Canertinib (CI-1033) Suppliers and Product Information

Canertinib is a potent, irreversible pan-erbB tyrosine kinase inhibitor used in cancer research. It inhibits EGFR (IC50 = 0.8 nM), HER-2 (IC50 = 19 nM), and ErbB-4 (IC50 = 7 nM). Canertinib blocks autophosphorylation of erbB2 and has shown efficacy in inhibiting the growth of A431 tumor xenografts in mice.

Frequently Asked Questions about Canertinib

Q: What is the mechanism of action of Canertinib?

A: Canertinib is an irreversible pan-erbB tyrosine kinase inhibitor. It binds to the ATP pocket within the tyrosine kinase domain of all erbB family members, forming a covalent bond that permanently inactivates the catalytically active erbB1, erbB2, and erbB4 family members. This also effectively inhibits erbB3-dependent signaling.

Q: What are the potential applications of Canertinib?

A: Canertinib was initially developed as an experimental drug candidate for cancer treatment. It has shown efficacy against esophageal squamous cell carcinoma in vitro and in vivo. Canertinib treatment significantly affects tumor metabolism, proliferation, and hypoxia as determined by PET. However, it's important to note that by 2015, Pfizer had discontinued the development of this drug.

Q: Are there any known drug interactions with Canertinib?

A: Canertinib has been reported as a substrate for the transporter protein OATP1B3. This interaction may alter its hepatic disposition and can potentially lead to transporter-mediated drug-drug interactions. However, Canertinib is not an inhibitor of the OATP1B1 or OATP1B3 transporters.