The specific binding of peptides to their receptors can be used to meet the key requirement in tumor targeting: selective addressing of neoplasm. Because of their small size, peptides exhibit faster blood clearance and higher target-to-background ratios compared to macromolecular compounds. In radiopharmacy, these advantages have been attended, and radiolabelled receptor-binding peptides have emerged as a new class of radiopharmaceuticals. Over the last years, nuclear medicine has evaluated various peptides for tumor scintigraphy. The challenge is to label bioactive peptides without affecting their receptor binding properties. Size, plasma protein binding, lipophilicity and sensitivity to proteolysis are to be considered, as well as biodistribution, metabolism and excretion characteristics. The variety of experiences gained in the development of peptide analogues and radiolabelling methods, and latest results from in vitro, in vivo and clinical studies will be presented. The tumor receptor-targeting approach with peptides can be extended to cancer chemotherapy. One of the major problems in classic chemotherapy is the non-specific toxicity of most anticancer agents against normal cells. Coupling cytotoxic drugs to macromolecular carriers has been shown to be a promising approach for efficient drug targeting. In the past few years, peptides were introduced as carriers. Different conjugates, composed of a peptide carrier and a cytotoxic moiety, have been investigated so far. Anticancer drugs were coupled to analogues of luteinizing hormone-releasing hormone, bombesin, somatostatin and neuropeptide Y. Suitable candidates maintained their binding affinity and could preserve the cytotoxic activity in vitro and in vivo, resulting in a peptide-mediated selective chemotherapy.