Name: | Floxuridine |
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PubChem Compound ID: | 10966793 |
Description: | An antineoplastic antimetabolite that is metabolized to fluorouracil when administered by rapid injection; 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. |
Molecular formula: | C9H11FN2O5 |
Molecular weight: | 246.193 g/mol |
Name: | Floxuridine |
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Name (isomeric): | DB00322 |
Drug Type: | small molecule |
Description: | An antineoplastic antimetabolite that is metabolized to fluorouracil when administered by rapid injection; 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. |
Synonyms: |
Floxiridina [INN-Spanish]; FDURD; Floxuridinum [INN-Latin]; Fluorodeoxyuridine; Deoxyfluorouridine; Fluoruridine Deoxyribose; FDUR; 5FDU; Floxuridin; 5 Fluorodeoxyuridine
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Brand: | FUDR |
Category: | Antimetabolites, Antimetabolites, Antineoplastic, Antineoplastics |
CAS number: | 50-91-9 |
Indication: | 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). |
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Pharmacology: |
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 ...
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Mechanism of Action: |
Floxuridine is rapidly catabolized to 5-fluorouracil, which is the active form of the drug. The primary effect is interference with DNA synthesis and to a lesser extent, inhibition of RNA formation through the drug's incorporation into RNA, thus leading to the production of fraudulent RNA. Fluorouracil also inhibits uracil riboside phophorylase, wh...
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Biotransformation: | Hepatic. |
Route of elimination: | The drug is excreted intact and as urea, fluorouracil, a-fluoro-bureidopropionic acid, dihydrofluorouracil, a-fluoro-b-guanidopropionic acid and a-fluoro-b-alanine in the urine; it is also expired as respiratory carbon dioxide. |
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). |
Affected organisms: | Humans and other mammals |
Drug interaction: |
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