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epitinib
- Development stage
- Phase 1
- Lead developer
- HUTCHMED
- 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
Epitinib is an orally active, selective small molecule inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It is specifically designed for optimal penetration of the blood-brain barrier and has demonstrated potent inhibitory effects on EGFR-mutant tumors in preclinical and clinical studies. Epitinib has shown promising efficacy in patients with non-small cell lung cancer (NSCLC) harboring EGFR mutations and brain metastases, as well as being investigated for glioblastoma with EGFR gene amplification. The drug exhibits a favorable safety profile consistent with other EGFR-TKIs and is under development primarily by Hutchison China MediTech (Chi-Med)[2][3][4][5][7][8].
- Other names
- epitinibHMPL-813HMPL813HMPL 813
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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