Pyrotinib is a new irreversible epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) dual tyrosine kinase inhibitor, and it has shown excellent clinical efficacy in treatment of HER2-positive breast cancer patients. The combination of pyrotinib and capecitabine in the treatment of advanced breast cancer has been recognized at home and abroad. Further exploration of whether there are other antitumor agents that work well in combination with pyrotinib, and whether pyrotinib can enhance clinical benefit in patients with early-stage or middle-stage breast cancer, could develop additional potential of pyrotinib. This article reviews the progress related to pyrotinib in recent years.