Clinical use of targeted biological treatment was initiated in 1970s following a discovery of hormonal receptors and targeted clinical use of tamoxifen. Deeper understanding of molecular principles of the process of metastasizing and cell communication and signalling have contributed to the development of targeted molecular biological treatments based on direct impact on the key target structures ofa tumour cell. Clinical effectiveness of targeted biological treatment has been shown in phase III clinical studies in advanced and metastasising solid tumours and importantly expanded our armamentarium of pharmacotherapeutic treatment options in breast cancer, colorectal cancer, non-small cell lung cancer, kidney cancer, hepatocellular carcinoma and gastrointestinal stromal tumour. Full implementation of targeted therapy is precluded by a lack of reliable predictors of efficacy of a number of targeted drugs. Therefore, full identification of such predictors is a subject to intensive clinical research. At present, selection of biological treatment is based on morphological, immunohistochemical and partly also molecular profile ofa tumour. The future of biological treatment lies in a selection that is based on full molecular characterization of the primary tumour as well as metastasis.