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SOS1 and SMARCA2 Degraders, RORγ and IRAK4 Inhibitors, and More: January 2024 Compound Collection
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 January 2024 along with highlights from some of our favorites, including molecules targeting SOS1, NLRP3, SMARCA2, and more.
A First-in-Class TRPA1 Antagonist Overcomes Toxicity Hurdles to Become Cough Candidate
Genentech’s GDC-6599 is the first oral TRP Ankyrin 1 (TRPA1) antagonist to reach Ph. IIa (NCT05660850) for chronic cough after preclinical studies and a Ph. I trial showed it was well-tolerated, in contrast to prior molecules. The transient receptor potential (TRP) family of ion channels has been the subject of intensive drug discovery efforts due to their critical role in the development and progression of pain, itch, and respiratory conditions.
The Post-Gleevec Era
Gleevec (imatinib) was the first tyrosine kinase inhibitor approved for the treatment of cancer and one of the first products to emerge from "rational drug design." It's invention changed chronic myeloid leukemia from an incurable death sentence to a manageable disease. Here's a look back on the tremendous value it's created over the last [...]
Leaving Academia to Discover a Billion-Dollar Drug: Reflections from a Thirty-Year Path to Momelotinib’s Approval
Momelotinib is a JAK inhibitor approved by the FDA in September 2023 for treating myelofibrosis. Last year, the molecule’s co-inventors, Andrew Wilks and Christopher Burns, gave a Drug Hunter Flash talk about the development of this drug with a fascinating mechanism of action.
In celebration of the molecule’s advancement, here we recap their brilliant story, including Wilks’ discovery of the JAK kinases and how he gave them their name, and the long, sometimes fraught journey of momelotinib through several companies before its acquisition and commercialization by GSK.
MK-0616: The 2023 Molecule of the Year
We asked the global drug discovery community to nominate and vote on their favorite molecule from 2023, and the results are in. The 2023 winner, with the most votes between ten molecules, is Merck’s oral macrocyclic peptide inhibitor of PCSK9, MK-0616, derived from mRNA display technology and shown to have clinical efficacy. Herein, we highlight what makes MK-0616 so impressive to the drug discovery community.
