Drug intelligence / Profile preview

YH42946

Development stage
Phase 2
Lead developer
Yuhan
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

YH42946 is a novel, orally available small molecule tyrosine kinase inhibitor that targets HER2 (also known as receptor protein-tyrosine kinase erbB-2) and EGFR exon 20 insertion mutations. It has demonstrated potency against diverse HER2 aberrations—including overexpression, amplification, and mutation—as well as activity against EGFR exon 20 insertions. Preclinical studies showed strong efficacy in both in vitro and in vivo models for tumors with these genetic alterations. The drug is being developed primarily for the treatment of locally advanced or metastatic solid tumors with HER2 aberrations or EGFR exon 20 insertions, including non-small cell lung cancer (NSCLC). The developer is Yuhan Corporation; the compound originated from Jintz Bio.

Other names
JIN-A04JIN-A-04JIN-A 04
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)Epidermal growth factor receptor (EGFR) exon 20 insertion mutant

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