floxuridine

Trade name: fudr

Small moleculeapproved

Approved

Dec 18, 1970

Floxuridine is a pyrimidine analog that acts as an inhibitor of the S-phase of cell division. This selectively kills rapidly dividing cells. Floxuridine is an anti-metabolite. Anti-metabolites masquerade as pyramidine-like molecules which prevents normal pyrimidines from being incorporated into DNA during the S phase of the cell cycle. Flurouracil (the end-product of catabolism of floxuridine) blocks an enzyme which converts cytosine nucleosides into the deoxy derivative. In addition, DNA synthesis is further inhibited because fluoruracil blocks the incorporation of the thymdine nucleotide into the DNA strand. Floxuridine is used for 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. Also for the palliative management of liver cancer (usually administered by hepatic intra-arterial infusion).Floxuridine first gained FDA approval in December 1970 under the brand name FUDR. The drug was initially marketed by Roche, which also did a lot of the initial work on 5-fluorouracil. The National Cancer Institute was an early developer of the drug. Roche sold its FUDR product line in 2001 to F H Faulding, which became Mayne Pharma. — NCATS

Clinical trial activity

57 trials · 43 clinical orgs · 8 marketing orgs

Phase 1
12
Phase 2
45
Phase 3
10
Phase 4
0

Earliest trial started Sep 1, 1994 (NCT00002842)

Timeline

1970s

  1. Dec 18, 1970

    Hospira — Earliest FDA Approval

  2. Dec 18, 1970

    Hospira — NDA Secondary Org

  3. Dec 18, 1970

    Hospira — NDA Organization

1990s

  1. Jan 1, 1994

    Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 1996

    Earliest Phase 3 Sponsor(trial)

  3. Jan 1, 1997

    Earliest Phase 1 Sponsor(trial)

2000s

  1. Apr 6, 2000

    West-Ward Pharmaceutical — Marketing Organization

  2. Apr 6, 2000

    Hikma — Marketing Organization

  3. Feb 22, 2001

    Fresenius — Marketing Organization

2010s

  1. Nov 22, 2017

    Sankyo — Marketing Organization

  2. Nov 22, 2017

    Lutipold — Marketing Organization

  3. Nov 22, 2017

    Daiichi Sankyo — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedPriority reviewDec 18, 1970

Chemistry & pharmacology

Loading structure…

SMILES

OC[C@H]1O[C@H](C[C@@H]1O)N2C=C(F)C(=O)NC2=O
Mol. weight
246.1924 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Parenteral
Availability
Prescription Only

Oral

No

Parenteral

Yes

Topical

No

Black box warning

Sources

Also known as

  • 1-(2-deoxy-beta-d-ribofuranosyl)-5-fluorouracil
  • 1-(2-deoxy-beta-d-ribofuranosyl)-5-fluorouracil
  • 1-beta-d-2'-deoxyribofuranosyl-5-flurouracil
  • 1-beta-d-2'-deoxyribofuranosyl-5-flurouracil
  • 1beta-d-2'-deoxyribofuranosyl-5-flurouracil
  • 1beta-d-2'-deoxyribofuranosyl-5-flurouracil
  • 2'-deoxy-5-fluorouridine
  • 2'-deoxy-5-fluorouridine
  • 5fdu
  • 5fdu
  • 5-fluoro-2-deoxyuridine
  • 5-fluoro-2-deoxyuridine
  • 5-fluoro-2-desoxyuridine
  • 5-fluoro-2-desoxyuridine
  • 5-fluorouracil 2'-deoxyriboside
  • 5-fluorouracil 2'-deoxyriboside
  • 5-fluorouracil deoxyriboside
  • 5-fluorouracil deoxyriboside
  • 5-fluorouracil deoxyriboside
  • beta-5-fluoro-2'-deoxyuridine
  • beta-5-fluoro-2'-deoxyuridine
  • deoxyfluorouridine
  • deoxyfluorouridine
  • fdu
  • fdu
  • floxiridina
  • floxiridina
  • floxuridin
  • floxuridin
  • floxuridin
  • floxuridine
  • floxuridine
  • floxuridine
  • floxuridine
  • floxuridine
  • floxuridine
  • floxuridine
  • floxuridine
  • floxuridine
  • floxuridine
  • floxuridine
  • floxuridinum
  • floxuridinum
  • fluorodeoxyuridine
  • fluorodeoxyuridine
  • fluoruridine deoxyribose
  • fluoruridine deoxyribose
  • fluoruridine deoxyribose
  • fudr
  • fudr
  • fudr
  • f.u.d.r.

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06857773Phase 3Nov 21, 2024Netherlands Cancer Institute
NCT06313203Phase 2Feb 13, 2024University of Oslo
NCT05863195Phase 3Dec 19, 2023ECOG-ACRIN Cancer Research Group, National Cancer Institute (NCI)
NCT05286814Phase 2Oct 24, 2022National Cancer Institute (NCI)
NCT04898504Phase 2Aug 31, 2021University of Oslo
NCT04891289Phase 2May 7, 2021Memorial Sloan-Kettering Cancer Center
NCT05865925Phase 1/Phase 2 (Phase 2)Apr 22, 2021Luye Pharma
NCT04668976Phase 2Nov 25, 2020Virginia Mason Medical Center
NCT04552093Phase 2/Phase 3 (Phase 3)Sep 9, 2020Erasmus University Rotterdam, Netherlands Cancer Institute
NCT04251715Phase 2May 4, 2020OHSU Knight Cancer Institute, Oregon Health and Science University
NCT04276090N/AMar 15, 2020University of Kentucky
NCT03856658Phase 2Feb 5, 2019Corewell Health West, The Spectrum Health Group
NCT03678428Phase 3Oct 31, 2018Sun Yat-Sen University
NCT03693807Phase 2Oct 18, 2018Memorial Sloan-Kettering Cancer Center
NCT03366155Phase 2Oct 5, 2018National Cancer Institute (NCI)
NCT03500874Phase 3Feb 28, 2018Sun Yat-Sen University
NCT03493061Phase 2Feb 1, 2018Sun Yat-Sen University
NCT02529774Phase 2/Phase 3 (Phase 3)Sep 1, 2015Fudan University
NCT02102789Phase 3Mar 1, 2014Sun Yat-Sen University
NCT01938729Phase 1Sep 1, 2013Cornell University, Ohio State University, The University of Texas, Dallas, Washington University in St. Louis
Showing 20 of 57 trials
Page 1 / 3

Organizations

Research & Development (43)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Cancer Institute (NCI)Government24731994
Cornell UniversityAcademic/Hospital161431996
New York UniversityAcademic/Hospital5411997
Sun Yat-Sen UniversityAcademic/Hospital4422014
University of MiamiAcademic/Hospital4312004
Washington University in St. LouisAcademic/Hospital4122012
City of Hope National Medical CenterAcademic/Hospital2211994
Memorial Sloan-Kettering Cancer CenterAcademic/Hospital2212018
National Institutes of Health (NIH)Government2221999
Netherlands Cancer InstituteAcademic/Hospital2212020
NSABP FoundationAcademic/Hospital2122002
Ohio State UniversityAcademic/Hospital2022013
The University of Texas, DallasAcademic/Hospital2022013
University of Medicine and Dentistry of New JerseyAcademic/Hospital2012000
University of OsloAcademic/Hospital2212021
Celator PharmaceuticalsFor profit1112006
Central South UniversityAcademic/Hospital1112011
Corewell Health WestAcademic/Hospital1112019
ECOG-ACRIN Cancer Research GroupAcademic/Hospital1112023
Erasmus University RotterdamAcademic/Hospital1012020
43 organizations
Page 1 / 3

Marketing (9)

OrganizationOrg typeRelationshipDate
Athenex, Inc.For profitMKTG
Daiichi SankyoFor profitMKTGNov 22, 2017
FreseniusFor profitMKTGFeb 22, 2001
HikmaFor profitMKTGApr 6, 2000
HospiraFor profitNDA2Dec 18, 1970
HospiraFor profitNDADec 18, 1970
LutipoldFor profitMKTGNov 22, 2017
SankyoFor profitMKTGNov 22, 2017
West-Ward PharmaceuticalFor profitMKTGApr 6, 2000