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    Molecule

    Pfizer’s oral, CDK4-selective inhibitor PF-07220060 has the potential to revolutionize treatment of HR+/HER2- breast cancer through avoiding the neutropenia DLTs associated with SoC CDK4/6 drugs and permitting greater coverage of the desired CDK4 target. Our full article outlines data presented at AACR 2024, covering the molecule’s course from in silico-informed screen, through structurally enabled optimization against CDK6 and GSK-3β to promising preclinical profile. Fresh clinical data showed efficacy and tolerability supporting PF-07220060's clinical progression.

    Motm

    In May, AstraZeneca reported positive Ph. I results for their oral small molecule PCSK9 inhibitor. PMV Pharma’s potential first-in-class p53 Y220C reactivator and Janssen’s selective OX2R (orexin-2 receptor) antagonist with positive Ph. III results are also featured this month. Additional molecules we found notable from May include a saxitoxin-derived NaV1.7 inhibitor from SiteOne Therapeutics and [...]

    Article

    In May 2024, several significant transactions worth millions and billions of dollars took place to advance next-generation neuroplastogens, KRAS G12C inhibitors, Pompe disease treatments, and molecular glues. We also highlight positive clinical readouts for hot targets such as tetrameric transthyretin (TTR) stabilizers, Hedgehog pathway inhibitors, plasma kallikrein inhibitors, dipeptidyl peptidase 1 (DPP-1) inhibitors, and PCSK9 inhibitors. Here's a recap of the most notable news highlights from May 2024!

    Molecule

    Cerevance’s CVN293 is an oral, CNS-penetrant, selective inhibitor of potassium efflux-mediated NLRP3-inflammasome activation in microglia for the treatment of neurodegenerative disorders. Cerevance’s NETSseq platform was used to discover a microglia-specific potassium efflux channel, KCNK13, which allows modulation of the NLRP3-inflammasome in the CNS without affecting peripheral innate immunity. Read the full article to discover highlights on the CNS-penetration of highly polar compounds and how particle size can be key to oral bioavailability

    Article

    To select April’s Molecules of the Month, our team evaluated hundreds of molecules from thousands of papers, press releases, conference presentations, and other materials. Here we’ve curated a roundup of more than 60 additional molecules that caught our interest from April, along with highlights we found most notable.