2022 Novel Small Molecule Drug Approvals

The highly anticipated First Time Disclosures session at the ACS Spring 2024 Meeting in New Orleans, organized by Nicole Goodwin and H. Rachel Lagiakos, presented a variety of new orally available small molecules. In case you missed any of these exciting molecules, from Oric’s CD73 inhibitor to Deciphera’s first-in-class ULK1/2 inhibitor, this article provides the structures and targets for the novel molecules disclosed at the session.

One of the key challenges in CNS projects is achieving sufficient unbound brain exposure to engage the target. To predict CNS exposure, scientists employ metrics like CNS MPO scores from Pfizer and Merck, Bayesian models, and methods for balancing physicochemical properties. However, these in silico metrics often fail to correlate well with experimental data. Schrödinger's team has discovered the energy of solvation (E-sol) metric, which accurately predicts Kp,uu and has been validated with CNS-penetrant DLK inhibitors. Explore more in this detailed Drug Hunter article.

In April 2024, there were promising examples of drug repurposing, significant clinical and regulatory milestones for therapies aimed at rare and pediatric diseases, the initiation of a rolling NDA submission for suzetrigine, substantial billion-dollar acquisitions, and positive trial results were reported for both a D1/D5 receptor agonist and a PARP1 inhibitor. However, the industry also had setbacks as demonstrated by the failed clinical trials for an MNK inhibitor and an NMDA receptor modulator. In case you missed anything, here’s a recap of the most notable news highlights from April 2024!

Here’s a rundown of August’s key clinical developments, including FDA approvals, potential upcoming approvals, notable trial readouts, new NDA submissions, and pipeline realignments.

This summary of September's major clinical updates features FDA approvals, drug withdrawals, anticipated regulatory decisions, notable trial results, new NDA submissions, clinical trial setbacks, and the initiation of new clinical trials.