Pyrotinib is an oral, irreversible HER1-2-4 TKI that has displayed in a phase III trial a significant activity in association with capecitabine in terms of PFS (11.1 months) compared with placebo (4.1 months, p < 0.001) in HER2-positive BC who were pre-treated with taxane and trastuzumab. This evidence concerns the gene ERBB2 and breast cancer.