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Ropidoxuridine is an orally available, halogenated pyrimidine and thymidine analogue that acts as a prodrug for 5-iododeoxyuridine (IUdR). It is being developed as a radiation sensitizer to enhance the effects of radiotherapy in cancer treatment, particularly for brain tumors such as glioblastoma. Upon oral administration, ropidoxuridine is converted by hepatic aldehyde oxidase to IUdR, which is then incorporated into DNA during replication. This incorporation increases the sensitivity of rapidly dividing cancer cells to ionizing radiation by promoting DNA strand breaks and reducing repair capacity. Ropidoxuridine has demonstrated improved anti-tumor activity and a lower toxicity profile compared to direct IUdR administration. The drug has received Orphan Drug Designation from the FDA for glioblastoma and is currently in Phase 2 clinical trials for this indication.
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