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]
References
- JB Smaill, GW Rewcastle, JA Loo, KD Greis, OH Chan, EL Reyner, E Lipka, HD Showalter. 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, 2000^
- CI-1033 (Canertinib), Selleck Chemicals^
- Canertinib - AdisInsight^