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!

Check out our new Scaled Clearance Calculator! Clearance is a key pharmacokinetic parameter in drug discovery, impacting half-life, oral bioavailability, and dosing. To simplify your PK calculations and predict in vivo clearance, we've created a user-friendly tool that scales in vitro data using intrinsic clearance values from microsomes or hepatocytes. Leveraging the Well-Stirred Model, this tool enables you to estimate microsomal clearance, hepatic clearance, and extraction ratio. Try our new calculator to optimize your drug discovery workflow! We’d like to extend a big thank you to Gilles Ouvry, Deepak Dalvie, Peter Eichhorn and Dean Brown for their feedback on the calculator! Check it out and simplify your DMPK calculations today: https://lnkd.in/gevVGgAh

STAT3 Target Review: Small Molecule Inhibitors | https://lnkd.in/ghFURp4H STAT3 hyperactivity is implicated in over 70% of human cancers. Despite three decades of research spanning small molecules, nucleotides, and heterobifunctional degraders, no STAT3-targeted therapy has achieved regulatory approval. Of the 11 small molecule compounds that have entered clinical trials, only four remain in active investigation. This review explores the successes and setbacks in the ongoing pursuit of the first STAT3-targeted oncology drug. Read on for a deep dive into these efforts and the evolving landscape of small molecule STAT3 inhibitor drug discovery. Read more: https://lnkd.in/ghFURp4H

?? **Top Drug Hunter Resources from 2024!** ?? Practical PK calculators, structure search, patent search, and more! Our resources have helped scientists streamline research and accelerate drug discovery. This quick recap video highlights some of our most popular resources from 2024! ?? Want full access to these resources and more? Connect with our team and explore our membership options here: https://lnkd.in/gt3ZTBE5 ?? Stay informed, stay ahead—because better tools mean better discoveries! #DrugDiscovery #Biotech #Pharma #Innovation

Sulfoximines in Medicinal Chemistry: Unlocking Novel Opportunities in Drug Design https://lnkd.in/gAD8Xvb6 Thursday, April 17th, 2025 8 AM PT / 11 AM ET / 5 PM CET In the past decade, sulfoximines, the aza analogues of sulfones, attracted much interest in the medicinal chemistry community, as exemplified by an ever-increasing number of scientific articles and commercially available sulfoximine building blocks. This led to numerous life science patent applications covering sulfoximine-containing biologically active molecules, of which several made it to clinical trials (e.g. ART0380, TNG-260, and IM-250). In this Flash Talk, Ulrich Luecking will explore emerging trends and opportunities in using sulfoximines in medicinal chemistry. He will cover their application in the construction of complex molecules, proteolysis-targeting chimeras (PROTACs), antibody-drug conjugates (ADCs), and the creation of novel warheads for covalent inhibition. Register here:?https://lnkd.in/gW7SmZxS

Exciting Panel at ACS Spring 2025 Thinking about a career transition? If you’re a synthetic organic chemist, grad student, post-doc, or a seasoned medicinal chemist at a crossroad trying to identify or transition to a different career path in academia, business, or industry, join us for an engaging panel discussion: ?? Building Your Brand as a Medicinal Chemist: Academic-Industrial Partnerships, Career Transitions and Company Generation ?? Date: Monday, March 24 ? Time: 12 - 2 PM ?? Location: San Diego Convention Center, Room 30B Whether you're an early-career scientist or a seasoned professional, this discussion will provide insights and strategies to elevate your career. Don't miss this opportunity to learn, network, and shape your future! See you there. #ACSSanDiego #MedicinalChemistry #CareerDevelopment ACS Division of Medicinal Chemistry

The Rise, Fall, and Possible Comeback of Fulacimstat | https://lnkd.in/e5vGhD7P Fulacimstat (BAY 1142524), a potent and selective human chymase inhibitor, was once a promising clinical candidate developed by Bayer | Pharmaceuticals for cardiac remodeling in heart failure. Early trials demonstrated excellent pharmacokinetics and safety, but when Ph. II studies failed to show efficacy over placebo, the program stalled. However, in 2023, a new study reignited interest—not for heart failure, but for DVT (deep vein thrombosis). More recently, a #JMEDCHEM Viewpoint advocated for its repurposing in thrombosis. This case study explores the SAR campaign that led to fulacimstat, its Ph. II setbacks in cardiac remodeling and chronic kidney disease, and the emerging research that may offer it a second chance in the clinic. Read more: https://lnkd.in/e5vGhD7P

Meet Vinícius Esteves Teixeira, Ph.D., Research Associate at Drug Hunter His academic journey began with a bachelor's degree in Chemistry, specializing in organic synthesis, from Universidade Federal de Pelotas Brazil. He later transitioned to Computational Chemistry, joining the Theoretical Chemistry Group at Federal University of Rio Grande do Sul Brazil in Porto Alegre, where he earned both his master's and PhD degrees in Computational and Theoretical Chemistry in 2020. Vinicius has extensive experience in education, having worked as a Physical Chemistry tutor at Brazilian universities and as a Senior Subject-Matter Expert in Chemistry at Study.com His professional experience also includes consulting on chemistry and medicine-related projects during his tenure at 20one Consulting. Currently residing in the Porto Alegre metropolitan area, Vinicius spends his free time watching movies, reading books, and following sports. Vinicius shares: Working alongside a team that's truly passionate about drug discovery, I realized that even a single compound has the potential to change lives and make a meaningful impact on the world. Drug discovery isn't just about developing new compounds; it's about hope. It's about creating a better world. Drug Hunter changed my life. It ignited my passion for drug discovery, and I am deeply committed to our mission. I'm excited to develop new projects, provide insights, and deliver high-quality data that empowers drug discovery scientists to make a difference.

Clinically Meaningful Disease-Modifying Treatment for PD with Selective D1/D5 Agonism | https://lnkd.in/gfR9KApt Tavapadon, a key asset in AbbVie's December 2023 acquisition of Cerevel Therapeutics is a potential first-in-class, selective partial agonist of the D1/D5 dopamine receptors currently being developed for PD (Parkinson’s disease). Importantly, it appears to enhance motor function while minimizing the well-documented side effects of non-selective and repeated D2/D3 dopamine receptors stimulation. Tavapadon’s safety and efficacy profile offers the potential for it to be utilized in the early stages of the disease, thus providing a near-term complementary asset to AbbVie’s existing product (Duopa?), which treats late-stage Parkinson’s disease. Check out the origin and development story of tavapadon, including encouraging late-stage clinical trial data in PD patients supporting AbbVie’s planned 2025 NDA submission—potentially delivering a key return on its Cerevel acquisition. Read more: https://lnkd.in/gfR9KApt

Drug Hunters in Tsukuba! ???? Wrapped up the second phase of our Japan trip in Tsukuba and Tokyo, visiting the forward-thinking scientists at Astellas Pharma, Eisai Co., Ltd., Daiichi Sankyo, and Otsuka Holdings Co., Ltd. subsidiary, Taiho Oncology, Inc. We learned Tsukuba was once the home of Novartis, Merck (Banyu), and others, but today it is anchored by Astellas and Eisai in a similar way to how the Shonan site in Yokohama is anchored by Takeda. I've continued to be amazed by how forward-thinking the Japanese scientists are. Astellas for example has had strong IN-HOUSE efforts in targeted protein degradation for many years, whereas many US companies have shied away from doing this themselves. They were ahead of the curve with a KRAS(G12D) degrader that advanced very quickly and remain ahead of the curve with investments in internal AI drug discovery and robotics. Many of the leaders of these companies trained at leading US institutions like Harvard and Scripps, and are fearless about using modern modalities. Activity in AI drug discovery, induced proximity, drug conjugates, robotics, RNA modulation, next-generation covalents, and beyond seem universal and the folks here are VERY aware of the latest developments across the board. That said, there is healthy respect here for the speed of the American biotech ecosystem, and folks wonder how American biotech companies move through clinical development so fast. You can tell that folks are eager to move new medicines forward with equal doses of passion and humility. It is impossible not to admire and quickly fall in love with the thoughtfulness of everything here in Japan. People are kind, attentive, and good-humored - despite some difficulties with English on occasion, outbursts of laughter were frequent at dinner. What do all scientists here have in common? They love to drink BEER! Flying next to Osaka for the final leg of our trip with Otsuka Pharmaceutical Co., Ltd., Shionogi Inc. (U.S.), ONO PHARMACEUTICAL CO., LTD., and Japan Tobacco Inc. (JT). Time has flown by quickly and we will miss Japan!