Fluorouracil
ADRUCIL
Pronunciation: floor-oe-YOOR-a-sil
What it isAntimetabolite blocking thymidylate synthase; colorectal and other cancers, and topically for actinic keratoses.
Why it mattersTopical 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)
Principal riskDPD deficiency causes life-threatening toxicity
Classes and tags
Clinical profile
Legacy pregnancy categoryD
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
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 before 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
Available strengths
- inj 25, 50 mg/mL
- sol 2, 5 %
- cream 0.5, 4, 5 %
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.
Cost
| Strength | #/mo | generic $/unit | CostPlus | |
|---|---|---|---|---|
| 25 mg/mL | inj | per unit | not offered | |
| 50 mg/mL | inj | per unit | not offered |
Generic entry1982
Open Fluorouracil in the interactive console ↗
Self-check
- Which enzyme deficiency can cause life-threatening systemic fluorouracil toxicity?
DPD deficiency. - What lesions can topical fluorouracil treat beyond visible lesions?
Subclinical lesions in the treatment field.