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May 21, 2023

Degrader Radar, Apr. '23: DCAF1, on CNS Degraders, and More

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2021 First-in-Class Small Molecule Drugs

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 [...]

Another KRASG12C Inhibitor in Ph. III, Bayer’s Massive FXIa Ph. III Clinical Trial, and 21 Other Molecules in the News

In this update of small molecules in the news for February 2023, we will cover recent: - Molecules in Motion : clinical trial updates and FDA filings - Negative Readouts : halted, discontinued or altered clinical trials - Million-Dollar Molecules : recent M&A’s, IPOs, and other fundraising - Potential Approvals : recent NDA filings and [...]

Compound Collection October 2023: 70 Molecules from October of Potential Interest

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.

Patent Highlights: Allosteric AR Modulators, Glycogen Synthase Inhibitors, and More

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.

2021 Large Molecule Drug Approvals Review – Pt. 2

This deep dive into 2021’s novel large molecule drug approvals is the 2 nd in a series of focus articles on 2021’s novel large molecule drugs. See part one here . For each of the 16 large molecule drug approvals of 2021 (excluding vaccines), we’ll [...]