Introduction and objectives: Breast cancer (BC) is the most common malignancy and the leading cause of cancer death among women. About 15–20% of all BCs are HER2-positive. Proper assessment of HER2 status is crucial to choose appropriate treatment. The review summarizes data on anti-HER2 drugs used to treat HER2-positive BC and provides basic information on new agents under investigation. Brief description of the state of knowledge.: Specific HER2-targeting drugs are available or are being evaluated in clinical trials. Anti-HER2 agents include: monoclonal antibodies, tyrosine kinase inhibitors, antibody-drug conjugates, bispecific antibodies, PI3K/AKT/mTOR inhibitors and heat shock protein 90 inhibitors, HER2-targeting vaccines and CDK4/6 inhibitors. The advent of anti-HER2 therapies increased the time of progression free survival and overall survival in BC patients. Results: Final analysis of the CLEOPATRA trial shows that the combination of trastuzumab, pertuzumab and taxane significantly improved outcomes in metastatic HER2-positive BC and it is currently preferred first-line treatment. The recommended second-line treatment is based on trastuzumab emtansine or on the combination of lapatinib and capecitabine. Some promising agents such as margetuximab or trastuzumab deruxtecan are still under investigation. Conclusions: Anti-HER2 directed treatment undoubtedly improves outcomes among patients with HER2-positive BC. Access to drugs such as trastuzumab, pertuzumab, lapatinib and T-DM1 improves prognosis even in patients with advanced disease. Further studies and clinical trials on novel anti-HER2 therapies are required. Nevertheless, BC treatment is becoming more effective and, hopefully, one day it may be possible to cure patients even with metastases.