floxuridine
Trade name: fudr
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
Earliest trial started Sep 1, 1994 (NCT00002842)
Timeline
1970s
1990s
2000s
- Apr 6, 2000
West-Ward Pharmaceutical — Marketing Organization
- Apr 6, 2000
Hikma — Marketing Organization
- Feb 22, 2001
Fresenius — Marketing Organization
2010s
- Nov 22, 2017
Sankyo — Marketing Organization
- Nov 22, 2017
Lutipold — Marketing Organization
- Nov 22, 2017
Daiichi Sankyo — Marketing Organization
Indications
Approved for
Studied for
- Adenocarcinoma · Phase 2
- Appendiceal Neoplasms · Phase 2
- Bile Duct Neoplasms · Phase 2
- Cholangiocarcinoma · Phase 2
- Colonic Neoplasms · Phase 2
- Colorectal Neoplasms · Phase 3
- Drug-Related Side Effects and Adverse Reactions · Phase 2
- Esophageal Neoplasms · Phase 2
- Fallopian Tube Neoplasms · Phase 1
- Floxuridine · Phase 3
- Gastrointestinal Stromal Tumors · Phase 2
- Hamartoma · Phase 2
- Intestinal Neoplasms · Phase 2
- Liver · Phase 1
- Liver Neoplasms · Phase 3
- Nasopharyngeal Carcinoma · Phase 1
- Neoplasm Metastasis · Phase 3
- Neoplasms · Phase 3
- Ovarian Neoplasms · Phase 2
- Pancreatic Neoplasms · Phase 2
- Rectal Neoplasms · Phase 2
- Stomach Neoplasms · Phase 2
- Vascular Access Devices · Phase 3
Mechanism of action
- Thymidylate synthaseINHIBITOR
TYMS inhibitor
Approval history
- approvedPriority reviewDec 18, 1970
Chemistry & pharmacology
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
Sources
- WikipediaFloxuridine ↗
- NCATS039LU44I5M ↗
- ChEMBLCHEMBL917 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06857773 | Phase 3 | Nov 21, 2024 | Netherlands Cancer Institute |
| NCT06313203 | Phase 2 | Feb 13, 2024 | University of Oslo |
| NCT05863195 | Phase 3 | Dec 19, 2023 | ECOG-ACRIN Cancer Research Group, National Cancer Institute (NCI) |
| NCT05286814 | Phase 2 | Oct 24, 2022 | National Cancer Institute (NCI) |
| NCT04898504 | Phase 2 | Aug 31, 2021 | University of Oslo |
| NCT04891289 | Phase 2 | May 7, 2021 | Memorial Sloan-Kettering Cancer Center |
| NCT05865925 | Phase 1/Phase 2 (Phase 2) | Apr 22, 2021 | Luye Pharma |
| NCT04668976 | Phase 2 | Nov 25, 2020 | Virginia Mason Medical Center |
| NCT04552093 | Phase 2/Phase 3 (Phase 3) | Sep 9, 2020 | Erasmus University Rotterdam, Netherlands Cancer Institute |
| NCT04251715 | Phase 2 | May 4, 2020 | OHSU Knight Cancer Institute, Oregon Health and Science University |
| NCT04276090 | N/A | Mar 15, 2020 | University of Kentucky |
| NCT03856658 | Phase 2 | Feb 5, 2019 | Corewell Health West, The Spectrum Health Group |
| NCT03678428 | Phase 3 | Oct 31, 2018 | Sun Yat-Sen University |
| NCT03693807 | Phase 2 | Oct 18, 2018 | Memorial Sloan-Kettering Cancer Center |
| NCT03366155 | Phase 2 | Oct 5, 2018 | National Cancer Institute (NCI) |
| NCT03500874 | Phase 3 | Feb 28, 2018 | Sun Yat-Sen University |
| NCT03493061 | Phase 2 | Feb 1, 2018 | Sun Yat-Sen University |
| NCT02529774 | Phase 2/Phase 3 (Phase 3) | Sep 1, 2015 | Fudan University |
| NCT02102789 | Phase 3 | Mar 1, 2014 | Sun Yat-Sen University |
| NCT01938729 | Phase 1 | Sep 1, 2013 | Cornell University, Ohio State University, The University of Texas, Dallas, Washington University in St. Louis |
Organizations
Research & Development (43)
Marketing (9)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Athenex, Inc. | For profit | MKTG | — |
| Daiichi Sankyo | For profit | MKTG | Nov 22, 2017 |
| Fresenius | For profit | MKTG | Feb 22, 2001 |
| Hikma | For profit | MKTG | Apr 6, 2000 |
| Hospira | For profit | NDA2 | Dec 18, 1970 |
| Hospira | For profit | NDA | Dec 18, 1970 |
| Lutipold | For profit | MKTG | Nov 22, 2017 |
| Sankyo | For profit | MKTG | Nov 22, 2017 |
| West-Ward Pharmaceutical | For profit | MKTG | Apr 6, 2000 |