Substantial progress has been made in recent years in understanding the molecular pathogenesis of malignant disorders, especially in identification of molecular targets for therapeutic interventions ("targeted therapies"). An important group of therapeutical targets are signaling cascades, e.g. protein tyrosine kinases (PTK) that are activated by mutations, translocations or overexpression. Small molecule inhibitors that compete with ATP and inhibit kinase activity have produced clinical impressive responses in chronic myeloid leukemia, gastrointestinal stroma tumors and non-small cell lung cancer. Another group of cellular targets is represented by tumor-selective cell surface proteins that can serve as target structures for antibodies. Therapeutical concepts using monoclonal antibodies have substantially improved response rates in patients with malignant lymphomas and are currently evaluated in other types of cancer. The definition of molecular target structures critical for the malignant phenotype is driving a new era of integrated diagnostics and therapeutics in the field of oncology.