Drug Hunter

A trusted, independent source of curated, factual information for the drug discovery community.

08/28/2026

AI agents are often discussed in the context of molecular design, but is that where they’ll have the greatest impact on drug discovery?

Rather than molecular design, the greatest near-term opportunity for agentic AI may instead lie in automating knowledge- and time intensive-tasks—including data QC, gathering relevant literature, and identifying competitor programs—freeing drug hunters to spend more time on experimental design, hypothesis generation, and creative thinking.

We review emerging benchmarks evaluating general purpose AI agents on real scientific workflows, discuss where they already outperform conventional LLMs, and examine the practical limitations—including hallucinations, citation reliability, paywalls, privacy, and the continued need for human validation—that still limit their broad adoption.

Members can read the full article here: https://drughunters.com/4zJKJsi

08/27/2026

In a milestone moment for metastatic PDAC (pancreatic ductal adenocarcinoma) treatment, Revolution Medicines’ daraxonrasib (Rasonque®) has been FDA-approved for previously treated metastatic forms of the cancer.

RAS has occupied a unique position in drug discovery and development. While it is central to oncology biology and clinically important—>90% of pancreatic cancer patients harbor RAS mutations—it has proven exceptionally challenging to drug. Daraxonrasib is an oral tri-complex molecular glue pan-RAS(ON) inhibitor designed to suppress GTP-bound RAS signaling across multiple mutants and wild-type RAS isoforms, and has fundamentally changed how the community thinks about the future of RAS-targeted therapies.

Check out our recently updated case study to find out why daraxonrasib was selected as the 2025 Drug Hunter Molecule of the Year, including:

- Why broad-spectrum RAS inhibition could be the next chapter in RAS-targeting drug discovery
- How structural elements of the compound impart its pan-RAS activity and predicted high barrier to resistance
- Key clinical successes that enabled the drug to receive Breakthrough Therapy designation and a National Priority Voucher from the FDA

Check out the full article on Drug Hunter: https://drughunters.com/4xyPK5p

08/26/2026

ACS Fall 2026 – First Time Disclosures | Open Access Article | https://drughunters.com/45PDkdm

The structures are here.

The First Time Disclosures sessions at ACS Fall 2026 in Chicago unveiled 13 small molecule programs spanning oncology, immunology, infectious diseases, dermatology, kidney and liver disease, and obesity.

Organized by the ACS MEDI Division and chaired by H. Rachel Lagiakos, the sessions featured:

- QuantaTherapeutics – QTX3034: a G12D-preferring, multi-KRAS allosteric inhibitor for pancreatic and colorectal cancers
- AcertaPharma / AstraZeneca – AZD3632: a menin inhibitor for myeloid malignancies
- Novartis – KFA115: a dual IKZF2/IKZF4 molecular glue degrader for advanced cancers
- Schrödinger – SGR-3515: a dual Wee1/Myt1 inhibitor for advanced solid tumors
- GenFleetTherapeutics – GFH647: a non-covalent BTK inhibitor for B cell malignancies
- VentusTherapeutics – VENT-03: a cGAS inhibitor for systemic and cutaneous lupus
- Pfizer – PF-07905428: a topical ACC inhibitor for acne vulgaris
- DeepAppleTherapeutics – DAT-003: an MRGPRX2 antagonist for mast cell-driven diseases
- BlueprintMedicines / Sanofi– BLU-808: a wild-type KIT inhibitor for chronic urticaria
- FimbrionTherapeutics / GSK – GSK3882347: a bacterial FimH antagonist for uncomplicated UTIs
- MazeTherapeutics – MZE829: an APOL1 inhibitor for APOL1-mediated kidney disease
- RectifyPharmaceuticals – RTY-406: a dual ABCB4/BSEP positive functional modulator for primary sclerosing cholangitis
- Pfizer – PF-07976016: a GIPR antagonist developed for obesity

Check out the full article for a preview of the therapeutic rationale, mechanisms of action, discovery highlights, and—of course—the structures behind each of these newly disclosed compounds.

Read more: https://drughunters.com/45PDkdm

08/25/2026

New coverage area: oligonucleotide therapeutics!

Bepirovirsen, GSK/Ionis Pharmaceuticals’ investigational A*O (antisense oligonucleotide) that targets HBV mRNA, achieved a 19% functional cure rate in Ph. 3 hepatitis B trials.

Interestingly, its efficacy is not solely reliant on HBV mRNA knockdown.

Evidence suggests bepirovirsen stimulates an immune response, a key differentiator from other programs, with broader implications for oligonucleotide drug discovery.

The drug was recently approved in Japan (Hibsago®) and is currently under FDA review for the treatment of chronic hepatitis B.

Members can read the full article here: https://drughunters.com/45JW51O

08/24/2026

Oligonucleotide therapeutics have progressed from an interesting concept to a validated drug modality, but their success has depended as much on advances in chemistry. This cheatsheet explores how modifications to the base, sugar, backbone, and conjugates have shaped today's FDA-approved oligonucleotides.

Members can read the full article here: https://drughunters.com/4cXtrOm

08/23/2026

Rethinking ERα Degradation as the Driver for SERD Efficacy | https://drughunters.com/4xhL0Bd

While SERDs have garnered success in breast cancer, the mechanistic details of SERD-mediated ERα degradation were unknown.

The recent preprint from the Winter and Thomä Labs have elucidated the proteins involved in degrading ERα. Further, through this mechanistic understanding, the study challenges the assumption in SERD development that ERα degradation is a main driver for therapeutic activity.

Instead, SERD-mediated degradation may actually be a downstream consequence rather than the primary pharmacological event.

This finding could reshape how future SERDs are optimized and evaluated.

Members can read the full article here: https://drughunters.com/4xhL0Bd

08/22/2026

BI-3406: A SOS1:KRAS Inhibitor with Potential Utility Beyond Oncology | https://drughunters.com/4xhLE1B

BI-3406 is a potent SOS1:KRAS PPI inhibitor discovered by Boehringer Ingelheim.
Designed to block SOS1-mediated conversion of KRAS from its GDP-bound “off” state to its GTP-bound “on” state, BI-3406 emerged from quinazoline HTS hit optimization that improved potency nearly 1,000-fold.

Although the compound will not enter the clinic, it shows single-agent TGI across multiple KRAS-mutant xenograft models and is a useful probe for SOS1–RAS biology, inspiring new SOS1-targeting modalities and potential applications in metabolic disease.

Read more on Drug Hunter: https://drughunters.com/4xhLE1B

08/21/2026

Atorvastatin (Lipitor®): How a Fifth-to-Market Drug Became a Blockbuster | https://drughunters.com/4zwawny

While natural products cracked open the therapeutic potential of HMGR inhibition in the early 1990’s, the synthetic atorvastatin (Lipitor®) blew the hinges off.

After LDL-C (low-density lipoprotein cholesterol) was established to be causative for atherosclerosis, pioneering natural products mevastatin and lovastatin (Mevacor®) helped establish and verify that interruption of cholesterol synthesis was therapeutically tractable, via HMGR (3-hydroxy-3-methylglutaryl-coenzyme A reductase) inhibition. Taking a chance on a pyrrole scaffold that canonical thinking could caution as “too reactive,” the Parke-Davis team optimized a clinical candidate that went on to outperform every prior on-market HMGR inhibitor head-to-head, and became the “go-to” drug for cardiovascular disease treatment and prevention.

In this month’s Classics in Drug Discovery, we revisit the origin story of atorvastatin, and dive into how the compound differentiated itself preclinically, clinically, and post-approval to enable its storied run as one of the most successful small molecules ever developed.

Check out the full story on Drug Hunter: https://drughunters.com/4zwawny

08/20/2026

Iptacopan/NVP-LNP023: A Serendipitous Structural Clue Enables Oral Factor B Inhibition | https://drughunters.com/4gLI48X

Novartis’ iptacopan/NVP-LNP023 illustrates how a strong rationale for pursuing a target can translate into broad clinical utility.
As an oral, first-in-class inhibitor of complement factor B, iptacopan selectively blocks the alternative complement pathway upstream of C3 amplification and terminal complement activation.

This mechanism has now achieved clinical translation across multiple complement-mediated diseases, with approvals in paroxysmal nocturnal hemoglobinuria, IgA nephropathy, and C3 glomerulopathy.

Read the full case study to learn how structure-guided optimization transformed an HTS-derived aminoimidazoline hit into an oral Factor B inhibitor with broad clinical relevance.

Read the full article on Drug Hunter: https://drughunters.com/4gLI48X

08/19/2026

Unsymmetrical N-substituted pyrazoles are common motifs in pharmaceuticals, yet their synthesis has long been hindered by poor regioselectivity and difficult separation of closely related isomers. A collaboration between the Levin Lab and Johnson & Johnson tackled this problem using an unconventional approach: strategic atom replacement of the sulfur atom within isothiazoles.

In this Chemistry Brief, we explore the development of this novel platform and its extension to a catalyst-controlled method that enables access to either N-aryl pyrazole regioisomer from the same starting material.

Read the full article on Drug Hunter: https://drughunters.com/4bNOtic

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