The hithero development of systemic treatment – cancer chemotherapy is presented and analysed. The main approaches to chemotherapy, such as induction chemotherapy, adjuvant chemotherapy, primary chemotherapy and individually planed chemotherapy, are discussed. The principal problems associated with present cancer chemotherapy include resistance of cancer cells to anticancer drugs and toxic effects of these drugs on healthy tissue, which requires dose reduction. The methods used to enhance the effectiveness and reduce toxicity of chemotherapy are presented together with some new aspects of systemic therapy. The available methods of targeted drug therapy and, in perspective, genetic treatment and control of cancerous tumors.