Like lapatinib and afatinib, it is a dual inhibitor of the human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. It inhibits them by covalently binding with a cysteine side chain in those proteins. Unlike related noncovalent inhibitors,<unk>  is effective against the T790M resistant variant of EGFR.<unk>  has an IC50 of 59 nM against HER2 and shows weak inhibition against KDR and Scr with IC50 values of 0.8 μM and 1.4 μM, respectively. In BT474 cells,<unk>  reduces HER2 autophosphorylation, and inhibited cyclin D1 expression while reduced proliferation has been observed A431 cells when treated with<unk>  at concentrations of 3 or 5 nM. In xenograft models with 3T3/neu tumors oral administration of<unk>  at 10, 20, 40 or 80 mg/kg was able to inhibit tumor growth while in SK-OV-3 models doses of 5 and 60 mg/kg significantly inhibited tumor growth.
Neratinib
Tucatinib
Fostamatinib
Dasatinib
Lapatinib
Ponatinib
Capmatinib
Pemigatinib