Radiotherapy-Activated Prodrug: Past, Present and Beyond

Area of Science:

• Oncology
• Radiochemistry
• Drug Delivery

Background:

• Radiotherapy combined with chemotherapy shows synergistic antitumor effects.
• Radiotherapy-activated prodrugs (RAPs) are emerging as a novel therapeutic strategy.
• RAPs exhibit low toxicity before activation and targeted effects post-irradiation.

Purpose of the Study:

• To summarize recent advancements in radiotherapy-activated prodrugs (RAPs).
• To discuss the mechanisms, types of ionizing radiation, chemical structures, and prodrug formats.
• To highlight current challenges and future directions in RAP research.

Main Methods:

• Review of scientific literature on RAPs.
• Analysis of RAP mechanisms involving water radiolysis.
• Categorization of RAPs based on ionizing radiation types, chemical structures, and formats.

Main Results:

• RAPs utilize reactive species from water radiolysis to release active drugs.
• Diverse chemical structures and prodrug formats have been developed for RAPs.
• The field encompasses various ionizing radiation types for prodrug activation.

Conclusions:

• RAPs represent a promising approach for targeted cancer therapy.
• Further research is needed to address current challenges and optimize RAP development.
• RAPs have the potential to significantly improve patient outcomes in radiotherapy.