Molecules of the Month

February 2023

A Merck HIV inhibitor with targeted cell-killing activity as a possible approach to finally eradicate HIV, a KIT-selective inhibitor with best-in-class potential for the treatment of GIST, a first-in-class dual ETA/AT1 antagonist recently approved for the rare kidney disease IgA nephropathy are just some of the examples for this month's MOTM. Learn more about the molecules by navigating to the full reviews on the right which cover: why the molecules matter, how they were discovered, the key steps behind optimization, how they work, why the targets were chosen, any interesting toxicology and clinical data, and more. In the meantime, as we release the full reviews, you can find the article links that inspired us to write up these stories below:

  1. PF-07258669, an oral MCR4 antagonist from Pfizer

  2. PYR01, a bifunctional, Gag-Pol allosteric glue from Merck

  3. GLPG2534, an oral IRAK4 inhibitor from Galapagos 

  4. TP0473292, a mGluR2/3 antagonist prodrug from Taisho

  5. M4205, a selective KIT inhibitor from Merck

  6. SEQ-9, an oral Mtb 23S ribosome inhibitor from Sanofi

  7. sparsentan, a recently approved, FIC, oral, once-daily, dual ETA/AT1 antagonist from Travere

  8. daprodustat, a recently approved, oral, once-daily, pan-PHD inhibitor from GSK

  9. pociredir, an oral, allosteric PRC2 inhibitor (EED) recently put on clinical hold from Fulcrum Therapeutics

  10. QR-6401, an oral, macrocyclic CDK2 inhibitor from Regor Therapeutic

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