. Author manuscript; available in PMC: 2022 Jun 1.

Published in final edited form as: Acad Radiol. 2020 Jun 7;28(6):849–858. doi: 10.1016/j.acra.2020.04.012

Table 2.

Radiosensitizing Agents and Oxygenation

Mechanism	Description	Clinical Use
Targeting hypoxic cells
Mitomycin C	Causes alkylation and crosslinking of DNA under anaerobic conditions	Hepatocellular carcinoma
Tirapazamine	Causes oxidative damage to pyrimidines	Non-small cell lung cancer (brain metastases), head & neck cancers
Cisplatin	Crosslinks DNA	Hepatocellular carcinoma
Increasing tumor O2
Efaproxiral	Decreases the oxygen binding affinity of hemoglobin through allosteric modification	Non-small cell lung cancer, metastatic breast cancer (brain metastases)
Perfluorocarbon O2 carriers	Increases O₂ concentrations	Experimental
Sensitization to radiotherapy
5-FU	Inhibits DNA synthesis (thymidine analog)	Metastatic colorectal cancer
Irinotecan	Inhibits topoisomerase I	Metastatic colorectal cancer
Paclitaxel	Inhibits microtubules	Metastatic breast cancer
Gemcitabine	Produces metabolites that cause early termination of DNA strands	Intrahepatic cholangiocarcinoma, metastatic breast cancer, pancreatic cancer
Motexafin gadolinium	Sensitizes cancer cells to ionizing radiation through targeting redox-dependent pathways and serves as an MRI contrast agent	Non-small cell lung cancer (brain metastases)