Enhanced Selective Inhibitors of Exon 20 Insertion Mutant EGFR for Cancer Treatment

Publication ID: 24-11857513_0006_PTD
Published: October 28, 2025
Category:Direct Improvements & Enhancements

Legal Citation

pr1or.art Inc., “Enhanced Selective Inhibitors of Exon 20 Insertion Mutant EGFR for Cancer Treatment,” Published Technical Disclosure No. 24-11857513_0006_PTD, Published October 28, 2025, available at https://archive.pr1or.art/24-11857513_0006_PTD
This technical disclosure describes improvements that would be readily apparent to a Person Having Ordinary Skill In The Art (PHOSITA) when considered in combination with the foundational architecture disclosed in U.S. Patent No. 11,857,513.

Summary of the Inventive Concept

This inventive concept presents a series of improvements and enhancements to the original selective inhibitor of exon 20 insertion mutant EGFR, offering targeted delivery, reduced systemic toxicity, and improved bioavailability for more effective cancer treatment.

Background and Problem Solved

The original patent disclosed a method for treating malignant lung tumors using a selective inhibitor of exon 20 insertion mutant EGFR. However, the original patent had limitations in terms of systemic toxicity and bioavailability. This new inventive concept addresses these limitations by introducing targeted delivery systems, improved formulations, and enhanced detection methods.

Detailed Description of the Inventive Concept

The new claims introduce a system for treating EGFR-related cancers, comprising a selective inhibitor of exon 20 insertion mutant EGFR formulated for targeted delivery to tumor cells with reduced systemic toxicity. Additionally, a method for identifying patients likely to respond to EGFR-targeted therapy is disclosed, which involves detecting the presence of exon 20 insertion mutations in EGFR and selecting patients with such mutations for treatment. Furthermore, a pharmaceutical composition with enhanced bioavailability and a kit for diagnosing EGFR-related cancers are also presented.

Novelty and Inventive Step

The new claims introduce the concept of targeted delivery and improved formulations, which are not obvious from the original patent. The inventive step lies in the combination of the selective inhibitor with targeted delivery systems and improved formulations, resulting in reduced systemic toxicity and improved bioavailability.

Alternative Embodiments and Variations

Alternative embodiments of the inventive concept could include using different types of targeted delivery systems, such as nanoparticles or liposomes, or combining the selective inhibitor with other anti-cancer agents. Variations of the pharmaceutical composition could include different carrier molecules or excipients to further enhance bioavailability.

Potential Commercial Applications and Market

The enhanced selective inhibitors of exon 20 insertion mutant EGFR have significant commercial potential in the cancer treatment market, particularly in the area of non-small cell lung cancer (NSCLC). The targeted delivery system and improved formulations could provide a competitive advantage in the market, and the diagnostic kit could also generate revenue through sales to research institutions and hospitals.

CPC Classifications

SectionClassGroup
A A61 A61K31/519
A A61 A61P35/00

Original Patent Information

Patent NumberUS 11,857,513
TitleSelective inhibitor of exon 20 insertion mutant EGFR
Assignee(s)TAIHO PHARMACEUTICAL CO., LTD.