BAY 2925976 is a novel oral ARα2C antagonist developed by Bayer for the treatment of OSA (obstructive sleep apnea), a widespread condition affecting nearly one billion people globally. Despite the availability of mechanical treatments like CPAP, poor adherence rates highlight the need for more effective interventions. BAY 2925976 demonstrated a preclinical proof of concept for ARα₂C modulation as a potential therapeutic approach for OSA. In this article, we detail the discovery of BAY 2925976, as highlighted by Michael Hahn at the ACS Fall 2024 First-Time Disclosures session in Denver, CO.

Ulotaront (SEP-363856) is a Phase III candidate with FDA Breakthrough Therapy Designation for the treatment of schizophrenia with demonstrated efficacy based on a physician-rated scale (PANSS) in a 4-week placebo-controlled trial and continued improvement in an open-label extension study. Reviewer Jake Schwarz says, “ulotaront was developed [...]

Context. HR1405-01 (Nanjing Heron Pharmaceutical) is an intravenous NSAID with inflammatory and analgesic activities. Oral NSAIDs (ibuprofen, naproxen..) are widely used, and it is interesting to see justification for a new intravenous NSAID. Intravenous ibuprofen was the first intravenous NSAID to be approved, following which a couple of [...]

Drug Hunter Reviewer Commentary. With over two decades of experience in neuroscience drug discovery, Drug Hunter reviewer Jake Schwarz says "mGluR2/3 agonists have been explored for schizophrenia, and agonists/PAMS could be tuned to give antagonist/NAM activity, but depression is a new indication. One of the more interesting depression [...]

JNJ-54175446 is an oral, CNS-penetrant P2X7 ion channel antagonist targeting a novel pathway linking neuroinflammation and depression, with recently published Ph. I data in major depressive disorder (NCT02902601, initiated in 2016). The Janssen program is notable as a pioneering early example of a neuroinflammation program started at a time before NLRP3 or neuroimmunology were commonly discussed topics, as they are today [...]