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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.
Patent Highlights: NLRP3 and NaV1.8 Inhibitors, SMARCA2 Degraders, and More from December 2023
The Drug Hunter team is piloting a new series highlighting notable disclosures in the patent literature to provide our readers a timely and scientifically flavorful synopsis of therapeutic targets being actively pursued, emerging industry breakthroughs, and fascinating chemical matter. Here we highlight 12 patents published in December 2023 that piqued our interest, and compiled a searchable table comprising key information from more than 180 additional patents of potential interest to drug hunters. If you have any suggestions on how to make this more useful, please let us know!
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 [...]
ACS Spring 2024: First Time Disclosures
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.
2023 Novel Small Molecule FDA Drug Approvals
The 34 small molecule drug approvals of 2023 are summarized in this poster and article with the structures, mechanisms of action, originators (& marketers), indications, and links to deep-dive reviews and more information about each drug.
