OBJECTIVES: The improvement of anticancer therapy using the nanotechnological approach is based on improving the pharmacokinetic properties (prolonged stay of the drug in the circulation and improved distribution in the target tissue), the solubility of the anticancer drugs and their stability in a biological environment. The objective of this thesis is to analyse the development of anticancer nanotherapeutics with the emphasis on evaluation of their transfer into clinical settings. As the liposomes, polymeric miceles, nanoparticles and drug-polymer conjugates are commercially the most successful nanotechnologies, the anticancer nanotherapeutics manufactured by the respective nanotechnological approach are described in this work. MATERIAL AND METHODS: The literature is searched by the research topic, research subject, authors and journal. The bibliographical database (PubMed) and the database with full text (Science Direct) were researched. In the review of relevant articles, the most important results, discussion and conclusions were selected and presented in this thesis. The approval procedures and the therapeutic use of anticancer nanotherapeutics were analysed using the existing medicinal product databases of the Agency for the medicinal products and medical devices (HALMED), European Medicines Agency (EMA), US Food and Drug Administration (FDA). The details of specific medicinal products were obtained from the European public assessement reports, Summarys of product characteristics, scientific discussions and web sites of medicinal product manufacturers. RESULTS: The effectivness of anticancer nanotherapeutics is impacted by multiple factors: (i) nanosystems must evade clearance by renal filtration and the reticuloendothelial system, (ii) extravasate throughVIthe enlarged endothelial gaps in tumors, (iii) penetrate through dense stroma in the tumor microenvironment to reach the tumor cells, (iv) remain in the tumor tissue for a prolonged period of time, and (iv) finally release the active agent to induce pharmacological effect. The nanosystem physicochemical properties determine the pharmacokinetics and drug bioavailability in the tumor. CONCLUSION: The unsuccessful clinical transfer of nanopharmaceuticals is due to the poor understanding of biological barriers, focus on development more complex nanopharmaceuticals while forgetting difficulties of overcoming biological barriers or scale-up by the pharmaceutical industry. The use of inadequate animal models in preclinical trials is also critical. The partnership and knowledge exchange between academia, industry, and regulatory agencies is crucial to make anticancer nanopharmaceuticals available to patients. The potential health benefits of nanopharmaceutical products can be realized only if such products are available and commercially viable. Therefore, the regulatory requirements must be sufficiently rigid to ensure the safety and quality of nanopharmaceuticals, but the potential negative impact of over-regulation on the introduction of innovative products to the market must also be considered.