AACR San Diego 2024: New Drugs on the Horizon + RMC-6236
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Drug-Induced Liver Injury: A Medicinal Chemist’s Perspective
DILI is a leading cause of acute liver failure, accounting for half of these cases and often resulting in drug withdrawals. Understanding and managing DILI risk as a medicinal chemist involves exploring the intricate interplay among properties and structural features. In this article, we provide a medicinal chemist's perspective on the current understanding of DILI mechanisms, highlight cutting-edge assay developments for a holistic assessment, and discuss strategies for predicting DILI risks.
MYT1, Pan-RAF, Pan-RAS and More: Dec. ’23 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 >60 additional molecules that were of interest in December 2023 along with highlights from some of the team’s favorites in the article.
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.
Deucravacitinib: 2022 Small Molecule of the Year
We asked the global drug discovery community to nominate and vote on their favorite molecule from 2022, and the results are in. The 2022 winner, with the most overall votes across the ten finalist molecules , is BMS’ oral, deuterated allosteric TYK2 inhibitor, deucravacitinib, the first new treatment for plaque psoriasis in nearly a decade [...]
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.
