Canertinib (CI-1033) is an experimental drug candidate for the treatment of cancer. It is an
irreversibletyrosine-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 the transporter protein
OATP1B3. Interaction of canertinib with OATP1B3 may alter its hepatic disposition and can lead to transporter mediated drug-drug interactions.[4] Canertinib is not an inhibitor of the
OATP1B1 or OATP1B3 transporters.[5]
References
^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.
PMID10753475.