FAVLYXA Fluorouracil 25 mg/mL Injection, Solution
🆔 Identity & classification
Where does this data come from?
🏷️ RxNorm drug class
This medicine belongs to the Nucleoside Metabolic Inhibitor class.
Where does this data come from?
🏭 Manufacturer & labeler
Where does this data come from?
🩺 Clinical
Fluorouracil is generally used in combination with other medications to treat colon cancer or rectal cancer (cancer that begins in the large intestine) that has gotten worse or spread to other parts of the body. Fluorouracil is used in combination with other medications to treat certain types of breast cancer after surgery to remove the tumor or radiation therapy. Fluorouracil is also used to treat cancer of the pancreas and stomach cancer. Fluorouracil is in a class of medications called antimetabolites. It works by slowing or stopping the growth of cancer cells in your body.
Read the full MedlinePlus article ↗- Fluorouracil is used to treat four types of cancer: colorectal (colon and rectal), breast, stomach, and pancreatic. You're almost certainly receiving it alongside other chemotherap...
- What cancers does fluorouracil treat, and why am I getting it with other drugs?
- There's an enzyme in your body called DPD that breaks down more than 80% of fluorouracil. Some people are born with gene changes (in a gene called DPYD) that mean their DPD enzyme...
- I heard there's a genetic test I should have before starting — what is that about?
Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Fluorouracil — tap one for details:
Fluorouracil may be associated with lower levels of 2 nutrients — worth a chat with your pharmacist, not a cause for alarm.
Where does this data come from?
Ask a licensed pharmacist directly — free, answered by our team.
🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
-
UNII 55X04QC32I
A strong alkaline chemical used to adjust and maintain the pH balance of liquid medicines. It helps keep the medicine stable and ensures it stays effective during storage.
-
UNII 059QF0KO0R
Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
2 inactive ingredients listed in the exact product block matched to this NDC.
Where does this data come from?
ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
Are inactive ingredients the same for every manufacturer?
Why might an inactive ingredient be missing?
Can inactive ingredients matter?
💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · quarterly | No Part D plan price is available for this NDC in our data. | |
Where does this data come from?
🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Favlyxa 25 mg/mL 83831-0143-01 | Avyxa | 1 vial | — | — | FDA listed | — |
| Favlyxa 25 mg/mLthis 83831-0164-10 | Avyxa | 1 vial | — | — | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
The FDA lists approved generic versions of this medicine, but that does not always mean a pharmacy can get one today. Patent rules, launch agreements, supply and pricing can affect when generics actually arrive.
Where does this data come from?
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
🔬 Reported adverse events (FAERS)
Top reported reactions
Age at onset
Reporter sex
Serious outcomes
Where does this data come from?
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 83831-0164-10 You're viewing this | 1 VIAL, MULTI-DOSE in 1 CARTON (83831-164-10) / 100 mL in 1 VIAL, MULTI-DOSE | 2026-07-15 | Active |
🧭 About this NDC listing & data coverage
What data is (and isn’t) available for this NDC — tap to expand
| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | — Not published for this NDC Applies only to products approved under an NDA/ANDA; many listings are out of scope. |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
Questions about this listing
Why is there no price listed?
Is the NDC printed on the package the same as the 11-digit billing NDC?
What do the three segments of this NDC mean?
Is this package still being marketed?
Who lists this product with the FDA?
Do I need a prescription for this product?
Where does this data come from?
📄 Full prescribing information FDA SPL
🚨 Boxed Warning ▾
WARNING: SERIOUS ADVERSE REACTIONS OR DEATH IN PATIENTS WITH COMPLETE DPD DEFICIENCY Increased risk of serious adverse reactions or death in patients with complete DPD deficiency. Test patients for genetic variants of DPYD prior to initiating FAVLYXA unless immediate treatment is necessary. Avoid use of FAVLYXA in patients with certain homozygous or compound heterozygous DPYD variants that result in complete DPD deficiency [see Warnings and Precautions (5.1) ].
WARNING: SERIOUS ADVERSE REACTIONS OR DEATH IN PATIENTS WITH COMPLETE DPD DEFICIENCY Increased risk of serious adverse reactions or death in patients with complete DPD deficiency. Test patients for genetic variants of DPYD prior to initiating FAVLYXA unless immediate treatment is necessary. Avoid use of FAVLYXA in patients with certain homozygous or compound heterozygous DPYD variants that result in complete DPD deficiency.
( 5.1 )
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE FAVLYXA is indicated for the treatment of patients with: FAVLYXA is a nucleoside metabolic inhibitor indicated for the treatment of patients with: Adenocarcinoma of the Colon and Rectum ( 1.1 ) Adenocarcinoma of the Breast ( 1.2 ) Gastric Adenocarcinoma ( 1.3 ) Pancreatic Adenocarcinoma ( 1.4 )
1.1 Adenocarcinoma of the Colon and Rectum
1.2 Adenocarcinoma of the Breast
1.3 Gastric Adenocarcinoma
1.4 Pancreatic Adenocarcinoma
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION FAVLYXA is recommended for administration either as an intravenous bolus or as an intravenous infusion. ( 2.1 ) Adenocarcinoma of the Colon and Rectum In combination with leucovorin or as a component of a multidrug chemotherapy regimen that includes leucovorin (infusional regimen): 400 mg/m 2 for one dose, followed by 2,400 mg/m 2 to 3,000 mg/m 2 over 46 hours on day 1 of each 2-week cycle or In combination with leucovorin (bolus regimen): 500 mg/m 2 on days 1, 8, 15, 22, 29 and 36 of each 8-week cycle.
( 2.2 ) Adenocarcinoma of the Breast in combination with a cyclophosphamide-based multidrug regimen: 500 mg/m 2 or 600 mg/m 2 on days 1 and 8 of each 28-day cycle (bolus regimen). ( 2.2 ) Gastric Adenocarcinoma in combination with a platinum-containing multidrug regimen: 200 mg/m 2 to 1,000 mg/m 2 over 24 hours (infusional regimen). ( 2.2 ) Pancreatic Adenocarcinoma in combination with leucovorin or as a component of a multidrug chemotherapy regimen that includes leucovorin: 400 mg/m 2 on day 1, followed by 2,400 mg/m 2 over 46 hours every 2 weeks (infusional regimen).
( 2.2 ) Refer to Section 2.3 for dosage modifications due to adverse reactions.
2.1Evaluation and Testing for DPD Deficiency Before Initiating FAVLYXA Prior to initiating FAVLYXA, test patients for genetic variants of the DPYD gene unless immediate treatment is necessary. An FDA-authorized test for the detection of the DPYD gene to identify patients at risk of serious adverse reactions with FAVLYXA is not currently available. Currently available tests used to identify DPYD variants may vary in accuracy and design (e.g., which DPYD variant(s) they identify).
Avoid use of FAVLYXA in patients known to have certain homozygous or compound heterozygous DPYD variants that result in complete DPD deficiency . No FAVLYXA dose has been proven safe for patients with complete DPD deficiency. For patients with partial DPD deficiency, individualize the dosage and modify based on tolerability and intent of treatment [see Warnings and Precautions (5.1) ] .
2.2Recommended Dosage FAVLYXA is recommended for administration either as an intravenous bolus or as an intravenous infusion. Dosage recommendations are in Table 1. Table 1: Recommended dosage of FAVLYXA Indication Recommended Dosage Duration of Treatment Adenocarcinoma of the Colon and Rectum In combination with leucovorin or as a component of a multidrug chemotherapy regimen that includes leucovorin 400 mg/m 2 for one dose, followed by 2,400 mg/m 2 to 3,000 mg/m 2 over 46 hours on day 1 of each 2-week cycle Until disease progression or unacceptable toxicity.
In combination with leucovorin alone (bolus regimen) 500 mg/m 2 on days 1, 8, 15, 22, 29 and 36 of each 8-week cycle Until disease progression or unacceptable toxicity. Adenocarcinoma of the Breast In combination with cyclophosphamide-based multidrug regimen (bolus regimen) 500 mg/m 2 or 600 mg/m 2 on days 1 and 8 of each 28-day cycle Until disease progression or unacceptable toxicity or 6 cycles Gastric Adenocarcinoma In combination with a platinum-containing multidrug regimen 200 mg/m 2 to 1,000 mg/m 2 over 24 hours Frequency in each cycle and length of each cycle depend on dose of FAVLYXA and specific regimen Pancreatic Adenocarcinoma In combination with leucovorin or as a component of a multidrug chemotherapy regimen that includes leucovorin 400 mg/m 2 on day 1, followed by 2,400 mg/m 2 over 46 hours every 2 weeks Until disease progression or unacceptable toxicity.
2.3Dosage Modifications for Adverse Reactions Withhold FAVLYXA for the following adverse reactions. Depending on the severity of the adverse reaction, either discontinue or resume FAVLYXA at a reduced dosage upon resolution or improvement to Grade 1: Grade 3 or 4 diarrhea [see Warnings and Precautions (5.5) ] Grade 2 or 3 palmar-plantar erythrodysesthesia (hand-foot syndrome) [see Warnings and Precautions (5.6) ] Grade 3 or 4 mucositis [see Warnings and Precautions (5.8) ] Gra…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Injection: FAVLYXA contains 25 mg/mL fluorouracil as a colorless to light yellow clear solution and is available as: 250 mg/10 mL (25 mg/mL) in a single-dose vial. 2,500 mg/100 mL (25 mg/mL) in a multiple-dose vial. Injection: 250 mg/10 mL (25 mg/mL) in a single-dose vial. ( 3 ) 2,500 mg/100 mL (25 mg/mL) in a multiple-dose vial. ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS None. None. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Cardiotoxicity: FAVLYXA can cause cardiotoxicity, including angina, myocardial infarction/ischemia, arrhythmia, and heart failure. Withhold FAVLYXA for cardiac toxicity. ( 5.2 ) Hyperammonemic Encephalopathy: Altered mental status, confusion, disorientation, coma, or ataxia with elevated serum ammonia level can occur within 72 hours of initiation of FAVLYXA.
Withhold FAVLYXA and initiate ammonia-lowering therapy. ( 5.3 ) Neurologic Toxicity: FAVLYXA can cause acute cerebellar syndrome, confusion, disorientation, ataxia, or visual disturbances. Withhold FAVLYXA for neurologic toxicity.
( 5.4 ) Diarrhea: FAVLYXA can cause severe diarrhea. Withhold FAVLYXA for severe diarrhea until resolved. ( 5.5 ) Palmar-Plantar Erythrodysesthesia Syndrome: Based on severity, withhold FAVLYXA until resolved or decreased to Grade 1, then resume at a reduced dose.
( 5.6 ) Myelosuppression: FAVLYXA can cause severe and fatal myelosuppression. Withhold FAVLYXA until severe myelosuppression resolves, then resume at a reduced dose. ( 5.7 ) Mucositis: FAVLYXA can cause severe mucositis.
Withhold FAVLYXA until resolved or decreased to Grade 1, then resume at a reduced dose. ( 5.8 ) Increased Risk of Bleeding with Concomitant Use of Warfarin: Concurrent administration with warfarin can result in clinically significant increases in coagulation parameters: Closely monitor INR and prothrombin time. ( 5.9 ) Embryofetal Toxicity: Can cause fetal harm.
Advise females and males of reproductive potential of the potential risk to a fetus and to use effective contraception. ( 5.10 , 8.1 , 8.3 )
5.1Serious Adverse Reactions or Death from Dihydropyrimidine Dehydrogenase (DPD) Deficiency Patients with certain homozygous or compound heterozygous variants in the DPYD gene known to result in complete or near complete absence of DPD activity (complete DPD deficiency) are at increased risk for acute early-onset toxicity and serious, including fatal adverse reactions due to FAVLYXA (e.g., mucositis, diarrhea, neutropenia, and neurotoxicity). Patients with partial DPD activity (partial DPD deficiency) may also have increased risk of serious or fatal adverse reactions.
Prior to initiating FAVLYXA, test patients for genetic variants of the DPYD gene unless immediate treatment is necessary [see Clinical Pharmacology (12.5) ] . Serious adverse reactions may still occur even if no DPYD variants are identified. Avoid use of FAVLYXA in patients with certain homozygous or compound heterozygous DPYD variants that result in complete DPD deficiency.
Withhold or permanently discontinue FAVLYXA based on clinical assessment of the onset, duration, and severity of adverse events in patients with evidence of acute early-onset or unusually severe reactions. No fluorouracil dose has been proven safe for patients with complete DPD deficiency. For patients with partial DPD deficiency, individualize the dosage and modify based on tolerability and intent of treatment.
An FDA-authorized test for the detection of genetic variants of the DPYD gene to identify patients at risk of serious adverse reactions with FAVLYXA treatment is not currently available. Currently available tests used to identify DPYD variants may vary in accuracy and design (e.g., which DPYD variant(s) they identify).
5.2Cardiotoxicity FAVLYXA can cause cardiotoxicity, including angina, myocardial infarction/ischemia, arrhythmia, and heart failure, based on postmarketing reports. Reported risk factors for cardiotoxicity are administration by continuous infusion rather than intravenous bolus and presence of coronary artery disease. Withhold FAVLYXA for cardiotoxicity.
The risks of resumption of FAVLYXA in patients with cardiotoxicity that has resolved have not been established [see Dosage and Administration (2.3) ].
5.3Hyperammonemic Encephalopathy FAVLYXA can cause hyperammonemic encephalopathy in the absence of liver disease or other identifiable cause, based on postmarketing reports. Signs or sympt…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following adverse reactions are discussed in more detail in other sections of the labeling: Serious adverse reactions or death from Dihydropyrimidine Dehydrogenase (DPD) deficiency [see Warnings and Precautions (5.1) ] Cardiotoxicity [see Warnings and Precautions (5.2) ] Hyperammonemic encephalopathy [see Warnings and Precautions (5.3) ] Neurologic toxicity [see Warnings and Precautions (5.4) ] Diarrhea [see Warnings and Precautions (5.5) ] Palmar-plantar erythrodysesthesia (hand-foot syndrome) [see Warnings and Precautions (5.6) ] Myelosuppression [see Warnings and Precautions (5.7) ] Mucositis [see Warnings and Precautions (5.8) ] Increased risk of bleeding with concomitant use of warfarin [see Warnings and Precautions (5.9) ] To report SUSPECTED ADVERSE REACTIONS, contact Avyxa Pharma, LLC at 1-888-520-0954 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.2Postmarketing Experience The following adverse reactions have been identified during postapproval use of fluorouracil. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Hematologic: pancytopenia [see Warnings and Precautions (5.7) ] Gastrointestinal: gastrointestinal ulceration, nausea, vomiting Allergic Reactions: anaphylaxis and generalized allergic reactions Neurologic: nystagmus, headache Dermatologic: dry skin; fissuring; photosensitivity, as manifested by erythema or increased pigmentation of the skin; vein pigmentation Ophthalmic: lacrimal duct stenosis, visual changes, lacrimation, photophobia Psychiatric: euphoria Miscellaneous: thrombophlebitis, epistaxis, nail changes (including loss of nails)
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS
7.1Effect of FAVLYXA on Other Drugs Vitamin K Antagonists Monitor INR and PT more frequently in patients receiving FAVLYXA and warfarin. Elevated INR and PT have been reported in patients taking fluorouracil concomitantly with warfarin.
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Lactation: Advise not to breastfeed ( 8.2 ) Infertility: May impair fertility. ( 8.3 )
8.1Pregnancy Risk Summary Based on mechanism of action and animal reproduction studies, FAVLYXA can cause fetal harm when administered during pregnancy [see Clinical Pharmacology (12.1) ]. Available data from observational studies with intravenous administration of fluorouracil during pregnancy are insufficient to identify a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. Administration of fluorouracil to rats and mice during selected periods of organogenesis, at doses lower than a human dose of 12 mg/kg, caused embryolethality and teratogenicity.
Malformations included cleft palate and skeletal defects. In monkeys, maternal doses of fluorouracil higher than an approximate human dose of 12 mg/kg resulted in abortion (see Data). In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2–4% and 15–20%, respectively.
Data Animal Data Malformations including cleft palate, skeletal defects and deformed appendages (paws and tails) were observed when fluorouracil was administered by intraperitoneal injection to mice at doses at or above 10 mg/kg (approximately 0.06 times a human dose of 12 mg/kg on a mg/m 2 basis) for 4 days during the period of organogenesis. Similar results were observed in hamsters administered fluorouracil intramuscularly at doses lower than those administered in commonly used clinical treatment regimens. In rats, administration of fluorouracil by intraperitoneal injection at doses greater than 15 mg/kg (approximately 0.2 times a human dose of 12 mg/kg on a mg/m 2 basis) for a single day during organogenesis resulted in delays in growth and malformations including micro-anophthalmos.
In monkeys, administration of fluorouracil during organogenesis at doses approximately equal to a human dose of 12 mg/kg on a mg/m 2 basis resulted in abortion; at a 50% lower dose, resorptions and decreased fetal body weights were reported.
8.2Lactation Risk Summary There are no data on the presence of fluorouracil or its metabolites in human milk, the effects on the breastfed child, or the effects on milk production. Because of the potential for serious adverse reactions in the breastfed child, advise patients not to breastfeed during treatment with FAVLYXA and for 1 week after the last dose.
8.3Females and Males of Reproductive Potential FAVLYXA can cause fetal harm when administered to a pregnant woman [see Use in Specific Populations (8.1 ) ] . Pregnancy Testing Verify that females of reproductive potential are not pregnant prior to initiating FAVLYXA [see Warnings and Precautions (5.10) , Use in Specific Populations (8.1 , 8.3) ]. Contraception Females Advise females of reproductive potential to use effective contraception during treatment with FAVLYXA and for 6 months after the last dose.
Males Based on genotoxicity findings, advise males with female partners of reproductive potential to use effective contraception during treatment with FAVLYXA and for 3 months after the last dose [see Nonclinical Toxicology (13.1) ]. Infertility Based on animal studies, FAVLYXA may impair fertility in females and males of reproductive potential [see Nonclinical Toxicology (13.1) ].
8.4Pediatric Use The safety and effectiveness of FAVLYXA in pediatric patients have not been established.
8.5Geriatric Use Reported clinical experience has not identified differences in safety or effectiveness between the elderly and younger patients.
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary Based on mechanism of action and animal reproduction studies, FAVLYXA can cause fetal harm when administered during pregnancy [see Clinical Pharmacology (12.1) ]. Available data from observational studies with intravenous administration of fluorouracil during pregnancy are insufficient to identify a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. Administration of fluorouracil to rats and mice during selected periods of organogenesis, at doses lower than a human dose of 12 mg/kg, caused embryolethality and teratogenicity.
Malformations included cleft palate and skeletal defects. In monkeys, maternal doses of fluorouracil higher than an approximate human dose of 12 mg/kg resulted in abortion (see Data). In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2–4% and 15–20%, respectively.
Data Animal Data Malformations including cleft palate, skeletal defects and deformed appendages (paws and tails) were observed when fluorouracil was administered by intraperitoneal injection to mice at doses at or above 10 mg/kg (approximately 0.06 times a human dose of 12 mg/kg on a mg/m 2 basis) for 4 days during the period of organogenesis. Similar results were observed in hamsters administered fluorouracil intramuscularly at doses lower than those administered in commonly used clinical treatment regimens. In rats, administration of fluorouracil by intraperitoneal injection at doses greater than 15 mg/kg (approximately 0.2 times a human dose of 12 mg/kg on a mg/m 2 basis) for a single day during organogenesis resulted in delays in growth and malformations including micro-anophthalmos.
In monkeys, administration of fluorouracil during organogenesis at doses approximately equal to a human dose of 12 mg/kg on a mg/m 2 basis resulted in abortion; at a 50% lower dose, resorptions and decreased fetal body weights were reported.
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of FAVLYXA in pediatric patients have not been established.
🧓 Geriatric Use ▾
8.5Geriatric Use Reported clinical experience has not identified differences in safety or effectiveness between the elderly and younger patients.
🆘 Overdosage ▾
10 OVERDOSAGE Administer uridine triacetate within 96 hours following the end of FAVLYXA infusion for management of fluorouracil overdose.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Fluorouracil is a nucleoside metabolic inhibitor that interferes with the synthesis of deoxyribonucleic acid (DNA) and to a lesser extent inhibits the formation of ribonucleic acid (RNA); these affect rapidly growing cells and may lead to cell death. Fluorouracil is converted to three main active metabolites: 5-fluoro-2′-deoxyuridine-5′-monophosphate (FdUMP), 5-fluorouridine-5′triphosphate (FUTP) and 5-fluoro-2′-deoxyuridine-5′-triphosphate (FdUTP). These metabolites have several effects including the inhibition of thymidylate synthase by FdUMP, incorporation of FUTP into RNA and incorporation of FdUTP into DNA.
12.2Pharmacodynamics Fluorouracil exposure-response relationships and the time course of the pharmacodynamic response are unknown.
12.3Pharmacokinetics Distribution Following bolus intravenous injection, fluorouracil distributes throughout the body including the intestinal mucosa, bone marrow, liver, cerebrospinal fluid and brain tissue. Elimination Following bolus intravenous injection, 5 to 20% of the parent drug is excreted unchanged in the urine in six hours. The remaining percentage of the administered dose is metabolized, primarily in the liver.
The metabolites of fluorouracil (e.g., urea and α-fluoro-ßalanine) are excreted in the urine over 3 to 4 hours. Following bolus intravenous injection of fluorouracil, as a single agent, the elimination half-life increased with dose from 8 to 20 minutes.
12.5Pharmacogenomics The DPYD gene encodes the enzyme DPD, which is responsible for the catabolism of >80% of fluorouracil. Approximately 3 to 5% of White populations have partial DPD deficiency and 0.2% of White populations have complete DPD deficiency, which may be due to certain genetic no function or decreased function variants in DPYD resulting in partial to complete or near complete absence of enzyme activity. DPD deficiency is estimated to be more prevalent in Black or African American populations compared to White populations.
Insufficient information is available to estimate the prevalence of DPD deficiency in other populations. Patients who are homozygous or compound heterozygous for no function DPYD variants (i.e., carry two DPYD variants that result in no DPD enzyme activity) or are compound heterozygous for a no function DPYD variant plus a decreased function DPYD variant have complete DPD deficiency and are at increased risk for acute early-onset of toxicity and serious life-threatening, or fatal adverse reactions due to increased systemic exposure to fluorouracil.
Partial DPD deficiency can result from the presence of either two decreased function DPYD variants or one normal function plus either a decreased function or a no function DPYD variant. Patients with partial DPD deficiency may also be at an increased risk for toxicity from fluorouracil. Several DPYD variants observed with variability across populations have been associated with reduced or no DPD activity, especially when present as homozygous or compound heterozygous variants.
These include c.1905+1G>A ( DPYD *2A), c.1679T>G ( DPYD *13), c.2846A>T, and c.1129-5923C>G (Haplotype B3). DPYD *2A and DPYD *13 are no function variants, and c.2846A>T, c.1129-5923C>G, and c557A>G are decreased function variants. This is not a complete listing of all DPYD variants that may result in DPD deficiency [see Warnings and Precautions (5.1) ] .
🧬 Mechanism of Action ▾
12.1Mechanism of Action Fluorouracil is a nucleoside metabolic inhibitor that interferes with the synthesis of deoxyribonucleic acid (DNA) and to a lesser extent inhibits the formation of ribonucleic acid (RNA); these affect rapidly growing cells and may lead to cell death. Fluorouracil is converted to three main active metabolites: 5-fluoro-2′-deoxyuridine-5′-monophosphate (FdUMP), 5-fluorouridine-5′triphosphate (FUTP) and 5-fluoro-2′-deoxyuridine-5′-triphosphate (FdUTP). These metabolites have several effects including the inhibition of thymidylate synthase by FdUMP, incorporation of FUTP into RNA and incorporation of FdUTP into DNA.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING
16.1How Supplied FAVLYXA™ Injection is a sterile colorless to light yellow clear solution available in single-dose vials and multiple-dose vials, individually packaged in a carton as follows: Strength Carton Contains NDC 250 mg/10 mL (25 mg/mL) 2,500 mg/100 mL (25 mg/mL) One single-dose vial One multiple-dose vial 83831-143-01 83831-164-10
16.2Storage Store at 20°C to 25°C (68°F to 77°F); excursions permitted from 15°C to 30°C (59°F to 86°F). [see USP Controlled Room Temperature]. Protect from light. Retain in carton until time of use. Fluorouracil is a hazardous drug. Follow applicable special handling and disposal procedures [see References (15) ] .
📋 Description ▾
11 DESCRIPTION FAVLYXA injection contains fluorouracil, a nucleoside metabolic inhibitor. Fluorouracil, a fluorinated pyrimidine, has a chemical name of 5-fluoro-2,4 (1 H ,3 H )-pyrimidinedione. Its structural formula is: Molecular formula: C 4 H 3 FN 2 O 2 Molecular weight: 130.08 g/mole FAVLYXA injection is a sterile, colorless to light yellow clear solution available in 250 mg/10 mL single-dose vials and 2,500 mg/100 mL multiple-dose vials for intravenous bolus or infusion administration.
Each mL contains 25 mg fluorouracil in water for injection. Sodium hydroxide is added to adjust the pH to 8.6 to 9.4. structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise patients of the following: Serious Adverse Reactions or Death from Dihydropyrimidine Dehydrogenase (DPD) Deficiency Prior to initiating FAVLYXA treatment, inform patients of the potential for serious or fatal adverse reactions due to DPD deficiency and testing for genetic variants of DPYD . Advise patients to immediately contact their healthcare provider if symptoms of severe mucositis, diarrhea, neutropenia, and neurotoxicity occur [see Warnings and Precautions (5.1) and Clinical Pharmacology (12.5) ] .
Cardiotoxicity Advise patients of the risk of cardiotoxicity and to immediately contact their healthcare provider for new onset of chest pain, shortness of breath, dizziness, or lightheadedness [see Warnings and Precautions (5.2) ] . Hyperammonemic Encephalopathy and Neurologic Toxicity Advise patients to immediately contact their healthcare provider or go to an emergency room for new onset of confusion, disorientation, or otherwise altered mental status; difficulty with balance or coordination; or visual disturbances [see Warnings and Precautions (5.3 , 5.4) ] .
Diarrhea Inform patients experiencing grade 2 or higher diarrhea (an increase of 4 to 6 stools/day or nocturnal stools) or experiencing severe bloody diarrhea with severe abdominal pain and fever to immediately contact their health care provider. Advise patients on the use of antidiarrheal treatments (e.g., loperamide) to manage diarrhea [see Warnings and Precautions (5.5) ] . Palmar-Plantar Erythrodysesthesia Syndrome Instruct patients experiencing grade 2 palmar-plantar erythrodysesthesia syndrome or greater to stop taking FAVLYXA immediately and to contact their healthcare provider.
Inform patients that initiation of symptomatic treatment is recommended, and hand-and-foot syndrome can lead to loss of fingerprints which could impact personal identification [see Warnings and Precautions (5.6) ] . Myelosuppression Inform patients who develop a fever of 100.5°F or greater or other evidence of potential infection to immediately contact their healthcare provider [see Warnings and Precautions (5.7) ] . Mucositis Inform patients experiencing grade 2 stomatitis (painful erythema, edema or ulcers of the mouth or tongue, but able to eat) or greater to contact their healthcare provider [see Warnings and Precautions (5.8) ] .
Increased Risk of Bleeding with Concomitant Warfarin Advise patients taking warfarin, that they are at an increased risk of severe bleeding while taking FAVLYXA. Advise these patients that INR should be monitored more frequently, and dosage modifications of warfarin may be required, while taking and after discontinuation of FAVLYXA. Advise these patients to immediately contact their healthcare provider if signs or symptoms of bleeding occur [see Warnings and Precautions (5.9) ].
Embryo-Fetal Toxicity Advise pregnant women and females of reproductive potential of the potential risk to a fetus. Advise females of reproductive potential to inform their healthcare provider of a known or suspected pregnancy [see Warnings and Precautions (5.10) , Use in Specific Populations (8.1) ] . Advise females of reproductive potential to use effective contraception during treatment with FAVLYXA and for 6 months after the last dose [see Use in Specific Populations (8.3) ] .
Advise males with female partners of reproductive potential to use effective contraception during treatment with FAVLYXA and for 3 months after the last dose [see Use in Specific Populations (8.3) ] . Lactation Advise females not to breastfeed during treatment with FAVLYXA and for 1 week after the last dose [see Use in Specific Populations (8.2) ] . Infertility Advise males and females of reproductive potential that FAVLYXA may impair fertility [see Use in Specific Populations (8.3) ] .
Drug interactions Advise patients to notify their healthcare provider of all drugs they are taking, including warfarin or other coumarin-derivative anticoagulants. Advise patients o…