Drug Hunter, Palo Alto, CA (2026)

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

09/30/2026

The definition of what is “druggable” is a moving target. Yesterday, over 400 attendees at Boston DOT spent an hour hearing from the leaders who are redefining it.

Discovery on Target's first-ever plenary panel brought together Erin Davis (BMS), Ryan Potts (Amgen), John Tallarico (Novartis), Klaus Urbahns (Biogen), Andrea Weston (Pfizer), and Ian Storer (AstraZeneca) to talk through a modality-agnostic approach to hard targets. They covered chimeras, conjugates, peptides, radioligands, and knowing when to reach for which.

Drug Hunter’s own Dennis Hu was honored to moderate such a powerful discussion. Thank you to each of the panelists for sharing their time and expertise.

This topic sits at the center of why Drug Hunter exists.

With the explosion of new capabilities, nearly every pharma R&D site in the world is wrestling with the same questions:

- What targets should we go after?
- Which modalities should we apply?
- How do we prioritize?
- How do we make confident decisions with limited resources?

Those decisions are only as good as the intelligence behind them.

09/29/2026

Molecules of the Month – August 2026 | https://drughunters.com/4hygw78

Drug Hunter’s August picks spotlight rusfertide, Protagonist Therapeutics’ hepcidin mimetic now FDA-approved for polycythemia vera; AstraZeneca’s AZD5462, an oral, allosteric RXFP1 agonist; and a metabolically activated molecular glue that relies on DCAF11 to recruit and degrade DDX18 and provides a new warhead for targeted protein degradation.

Rounding out the list:

– AUT00206 — Autifony Therapeutics’ Kv3.1/3.2 positive modulator aimed at treatment of the cognitive and negative symptoms of schizophrenia

– VVD-338213 — Vividion Therapeutics’ brain-penetrant, covalent NLRP3 inhibitor that engages a previously uncharacterized allosteric pocket

– TSL-1502 — a β-glucuronidase-activated PARP1/2 inhibitor prodrug designed to locally release its active inhibitor in tumors

– forvisirvat — a brain-penetrant SIRT6 activator derived from the natural product griseofulvin and advanced into clinical development for major depressive disorder

– dCASP2-3 — Amgen’s VHL-recruiting molecular glue degrader of caspase-2
– tilpisertib fosmecarbil — Gilead Sciences’ oral prodrug of the TPL2 inhibitor GS-4875, now being evaluated in ulcerative colitis

– T2-MCP-19 — Genentech and Université de Sherbrooke’s highly selective macrocyclic peptide TMPRSS2 inhibitor enabled by mRNA display and backbone modification
Read the full article to explore the molecules that made our August 2026 list.

Full article: https://drughunters.com/4hygw78

09/29/2026

Parkinson’s disease has a new targeted treatment option: tavapadon (Juvmo®), the first selective D1/D5 receptor agonist approved by the FDA for adults with Parkinson’s disease.

Originally discovered by Pfizer, tavapadon emerged from efforts to move beyond traditional catechol-based D1 receptor agonists and identify non-catechol molecules with improved physicochemical properties.

Pfizer contributed tavapadon and other neuroscience assets to Therapeutics when the company was formed with Bain Capital in 2018.

The program subsequently advanced through Ph. 2 and Ph. 3 development at Cerevel, which AbbVie acquired in 2023 in an $8.7 billion transaction centered on its broader neuroscience pipeline.

In celebration of tavapadon’s regulatory success, take a look back at our 2025 molecule case study, where we break down why non-catechol D1/D5 agonists could be important for Parkinson’s disease, the trade-offs of targeting D1/D5 receptors, and how tavapadon differentiates from other oral therapies.

Full article on Drug Hunter: https://drughunters.com/4ygFJKs

09/28/2026

Can oral small molecules challenge IL-17 biologics?
IL-17A and its receptor are clinically validated targets for inflammatory diseases, but translating the success of injectable biologics into oral small molecules has proven difficult.

Early programs such as LY3509754 established human target engagement but were halted by liver safety concerns, while newer agents including UCB6492, simepdekinra, ASC50, and ZB021 are testing whether direct IL-17 inhibition can deliver biologic-like efficacy with practical dosing and acceptable safety.

In our latest Insights article, Drug Hunter explores the promise and risks of small molecule IL-17 inhibition and the new wave of oral inhibitors now entering the clinic.

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

09/27/2026

The Sulfoximine Paradox: Understanding the Unique Physicochemical Properties of Secondary Sulfonamide Bioisosteres
https://drughunters.com/3VgqBOD
Thursday, October 15th, 2026 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 Flash Talk, Michael D. 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/4hrW4Vs

09/26/2026

Quanta’s G12D-Preferring Multi-KRAS Inhibitor QTX3034 | https://drughunters.com/47fkkFE

QTX3034 is Quanta Therapeutics’ allosteric, G12D-preferring multi-KRAS inhibitor currently in Ph. 1 development.

First disclosed at the ACS Fall 2026 First Time Disclosures session, the spirocyclic inhibitor emerged from iterative structure-based design, with the discovery team ultimately balancing sub-nanomolar potency with the oral exposure needed for clinical development.

In an ongoing Ph. 1 trial in patients with KRAS(G12D)-mutant advanced solid tumors, QTX3034 has demonstrated an early clinical signal as both monotherapy and in combination with cetuximab.

Check out our article on QTX3034 to learn about its optimization path, preliminary clinical results, and how it fits into the rapidly growing KRAS inhibitor landscape.

Read more on Drug Hunter: https://drughunters.com/47fkkFE

09/25/2026

Incyte Unveils Oral, G12D-Selective KRAS Inhibitor at ACS Chicago 2026 | https://drughunters.com/46ZXL81

At ACS Fall 2026 in Chicago, Alexander “Sasha” Sokolsky presented the structure and discovery story of INCB161734 (matching zecdarasib from INN Proposed List 135): A compelling case study in engineering oral bioavailability into a potent compound series with poor ADME properties. Zecdarasib, Incyte’s inhibitor of G12D mutations of KRAS (Kirsten rat sarcoma viral oncogene homolog), also recently began a Ph. 3 trial (NCT07522073) in combination with chemotherapy for patients with KRAS G12D-mutated metastatic PDAC (pancreatic ductal adenocarcinoma).

The G12D mutation of KRAS is extremely prevalent, estimated to account for ~20% of new cancers, and is attributed to ~45% of aggressive PDAC tumors. While two KRAS G12C mutant inhibitors, sotorasib (Lumakras®) and adagrasib (Krazati®), have been approved for several years, G12D-selective therapeutics have yet to reach that regulatory milestone.

Check out our article about zecdarasib, which includes updates from the recent conference disclosure, to learn more about Incyte’s tireless work to identify a potent, orally bioavailable G12D-selective inhibitor.

Read more on Drug Hunter: https://drughunters.com/46ZXL81

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