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Idoxuridine is a pyrimidine nucleoside analog and the first antiviral agent approved for clinical use. It is primarily indicated for the topical treatment of herpes simplex virus (HSV) keratitis. As an analog of thymidine, idoxuridine is phosphorylated by cellular and viral kinases into its active triphosphate form. This metabolite is then incorporated into viral DNA by DNA polymerase in place of thymidine. The resulting DNA is structurally defective, leading to errors in transcription and translation, which ultimately inhibits viral replication. While effective against HSV-1 and HSV-2, its clinical use has largely been superseded by more selective and less toxic antivirals such as trifluridine and acyclovir due to idoxuridine's lack of specificity, which can lead to host cell toxicity.
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