Drug Hunter

Drug Hunters in Denver! Another FANTASTIC evening with a fascinating group of stellar drug hunters in Denver! Got to hear stories from several hundreds years of collective drug discovery experience, including from one of the inventors of the first antibody-drug conjugate (ADC), pioneers of first-in-class molecules against KRAS and other targets, and more. Great to see folks from all over the world come in and hear their inspiring stories. Thank you for all who stayed out this evening Jennifer Allen, Bernhard Fasching, Julia Haas, Wendy Young, Denise Grünenfelder, Zhonghua Pei, Christa Müller, Philippe Mochirian, Anil Padyana, Claude Q., Michael Deligny, Jonathan Hempel, Jie Jack Li, Josh Haimson, Eric Newcomb, Magid Abou-Gharbia, and special thanks our team members Dennis Koester, Matthew Hesse, Shaima Qunies for co-hosting!

A First-In-Class Intracellular Checkpoint Inhibitor of DGK ⍺ and ζ Stemming from Phenotypic Screening | https://lnkd.in/g78zqBCU BMS-986408 is an oral, dual DGK ⍺ and ζ inhibitor currently in a Ph. I/II clinical trial as a single agent and in combination with PD-1 inhibitor nivolumab or with nivolumab and CTLA-4 inhibitor ipilimumab in patients with solid tumors. The compound was identified stemming from a phenotypic screening approach, and subsequent target deconvolution revealed DGK to be the target. If approved, it would be a first-in-class intracellular checkpoint inhibitor of DGK. Bristol Myers Squibb presented the discovery story of BMS-986408 at the American Chemical Society Fall 2024 Meeting in Denver, which was an excellent case study on how to overcome a DILI risk associated with BSEP inhibition, as well as how to improve solubility and PK properties of your compounds through the introduction of polarity, reduction of aromatic rings, and increase in f(sp3). Full article: https://lnkd.in/g78zqBCU

A Next-Generation, Mutant-Selective PI3Kα Allosteric Inhibitor from Scorpion Tx with a Potentially Improved Safety Profile | https://lnkd.in/grrEWg7b STX-478 is an oral, CNS-penetrant, WT-sparing allosteric inhibitor of mutant PI3Kα, a key player in many cancers. The selectivity profile of this compound may be a key differentiator in the clinic by avoiding the metabolic dysfunction seen in current generation pan-PI3Kα inhibitors. Scorpion Therapeutics recently highlighted promising efficacy and safety data for STX-478 in their ESMO 2024 presentation, including key hyperglycemia data which we’ve covered in this updated article! This full case study explores the discovery and lead optimization of STX-478, its pharmacology, preclinical and clinical data, and how it compares to other PI3Kα inhibitors in the field. Read it on Drug Hunter | https://lnkd.in/grrEWg7b

📣Reminder📣 Patent Pulse: A Spotlight on Recent Highlights from Small Molecule Patents | https://lnkd.in/eh862RA2 Fri, Oct 18, 2024 9 AM PDT / 12 PM EDT / 6 PM CEST Curious about the latest insights from recent patent literature? Interested in exploring the patented chemical matter for exciting targets like GLP-1R, IL-17A, SARM1, DHX-9, and many more targets? Want to know why these targets are so promising and how the discussed chemical matter differentiates? Or perhaps you'd like to learn how to spot emerging hot targets before they become mainstream? Join Dennis X. Hu, Lewis Pennington, Matthew Hesse, and Dennis Koester for a Coffee Chat this Friday, where we’ll highlight the team's favorite recent patents. Feel free to submit your questions during the registration and bring many more to the session! This format is all about audience interaction, and we’re excited to address your questions live. Submit your questions with your registration here: https://lnkd.in/eh862RA2

Molecule One-Pager: ARV-471 (vepdegestrant) | https://lnkd.in/g7ykPxc9 Arvinas’ ARV-471 is an orally bioavailable CRBN-based ER PROTAC degrader for treating patients with ER+/HER2-breast cancer and the first PROTAC to enter Ph. III clinical trials. For a long time, the scientific community was skeptical that PROTACs could be suitable for once-daily oral dosing, and molecules like ARV-471 have ended that dogma. This molecule one-pager serves as a reference guide, offering an overview of the scientific significance of Arvinas' ARV-471 program. It includes links to key presentations, publications, patents, preclinical and clinical PK data summaries, and more. Check out the one-pager for ARV-471: https://lnkd.in/g7ykPxc9

A Small Molecule Superagonist Acquired for $2.6B by Lundbeck Lundbeck just purchased Longboard Pharmaceuticals for its lead asset, bexicaserin, a superagonist for 5-HT2C with a potential best-in-class profile. This molecule was one of the main subject of Drug Hunter's scientific spotlights back in January 2024. Featured in the same issue was Jnana Therapeutics' JNT-517, which contributed to Otsuka Pharmaceutical Co., Ltd.'s >$1B acquisition of Jnana in August 2024. The Drug Hunter team has a track record of spotting high-value, scientifically notable programs early in development, from patents to conference disclosures, obscure pre-prints to posters. Make sure your company has a membership so you can spot these things early: https://lnkd.in/gXdGmv93

Genentech Secures FDA Approval for Inavolisib in Advanced HR+, HER2- Breast Cancer | https://lnkd.in/gUFT-ybY Inavolisib is a PI3Kα isoform-selective kinase inhibitor and monovalent degrader of the mutant p110α catalytic subunit of mutant PI3Kα. The molecule selectively depletes mutant p110α in cancer cells with active RTK (receptor tyrosine kinase) signaling and is in several ongoing or planned Ph. III trials for breast cancer. Yesterday, the FDA approved inavolisib (Itovebi) for the treatment of advanced HR+/HER2- breast cancer with a PIK3CA mutation. This approval is based on results from the Ph. III INAVO120 study. The primary efficacy outcome of PFS showed a significant improvement with the inavolisib + palbociclib + fulvestrant combination compared to the placebo + palbociclib + fulvestrant arm. Median PFS was 15.0 months versus 7.3 months, respectively. The ORR was also higher in the inavolisib arm at 58%, compared to 25% in the placebo arm. Additionally, the DOR was longer in the inavolisib arm (18.4 months vs. 9.6 months). This article reviews how it works, how it was discovered, and why it matters. Full article: https://lnkd.in/gUFT-ybY

The Chemist's Playbook: Impactful Bioisosteres for Modern Drug Design | https://lnkd.in/gJ-RmHbW Thu, Oct 24, 2024  8 AM PDT / 11 AM EDT / 5 PM CEST The ever-expanding drug discovery enterprise began to exploit bioisosterism as a form of molecular recognition to identify and advance candidate molecules. There are many reasons to explore biosiosteres in drug discovery. May it be to improve potency or drug-like properties or to eliminate an undesired potential toxicophore. In this Flash Talk, Nicholas A. Meanwell will explore the history of bioisosterism. He will present several case studies with established and emerging bioisosteres addressing a range of challenges in drug discovery. He will dive into examples of carboxylic acid, amide, phosphate, phenyl and hydrogen bioisosteres focusing on molecule case studies that had an impact on the contemporary pharmacopeia. Don't miss this Flash Talk by a renowned expert in the field. Following the presentation, Nicholas will be available to answer your questions during a live Q&A session. Register here: https://lnkd.in/gJ-RmHbW

Key Clinical Compound Updates from September 2024 | https://lnkd.in/gyFBZHnM In September, there were notable clinical and regulatory milestones, including FDA approvals, NDA submissions, positive clinical trial results, the launch of new trials, and a few trial setbacks. Discover the latest developments here: https://lnkd.in/gyFBZHnM

Who are the BEST business development professionals in Boston? Drug Hunter is hiring! Today Drug Hunter serves >175 of the world's top pharma and biotech companies, providing a subscription knowledge base that helps R&D professionals discover the medicines of the future. Our team is seeking our first Greater Boston-area commercial team member to continue Drug Hunter's rapid growth and adoption in one of the centers the world's biotechnology and pharmaceutical industries. This role will be responsible for managing new and existing relationships end-to-end with hundreds of exciting biotech companies. You'll get to meet interesting people every day! To be successful in this role, you will need to be able to work in a fast-paced, team-based, high-growth environment and effectively teach new customers why Drug Hunter is different from legacy service providers and why our customers have found Drug Hunter invaluable for their work. Check out this role or explore our careers page here: https://lnkd.in/gc6r6kmC