Drug intelligence / Profile preview

xzp-5809

Development stage
Discontinued
Lead developer
Sihuan Pharmaceutical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

XZP-5809 is a novel third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) developed as a targeted therapy for non-small cell lung cancer (NSCLC) with EGFR mutations, particularly those harboring the T790M resistance mutation. It is designed to irreversibly bind to mutant forms of EGFR, including exon 19 deletion, L858R mutation, and the acquired resistance T790M mutation. XZP-5809 demonstrates higher activity against gene-mutated EGFR and lower activity against wild-type EGFR, aiming to improve efficacy while reducing off-target effects. The drug is orally administered and has shown promising preclinical safety and efficacy profiles. Its primary indication is for patients with locally advanced or metastatic NSCLC who have progressed after prior treatment with first or second-generation EGFR-TKIs[1][2][3][7].

Other names
egfr inhibitor xzp-5809 tartrate
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)

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