Abstract: Ferroptosis is a new form of non-apoptotic cell death, regulated by multiple cellular metabolic pathways such as iron handling as well as metabolism of amino acids and lipids. It has been shown to be involved in various diseases including cancers, ischemia-reperfusion injury and degenerative pathologies. Up to now, numerous ferroptosis inhibitors targeting various signaling pathways relevant to the above diseases have been discovered. In this review, current knowledge on the modulation of ferroptosis was elaborated, followed by summarizing recent ferroptosis inhibitors together with their pharmacological activities, in an attempt to boost a perspective for future study.