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Pyrimidine analogues and fluoropyrimidinesIn useOrigin unclearNeeds review

Floxuridine (FUDR)

Also known as FUDR, 5-fluoro-2'-deoxyuridine

A fluorinated deoxyuridine given by injection. Its current US label covers palliative treatment of gastrointestinal adenocarcinoma metastatic to the liver, by continuous regional intra-arterial infusion.

From discovery to approval

  1. c. 1958 · Earliest report found

    A 2009 meeting report calls it the second fluoropyrimidine introduced by Heidelberger, after fluorouracil. The earliest record found is a 1958 paper, titled as reporting effects of 5-fluorouridine and 5-fluoro-2'-deoxyuridine on transplanted tumours. The synthesis was not traced.[2][3][4][5]

  2. 1970-12-18 · FDA regular · 12 years after first description

    Original approval (ORIG-1) of NDA 016929, classed as a Type 1 new molecular entity with priority review in the Drugs@FDA history. The original letter and label are not available there, so the indication at approval is not stated here; the current label lists palliative management of gastrointestinal adenocarcinoma metastatic to the liver by continuous regional intra-arterial infusion. The type regular is an inference: no accelerated-approval wording was found.[6]

How it works

When given by rapid intra-arterial injection it is apparently catabolised to fluorouracil, with the same effects: mainly interference with DNA synthesis and, to a lesser extent, inhibition of RNA formation. Continuous arterial infusion enhances its direct anabolism to floxuridine monophosphate, increasing the inhibition of DNA.[1]

Where it came from and why

No source read states why floxuridine was made. A 1962 paper, titled as comparing it with fluorouracil in far-advanced breast and colon lesions, and a 1960 paper on its clinical evaluation in childhood acute leukaemia show it was studied soon after fluorouracil.

Cancers

  • Colorectal and other gastrointestinal cancer with liver metastases

    The current US label lists palliative management of gastrointestinal adenocarcinoma metastatic to the liver by continuous regional intra-arterial infusion in carefully selected patients; a 2014 review covers hepatic arterial infusion pump chemotherapy with floxuridine for colorectal liver metastases.[1]

  • Acute leukaemia in children

    A 1960 paper is titled as a clinical evaluation of 5-fluoro-2'-deoxyuridine in acute leukaemia in children (title only; no abstract in PubMed).[4]

  • Breast and colon cancer

    A 1962 paper is titled as comparing fluorouracil and 5-fluoro-2'-deoxyuridine in far-advanced breast and colon lesions (title only).[5]

Worth knowing

  • The US label says floxuridine is effective in the palliative management stated, when given by continuous regional intra-arterial infusion in carefully selected patients considered incurable by surgery or other means; patients whose disease extends beyond an area infusable through one artery should usually be considered for systemic therapy.[1]
  • The label says that when floxuridine is given by rapid intra-arterial injection it is apparently rapidly catabolised to fluorouracil, so rapid injection produces the same toxic and antimetabolic effects as fluorouracil.[1]
  • A 2009 meeting report describes floxuridine as the second fluoropyrimidine introduced by Heidelberger, and notes phase II and III studies by Nancy Kemeny of intra-arterial use in patients with liver metastases.[2]
  • A 2014 review states that the major obstacles to wide adoption of hepatic arterial infusion pump therapy include technical expertise for pump insertion and maintenance and for floxuridine dose modification.[7]

References

  1. Fresenius Kabi USA, LLC. Floxuridine for injection, USP: prescribing information. DailyMed, set ID c8edabc1-67cd-421b-a147-7c1f19f05b8e, published 21 October 2024. Source
  2. Muggia FM, Peters GJ, Landolph JR Jr. XIII International Charles Heidelberger Symposium and 50 Years of Fluoropyrimidines in Cancer Therapy Held on september 6 to 8, 2007 at New York University Cancer Institute, Smilow Conference Center. Mol Cancer Ther. 2009;8(5):992-9. PubMedDOI
  3. HEIDELBERGER C, GRIESBACH L, CRUZ O, SCHNITZER RJ, GRUNBERG E. Fluorinated pyrimidines. VI. Effects of 5-fluorouridine and 5-fluoro-2'-deoxyuridine on transplanted tumors. Proc Soc Exp Biol Med. 1958;97(2):470-5. PubMedDOI
  4. HARTMANN JR, ERLANDSON M, MURPHY ML, ORIGENES ML Jr, SITARZ A. The clinical evaluation of 5-fluoro-2'-deoxyuridine in acute leukemia in children. Cancer Chemother Rep. 1960;8:84-96. PubMed
  5. CURRERI AR, ANSFIELD FJ. Comparison of 5-fluorouracil and 5-fluoro-2'-deoxyuridine in the treatment of far-advanced breast and colon lesions. Cancer Chemother Rep. 1962;16:387-8. PubMed
  6. U.S. Food and Drug Administration. Drugs@FDA: Approval date(s) and history, letters, labels, reviews for NDA 016929 (floxuridine; FUDR). Page read 2026-10-26. Source
  7. Ko YJ, Karanicolas PJ. Hepatic arterial infusion pump chemotherapy for colorectal liver metastases: an old technology in a new era. Curr Oncol. 2014;21(1):e116-21. PubMedDOI