NaV1.8 Inhibitor Roundup: From Abbott to Vertex

There continue to be opportunities for another KRAS(G12C) inhibitor to prove itself best-in-class.

This roundup highlights twelve KRAS(G12C) molecules to know, with links to recent case studies on Drug Hunter going in more detail.

Drug Hunter has sifted through news articles, press releases, financial disclosures, SEC filings and more to bring you a roundup of 2023's biggest mergers and acquisitions (M&A) in the drug discovery world. In this 4-part series we will give you an open-access overview of the M&A landscape, and then for Drug Hunter members in the coming weeks, we will be providing in-depth coverage and analysis of the small molecule-focused (parts 2 & 3) and biologics-based deals (part 4). This premium content includes background on the targets, chemical/biological matter and clinical data driving these deals.

Peptidic GLP-1R agonists have received significant media coverage over the past year for their astounding efficacy in several indications. GLP-1R agonists now appear to be efficacious in reducing heart disease risk and in treating certain chronic kidney diseases, expanding their likely future use. This review by Oliver Philps provides an overview of GLP-1 agonists and where they fit in the treatment of diabetes, how the peptide drugs evolved over time to today’s weight loss medications, and what to expect next...

NaV1.8 has become an industry focal point in the pursuit of pain therapeutics thanks to the success of Vertex’s selective inhibitor, VX-548, in Ph. III clinical trials for acute pain and Ph. II results in diabetic peripheral neuropathy. Unlike opioid receptor modulation, NaV1.8 inhibition does not carry the same addiction risks in part due to its lack of expression in the brain. Following our recent review of the leading NaV1.8 inhibitor VX-548, this article provides more details on the history of target validation for NaV1.8 in pain and why this could be the new frontier for pain management.

The team reviews hundreds of compounds from thousands of papers, press releases, and other sources each month to select candidates for Molecules of the Month. Here we have compiled a table of >70 additional molecules that were of interest in November 2023 along with some highlights from some of our favorites below.