Discover Community Create You

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

Discovery of STX-721, a Covalent, Potent, and Highly Mutant-Selective EGFR/HER2 Exon20 Insertion Inhibitor for the Treatment of Non-Small Cell Lung Cancer.

Journal of medicinal chemistry - 13 Feb 2025

Milgram Benjamin C, Borrelli Deanna R, Brooijmans Natasja, Henderson Jack A, Hilbert Brendan J, Huff Michael R, Ito Takahiro, Jackson Erica L, Jonsson Philip, Ladd Brendon, O'Hearn Erin L, Pagliarini Raymond A, Roberts Simon A, Ronseaux Sébastien, Stuart Darrin D, Wang Weixue, Guzman-Perez Angel

Abstract excerpt

After L858R and ex19del epidermal growth factor receptor (EGFR) mutations, ex20ins mutations are the third most common class of driver-mutations in non-small cell lung cancer (NSCLC). Unfortunately, first-, second-, and third-generation EGFR tyrosine kinase inhibitors (TKIs) are generally ineffective for ex20ins patients due to insufficient mutant activity and selectivity over wild-type EGFR, leading to...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Cancer therapeutics and mechanisms

Methodology Data sources Editorial policy Privacy Delete account & data About Contact Helena Bioinformatics

Share to HER2/EGFR in Cancer Research

Share to Lung Cancer Treatments and Mutations

Source

Open in PubMed Open full text

Identifiers

PMID: 39824516
DOI: 10.1021/acs.jmedchem.4c02377
PMCID: PMC11831596

Genes

EGFR

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 23 Oct 2026.

Related research

Semantic proximity does not establish scientific evidence. Graph snapshot: 2026-09-29.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Discovery of STX-721, a Covalent, Potent, and Highly Mutant-Selective EGFR/HER2 Exon20 Insertion Inhibitor for the Treatment of Non-Small Cell Lung Cancer.PMID 39824516Read ↗

STX-721, a Covalent EGFR/HER2 Exon 20 Inhibitor, Utilizes Exon 20–Mutant Dynamic Protein States and Achieves Unique Mutant Selectivity Across Human Cancer ModelsSemantic proximity Read ↗

The current landscape, advancements, and prospects in the treatment of patients with EGFR exon 20 insertion mutations warrant scientific elucidationSemantic proximity Read ↗

Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors.Semantic proximity Read ↗

EGFR exon 20 insertion mutations in non-small cell lung cancerSemantic proximity Read ↗

Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor.Semantic proximity Read ↗

EGFR exon20 insertion mutations in non-small cell lung cancer: Clinical implications and recent advances in targeted therapies.Semantic proximity Read ↗

Discovery of YK-029A, a novel mutant EGFR inhibitor targeting both T790 M and exon 20 insertion mutations, as a treatment for NSCLC.Semantic proximity Read ↗

Therapeutic Advances in Non-Small Cell Lung Cancer Harboring EGFR Exon 20 Insertion Mutations: From Molecular Biology to Targeted Therapy.Semantic proximity Read ↗

Targeting EGFR Exon 20 Insertion Mutations in Non-small-Cell Lung Cancer: Changes in Treatment Strategies are Coming.Semantic proximity Read ↗

Structural Mechanism and Inhibitors Targeting EGFR Exon 20 Insertion (Ex20ins) Mutations.Semantic proximity Read ↗

Novel drugs targeting EGFR and HER2 exon 20 mutations in metastatic NSCLC.Semantic proximity Read ↗

Advances in the Diagnosis and Treatment of Advanced Non-Small-Cell Lung Cancer With EGFR Exon 20 Insertion Mutation.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.