Li Yue, Zhao Long, Li Xiao-Feng
Department of Nuclear Medicine, The Second Clinical Medical College, Jinan University (Shenzhen People's Hospital), Shenzhen, China.
The First Affiliated Hospital, Jinan University, Guangzhou, China.
Front Pharmacol. 2021 Apr 19;12:636892. doi: 10.3389/fphar.2021.636892. eCollection 2021.
Hypoxia is an important feature of most solid tumors, conferring resistance to radiation and many forms of chemotherapy. However, it is possible to exploit the presence of tumor hypoxia with hypoxia-activated prodrugs (HAPs), agents that in low oxygen conditions undergo bioreduction to yield cytotoxic metabolites. Although many such agents have been developed, we will focus here on TH-302. TH-302 has been extensively studied, and we discuss its mechanism of action, as well as its efficacy in preclinical and clinical studies, with the aim of identifying future research directions.
缺氧是大多数实体瘤的一个重要特征，会导致肿瘤对放疗和多种化疗产生抗性。然而，利用肿瘤缺氧现象使用缺氧激活前体药物（HAPs）是可行的，这类药物在低氧条件下会发生生物还原反应，产生具有细胞毒性的代谢产物。尽管已经研发出了许多此类药物，但我们在此将重点关注TH-302。TH-302已经得到了广泛研究，我们将讨论其作用机制以及在临床前和临床研究中的疗效，旨在确定未来的研究方向。
