Ferroptosis is a new iron-dependent form of programmed cell death characterized by iron accumulation and lipid peroxidation. In recent years, ferroptosis has garnered enormous interest in disease treatment research communities in pursuit to reveal the mechanism and key targets of ferroptosis because ferroptosis is closely related to the pathophysiological processes of many diseases. Recent studies have shown some key targets, such as glutathione peroxidase 4 (GPX4) and System Xc, and several inducers and inhibitors have been developed to regulate these key targets. With the emergence of new ferroptosis targets, studies on inducers and inhibitors have made new developments. The selection and use of inducers and inhibitors are very important for related work. This paper briefly introduces important regulatory targets in the ferroptosis metabolic pathway, lists and categorizes commonly used and recently developed inducers and inhibitors, and discusses their medical application. The paper ends of with potential future research direction for ferroptosis.