Terlipressin: Longer Peptide Effect Half-Life via an Active Metabolite

This article highlights million-dollar molecules that were recently in the news with related patent applications that give clues to their structures and properties. This edition includes Maze’s glycogen synthase 1 (GYS1) inhibitors that were recently licensed to Sanofi, allosteric androgen receptor (AR) modulators that may be of interest to targeted protein degradation researchers, brain-penetrant HER2 and ROCK2 inhibitors, and MDM2 degraders.

In 2021 there were: 50 novel drugs approved by the FDA 27 that CDER considers first-in-class (FIC) 16 first-in-class small molecules (according to CDER) These drugs are the first in their therapeutic class to have a particular mechanism of action [...]

Several multi-million dollar acquisitions or license agreements took place in November 2023 for hot drug targets, with assets from selective PARP1 inhibitors to GLP1R agonists, and others. This recent news roundup highlights the notable acquisitions by pharma companies for rights to molecules in a range of different indications, with illustrative patent examples for undisclosed structures.

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 October 2023 but we did not have space for in MOTM. A few highlights are also discussed, including Novartis’s Werner helicase (WRN) inhibitor, APJ agonist AMG985 molecular glue degrader golcadomide, and more in the full article.

There were 16 acquisitions of companies with small molecule drug assets in 2021 and one merger. Here is a more in-depth look into all of the lead small molecules acquired in 2021, including a review of: The lead molecules in each acquisition and their structural representations where disclosed The mechanism of action, stage, and indication of [...]