Canertinib (CI-1033) is an experimental drug candidate for the treatment of cancer. It is an

irreversible Irreversible may refer to: * Irreversible process, in thermodynamics, a process that is not reversible *'' Irréversible'', a 2002 film * ''Irréversible'' (soundtrack), soundtrack to the film ''Irréversible'' * An album recorded by hip-hop artis ...

tyrosine-kinase inhibitor A tyrosine kinase inhibitor (TKI) is a pharmaceutical drug that inhibits tyrosine kinases. Tyrosine kinases are enzymes responsible for the activation of many proteins by signal transduction cascades. The proteins are activated by adding a phosph ...

with activity against EGFR (IC₅₀ 0.8 nM),

HER-2 Receptor tyrosine-protein kinase erbB-2 is a protein that in humans is encoded by the ''ERBB2'' gene. ERBB is abbreviated from erythroblastic oncogene B, a gene originally isolated from the avian genome. The human protein is also frequently refer ...

(IC₅₀ 19 nM) and ErbB-4 (IC₅₀ 7 nM). By 2015, Pfizer had discontinued development of the drug. Canertinib has been reported as a substrate for the transporter protein

OATP1B3 Solute carrier organic anion transporter family member 1B3 (SLCO1B3) also known as organic anion-transporting polypeptide 1B3 (OATP1B3) is a protein that in humans is encoded by the ''SLCO1B3'' gene. OATP1B3 is a 12-transmembrane domain influx tra ...

. Interaction of canertinib with OATP1B3 may alter its hepatic disposition and can lead to transporter mediated drug-drug interactions. Canertinib is not an inhibitor of the

OATP1B1 Solute carrier organic anion transporter family member 1B1 is a protein that in humans is encoded by the ''SLCO1B1'' gene. Pharmacogenomic research indicates that genetic variations in this gene are associated with response to simvastatin. Clinical ...

or OATP1B3 transporters.

References

Acrylamides Tyrosine kinase inhibitors Quinazolines 4-Morpholinyl compunds Fluoroarenes Chloroarenes Experimental cancer drugs Abandoned drugs {{antineoplastic-drug-stub