The October edition of Small Molecules of the Month includes several potential best-in-class clinical candidates including but not limited to a second-gen LPA1 antagonist from BMS, two muscle modulators from Cytokinetics, and a Janssen pan-genotype, pan-serotype Dengue virus inhibitor. There are several interesting modalities including an oral macrocyclic peptide from Merck, a tumor-specific prodrug from BMS, and a CRBN-based degrader that no-longer needs two imide motifs from St. Jude. As always, there’s plenty of interesting chemical groups – a hydrazine, furenone, pyrrole, decalin, strained macrocycle, quaternary ammonium, … enjoy!
Full summaries, a PDF download, and links to articles are below. Reviewer Joachim Rudolph also points us in the direction of MRTX1133, a potent KRAS G12D inhibitor which was recently disclosed at an AACR-NCI-EORTC virtual conference, but has not been published at the time of this article's publication.
A slide deck with more details about each molecule is available.Upgrade Membership to Download Slide Deck