Abstract: Guided pesticide can directionally translocate and accumulate to specified parts in plants. Improving the conductivity of xenobiotics can dramatically enhance systematic distribution of plants to achieve precise control. In this work, the idea of molecular design of guided pesticide was reviewed, as well as research progress on sugar guided pesticide and amino acid guided pesticide regarding its phloem translocation and biological activities. It is pointed that the structure-activity relationship (SAR) between pesticide molecules and relevant amino acids transporter would be a research focus for the next few years. In addition, a novel guided pesticide taking elicitor as guided group and possessing properties of plant activator is put forward to develop, which not only can control plant pests by phloem translocation but also activate defense reactions of host.