Floxuridine (FUDR)

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General information

Class/mechanism: Pyrimidine analog, antimetabolite, inhibitor of thymidylate synthase. When given by rapid intraarterial injection, it is rapidly catabolized in vivo to fluorouracil (5-FU), which is metabolized to 5-fluoro-2'-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). FdUMP inhibits DNA synthesis by binding to thymidylate synthase and inhibiting production of thymidylate; FUTP interferes with RNA processing when it is mistakenly incorporated in place of uridine triphosphate (UTP). When FUDR is given by continuous intraarterial infusion, direct anabolism to FUDR-monophosphate is enhanced, which increases the inhibition of DNA.[1][2]
Route: IA (intraarterial)
Extravasation: irritant

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]

Patient drug information

Disease for which it is used

History of changes in FDA indication

  • 12/18/1970: Initial FDA approval for the palliative management of gastrointestinal adenocarcinoma metastatic to the liver, when given by continuous regional intra-arterial infusion in carefully selected patients who are considered incurable by surgery or other means. Patients with known disease extending beyond an area capable of infusion via a single artery should, except in unusual circumstances, be considered for systemic therapy with other chemotherapeutic agents.

Also known as

  • Code name: WR-138720
  • Generic names: floxuridin, fluorodeoxyuridine, fluorouridine deoxyribose
  • Brand name: FUDF

References