.

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CETSA® (Cellular Thermal Shift Assay) is an increasingly used orthogonal assay technology for measuring intracellular target engagement. To enable fast and robust screening of an increased number of compounds, Pelago developed a high-throughput format of the assay that can be utilized for library screening and hit confirmation efforts.
Pelago is now opening screening campaigns to multiple partners at a time, to reduce the overall cost for everyone (CETSA® Speed DATE). Their next screening campaign on the EGFR pathway is currently accepting compounds and closes on March 31You can go here to submit compounds or get in touch with their team about it.
Learn About CETSA® Speed DATE Screen
We worked with the Pelago team to get a further 10% discount on this screening campaign for our subscribers, using code:
This is a reader benefit - we do not get a commission. Hope this is helpful!
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