Insect growth regulators (IGRs) are specialized insecticides that can cause the death of insect populations by disturbing the normal life cycle of insects, increasing individual mortality, or disturbing their activity capabilities. Compared to traditional pesticides, which act on neurological system, the functional mechanism of IGRs differs in that it has a lower toxicity level. This leads to lower contamination probability, limited influence on natural past enemies and beneficial organisms, thus more favorable to the development of sustainable agriculture. This review describes in details the classification of IGRs. The toxicological mechanisms of three important IGRs (juvenile hormone analog, chitin synthesis inhibitor and molting hormone analog) are described as well as the theories that may explain the development of insecticide resistant in some pests. This review provides insights that can be used to better develop new IGRs and understand their application potential.