GDC-6599
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…
Molecules of the Month – August 2023
This month features many of the big reveals from the ACS fall 2023 first disclosures including Nurix’s BTK degrader and RAPT’s CCR4 autoimmune therapy. Several of the molecules making the August list are in Ph. III clinical trials such as Vertex’s sodium channel inhibitor for acute pain and Denali Therapeutics’ CNS-penetrant eIF2B activator for ALS. …
ACS Fall 2023 First Disclosures Â
The First Disclosures sessions at the 2023 ACS Fall Meeting in San Francisco, organized by Nikki Goodwin, presented a variety of new orally available small molecules. The standing room-only sessions were so highly attended that many attendees were unfortunately kicked out due to the fire code. In case you missed any of these exciting molecules,…
More LRRK2 On-Target Toxicity?
LRRK2 has been a hotly pursued drug target for Parkinson’s Disease based on human genetics. Clinical advancement of LRRK2 inhibitors was initially stalled by concerns about on-target lung findings in primates, but these were ameliorated by a Merck/Genentech/Pfizer/MJFF study showing that these lung changes were reversible, and Biogen/Denali has currently a small molecule (BIIB122/DNL151) in…
Must-See Sessions for ACS SF 2023
To help drug discovery professionals get the most out of your trip to ACS San Francisco 2023, we compiled a table of sessions that are likely to be of high interest to industry scientists here. You can filter by conference day, time, and see descriptions of the talks and key topics all in one place.…
Molecules of the Month – July 2023
This month features big announcements from Biogen on their acquisition of Reata and their Nrf2 activator for Friedreich’s ataxia and from BridgeBio on their TTR stabilizer with positive Ph. III data for their ATTR-CM treatment. A pair of KRAS inhibitors from Chugai (macrocycle) and AstraZeneca (brain-penetrant) also makes the list for their notable pharmacology. Other…