Ivermectin (IVM), a semi‐synthetic macrolide parasiticide, has demonstrated considerable effectiveness in combating internal and external parasites, particularly nematodes and arthropods. Its remarkable ability to control parasites has earned it significant recognition, culminating in Satoshi Omura and William C. Campbell's receipt of the 2015 Nobel Prize in Physiology or Medicine for their contributions to the development of IVM. In recent years, investigations have revealed that IVM possesses antitumor properties. It can suppress the growth of various cancer cells, including glioma, through a multitude of mechanisms such as selective targeting of tumor‐specific proteins, inducing programmed cell death, and modulation of tumor‐related signaling pathways. Hence, IVM holds tremendous potential as a novel anticancer drug. This review seeks to provide an overview of the underlying mechanisms that enable IVM's capacity to suppress glioma. Furthermore, it aims to elucidate the challenges and prospects associated with utilizing IVM as a new anticancer agent. Ivermectin was a key focus of the Nobel Prize in Physiology or Medicine. It also can suppress the growth of glioma, through a multitude of mechanisms. This article provides comprehensive insights into the specific mechanisms of IVM's anti‐glioma action in three aspects, such as IVM‐glioma molecular mechanism, basic and clinical experiments, and new directions for glioma treatment (combination therapies).