Where Do Recent Small Molecule Clinical Candidates Come From?

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.

Drug Hunter has sifted through news articles, press releases, financial disclosures, SEC filings and more to bring you a roundup of 2023's biggest mergers and acquisitions (M&A) in the drug discovery world. In this 4-part series we will give you an open-access overview of the M&A landscape, and then for Drug Hunter members in the coming weeks, we will be providing in-depth coverage and analysis of the small molecule-focused (parts 2 & 3) and biologics-based deals (part 4). This premium content includes background on the targets, chemical/biological matter and clinical data driving these deals.

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.

Drug Hunter has sifted through news articles, press releases, financial disclosures, SEC filings, and more to bring you a roundup of 2023’s biggest mergers and acquisitions (M&A) in the drug discovery world. Following our open-access industry overview, in the final installment of this four-part series we bring you the biologics-focused deals opening checkbooks in 2023.

In this Flash Talk, Katarina Leftheris highlights how advances in our understanding of ADME requirements, screening technologies, formulations development and computational modeling helped macrocycles back on the center stage of the industry.

As part of our Flash Talk webinar series, we present a PDF of Katarina Letheris'slide deck, entitled "Advancing Macrocycles in Drug Discovery". Check out the recording of the talk on our Drug Hunter YouTube channel.