Canertinib Explained

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 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]

Notes and References

1. 10753475 . 2000 . Smaill . JB . Rewcastle . GW . Loo . JA . Greis . KD . Chan . OH . Reyner . EL . Lipka . E . Showalter . HD . Vincent . PW . Elliott . William L . Denny . William A . 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 . 43 . 7 . 1380–97 . Journal of Medicinal Chemistry . 10.1021/jm990482t. 8 .
2. http://www.selleckchem.com/products/CI-1033%28Canertinib%29.html CI-1033 (Canertinib)
3. Web site: Canertinib - AdisInsight.
4. Khurana V, Minocha M, Pal D, Mitra AK . Role of OATP-1B1 and/or OATP-1B3 in hepatic disposition of tyrosine kinase inhibitors. . Drug Metabol Drug Interact. . 29. 3 . 179–90 . March 2014 . 24643910 . 10.1515/dmdi-2013-0062 . 4407685.
5. Khurana V, Minocha M, Pal D, Mitra AK . Inhibition of OATP-1B1 and OATP-1B3 by tyrosine kinase inhibitors. . Drug Metabol Drug Interact. . 29. 4 . 249–59 . May 2014 . 24807167 . 10.1515/dmdi-2014-0014 . 4407688.