Afatinib-d6 is intended for use as an internal standard for the quantification of afatinib by GC- or LC-MS. Afatinib is an irreversible inhibitor of epidermal growth factor receptor (EGFR) and ErbB2 (IC50s = 0.5 and 14 nM, respectively).1 It increases the cytotoxicity of adriamycin in a concentration-dependent manner in multidrug-resistant A549T lung cancer cells overexpressing P-glycoprotein.2 Afatinib (20 mg/kg) reduces tumor growth in ErbB2-amplified NCI-N87 and NUGC4 gastric cancer mouse xenograft models.3 Formulations containing afatinib have been used in the treatment of non-small cell lung cancer.
1.Eskens, F.A.L.M., Mom, C.H., Planting, A.S.T., et al.A phase I dose escalation study of BIBW 2992, an irreversible dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) tyrosine kinase in a 2-week on, 2-week off schedule in patients with advanced solid tumoursBr. J. Cancer98(1)80-85(2008) 2.Zhang, Y., Wang, C.-Y., Duan, Y.-J., et al.Afatinib decreases P-glycoprotein expression to promote adriamycin toxicity of A549T cellsJ. Cell. Biochem.119(1)414-423(2018) 3.Yoshioka, T., Shien, K., Namba, K., et al.Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancerCancer Sci.109(4)1166-1176(2018)