Drug Hunter

Name: Drug Hunter
Address: Palo Alto, CA, US
Telephone: +16504587087
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A trusted, independent source of curated, factual information for the drug discovery community.

10/12/2026

Reminder: Live Flash Talk this Thursday👇

The Sulfoximine Paradox: Understanding the Unique Physicochemical Properties of Secondary Sulfonamide Bioisosteres
https://drughunters.com/4jPFC47

🗓️ Thursday, Oct. 15th
⏰ 8 AM PT | 11 AM ET | 5 PM CET

Secondary sulfonamides occur in approved medicines at a far lower rate than in screening libraries. This highlights the potential for isosteres that could achieve similar interactions but with distinct properties.

In this Thursday's Flash Talk, Michael Shultz, Director in Global Discovery Chemistry at Novartis, will discuss the unique properties of sulfoximines as secondary sulfonamide isosteres. In particular, he will present the observed differences in properties such as aqueous solubility and plasma protein binding, using MMP analysis, highlighting where values like predicted logP or fu fall short.

🔗 Register now to learn more about the sulfoximine paradox: https://drughunters.com/4jPFC47

10/10/2026

Dual JAK1/TYK2 Inhibitor Brepocitinib Finds Success in Rare Autoimmune Disease | https://drughunters.com/4ybk5X4

Brepocitinib, Pfizer/Priovant Therapeutics’ dual JAK1/TYK2 inhibitor, has been FDA-approved as the first oral treatment of the rare inflammatory disease dermatomyositis. After its initial development as a candidate therapy for several major autoimmune diseases, brepocitinib was repositioned to focus on several rare immune disorders, including dermatomyositis, where it has had clinical success.

Check out our recent coverage of brepocitinib’s development to learn the therapeutic strategy behind dual inhibition of JAK1 and TYK2, and selectivity over JAK2/3; results from evaluation in major autoimmune diseases before it was strategically re-aligned to focus on several rare immune-mediated disorders; and key results from the Ph. 3 VALOR trial that enabled the approval.

Read more on Drug Hunter: https://drughunters.com/4ybk5X4

10/09/2026

Targeting ARID1B by Converting Binders Into Degraders | https://drughunters.com/3VWHsGw

ARID1B presents a synthetic lethal vulnerability in ARID1A-mutated cancers, but its size, disorder, and lack of conventional ligandable sites make it a challenging drug discovery target. Foghorn Therapeutics’ work shows how detailed characterization of ternary complex formation and degradation kinetics can turn weak binders into selective, cellularly active degraders. This discovery strategy for FHT-654 to degrade ARID1B is a useful approach for tackling difficult targets.

Read more on Drug Hunter: https://drughunters.com/3VWHsGw

10/08/2026

Dual ABCB4/BSEP Positive Functional Modulator RTY-406 Enters Phase 1 for PSC | https://drughunters.com/4rRTsFc

RTY-406 is Pharmaceuticals’ oral dual ABCB4/BSEP (ATP-binding cassette subfamily B member 4 / bile salt export pump) positive functional modulator in clinical development for PSC (primary sclerosing cholangitis), and could provide the first clinical test of this dual-target therapeutic approach.
Unveiled during the First Time Disclosures session at the ACS Fall 2026 meeting in Chicago, RTY-406 demonstrated modulation of both transporters in a PSC mouse model and in healthy cynomolgus monkeys, supporting its advancement into clinical development.

Check out our coverage of RTY-406 to learn more about its discovery, including how the Rectify team reduced the predicted human dose from >1 g BID to 53 mg QD through iterative potency, conformational, and ADME optimization.

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

10/07/2026

Leveraging Platform Innovation to Tackle Tough Targets
https://drughunters.com/4AT19Pq
Thursday, October 22nd, 2026
8 AM PT | 11 AM ET | 5 PM CET

Drug discovery is increasingly focused on biological targets once considered undruggable. In this difficult-to-drug space, success depends on understanding how the target should be modulated, identifying molecules capable of delivering the desired mechanism, and rapidly establishing confidence in their activity.

In this Flash Talk, Andrea Weston, Head of Discovery Biology and Pharmacology at Pfizer, will explore how the thoughtful integration of platform technologies can improve the probability of success against challenging targets. She will highlight how the right protein reagents and cellular models can be critical to successful lead identification, and how defining the desired mechanism of action before screening can better position programs for success. Andrea will also examine current hit-finding strategies and emerging approaches for elucidating small-molecule MoAs, sharing how these advances are collectively expanding the boundaries of druggability and creating new opportunities to discover transformative medicines. Register now to learn more about recent advances in platform technologies and their applications towards difficult-to-drug targets: https://drughunters.com/4j8F3lS

10/06/2026

Our team has spent the last few months visiting drug hunters across the globe.
These visits are how we learn more about the current challenges faced by scientists in the industry and how Drug Hunter can be used to tackle those problems! The trips are also just a good time.

And now the team going on these visits is growing. If this looks like the kind of work you are excited about, check out the link below for open roles: https://drughunters.com/4hFTzPr

10/05/2026

In this Flash Talk Georg Winter shared how TPD can serve as a tool to both disrupt and activate signaling pathways.

Despite the utilization of induced proximity strategies in clinical candidates and approved drugs, details on MoA remain unclear. Georg presented how his lab and Nicolas Thomä's worked to elucidate the MoA of SERDs like fulvestrant. He demonstrated that SERD binding induces ERα SUMOylation followed by ubiquitination and degradation mediated by STUbLs. Similar SUMOylation and immobilization mechanism were actually identified for several non-ER targeting clinical candidates.

While heterobifunctional degraders are aimed at a loss of function, Georg also presented the application of heterobifunctional molecules to reprogram rather than eliminate a target. In particular, he discussed how the heterobifunctional ligand TRIP-1 could induce ternary complex formation between SMARCA4 and BCL6 to promote the transcription of pro-apoptotic genes. In vitro data indicates that this approach can provide superior induction of apoptosis and cell death relative to BCL6 inhibition or degradation.

If you want to learn more about how a detailed MoA understanding can inspire the next generation of induced proximity drugs, watch the full Flash Talk on our YouTube channel: https://drughunters.com/4y302Kw

10/04/2026

The application of biocatalysis in drug discovery has seen a rapid rise in recent years, propelled by improvements in, and accessibility to, technologies like directed evolution.

In our review of biocatalysis in process development, we detail the general ways in which biocatalysts have been integrated and their relevant advantages compared to traditional chemosynthetic methods.

Read our article to learn more about the evolving roles of biocatalysts in process-scale manufacturing: https://drughunters.com/4hqWdd9

10/02/2026

This month’s Drug Hunter Patent Gazette showcases novel approaches to four unique drug discovery targets:

- AstraZeneca’s first disclosure of KRAS(G13D) inhibitors
- Activators of KCC2 from three companies looking at both CNS and metabolic disease indications
- Mutant-selective PI3Ka inhibitors from PIKavation may shine light on the multibillion-dollar deal the company signed with Novartis in February 2026
- APJ agonists from Roche that look to succeed in metabolic disease where multiple companies have fallen short in cardiorenal disease

These disclosures highlight potential first-in-class and best-in-class molecules, an apparent pivot to a new indication for a well-known CNS target, multiple novel approaches to metabolic disease, and interesting scaffolds in the KRAS space!

Read the August 2026 Patent Gazette on Drug Hunter: https://drughunters.com/47xYj4Y

10/01/2026

VENT-03 (Iptocigistat), a Potential Oral Therapy for Lupus and Other Type 1 Interferonopathies | https://drughunters.com/46S71uP

VENT-03 is an oral inhibitor of cGAS, currently in Ph. 2 trials for SLE. Preclinically, VENT-03 demonstrates dose-dependent reductions of cGAMP levels as well as reductions in relevant inflammatory biomarkers, with a PK profile supporting once-daily dosing.

While other small molecule assets are currently under clinical evaluation, VENT-03 will provide the first readout on the clinical efficacy of cGAS inhibition in lupus.

Read more on Drug Hunter: https://drughunters.com/46S71uP

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