An oral macrocyclic peptide PCSK9 inhibitor entering Ph. III for hypercholesterolemia later this year, a Ph. I/Ib KRASG12C(ON) tri-complex inhibitor for the treatment of advanced solid tumors, an oral mutant-selective BRAFC600X degrader in Ph. I for BRAF-driven cancers, and an orally available AR-degrading PROTAC in Ph. II for advanced prostate cancers 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 (when released) 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 throughout this month, you can find the article links that inspired us to write up these stories below:
MK-0616 - an oral, macrocyclic peptide inhibitor of PCSK9 entering Ph. III for hypercholesterolemia from Merck
RMC-6291 - a Ph. I/Ib oral I/Ib KRASG12C(ON) tri-complex inhibitor for the treatment of advanced solid tumors from Revolution Medicines
camlipixant - a Ph. III oral, twice-daily P2X3 receptor antagonist for first-line treatment of refractory chronic cough from AstraZeneca/Neomed/Bellus Health/GSK
BAY-747 - a Ph. I oral, once-daily sGC stimulator from Bayer
gepotidacin - a Ph. III oral, twice-daily antibacterial Type II topoisomerase inhibitor for the treatment of uncomplicated UTIs from Glaxo
CFT1946 - a Ph. I oral, mutant-selective BRAFV600X degrader for the treatment of BRAF-driven cancers from C4 Therapeutics
IOA-244 - a Ph. I oral, once-daily non-competitive PI3Kd inhibitor for the treatment of metastatic cancers from Merck Serono/iOnctura
ARV-766 - a Ph. II oral AR-degrading PROTAC for advanced prostate cancer from Arvinas
difamilast - a topical PDE4B-selective inhibitor from Otsuka
navoximod - a Ph. I oral IDO1 inhibitor for the treatment of cancer from Newlink/Genentech
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