Deoxyfluorouridine

Deoxyfluorouridine Uses, Dosage, Side Effects, Food Interaction and all others data.

An antineoplastic antimetabolite that is metabolized to fluorouracil when administered by rapid injection. Deoxyfluorouridine is available as a sterile, nonpyrogenic, lyophilized powder for reconstitution. When administered by slow, continuous, intra-arterial infusion, it is converted to floxuridine monophosphate. It has been used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract.

Deoxyfluorouridine is an anti-metabolite or a pyrimidine analog that works by disrupting the process S-phase of cell division, selectively targeting rapidly dividing cells. Due to the structural similarities, antimetabolites act as pyrimidine-like molecules and prevent normal pyrimidines from being incorporated into DNA. After successful biotransformation, floxuridine is converted into an active component, flurouracil, which blocks the enzyme which converts cytosine nucleosides into the deoxy derivative. Flurouracil also physically prevents the incorporation of thymidine nucleotides into the DNA strand by taking their place, further preventing DNA synthesis.

Trade Name Deoxyfluorouridine
Availability Prescription only
Generic Floxuridine
Floxuridine Other Names 5-Fluorodeoxyuridine, 5FDU, Deoxyfluorouridine, Floxiridina, Floxuridin, Floxuridine, Floxuridinum, Fluorodeoxyuridine, Fluoruridine deoxyribose
Type
Formula C9H11FN2O5
Weight Average: 246.1924
Monoisotopic: 246.065199677
Groups Approved
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Deoxyfluorouridine
Deoxyfluorouridine

Uses

Deoxyfluorouridine is an antimetabolite used as palliative management for liver metastases of gastrointestinal malignancy.

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).

Deoxyfluorouridine is also used to associated treatment for these conditions: Metastatic Hepatic Cancer, Stage 4 gastrointestinal adenocarcinoma

How Deoxyfluorouridine works

Deoxyfluorouridine rapidly undergoes catabolism to form 5-fluorouracil, which is the active component of the drug. 5-Fluorouracil primarily works by interfering with DNA synthesis; however, it may also inhibit the formation of fraudulent RNA via physical incorporation into the RNA. It is also an inhibitor of riboside phophorylase, preventing the utilization of pre-formed uracil in RNA synthesis. Deoxyfluorouridine can also form 5-fluoro-2'-deoxyuridine-5'-phosphate (FUDR-MP), which is the monophosphate of floxuridine that inhibits thymidylate synthetase that plays a role in the methylation of deoxyuridylic acid to thymidylic acid during DNA synthesis. FUDR-MP thus interferes with DNA synthesis.

Toxicity

Oral, rat LD50: 215 mg/kg. Signs of overdose include nausea, vomiting, diarrhea, gastrointestinal ulceration and bleeding, and bone marrow depression (including thrombocytopenia, leukopenia and agranulocytosis).

Food Interaction

No interactions found.

Elimination Route

Deoxyfluorouridine can be excreted as unchanged drug, urea, fluorouracil, a-fluoro-bureidopropionic acid, dihydrofluorouracil, a-fluoro-b-guanidopropionic acid and a-fluoro-b-alanine via the kidneys. Deoxyfluorouridine may also be excreted as respiratory carbon dioxide.

Innovators Monograph

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*** Taking medicines without doctor's advice can cause long-term problems.
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