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Synonyms: apatinib (in China) | YN968D1
rivoceranib is an approved drug (2014 (Chinese NMPA))
Compound class: Synthetic organic
Comment: Rivoceranib (a.k.a. apatinib) is an orally bioavailable, small-molecule multitargeted tyrosine kinase inhibitor, with substantial inhibitory action against vascular endothelial growth factor receptor-2, but it also inhibits c-Kit and c-SRC tyrosine kinases . The drug is administered as the mesylate salt (PubChem CID 45139106). Its principal clinical effect is as an angiogenesis inhibitor.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
Rivoceranib- orphan designation.
Accessed on 17/02/2021. Modified on 17/02/2021. fda.gov, https://www.accessdata.fda.gov/scripts/opdlisting/oopd/detailedIndex.cfm?cfgridkey=798720
2. Li J, Zhao X, Chen L, Guo H, Lv F, Jia K, Yv K, Wang F, Li C, Qian J et al.. (2010)
Safety and pharmacokinetics of novel selective vascular endothelial growth factor receptor-2 inhibitor YN968D1 in patients with advanced malignancies.
BMC Cancer, 10: 529. [PMID:20923544]
3. Mi YJ, Liang YJ, Huang HB, Zhao HY, Wu CP, Wang F, Tao LY, Zhang CZ, Dai CL, Tiwari AK et al.. (2010)
Apatinib (YN968D1) reverses multidrug resistance by inhibiting the efflux function of multiple ATP-binding cassette transporters.
Cancer Res, 70 (20): 7981-91. [PMID:20876799]
4. Tian S, Quan H, Xie C, Guo H, Lü F, Xu Y, Li J, Lou L. (2011)
YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo.
Cancer Sci, 102 (7): 1374-80. [PMID:21443688]