Drug intelligence / Profile preview

BPI-15086

Development stage
Phase 1
Lead developer
Betta Pharmaceuticals
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

BPI-15086 is an orally available, third-generation, ATP-competitive, irreversible small molecule inhibitor that selectively targets mutant forms of the epidermal growth factor receptor (EGFR), including the T790M resistance mutation. It is designed to overcome acquired resistance to earlier EGFR tyrosine kinase inhibitors (TKIs) in patients with non-small cell lung cancer (NSCLC) who have developed the T790M mutation after prior EGFR-TKI therapy. The drug has demonstrated safety and tolerability in phase I clinical trials and shows potential antineoplastic activity by inhibiting EGFR signaling pathways critical for tumor cell proliferation and survival[1][3][5].

02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)

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