Drug Hunter, Palo Alto, CA (2026)

02/26/2026

January 2026 Patent Highlights | https://drughunters.com/4seZHBX

January 2026 Patent Highlights are live!

Each month, the Drug Hunter team screens thousands of newly published IP disclosures and selects a short list of the most impactful applications shaping drug discovery.

This month, we cover Triana’s ALK degraders, Nxera’s EP4 antagonist, Ferro Therapeutics’ alkyne-warhead GPX4 inhibitors targeting ferroptosis biology, Eli Lilly’s small molecule GCGR agonists, as well as parallel TMEM175 modulator filings from Expert Systems and Genentech that expand the lysosomal ion-channel landscape in neurodegeneration.

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

02/25/2026

Dotinurad: a ‘Next-Gen’ Uricosuric Looking to Crack the US Gout Market | https://drughunters.com/4aVBRUU

Dotinurad (FYU-981) is a URAT1 inhibitor approved for gout/hyperuricemia in Japan and China (Urece®) and is now in late-stage development in the US.

By blocking renal proximal-tubule uric acid reabsorption, dotinurad increases urinary urate excretion and lowers serum urate, the key biochemical driver of gout.

The molecule was optimized from the historical uricosuric benzbromarone in an effort to retain urate-lowering efficacy while reducing instances of rare but serious hepatotoxicity.

Building on its clinical experience overseas, Crystalys has initiated two Ph. 3 trials benchmarking dotinurad against first-line gout treatment allopurinol, with primary completion expected in late 2027.

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

02/24/2026

Lysine Targeting: A Next-Generation Option for Covalent Inhibitors | https://drughunters.com/4aUcymd

Since the FDA approval of afatinib and ibrutinib in 2013, cysteine-targeted covalent inhibitors have become an important strategy in drug discovery. However, cysteines are scarce, mutation-prone thiols, so medicinal chemists are now turning to catalytic lysines because they are more abundant, functionally essential, and often harder for tumors to “escape” by mutation.

A growing toolkit of lysine-reactive warheads is enabling selective covalent engagement across kinases and beyond. From chemoproteomic probes that can map ligandable lysines at scale, to lysine targeting small molecule inhibitors moving toward clinical development, this review highlights the emerging capabilities afforded by lysine-targeting.

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

02/24/2026

How to Use Drug Hunter: A Medicinal Chemist’s Guide to Tox Risk Mitigation | https://drughunters.com/4rIy4Bp
Tuesday, March 10th, 2026
8 AM PT | 11 AM ET | 5 PM CET

Preclinical safety remains one of the most common causes of project failure in early drug discovery. While most teams routinely screen for hERG, CYPs, and other standard liabilities, unexpected toxicities continue to derail promising programs often late, and at great expense. Many of these risks are hidden in case studies, patents, and conference disclosures rather than clearly spelled out in the peer-reviewed literature.

In this webinar, we will discuss how Drug Hunter can be used to proactively identify and contextualize toxicity risks, uncover mechanistic insights behind historical program failures, and design smarter backup strategies before entering DRF and IND-enabling studies. We will demonstrate how to leverage curated case studies to spot red flags early.

Join us live and bring your questions on tox risk mitigation, design strategies, and how to avoid the late-stage surprises that kill otherwise great molecules.

Sign up here: https://drughunters.com/4rIy4Bp

02/23/2026

In this Flash Talk, Stahl highlighted the skill of molecular storytelling and the difference between storytelling and data analysis. A drug discovery story will often take the form of a tree, with the hits representing the roots and subsequent SAR leading to the molecules that make up various branches, each of which is an important teaching moment in the story.

Martin shared examples where individual data points were used to inspire the design of the next compound and ultimately overcome the compound-related challenges. For example, importance of understanding amine basicity in order to improve compound properties in the discovery of risdiplam or the distribution of polarity to reduce lipophilicity while maintaining permeability in the discovery of HRO761.

If you are interested in the art of molecular storytelling and the importance of placing SAR into the context of a broader set of data, watch the full Flash Talk on our YouTube channel to get inspired: https://drughunters.com/4aZ6YzX

02/23/2026

Target Selection Strategy | https://drughunters.com/3ZOAToo

Decisions regarding target selection vary across organizations: From well-defined practices to free-form debates, what are the considerations for selecting quality targets?

In the first lecture of the Target Identification & Validation module, we discuss the importance of reverse engineering an ideal drug product into goals for a development candidate, which are incorporated into and assessed with a screening cascade.

We will also discuss the significance of developing biomarker-driven hypotheses during discovery for both validating proof of mechanism to both increase program likelihood of success or ability to fail fast.

Happy Learning! 🎓

02/20/2026

Is Polθ A Synthetic Lethal Target That Can Overcome PARP Resistance? | https://drughunters.com/4rZH2d4

Polθ is having a moment in oncology. This review explores the underlying biology of theta-mediated end joining, why HR-deficient and PARP inhibitor-resistant tumors become dependent on POLQ, and how that dependency creates a compelling synthetic lethal opportunity.

The article also outlines two primary small molecule strategies, inhibitors of the C-terminal polymerase domain and binders of the ATPase/helicase-domain, and discusses what each approach implies for selectivity, resistance, and combination with PARP inhibitors. It also highlights compounds currently in clinical development.

The patent landscape is rapidly expanding, with dozens of composition-of-matter filings across both domains and multiple undisclosed chemotypes progressing through early trials, placing Polθ firmly in “must-watch” territory.

Read it on Drug Hunter: https://drughunters.com/4rZH2d4

02/20/2026

Dose as the Ultimate MPO Endpoint
https://drughunters.com/4rtfs8s
Thursday, March 19th, 2026
8 AM PT | 11 AM ET | 5 PM CET

Small molecule drug design is a multiparametric optimization challenge, requiring careful balancing of interconnected molecular properties to achieve the right exposure, pharmacological effect, and ultimately clinical success.

In this Flash Talk, Maurer, Vice President of Scientific Research at Pfizer, will discuss how dose predictions can help accelerate drug design and improve confidence in expected clinical performance. He will highlight the challenges of integrating dose predictions into lead optimization workflows and share strategic and technical perspectives on the current and future role in drug discovery.

If you are curious about how integrating dose predictions earlier in the design cycle can improve decision-making, streamline lead optimization, and help teams develop valuable clinical candidates, secure your spot now: https://drughunters.com/4rtfs8s

02/19/2026

The NK1R Antagonist Tradipitant Gains FDA Approval in Motion Sickness, with Promising Data in GLP-1R Agonist-Induced Nausea | https://drughunters.com/4kI4sl7

The final FDA approval of 2025 went to Vanda’s NK1R antagonist tradipitant (Nereus®) for the treatment of motion-induced nausea and vomiting.

While the value of NK1R antagonists as antiemetics is well established, tradipitant is the first new drug to be approved for motion sickness in over 40 years.

This approval marks a major win for Vanda, but it is the recent positive Ph. 2 data for tradipitant in mitigating GLP-1R agonist-induced nausea and vomiting that may hint at the true potential of this molecule.

Read it on Drug Hunter: https://drughunters.com/4kI4sl7

02/18/2026

Aceclidine’s Second Act: From a 1970s Glaucoma Drug to FDA-Approved Presbyopia Drop | https://drughunters.com/4aVo1Tr

Aceclidine (Vizz®) is a predominantly pupil-selective muscarinic agonist approved in 2025 as an ophthalmic solution for presbyopia (age-related near-vision loss). It improves near vision by inducing miosis—primarily via the iris sphincter—with minimal ciliary muscle stimulation, leveraging a “pinhole” depth-of-focus effect.

The approval was supported by the Ph. 3 CLARITY program, where once-daily aceclidine delivered clinically meaningful gains in near vision without loss of distance visual acuity.

The compound is fast-acting with potentially greater tolerability than approved pilocarpine- and carbachol-based eye drops. Originally marketed for glaucoma in Europe decades ago, aceclidine was advanced for presbyopia by LENZ Therapeutics (formerly Presbyopia Therapies).

Read more on Drug Hunter: https://drughunters.com/4aVo1Tr

02/18/2026

In this Flash Talk, Julia Minitti and Deborah Smith shared the complex IP strategies required to effectively protect ADCs. They discussed how the modular nature of ADCs creates opportunities and challenges for patentability, particularly with respect to written description and enablement requirements.

Through a discussion of claim strategies, including full composition claims, component-focused claims, and intermediate protections, they illustrated a roadmap to strengthen and extend protection.

They also shared key lessons from the recent Enhertu case study, offering practical guidance on filing strategy, ownership considerations, and freedom-to-operate analysis.

If you are working on ADCs or thinking about lifecycle management early in development, watch the full Flash Talk on our YouTube channel to get inspired: https://drughunters.com/4qGoDRG

02/17/2026

Safer CNS Drugs with BrainOnlyTM Pharmacology | https://drughunters.com/40f8N5D

Following the recent approval of therapies like Cobenfy™ and Vyalev™, there has been renewed interest in the application of fixed-dose protective agents for CNS-related diseases.

This approach pairs a drug with proven efficacy but undesirable side-effects with a peripherally-restricted compound that limits target inhibition/activation to the CNS. In this article we discuss Montara Therapeutic’s application of this approach to the treatment of TSC epilepsy via mTOR inhibition using their recently developed combination drug MTX-E1. We also cover preliminary POC data on their new induced proximity modality, BrainTACs™ and its potential for CNS-selective LRRK2 inhibition for the treatment of Parkinson’s disease.

Check out the full article on Drug Hunter: https://drughunters.com/40f8N5D

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