Floxuridine is a fluorinated pyrimidine nucleoside analogue and antineoplastic antimetabolite. Chemically, it is known as 2′-deoxy-5-fluorouridine and is closely related to 5-fluorouracil. Floxuridine has the molecular formula C₉H₁₁FN₂O₅, molecular weight 246.19 g/mol, and CAS Registry Number 50-91-9.
Floxuridine interferes primarily with DNA synthesis through its conversion to active metabolites, including fluorodeoxyuridine monophosphate, which inhibits thymidylate synthase. It can also affect RNA synthesis.
Floxuridine is described as a white to off-white, odorless solid and is freely soluble in water. A 2% aqueous solution has a reported pH of 4.0–5.5.
The compound is recognized in the USP-NF monograph, which specifies an assay of NLT 98.5% and NMT 101.0%, calculated on the dried basis.
Floxuridine is an antineoplastic antimetabolite. The pharmaceutical product Floxuridine for Injection is supplied as a sterile, nonpyrogenic lyophilized powder and is intended for intra-arterial infusion.
Floxuridine is converted to metabolites that interfere with DNA synthesis. Its active metabolite inhibits thymidylate synthase, reducing the availability of thymidine required for DNA synthesis. Floxuridine can also inhibit RNA formation to a lesser extent.
Floxuridine has an established USP monograph. USP specifies:
Floxuridine should be stored and handled according to the applicable manufacturer specification, pharmacopoeial requirements and safety documentation. As an antineoplastic compound, appropriate occupational handling controls should be followed.
Floxuridine API should be packed in suitable pharmaceutical-grade, tightly closed containers that protect the material from contamination and inappropriate environmental exposure.
Floxuridine is a well-characterized fluorinated pyrimidine with an established USP-NF monograph and defined pharmacopoeial assay requirements. For pharmaceutical sourcing, quality evaluation should focus on identity, assay, impurities, moisture-related characteristics and compliance with the applicable pharmacopeial specification.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.5%–101.0% on dried basis |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | NMT 0.5% |
| Melting Point | 145–153 °C |