Drug Hunter, Palo Alto, CA (2026)

12/29/2025

OPEN ACCESS - Top 10 Most Popular Drug Hunter Case Studies of 2025 | https://drughunters.com/45woXKX

2025 was an exciting year for drug discovery, with the FDA approving more than 40 new therapies and a parallel wave of structually and mechanisticaly innovative molecules advancing into late-stage clinical development.

Throughout the year, Drug Hunter covered the science behind these exciting drug discovery stories, highlighting how progress in screening technologies, structural biology, medicinal chemistry, and CMC continues to expand the druggable target space for small molecules and emerging modalities.

Explore the 10 most popular case studies of 2025 to be inspired by new approaches to long-standing challenges, the rise of oral macrocycles, inventive strategies to optimize PK and much more!

Which Drug Hunter case study did you enjoy most in 2025? 👇

12/26/2025

Safer CNS Drugs with BrainOnly Pharmacology | https://drughunters.com/45fPNa4
Thursday, January 22, 2026
8 AM PT | 11 AM ET | 5 PM CET

The development of CNS therapies is frequently limited by systemic toxicities, as many validated CNS targets are expressed in peripheral tissues, and their engagement outside the brain can lead to dose-limiting adverse events. Achieving brain-specific pharmacology without compromising efficacy remains a major challenge in treating neurological and psychiatric diseases.

In this Flash Talk, Nicholas Hertz will present Montara’s BrainOnly™ platform, a modular strategy designed to selectively block FKBP12-dependent drug activity outside the central nervous system. This approach employs a universal peripheral blocker, MT1110, which saturates FKBP12 binding sites in peripheral tissues and prevents FKBP12-dependent agents from adopting their active conformation outside the brain.

Nick will highlight how this platform can be applied to both naturally FKBP12-dependent molecules, such as rapalogs targeting mTOR, as well as synthetic bifunctional molecules. He will discuss how this strategy enables brain-restricted pharmacology, expands the therapeutic index, and offers a generalizable solution for safer CNS drug development.

Register to learn how this unconventional strategy enables selective targeting of the brain: https://drughunters.com/45fPNa4

12/23/2025

Drug Hunter’s November picks spotlight ganaplacide/lumefantrine (GanLum), Novartis and Medicines for Malaria Venture’s non-artemisinin combo that matched Coartem in Ph. 3 while targeting resistant P. falciparum and blocking transmission; asundexian, Bayer’s oral FXIa inhibitor that cut recurrent ischemic stroke risk on top of antiplatelet therapy without increasing major bleeding; and Q901, a highly selective CDK7 inhibitor that collapses MYC/E2F programs and resensitizes tumors to TOP1 inhibitor–based ADCs in preclinical models.

Rounding out the list:

– NG101 — Neurogastrx’s peripherally restricted D2 antagonist that significantly reduced semaglutide-induced nausea/vomiting while preserving GLP-1R agonist’s central satiety signaling
– G-6599 — Genentech’s target-anchored SMARCA2/4 degrader that co-opts FBXO22 via a covalent mechanism
– olverembatinib — Ascentage Pharma’s multikinase inhibitor with benchmark clinical benefit and prolonged PFS in TKI-refractory, SDH-deficient GIST
– INVA8001 — Invea Therapeutics' highly selective chymase inhibitor that dampens mast cell–driven inflammation, fibrosis, and biliary senescence in PSC models
– MKP10241 — Mankind Pharma’s GPR119 agonist that improves glycemia, weight, lipids, and MASH in preclinical models and has now entered Ph. 1
– ontunisertib — Agomab Therapeutics’ GI-restricted ALK5 inhibitor with encouraging Ph. 2a signals in fibrostenosing Crohn’s and the potential to become a first-in-class anti-fibrotic in this setting
– DLG-41 — a GAS41 YEATS-domain inhibitor that selectively impairs nSCLC cell growth and validates a new epigenetic reader target

Read the full article to explore the molecules that made our November 2025 list.

Full article: https://drughunters.com/4shCQGW

12/22/2025

Antibiotic Gepotidacin (Blujepa®) Gets Expanded Use for Gonorrhea | https://drughunters.com/4pPuPqL

Gepotidacin is an oral bacterial type II topoisomerase inhibitor that was approved in March 2025 for uncomplicated UTIs (Blujepa®) and in December 2025 for gonorrhea.

The compound is a dual inhibitor of bacterial DNA gyrase and topoisomerase IV, a shared target of fluoroquinolone antibiotics, but its distinct binding mode and mechanism of action help it overcome fluoroquinolone resistance mechanisms.

Gepotidacin approval was the first new class of antibiotics for UTIs and gonorrhea in nearly three decades. One day after its expanded use approval, fellow type II isomerase inhibitor zoliflodacin (Nuzolvence®) was also approved for gonorrhea, together positioned to help combat the crisis of MDR gonococcal infections.

Read it on Drug Hunter: https://drughunters.com/4pPuPqL

12/22/2025

Prodrug Playbook: A Practical Drug Hunter Workflow | https://drughunters.com/44CcTHN
Tuesday, January 13th, 2026
8 AM PT | 11 AM ET | 5 PM CET

Prodrugs are a well-established strategy to improve the physicochemical, biopharmaceutical, and pharmacokinetic properties of drug candidates, including solubility, permeability, metabolic stability, and oral bioavailability.

Join our upcoming session to explore practical workflows using Drug Hunter’s tools to:
👉Understand when and why prodrug strategies are applied in drug discovery
👉Survey the most commonly used prodrug approaches and design principles
👉Analyze recent patent highlights to uncover emerging trends and successful precedents

Join us live and bring your questions on when and how prodrug strategies can unlock better drug candidates.

Sign up here to secure your spot: https://drughunters.com/44CcTHN

12/19/2025

November 2025 Patent Highlights

Each month, the Drug Hunter team reviews thousands of IP disclosures to curate the patents and applications most likely to move the field. From our annotated patent search table (updated weekly), we translate standout filings into practical takeaways: what was claimed, what the molecules look like, and why it matters for therapeutic strategy.

November 2025 Patent Highlights span targeted protein degradation and hard-to-drug signaling nodes:
• Captor Therapeutics: CRBN-based NEK7 degraders
• Daiichi Sankyo: SF1 antagonists and SF1–targeting heterobifunctional degraders
• Kymera Therapeutics: small-molecule STAT6 inhibitors
• SiteOne Therapeutics: NaV1.8 inhibitors for pain
• Lilly: non-peptide amylin and/or calcitonin receptor agonists, as the field searches for credible oral alternatives to peptide DACRAs

If you’re tracking emerging chemotypes, modality shifts, and competitive IP signaling, this month’s patent highlights are a must-read.

Read it on Drug Hunter: https://drughunters.com/4j2qmOU

12/18/2025

Targeting NLRP3: DFV890 and Beyond | https://drughunters.com/3MIfI3U

Inhibiting the NLRP3 inflammasome has attracted significant interest over the past decade, due to its therapeutic potential to treat oncological, cardiovascular, immunological, and neurodegenerative diseases.

In this article, we discuss Novartis’ multi-generation medicinal chemistry campaign to develop small-molecule NLRP3 inhibitors for both peripheral and neurological immune disorders. The quest began with Pfizer’s MCC950 and progressed to the clinically advanced DFV890, which incorporates a unique sulfonimidamide motif designed to reduce hydrolysis compared to the sulfonylurea commonly found in earlier inhibitors.

Pushing beyond known chemotypes, an imaging-based pyroptosis-protection HTS, combined with a scaffold morphing exercise, led to the identification of a novel class of pyridazine phenols and the discovery of NP3-253, a potent, selective, and brain-penetrant NLRP3 inhibitor.

Read it on Drug Hunter: https://drughunters.com/3MIfI3U

12/17/2025

Mirdametinib: Rescuing a Shelved MEK Inhibitor for NF1 Plexiform Neurofibromas | https://drughunters.com/4pM42vI

Mirdametinib (Gomekli®) is an oral, brain-penetrant MEK1/2 inhibitor that received FDA approval in February for adults and children with NF1-PN (neurofibromatosis type 1–associated plexiform neurofibromas).

The approval was based on the Ph. 2b ReNeu trial, where 52% of children and 41% of adults achieved ≥20% tumor volume reduction. Among responders, more than half of patients saw >50% tumor shrinkage.

Mirdametinib is the second MEK inhibitor approved for this rare disease, following selumetinib (Koselugo®), which was first approved for pediatric NF1-PN in 2020 and expanded in 2025 to include adults.

Read more on Drug Hunter: https://drughunters.com/4pM42vI

12/16/2025

Fenebrutinib: A Reversible, CNS-Active BTK Inhibitor With Positive Phase 3 Results in MS Approaching a Potential NDA Filing | https://drughunters.com/4qhLPpM

Fenebrutinib (GDC-0853) is a reversible, non-covalent BTK inhibitor from Roche/Genentech that has delivered positive results in the first readout from a trio of pivotal Ph. 3 trials in MS.

These late-stage results build on Roche’s September 2024 report from the Ph. 2 FENopta trial in RMS, where 96% patients treated with fenebrutinib were relapse-free at one year and showed no change in disability over 48 weeks. Taken together, the data have been described as “unprecedented” and suggest that fenebrutinib could become a “best-in-disease” medicine as the first high-efficacy, oral treatment option for people with either RMS or PPMS.

This article reviews the unique properties of fenebrutinib, including its long residence time, potential brain pe*******on, and highlights from its discovery and development now spanning over a decade.

Read it on Drug Hunter: https://drughunters.com/4qhLPpM

12/15/2025

Patenting Strategies for Small Molecule Drugs | https://drughunters.com/4iYqIGd

In December 2025, the Federal Circuit invalidated Seagen’s patent for inadequate written description, saving Daiichi Sankyo and AstraZeneca an estimated $640 million in potential royalties and removing a major legal uncertainty surrounding Enhertu®.

Drug development is shaped by high R&D costs, stringent regulatory hurdles, and intense competitive pressure. In this environment, robust patent protection is essential to justify and sustain investment in innovative medicines.

In this article, we review the fundamentals of patent law with a focus on the core requirements for patentability — utility, novelty, non-obviousness, and sufficient enablement and written description — and examine how these standards shape effective life-cycle patent strategies.

Read it on Drug Hunter: https://drughunters.com/4iYqIGd

12/15/2025

In this Year-End Special Flash Talk, Dennis Koester presented the scientific trends and breakthroughs defining the 2024 Molecule of the Year candidates.

Across 2024’s standout molecules, Dennis highlighted how oral small molecules and macrocyclic peptides are increasingly competing with mAbs in traditionally biologics-dominated targets, including PCSK9 and IL-23R. These examples show how advances in screening, structural biology, and medicinal chemistry are expanding the druggable targets space for small molecules.

A major highlight was the FDA approval of suzetrigine, the first new pain drug class in over 20 years. Vertex’s highly selective NaV1.8 inhibitor offers a non-addictive alternative to opioids and marks a milestone in an area of high unmet need. Beyond pain, 2024 also delivered progress against historically difficult targets, including WRN helicase, mutant KRAS, and others.

Another defining trend was the rapid maturation of induced proximity modalities, moving from early proof-of-concept into clinically validated strategies. From monovalent degraders like inavolisib (PI3Kα) to heterobifunctional and CNS-penetrant degraders outside of oncology, these programs highlight increasingly differentiated pharmacology and selectivity.

Watch the full Flash Talk on our YouTube channel to explore these trends in depth: https://drughunters.com/4iX97yC

12/12/2025

A Compendium of Pharmaceutically Used Salts to Help Flavor Your Drug Formulation | https://drughunters.com/4iTyH7D

The Drug Hunter data team presents a curated overview of ‘inactive’ salts used in drug products. Many drugs are formulated as salts, which have a dramatic effect on pharmacokinetic profile. Therefore, choosing the correct counterion in a salt formulation is essential for development candidate selection.

Here, we show a hierarchical organization of salt counterions across drugs, along with acid/base properties and molecular class as well as their relative usage across FDA drug approvals.

Read it on Drug Hunter: https://drughunters.com/4iTyH7D

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