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:
PF-07258669, an oral MCR4 antagonist from Pfizer
PYR01, a bifunctional, Gag-Pol allosteric glue from Merck
GLPG2534, an oral IRAK4 inhibitor from Galapagos
TP0473292, a mGluR2/3 antagonist prodrug from Taisho
M4205, a selective KIT inhibitor from Merck
SEQ-9, an oral Mtb 23S ribosome inhibitor from Sanofi
sparsentan, a recently approved, FIC, oral, once-daily, dual ETA/AT1 antagonist from Travere
daprodustat, a recently approved, oral, once-daily, pan-PHD inhibitor from GSK
pociredir, an oral, allosteric PRC2 inhibitor (EED) recently put on clinical hold from Fulcrum Therapeutics
QR-6401, an oral, macrocyclic CDK2 inhibitor from Regor Therapeutic
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