Application of medicine capable of simultaneously targeting tyrosine kinase activity of EGFR (Epidermal Growth Factor Receptor) and GEF activity

By simultaneously targeting the tyrosine kinase activity and GEF activity of EGFR, especially by regulating its 804th glutamate residue, the high drug resistance of existing EGFR inhibitors is solved, achieving highly effective treatment of EGFR-driven tumors.

CN121466293APending Publication Date: 2026-02-06SUN YAT SEN UNIVERSITY CANCER CENTER (CANCER HOSPITAL AFFILIATED TO SUN YAT SEN UNIVERSITY CANCER RESEARCH INSTITUTE OF SUN YAT SEN UNIVERSITY) +1
0 Cites 1 Cited by

Patent Information

Application Number
CN202510419394.2
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-04-03
Publication Date
2026-02-06

AI Technical Summary

Technical Problem

Existing EGFR inhibitors primarily target its intracellular kinase domain, leading to high rates of drug resistance and failing to effectively address the resistance problem in the non-kinase-dependent pathway of EGFR.

Method used

A pharmaceutical composition is provided that simultaneously targets the tyrosine kinase activity and GEF activity of EGFR, using small molecule compounds, nanomaterials, or gene editing technology to inhibit the kinase activity and GEF activity of EGFR, particularly by acting on the 804th glutamate residue of EGFR to regulate the nucleotide exchange of Rheb to inhibit the mTORC1 signaling pathway.

Benefits of technology

It effectively inhibits EGFR-driven tumor growth, especially in cancers such as lung cancer, colon cancer, and breast cancer, reduces drug resistance, and provides a more precise, efficient, and safe treatment strategy.

✦ Generated by Eureka AI based on patent content.
Patent Text Reader

Abstract

The invention provides application of an EGFR (epidermal growth factor receptor) inhibitor in preparation of a medicine for treating diseases mediated by the activity of a guanylate exchange factor (GEF) or jointly mediated by the activity of the guanylate exchange factor (GEF) and the activity of EGFR tyrosine kinase. The diseases are cancers selected from the following groups: lung cancer, colon cancer, breast cancer, endometrial cancer, thyroid cancer, glioma, squamous cell carcinoma, prostate cancer, melanoma, leukemia and glioblastoma. Specifically, the invention discovers that EGFR has a GEF function for promoting activation of Ras homologous protein (Rhb) besides traditional tyrosine kinase activity, the function does not depend on the tyrosine kinase activity and plays a key role by depending on a glutamic acid residue at the 804th site on an EGFR molecule, the Rhb-GEF activity of EGFR causes allosteric activation of a mammal rapamycin target protein complex 1 (mTORC1), and the activity of the EGFR causes allosteric activation of the mammal rapamycin target protein complex 1 (mTORC1). The tumor growth is finally promoted.
Need to check novelty before this filing date? Find Prior Art