Drug intelligence / Profile preview

ANS014004

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

Overview

ANS014004 is a novel, orally bioavailable small-molecule type II c-Met tyrosine kinase inhibitor (TKI) developed by Avistone Biotechnology. It selectively targets and binds to the inactive state of the c-Met receptor (DFG-out conformation) in the ATP pocket, inhibiting its activity—including various oncogenic MET alterations such as MET exon 14 skipping mutations, MET amplification, overexpression, and fusion. ANS014004 is designed to overcome resistance mechanisms that limit current type I c-Met inhibitors by targeting additional acquired mutations (e.g., D1228 and Y1230). The drug is currently being evaluated in Phase 1 clinical trials as monotherapy for patients with locally advanced or metastatic solid tumors harboring pathogenic MET alterations.

02

Targets

MET (Mesenchymal-epithelial transition factor receptor)

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