Pyrotinib is an irreversible dual pan-ErbB receptor tyrosine kinase inhibitor 
developed for the treatment of HER2-positive advanced solid tumours. Based on 
positive results in a phase II trial, the drug recently received conditional 
approval in China for use in combination with capecitabine for the treatment of 
HER2-positive, advanced or metastatic breast cancer in patients previously 
treated with anthracycline or taxane chemotherapy. This article summarizes the 
milestones in the development of pyrotinib leading to this first global approval 
for the treatment of HER2-positive advanced breast cancer.