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Floxuridine | CAS No: 50-91-9 | GMP-certified suppliers
A medication that provides palliative treatment for liver metastases from gastrointestinal adenocarcinoma and primary liver cancer through targeted intra-arterial infusion in selected patients.
Therapeutic categories
Primary indications
- 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)
Product Snapshot
- Floxuridine is available as a lyophilized powder for injection intended for intra-arterial administration
- It is primarily used for palliative management of metastatic gastrointestinal adenocarcinoma to the liver and liver cancer
- Floxuridine is approved for use in the United States
Clinical Overview
Clinically, floxuridine is indicated for palliative treatment of hepatic metastases originating from gastrointestinal adenocarcinomas and for palliation in primary liver malignancies. Administration is typically achieved through slow, continuous intra-arterial infusion directly into the hepatic artery in selected patients who are considered unsuitable for curative surgical intervention or other therapeutic modalities.
Pharmacodynamically, floxuridine functions as a pyrimidine analog that disrupts the S phase of cell division by mimicking endogenous pyrimidines and inhibiting DNA synthesis. Upon administration, it is rapidly catabolized to 5-fluorouracil (5-FU), the active antineoplastic agent. 5-FU inhibits thymidylate synthetase via its active metabolite 5-fluoro-2'-deoxyuridine-5'-phosphate (FUDR-MP), obstructing the methylation of deoxyuridylic acid to thymidylic acid and thereby hindering DNA replication. Additionally, 5-FU can incorporate into RNA, interrupting normal RNA function, and inhibit riboside phosphorylase activity, which affects uracil salvage pathways.
Pharmacokinetic considerations include rapid metabolism to 5-FU and predominantly renal excretion. Floxuridine demonstrates a narrow therapeutic index and notable myelosuppressive effects, necessitating monitoring for hematologic toxicity. Its profile as a strong inhibitor of cytochrome P450 CYP2C9 also warrants consideration for potential drug interactions.
Safety monitoring focuses on toxicity management, including bone marrow suppression and hepatic function assessment. Given its administration route and narrow therapeutic window, use is confined to specialized oncology treatment settings.
When sourcing floxuridine API, attention should be directed to its purity, sterility, and compliance with pharmacopeial standards. The lyophilized powder form requires strict control of microbial contamination and endotoxin levels. Quality assurance must also verify stability parameters pertinent to storage and reconstitution protocols to ensure clinical efficacy and safety.
Identification & chemistry
| Generic name | Floxuridine |
|---|---|
| Molecule type | Small molecule |
| CAS | 50-91-9 |
| UNII | 039LU44I5M |
| DrugBank ID | DB00322 |
Pharmacology
| Summary | Floxuridine is an antimetabolite pyrimidine analog prodrug that is rapidly converted to 5-fluorouracil, its active metabolite. It exerts its therapeutic effects primarily by inhibiting thymidylate synthase, disrupting DNA synthesis, and interfering with RNA processing, thereby targeting rapidly proliferating cells. This mechanism underlies its use in palliative treatment of metastatic gastrointestinal and liver cancers. |
|---|---|
| Mechanism of action | Floxuridine 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. Floxuridine 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. |
| Pharmacodynamics | Floxuridine 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. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Thymidylate synthase | Humans |
ADME / PK
| Metabolism | Hepatic. |
|---|---|
| Route of elimination | Floxuridine 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. Floxuridine may also be excreted as respiratory carbon dioxide. |
Formulation & handling
- Floxuridine is a small molecule cytotoxic agent intended for intra-arterial injectable administration as a lyophilized powder for solution.
- Its relatively high water solubility and negative LogP suggest good aqueous dissolution but limited lipid membrane permeability, impacting formulation strategies.
- Stability considerations include proper storage of the lyophilized powder to maintain potency and avoid degradation prior to reconstitution.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is currently marketed in the US with patents expired, allowing for generic competition and indicating a mature market phase. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | Floxuridine is supplied by multiple manufacturers and packagers, including App Pharmaceuticals LLC, Bedford Laboratories, Ben Venue Laboratories Inc., Ethex Corp., and Hospira Inc., primarily serving the US market. Several branded products are available under similar names, indicating a presence of originator companies with established branded offerings. Given the availability of multiple manufacturers and the US-focused market, patent expiry likely supports existing generic competition. |
|---|
Safety
| Toxicity | Oral, rat LD<sub>50</sub>: 215 mg/kg. Signs of overdose include nausea, vomiting, diarrhea, gastrointestinal ulceration and bleeding, and bone marrow depression (including thrombocytopenia, leukopenia and agranulocytosis). |
|---|
- Handle with appropriate protective equipment to avoid ingestion or inhalation due to significant toxicity (oral LD50 in rats: 215 mg/kg)
- Avoid skin and eye contact
- Potential for systemic toxicity upon exposure
Floxuridine is a type of Antimetabolites
Antimetabolites are a prominent category of pharmaceutical active pharmaceutical ingredients (APIs) utilized in the treatment of various diseases, particularly cancer. These compounds are structurally similar to naturally occurring metabolites essential for cellular processes such as DNA and RNA synthesis. By mimicking these metabolites, antimetabolites interfere with the normal functioning of cellular pathways, leading to inhibition of cancer cell growth and proliferation.
One of the widely used antimetabolites is methotrexate, a folic acid antagonist that inhibits the enzyme dihydrofolate reductase, disrupting the production of DNA and RNA. This disruption impedes the growth of rapidly dividing cancer cells. Another common antimetabolite is 5-fluorouracil (5-FU), which inhibits the enzyme thymidylate synthase, thereby interfering with DNA synthesis and inhibiting cancer cell proliferation.
Antimetabolites can be classified into several subcategories based on their mechanism of action and chemical structure. These include purine and pyrimidine analogs, folic acid antagonists, and pyrimidine synthesis inhibitors. Examples of antimetabolites in these subcategories include azathioprine, cytarabine, and gemcitabine.
Despite their effectiveness, antimetabolites can exhibit certain side effects due to their interference with normal cellular processes. These side effects may include gastrointestinal disturbances, myelosuppression (reduced production of blood cells), and hepatotoxicity.
In conclusion, antimetabolites are a vital category of pharmaceutical APIs used in the treatment of various diseases, especially cancer. By mimicking natural metabolites and disrupting crucial cellular processes, these compounds effectively inhibit cancer cell growth and proliferation. However, their usage should be carefully monitored due to potential side effects.
Floxuridine API manufacturers & distributors
Compare qualified Floxuridine API suppliers worldwide. We currently have 2 companies offering Floxuridine API, with manufacturing taking place in 2 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Reliable Biopharm | Producer | United States | United States | CoA, USDMF | 11 products |
| Zhejiang Hisun Pharma | Producer | China | China | CoA, USDMF | 69 products |
When sending a request, specify which Floxuridine API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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