Quinazoline carboxamide azetidine compounds for use in treating hormone dependent diseases

A quinazoline carboxamide azetidine compound combined with a SERD like elacestrant addresses endocrine resistance in ER+ breast cancer by re-sensitizing tumors, enhancing treatment efficacy in patients with mutated ESR1.

AU2025220299A1Pending Publication Date: 2026-07-16EVEXTA BIO
View PDF 0 Cites 0 Cited by

Patent Information

Authority / Receiving Office
AU · AU
Patent Type
Applications
Current Assignee / Owner
EVEXTA BIO
Filing Date
2025-02-05
Publication Date
2026-07-16

AI Technical Summary

Technical Problem

Existing endocrine therapies for estrogen receptor-positive (ER+) breast cancer are often ineffective due to resistance mechanisms, such as mutations in the Estrogen Receptor 1 (ESR1) gene and alterations in signaling pathways, leading to treatment failure and recurrence in most patients.

Method used

A combination therapy involving a quinazoline carboxamide azetidine compound, such as 4-[(S)-2-Azetidin-1-yl-1-(4-chloro-3-trifluoromethyl-phenyl)-ethylamino]-quinazoline-8-carboxylic acid amide (M2698), preferably with a Selective Estrogen Receptor Degrader (SERD) like elacestrant, to sensitize ER+ cancerous tumors resistant to endocrine therapy.

Benefits of technology

The combination therapy effectively re-sensitizes ER+ tumors to endocrine treatment, improving progression-free survival and overall survival in patients with ER+ breast cancer, particularly those with mutated ESR1 tumors.

✦ Generated by Eureka AI based on patent content.

Smart Images

  • Figure 00000095_0000
    Figure 00000095_0000
  • Figure 00000096_0000
    Figure 00000096_0000
  • Figure 00000097_0000
    Figure 00000097_0000
Patent Text Reader

Abstract

The present invention relates to a quinazoline carboxamide azetidine compound, and to pharmaceutical combinations and compositions comprising such a compound preferably together with at least one distinct therapeutic agent, preferably anti-cancer agent, as well as to uses thereof for treating a disease, preferably a cancer, even more preferably estrogen receptor-positive (ER+) cancer, in particular in a subject resistant to endocrinal therapy.
Need to check novelty before this filing date? Find Prior Art