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doxifluridine

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doxifluridine

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Doxifluridine (5'-deoxy-5-fluorouridine) is a second generation nucleoside analog prodrug developed by Roche and used as a cytostatic agent in chemotherapy in several Asian countries including China and South Korea. Doxifluridine is not FDA-approved for use in the USA. It is currently being evaluated in several clinical trials as a stand-alone or combination therapy treatment.

Chemical data

Formula
C9H11FN2O5
Molecular weight
246.19 g/mol
IUPAC name
1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-methyloxolan-2-yl]-5-fluoropyrimidine-2,4-dione
SMILES
C[C@@H]1[C@H]([C@H]([C@@H](O1)N2C=C(C(=O)NC2=O)F)O)O
InChIKey
ZWAOHEXOSAUJHY-ZIYNGMLESA-N
XLogP
-1.7
Polar surface area
99.1 Ų
H-bond donors
3
H-bond acceptors
6
Formal charge
0

via PubChem

Drug data · ChEMBL

Max clinical phase
Phase 3
Molecule type
Small molecule
Indications
gastric cancer

via ChEMBL · EBI

Wikidata facts

Mass
246.065
Has use
medication
Show 5 more facts
chemical formula
C₉H₁₁FN₂O₅
canonical SMILES
CC1C(C(C(O1)N2C=C(C(=O)NC2=O)F)O)O
isomeric SMILES
C[C@@H]1[C@H]([C@H]([C@@H](O1)N2C=C(C(=O)NC2=O)F)O)O
subject has role
Orexigenic
Commons category
Doxifluridine
Sources (2)

via Wikidata · CC0

~2 min read

Encyclopedic overview

4 sections
Contents
  • Biology
  • Side effects
  • Brand names
  • References

Doxifluridine (5'-deoxy-5-fluorouridine) is a second generation nucleoside analog prodrug developed by Roche and used as a cytostatic agent in chemotherapy in several Asian countries including China and South Korea. Doxifluridine is not FDA-approved for use in the USA. It is currently being evaluated in several clinical trials as a stand-alone or combination therapy treatment.

==Biology== 5-Fluorouracil (5-FU), the nucleobase of doxifluridine, is currently an FDA-approved antimetabolite. 5-FU is normally administered intravenously to prevent its degradation by dihydropyrimidine dehydrogenase in the gut wall. Doxifluridine is a fluoropyrimidine derivative of 5-FU, thus a second-generation nucleoside prodrug. Doxifluridine was designed to improve oral bioavailability in order to avoid dihydropyrimidine dehydrogenase degradation in the digestive system.

Excerpted from Wikipedia’s “doxifluridine” article, available under the CC BY-SA 4.0 licence.

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