Targeting Hypoxia: Hypoxia-Activated Prodrugs in Cancer Therapy

Hypoxia is an important characteristic of most solid malignancies, and is closely related to tumor prognosis and therapeutic resistance. Hypoxia is one of the most important factors associated with resistance to conventional radiotherapy and chemotherapy. Therapies targeting tumor hypoxia have attracted considerable attention. Hypoxia-activated prodrugs (HAPs) are bioreductive drugs that are selectively activated under hypoxic conditions and that can accurately target the hypoxic regions of solid tumors. Both single-agent and combined use with other drugs have shown promising antitumor effects. In this review, we discuss the mechanism of action and the current preclinical and clinical progress of several of the most widely used HAPs, summarize their existing problems and shortcomings, and discuss future research prospects.

Automated summary

Hypoxia is a crucial characteristic of most solid malignancies, impacting tumor prognosis and treatment resistance. Therapies targeting tumor hypoxia, such as hypoxia-activated prodrugs (HAPs), have shown promising antitumor effects either alone or in combination with other drugs. Further research is needed to address the existing challenges and explore future prospects.