Canertinib

From Wikipedia, the free encyclopedia
Jump to navigation Jump to search
Canertinib
Canertinib.svg
Names
IUPAC name
N-{4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-(morpholin-4-yl)propoxy]quinazolin-6-yl}prop-2-enamide
Other names
CI-1033; PD-183805
Identifiers
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
UNII
Properties
C24H25ClFN5O3
Molar mass 485.94 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
☒N verify (what is ☑Y☒N ?)
Infobox references

Canertinib (CI-1033) is an experimental drug candidate for the treatment of cancer. It is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM).[1][2] By 2015, Pfizer had discontinued development of the drug.[3]

Canertinib has been reported as a substrate for OATP1B3. Interaction of canertinib with OATP1B3 may alter its hepatic disposition and can lead to transporter mediated drug-drug interactions.[4] Also, canertinib is not an inhibitor of OATP-1B1 or OATP-1B3 transporter.[5]

References[edit]

  1. ^ Smaill, JB; Rewcastle, GW; Loo, JA; Greis, KD; Chan, OH; Reyner, EL; Lipka, E; Showalter, HD; et al. (2000). "Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido3,2-dpyrimidine-6-acrylamides bearing additional solubilizing functions". Journal of Medicinal Chemistry. 43 (7): 1380–97. doi:10.1021/jm990482t. PMID 10753475.
  2. ^ CI-1033 (Canertinib), Selleck Chemicals
  3. ^ http://adisinsight.springer.com/drugs/800012072
  4. ^ Khurana V, Minocha M, Pal D, Mitra AK (March 2014). "Role of OATP-1B1 and/or OATP-1B3 in hepatic disposition of tyrosine kinase inhibitors". Drug Metabol Drug Interact. 29 (3): 1–11. doi:10.1515/dmdi-2013-0062. PMC 4407685. PMID 24643910.
  5. ^ Khurana V, Minocha M, Pal D, Mitra AK (May 2014). "Inhibition of OATP-1B1 and OATP-1B3 by tyrosine kinase inhibitors". Drug Metabol Drug Interact. 29 (4): 1–11. doi:10.1515/dmdi-2014-0014. PMC 4407688. PMID 24807167.