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sapitinib
- Development stage
- Phase 2
- Lead developer
- AstraZeneca
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Sapitinib is an oral, reversible, and equipotent small molecule inhibitor of the epidermal growth factor receptor (EGFR) family, specifically targeting EGFR (ErbB1), HER2 (ErbB2), and HER3 (ErbB3) tyrosine kinases. By competitively inhibiting ATP binding to these receptors, sapitinib blocks downstream signaling pathways involved in cellular proliferation and angiogenesis. This mechanism underlies its potential antineoplastic activity in tumors expressing erbB family receptors. Sapitinib has demonstrated potent inhibition of EGF-driven cellular proliferation in preclinical models and has been evaluated in clinical trials for various cancers including breast cancer, colorectal cancer, gastric cancer, and non-small cell lung carcinoma[1][2][3][4][6]. The drug was developed by AstraZeneca.
- Brand names
- sapitinib
- Other names
- Sapitinib [INN]Sapitinib [WHO-DD]sapitinibumSapatinibErbB Kinase Inhibitor AZD8931
02
Targets
EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB3 (Erb-b2 receptor tyrosine kinase 3)
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