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larotinib
- Development stage
- Phase 2
- Lead developer
- Sunshine Lake Pharma
- 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
Larotinib is a first-generation, orally active, small molecule tyrosine kinase inhibitor that targets the epidermal growth factor receptor (EGFR) and other members of the ErbB family, including HER2. It acts as a reversible pan-ErbB inhibitor with antineoplastic activity. Larotinib has demonstrated promising antitumor activity and manageable safety profiles in patients with advanced esophageal squamous cell carcinoma (ESCC) exhibiting EGFR overexpression or amplification who have been previously treated. Preclinical studies indicate high selectivity for EGFR kinase and favorable tumor tissue penetration. Clinical trials have also explored its use in metastatic pancreatic cancer and other advanced solid tumors[1][2][3][4][7].
- Brand names
- Dongningguan
- Other names
- larotinib mesylate
02
Targets
EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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