Apatinib

Not to be confused with afatinib or lapatinib.
Apatinib
Clinical data
Other namesRivoceranib; YN968D1
Routes of
administration		Oral
ATC code
  • none
Identifiers
  • N-(4-(1-Cyanocyclopentyl)phenyl)-2-((pyridin-4-ylmethyl)amino)nicotinamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC24H23N5O
Molar mass397.482 g·mol−1
3D model (JSmol)
  • N#CC1(c2ccc(NC(=O)c3cccnc3NCc3ccncc3)cc2)CCCC1
  • InChI=1S/C24H23N5O/c25-17-24(11-1-2-12-24)19-5-7-20(8-6-19)29-23(30)21-4-3-13-27-22(21)28-16-18-9-14-26-15-10-18/h3-10,13-15H,1-2,11-12,16H2,(H,27,28)(H,29,30) checkY
  • Key:WPEWQEMJFLWMLV-UHFFFAOYSA-N checkY
  (verify)

Apatinib, also known as rivoceranib, is a tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor-2 (VEGFR2, also known as KDR). It is an orally bioavailable, small molecule agent which is thought to inhibit angiogenesis in cancer cells; specifically, apatinib inhibits VEGF-mediated endothelial cell migration and proliferation thus blocking new blood vessel formation in tumor tissue. This agent also mildly inhibits c-Kit and c-SRC tyrosine kinases.[1]

Apatinib was first synthesized by Advenchen Laboratories in California, USA and licensed out global rights to HLB (Korea) in 2020 and is being developed by Jiangsu Hengrui Medicine (China), LSK BioPartners (US) and HLB Life Science (Korea).[2] It is an investigational cancer drug currently undergoing clinical trials as a potential targeted treatment for metastatic gastric carcinoma, metastatic breast cancer, adenoid cystic carcinoma, and advanced hepatocellular carcinoma.

  1. ^ "Rivoceranib mesylate". National Cancer Institute. 2011-02-02. Retrieved 2023-06-24.
  2. ^ "Apatinib Mesylate (YN968D1)". LSK BioPartners. Archived from the original on 2011-07-13.