Fluorouracil
ADRUCIL
What it isAntimetabolite blocking thymidylate synthase; colorectal and other cancers, and topically for actinic keratoses.
Why it mattersThe topical form clears field cancerization that cryotherapy cannot reach, treating visible and subclinical lesions together.
What it changesDPD deficiency causes life-threatening systemic toxicity, so testing is advised before systemic use. Topical treatment produces an alarming inflammatory reaction that must be explained in advance.
FDA-approved for
- colorectal, breast, gastric and pancreatic cancer
- actinic keratosis and superficial basal cell carcinoma (topical)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Colorectal adenocarcinoma (infusional, with leucovorin ± oxaliplatin/irinotecan) | Adults | 400 mg/m² IV bolus day 1 | then 2400–3000 mg/m² CI over 46 h q2wk | |
| Colorectal adenocarcinoma (bolus, with leucovorin) | Adults | 500 mg/m² IV bolus days 1,8,15,22,29,36 | 8-week cycles | |
| Breast adenocarcinoma (cyclophosphamide-based regimen) | Adults | 500 or 600 mg/m² IV days 1 and 8 | q28 days × 6 cycles | |
| Gastric adenocarcinoma (platinum-based regimen) | Adults | 200–1000 mg/m² CI over 24 h | per regimen | |
| Pancreatic adenocarcinoma (infusional, with leucovorin) | Adults | 400 mg/m² IV bolus day 1 | then 2400 mg/m² CI over 46 h q2wk |
Renal Undefined
Hepatic Undefined
Instructions
- Test for DPYD gene variants prior to initiating unless immediate treatment is necessary
- IV bolus or infusion; do not inject the entire vial contents directly into a patient
- Do not administer in the same IV line concomitantly with other products
- Withhold and resume at a reduced dose for cardiac, neurologic, GI, hematologic, or dermatologic toxicity
Cautions
- Cardiotoxicity (angina, MI/ischemia, arrhythmia, heart failure)
- Hyperammonemic encephalopathy
- Neurologic toxicity (acute cerebellar syndrome)
- Severe diarrhea
- Palmar-plantar erythrodysesthesia (hand-foot syndrome)
- Severe/fatal myelosuppression
- Mucositis
- Elevated INR with warfarin
- Embryofetal toxicity
Adverse reactions
- Myelosuppression (neutropenia, thrombocytopenia, anemia)
- Diarrhea
- Mucositis / stomatitis
- Hand-foot syndrome
- Nausea
- Vomiting
- Alopecia
- Cardiotoxicity
Pregnancy Category D; can cause fetal harm. Teratogenic/embryolethal in animals. Advise effective contraception during and for 3 months after therapy.
Lactation Unknown if present in human milk; discontinue nursing or the drug given potential for serious adverse reactions in infants.
NO BOXED WARNINGS
Principal riskDPD deficiency causes life-threatening toxicity
Cost, est. cash$50–$10,000/month or cycle
Generic entry1982
Classes and tags
Clinical profile
Legacy pregnancy categoryD
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
Mechanism of action: Fluorouracil ballicule
