5-Fluorouracil

---

Product Name :	5-Fluorouracil
Specs :	USP/BP/EP
Cas No.：	51-21-8
Product Serie：	Anti-Cancer Drug
Product  Details ：	Molecular Formula: C4H3FN2O2    Molecular Weight: 130.08

Back      Home

Overview

A cornerstone of antineoplastic therapy, it belongs to the antimetabolite class, interfering with DNA and RNA synthesis by replacing thymine in nucleic acid chains. This white crystalline powder is slightly soluble in water, stable under refrigeration, and highly reactive, making it a versatile agent in both systemic and topical cancer treatment. Discovered in the 1950s, it remains a gold standard for solid tumor therapy due to its broad-spectrum activity and established efficacy across diverse cancer types.

Features

Mechanism of Action:

DNA/RNA Interruption: Converted intracellularly to 5-fluorodeoxyuridine monophosphate (5-FdUMP), which inhibits thymidylate synthase, blocking thymidine synthesis and inducing single-strand DNA breaks.

S-Phase Specificity: Primarily targets rapidly dividing cells, though it also exhibits activity in non-dividing cells via RNA misincorporation, expanding its utility in slow-growing tumors.

Pharmacokinetic Flexibility:

Route Diversity: Administered intravenously (IV), topically (cream), or intra-arterially (for hepatic metastases), with IV formulations achieving peak plasma concentrations of 1-2 μg/mL and a short half-life of 10-20 minutes, necessitating continuous infusion for sustained exposure.

Tumor Targeting: Poor lipid solubility limits CNS penetration, reducing neurotoxicity, while high accumulation in tumor tissues (3x normal cells) enhances therapeutic index.

Clinical Utility:

Broad Antitumor Spectrum: Effective against adenocarcinomas (gastric, colorectal, breast, pancreatic), squamous cell carcinomas (head/neck, skin), and Kaposi's sarcoma.

Combination Synergy: Enhances cisplatin, oxaliplatin, and irinotecan efficacy in FOLFOX/FOLFIRI regimens, and synergizes with radiation therapy via radiosensitization.

Topical Efficacy:

Dermatological Applications: 5-FU cream (5% concentration) induces apoptosis in actinic keratosis and superficial basal cell carcinoma, leveraging local delivery to minimize systemic toxicity.

Applications

Oncological Therapies:

Gastrointestinal Cancers: First-line for advanced gastric/colorectal cancer, often combined with leucovorin to enhance thymidylate synthase inhibition (e.g., LV5FU2 protocol).

Breast Cancer: Used in adjuvant therapy (CAF regimen: cyclophosphamide, doxorubicin, 5-FU) to reduce recurrence in HER2-negative tumors.

Head and Neck Cancer: Combined with cisplatin and radiation (chemoradiation) to improve locoregional control in squamous cell carcinomas.

Research Applications:

Antiviral Studies: Investigated for inhibiting RNA viruses due to its nucleoside analog properties, though clinical use remains restricted to oncology.

Pharmacodynamic Modeling: Serves as a model compound for developing prodrugs (e.g., capecitabine, its oral prodrug) with improved bioavailability and reduced toxicity.

Safety Considerations

While myelosuppression (neutropenia, thrombocytopenia) and mucositis are common, dose adjustment based on creatinine clearance (eGFR <30 mL/min) and LFT monitoring mitigate risks. Our product adheres to ICH Q7 guidelines, with residual solvent limits (ethanol ≤500ppm, DMSO ≤1000ppm) and endotoxin levels <0.25 EU/mg, ensuring compliance with parenteral standards.