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apatinib
- Development stage
- Unknown
- Lead developer
- Hengrui Pharmaceutical
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Apatinib (also known as rivoceranib) is an orally bioavailable, small-molecule tyrosine kinase inhibitor that selectively targets vascular endothelial growth factor receptor-2 (VEGFR-2). Originally developed by Jiangsu Hengrui Pharmaceuticals, it is approved in China for the treatment of advanced gastric adenocarcinoma and metastatic hepatocellular carcinoma. In the specific context of research conducted by West China Hospital, apatinib is being investigated in combination with platinum-based doublet chemotherapy (pemetrexed plus cisplatin or carboplatin) as a first-line treatment for patients with advanced EGFR wild-type non-squamous non-small cell lung cancer (NSCLC). Its mechanism involves inhibiting tumor-induced angiogenesis by blocking the VEGF/VEGFR-2 signaling pathway, which is critical for tumor growth and progression. The combination regimen aims to enhance antitumor efficacy by combining anti-angiogenic therapy with standard cytotoxic chemotherapy.
- Brand names
- AiTan
- Other names
- apatinib mesylaterivoceranib
02
Targets
PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR-1 (Vascular endothelial growth factor receptor 1)SRC (Proto-oncogene tyrosine-protein kinase Src)KIT (c-KIT proto-oncogene receptor tyrosine kinase)RET (Rearranged during transfection receptor tyrosine kinase)
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