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Repurposed Sheep Antiparasitic Monepantel (NUZ-001) Enters HEALEY-ALS Platform Trial An mTOR inhibitor that induces autophagy, Neurizon Therapeutics' NUZ-001, aims to enhance the clearance of aggregation-prone proteins, a hallmark of ALS. Read it on Drug Hunter: drughunters.com/3LAg9wD

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Discovery of CHF6333: An Inhaled Neutrophil Elastase Inhibitor | lnkd.in/gKeQPiE6 This case study summarizes the discovery and optimization of CHF6333, as presented by Fabio Rancati at the RSC/SCI 23rd Medicinal Chemistry Symposium. Read it on Drug Hunter: lnkd.in/gKeQPiE6

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Sepiapterin (Sephience®), an orally bioavailable PAH (phenylalanine hydroxylase) activator from PTC Therapeutics, was approved in July 2025 for the treatment of PKU (phenylketonuria), a condition characterized by neurotoxic Phe (phenylalanine) accumulation. Read more | drughunters.com/4qXq9Ak

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drughunters.com/43lGuVj Starting January 2026, the Drug Hunter team will release bite-size, <30 minute recorded lectures that distill the modern biopharma industry and drug discovery to essential knowledge for scientists Sign Up for the Course Navigation Webinar on Dec 9th: drughunters.com/47wNwsR

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Pfizer recently disclosed the discovery journey of PF-07293893, an oral, selective activator of AMPKγ3 developed for the treatment of HFpEF (heart failure with preserved ejection fraction). Read it on Drug Hunter: drughunter.com/molecule/pf-...

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Darovasertib is a potential first-in-class, oral pan-PKC inhibitor with both Orphan Drug and Breakthrough Therapy designations and is one of the most clinically advanced targeted therapies for uveal melanoma. Read it on Drug Hunter: drughunter.com/molecule/dar...

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Cracking the Entry Code: CD36 as a Key Receptor for Heterobifunctional Degrader Cellular Uptake CD36 has recently been identified by Wang et al. as a mediator of cellular uptake for heterobifunctional degraders and other beyond-rule-of-five (bRo5) molecules. Read more: drughunters.com/464k5MG

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PF-07853578: Leveraging Chemical Biology to Target a Genetically Defined Driver of MASLD | PF-07853578 covalently binds to PNPLA3(I148M), displacing it from lipid droplets and promoting its degradation: a novel strategy to restore lipid metabolism. Read more: drughunter.com/molecule/pf-...

Big Money Bets from June 2025 | drughunters.com/44NDWzb In our June recap of biopharma deals, we highlight Sanofi acquiring Blueprint for $9.1B, Novo Nordisk partnering with Deep Apple Therapeutics on small molecule obesity drugs, and more! Read it on Drug Hunter: drughunters.com/44NDWzb

Can Brensocatib Open the Door for Neutrophil-Modulating Drugs? | drughunters.com/3ItDcb2 If approved, brensocatib would not only address a major unmet medical need but also serve as a template for rational neutrophil-targeting drug design. Read it on Drug Hunter: drughunters.com/3ItDcb2

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BBO-10203, A Potential First-in-Class PI3Kα:RAS Protein-Protein Interaction Inhibitor Advances to Phase I Trials | drughunters.com/4ksBKTl Learn more about BBO-10203, including its discovery, binding mode and much more in our full Drug Hunter case study! Read more: drughunters.com/4ksBKTl

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JNJ-6640 Reveals Purine Deprivation Strategy Against Drug-Resistant TB Read it on Drug Hunter: drughunters.com/3TwdLYr

IRF5 Target Review: Highlighting Two Divergent Approaches to an "Undruggable" Transcription Factor Read it on Drug Hunter | drughunters.com/4ktbY1l

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Key Clinical Updates from April 2025 In our recap of April’s clinical updates, we highlight the accelerated approval of Novartis’ atrasentan for immunoglobulin A nephropathy and two oral GLP-1 receptor agonists that are ready to seek approval from the FDA. Read now | drughunters.com/3ZsymjF

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Drug Hunter April 2025 Annotated Searchable Patent Table | drughunters.com/4mq3tGE This month’s collection features an exciting array of innovations, including antiviral agents, LRRK2 degraders, SARM1 inhibitors, CK1α degraders and more! Read it on Drug Hunter | drughunters.com/4mq3tGE

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Pretzel recently announced initiation of recruitment for a Ph. I study for their undisclosed lead POLγ-targeting asset, PX578, which is likely similar to PZL-A based on their recent patent publications. Read it on Drug Hunter | drughunters.com/4mpQQeO

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Bayer Discloses its Selective Dual Factor IIa/Xa Inhibitor, BAY 3389934 In this molecule profile, we highlight the key structural features behind the discovery of BAY 3389934 as a nanomolar-potent, highly soluble compound designed for i.v. administration. Read now | drughunters.com/4mimeeQ

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Now in Ph. I trials for advanced solid tumors, RP-1664 represents a promising test of whether PLK4 inhibition can serve as a precision oncology strategy in TRIM37-amplified cancers such as breast adenocarcinoma and neuroblastoma. Read more: t.co/YV8luFWahY

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Explore our bioisosteres cheat sheet. Check out how these bioisosteres impact drug properties, improve oral bioavailability, and reduce potential liabilities, ultimately shaping the success of modern therapeutics. Read more: drughunters.com/4mc2REq

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In our recap of April biopharma deals, we highlight Nurix licensing a transcription-factor degrader to Sanofi, Prazer Therapeutics raising $20M for targeted protein degraders, and Merck KGaA buying SpringWorks for $3.9B. Read more: t.co/dvj6F2s4KD

BMS-986458 is an orally bioavailable CRBN-mediated heterobifunctional degrader of BCL6 currently in Ph. I/II clinical trials for relapsed/refractory non-Hodgkin lymphomas. Read it on Drug Hunter | drughunters.com/3RWISvv

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GSK and IDEAYA’s (S)-27 is a preclinical, covalent acrylamide inhibitor of WRN helicase—a validated synthetic lethality target in MSI-H tumors. Read more: drughunters.com/4k3Dvqi

A Fluorinated Macrobicyclic Antibiotic with Gram-Negative Activity | drughunters.com/43kiq5m BT-33 is a compelling example of how rigidification and conformational preorganization can revitalize legacy scaffolds for modern antibacterial challenges. Read more: drughunters.com/43kiq5m

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Alumis’ lead candidate ESK-001 is a potential best-in-class allosteric TYK2 inhibitor for immune-mediated diseases like plaque psoriasis and SLE. Read more: drughunters.com/4iPPpDi

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Currently in Ph. II/III trials for narcolepsy type 1, narcolepsy type 2, and idiopathic hypersomnia, ALKS 2680 is helping to redefine the therapeutic landscape for sleep-wake disorders. Read more: drughunters.com/42FAtCP

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New Drugs on the Horizon from #AACR2025! 12 clinical molecules, 12 fresh stories from the frontlines of drug discovery. The full article covers the science, mechanism of action, and clinical context behind each of these new drug compounds. Read more: t.co/h10fFwojvX

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Bioisosteres for Drug Hunters: Part 3 - Phenyl Rings In Part 3 of our bioisosteres series, we dive into phenyl rings bioisosteres in medicinal chemistry and emerging C(sp3)-rich motifs that are gaining attention for their potential in modern drug design. Read Now | drughunters.com/4jU7RLP

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BMS Rescues Oral Macrocyclic Peptide PD-L1 Inhibitor Program Through a HSA Binding Tail | Recently disclosed at the ACS Spring 2025 meeting, we reveal how this macrocycle was discovered, and the HSA binding and formulation optimization of this compound. Read Now | drughunters.com/44Ny7mN

March 2025 Patent Highlights | drughunters.com/4jVX0Bi March's highlights include heterobifunctional degraders for BCL6 from Treeline Biosciences and STAT6 from Kymera, macrocyclic peptide IL-23R antagonists from Sanofi and FoRx Therapeutics' PARG inhibitors which feature a novel covalent handle.

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Is Orforglipron Set to be the First Approved Small-Molecule GLP-1R Agonist? Read Drug Hunter's updated case study on orforglipron to discover the history of this compound, how it differentiates from the competition and the data driving it towards an NDA. Read more | drughunters.com/4jhiMPI

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CDK2 Target Review: Competitive Landscape, Key Data, and New Modalities Our target review highlights the top clinical candidates and emerging preclinical modalities in the race for the first approved CDK2 drug. Read it on Drug Hunter | drughunters.com/42D8K4i

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Molecules of the Month – March 2025 Find out what molecules made our March 2025 Molecules of the Month list, and check out recent articles for each. Full article: t.co/S8h3jHXuid

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March 2025 Annotated Searchable Patent Table This month’s collection features an exciting array of innovations, including IL-23R antagonists, STAT6 degraders, covalent PARG inhibitors, NaV1.8 inhibitors and more! Read it on Drug Hunter | drughunters.com/42BqSf7

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Another Oral GlyT1 Inhibitor Meets a Familiar End This article covers the discovery, development, and Phase III failure of iclepertin, detailing its structure, pharmacology, clinical journey, and the challenges of GlyT1-targeted therapies. Read more: drughunters.com/43TctNC

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A Promising Phenolic Atropisomeric PKMYT1 Inhibitor Candidate Facing an Uncertain Future Repare’s RP-6306 (lunresertib) showed clean WEE1 selectivity and strong preclinical data, but recent strategic shifts raise questions about its future. Read more: t.co/4nEgYAdOxj

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Following the first part of our radiotherapeutics review, we bring you coverage of the deals that are driving the revival of this field and dive into the clinical landscape to highlight the coming, next-generation radiotherapeutics. Read it on Drug Hunter | drughunters.com/3EnjKee

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Key Clinical Updates March 2025 | drughunters.com/4jrhamk In our recap of March’s clinical updates, we highlight the FDA’s approval of two first-in-class treatments for rare diseases – C3 glomerulopathy and Prader–Willi syndrome – in addition to the first new antibiotic for UTIs in almost 30 years.

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2024 MOLECULE OF THE YEAR The 2024 winner, earning the most votes out of ten finalists, is Vertex’s suzetrigine (VX-548): a first-in-class, FDA-approved, non-addictive oral NaV1.8 inhibitor for the treatment of moderate to severe acute pain. Read more: t.co/dbns7fjNeG

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Drug Hunter February 2025 Patent Highlights | drughunters.com/3XKAmTN Every month, the Drug Hunter team reviews thousands of IP disclosures to bring you a curated selection of the most impactful patents and applications in drug discovery. Read it on Drug Hunter | drughunters.com/3XKAmTN

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In this article, we explore why STAT3 remains an attractive therapeutic target and how advances in structural biology, particularly X-ray structures of STAT3 complexes, have enabled the design of bRo5 molecules like KT-333. Read more: drughunters.com/3FV7LVA

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First Time Disclosures from #ACSSpring2025 are out! 12 clinical molecules, 12 fresh stories from the frontlines of drug discovery. The full article covers the science, mechanism of action, and clinical context behind each of these new drug compounds. Read more: drughunters.com/3FJ7QM4

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Drug Hunter February 2025 Annotated Searchable Patent Table | drughunters.com/3XyLEu8 Keeping up with the constantly evolving drug discovery IP landscape can be challenging, but we're here to simplify the process for you! Read it on Drug Hunter | drughunters.com/3XyLEu8

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Icotrokinra is a potential first-in-class, orally bioavailable macrocyclic peptide antagonist of IL-23R, currently in clinical trials for multiple inflammatory diseases. Read more: drughunters.com/4j211n1

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drughunter.com @drughunter.com · 10/03/2025

Molecules of the Month – February 2025 Read the full article to find out what compounds made our February 2025 Molecules of the Month list, and check out recent articles for each. Full article: t.co/uw6XTkiclW t.co/xK7tNrvIvy

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Flash Talk Now Live on YouTube! lnkd.in/grfUAUbF As a bonus, Aleksey also answered audience questions that we didn't get to in the live session—check them out here: lnkd.in/gEGZ6hPJ Don't miss this deep dive into cutting-edge computational drug discovery!

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drughunter.com @drughunter.com · 10/03/2025

🌟 2024 Molecule of the Year Nominees 🌟 We asked the drug discovery community to nominate molecules for our annual Molecules of the Year based on what you found most technically impressive and impactful. Nominees for 2024’s Molecule of the Year: lnkd.in/eQ9_WGny Vote here: lnkd.in/ewta-rkN