胶质母细胞瘤是源自胶质干细胞或祖细胞的原发性脑肿瘤。男性和女性的胶质母细胞瘤发病率存在较大差异。研究表明瘤体的性别差异可能与雄激素受体信号通路有关。男性患胶质母细胞瘤的患病率高于女性。异常激活雄激素受体信号通路，或者雄激素受体信号通路与其他信号通路之间的相互作用，促进了胶质母细胞瘤的发展。因此，靶向雄激素受体被认为是治疗胶质母细胞瘤的希望之选。本综述研究了通过靶向雄激素受体治疗胶质母细胞瘤的药物研究动态。符合预期的第一个发现是，以恩扎鲁胺为代表的雄激素受体拮抗剂已经被研究并显示出抗胶质母细胞瘤的效果。此外，研究发现5α还原酶抑制剂和雄激素受体拮抗剂的联合使用比单一使用效果更好。类似的结果也在表皮生长因子受体抑制剂和雄激素受体拮抗剂的联合使用中得到。此外，已有四种小分子化合物通过直接或间接靶向雄激素受体显示出显著的抗胶质母细胞瘤效果。预期之一的小分子化合物赛维特隆也已进入II期临床试验阶段。这些发现表明，通过靶向雄激素受体治疗胶质母细胞瘤可能是一种有希望的治疗选择。版权所有 © 2023 Elsevier B.V. 保留所有权利。

Glioblastomas are primary brain tumors that originate from glial stem cells or progenitor cells. There is a large difference in the incidence of glioblastoma between males and females. Studies revealed that the gender differences in the tumor may be attributable to the androgen receptor signaling axis. The incidence rate of glioblastoma in men is higher than that in women. Aberrant activation of the androgen receptor signaling pathway, or interactions between the androgen receptor signaling axis and other signaling axes promote the development of glioblastoma. Therefore, targeting the androgen receptor holds promise as a therapeutic approach for glioblastoma. This review investigates the dynamics of drug research into the treatment of glioblastoma by targeting the androgen receptor. The first finding in line with expectations is that androgen receptor antagonists, represented by enzalutamide, have been studied and shown to have anti-glioblastoma effects. In addition, it was found that the combination of 5-alpha reductase inhibitors and androgen receptor antagonists resulted in better therapeutic outcomes than each of them alone. Similar results were obtained with the combination of an epidermal growth factor receptor inhibitor and an androgen receptor antagonist. In addition, four small molecule compounds have been shown to exert significant anti-glioblastoma effects by directly or indirectly targeting the androgen receptor. Expectantly, one of these small molecules, seviteronel, progressed to the Phase II clinical trial stage. These findings suggest that targeting the androgen receptor for glioblastoma may be a promising therapeutic option.Copyright © 2023 Elsevier B.V. All rights reserved.