Trastuzumab (Herceptin) is the first monoclonal antibody to be approved for the treatment of a solid tumour and is directed against the c-erb-B2 receptor. c-erb-B2 is a member of the epidermal growth factor family and approximately 25% of breast cancers express such receptors, which appear to confer a poorer prognosis and may be an indicator of resistance to cytotoxic chemotherapy. This review assesses the mechanisms of action of trastuzumab, discusses the measurement of the HER-2/neu gene and its products, and describes the preclinical and clinical studies that have been instrumental to date in the emergence of trastuzumab in clinical practice.