FDA-filed SPL labeling · retrieved through openFDA

Trifluridine and Tipiracil

Trifluridine and tipiracil is a chemotherapy combination used to treat metastatic colorectal cancer and metastatic gastric or gastroesophageal junction cancer in adults who have already received other treatments.

Brand name Lonsurf
Drug classes Nucleoside Analog Antiviral
Rx Form 1 Route Oral
Dr. Brian Staiger, PharmD, BCPS
Reviewed by Last reviewed Jul 10, 2026
🧬 Where this information comes from Click to expand

The clinical label records used on this page are FDA-filed Structured Product Labeling (SPL) retrieved through openFDA. We identified 1 clinical label set within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. Forms, routes, brands, labelers, strengths, and NDC product-record counts are built separately from matching FDA National Drug Code Directory records. The linked DailyMed document is a representative official source for verification, not the page’s only clinical source. View the linked label on DailyMed →

At a glance
Linked label effectiveNov 5, 2025
AvailabilityRx
Earliest approval/marketing year 2015
FDA-listed product records 6
Boxed warningNone found in compared labels
How we combine label and product data →
No current FDA shortage listed · checked Sep 22, 2026
Trifluridine and Tipiracil at a glance The quick version — the full detail is in the Patient Information Guide below.
💊
HelloPharmacist Editorial Team Bottom Line
Lonsurf (trifluridine and tipiracil) is an oral chemotherapy used for metastatic colorectal cancer and metastatic gastric or gastroesophageal junction cancer after other treatments have been tried. Its most serious risk is severely lowering blood counts, which requires regular monitoring and can lead to dangerous infections. If you are of childbearing potential, reliable contraception is essential throughout treatment.

📖 Trifluridine and Tipiracil: Patient Information Guide

A plain-language walkthrough of Trifluridine and Tipiracil — what it treats, how it works, how it’s taken, side effects, warnings and interactions. Tap any section to expand it.

🎯What it's used for

Trifluridine and tipiracil (brand name Lonsurf) is a combination chemotherapy approved for two types of advanced cancer in adults:

  • Metastatic colorectal cancer: Lonsurf is used alone or combined with bevacizumab in patients who have already received fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF therapy, and — if their tumor is RAS wild-type — an anti-EGFR therapy.
  • Metastatic gastric or gastroesophageal junction adenocarcinoma: Lonsurf is used in patients who have received at least two prior chemotherapy regimens that included a fluoropyrimidine, a platinum drug, a taxane or irinotecan, and (if appropriate) HER2/neu-targeted therapy.
⚙️How it works

Lonsurf combines two drugs that work as a team. Trifluridine is a nucleoside analog — a molecule that mimics one of DNA's building blocks. Cancer cells absorb it and accidentally incorporate it into their DNA, which interferes with DNA synthesis and stops the cells from multiplying. Tipiracil blocks an enzyme called thymidine phosphorylase that would otherwise break trifluridine down too quickly. By slowing that breakdown, tipiracil keeps trifluridine active much longer — studies show trifluridine exposure is dramatically higher when the two are combined than when trifluridine is taken alone.

💊How it's taken

Lonsurf tablets are taken by mouth, twice a day, with food. The schedule follows a set pattern within a 28-day cycle: tablets are taken on days 1 through 5, then there is a break, and then again on days 8 through 12, followed by a rest period until the next cycle begins.

  • Swallow tablets whole — do not crush or split them.
  • If you miss or vomit a dose, skip it and take your next dose as scheduled — do not double up.
  • Your doctor calculates your dose based on your body surface area (height and weight). People with severe kidney impairment receive a lower starting dose.
  • Up to three dose reductions may be made if side effects require it — your doctor will guide you on this.
🤒Side effects — in detail

The most common side effects with Lonsurf — reported in 10% or more of patients — include:

  • Neutropenia (low white blood cells, raising infection risk)
  • Anemia (low red blood cells, causing tiredness and paleness)
  • Thrombocytopenia (low platelets, raising bleeding/bruising risk)
  • Fatigue or weakness
  • Nausea
  • Decreased appetite
  • Diarrhea
  • Vomiting
  • Abdominal pain
  • Fever (pyrexia)

Seek medical attention immediately if you develop fever or chills, signs of infection, unusual bleeding, or feel extremely unwell — these may signal life-threatening low blood counts or sepsis (a serious bloodstream infection).

⚠️Warnings & precautions
  • Severe myelosuppression (dangerously low blood counts): This is the most serious risk. Lonsurf can cause life-threatening drops in white blood cells, red blood cells, and platelets. Infections and sepsis have been fatal in a small number of patients. Blood counts are checked before each cycle starts and again on day 15. Doses may be held or reduced based on results.
  • Embryo-fetal toxicity: Lonsurf can cause serious harm or death to an unborn baby. Animal studies showed harm at doses below those used in people. Women who could become pregnant must use effective contraception during treatment and for at least 6 months after the last dose. Men should use condoms for at least 3 months after the last dose.
  • Breastfeeding: Do not breastfeed during treatment or for 1 day after the final dose, due to potential serious harm to a nursing infant.
  • Older adults: Patients 65 and older had higher rates of severe neutropenia, anemia, and thrombocytopenia and need close monitoring.
🔀What it interacts with

The FDA label for Lonsurf does not identify specific drug-drug interactions, but there are important handling and co-administration considerations:

  • Bevacizumab: Lonsurf may be used in combination with bevacizumab for metastatic colorectal cancer — refer to bevacizumab's own prescribing information for its dose and side-effect management.
  • Cytotoxic drug precautions: Lonsurf is a chemotherapy agent; always tell every member of your healthcare team (including dentists and other prescribers) that you are taking it.

This is not a complete list of interactions. Always talk with your doctor or pharmacist before starting, stopping, or changing any medication.

📋Before taking it
  • Pregnancy: Lonsurf can cause fetal harm. Confirm you are not pregnant before starting. Use effective contraception during treatment and for at least 6 months after your last dose.
  • Breastfeeding: Do not breastfeed during treatment or for 1 day after stopping — the drug or its breakdown products may pass into breast milk and could harm a nursing infant.
  • Males planning a family: Use condoms during treatment and for at least 3 months after your last dose due to the potential for the drug to affect genetic material (genotoxicity).
  • Severe kidney impairment: A lower dose is required. Tell your doctor if you have kidney disease or are on dialysis.
  • Moderate or severe liver impairment: Do not start Lonsurf if you have baseline moderate or severe liver impairment (hepatic impairment).
  • Older adults (65+): Higher risk of severe blood count drops — expect closer monitoring.
  • Children: Safety and effectiveness have not been established in pediatric patients.
📡Pharmacodynamics — effects in the body

Studies in patients with advanced solid tumors showed that Lonsurf, taken at the recommended dose, did not cause large changes in the heart's electrical activity (specifically, the QTc interval — a measure of heart rhythm timing). This suggests it is unlikely to cause the type of dangerous irregular heartbeat sometimes seen with other cancer drugs.

🔬Pharmacokinetics — how your body processes it

After taking Lonsurf by mouth, trifluridine reaches peak blood levels in about 2 hours. Tipiracil dramatically increases how much trifluridine the body absorbs — up to 37 times more exposure compared to taking trifluridine alone. A high-fat meal can lower peak blood levels of both ingredients but does not meaningfully change the total amount of trifluridine absorbed over time. Trifluridine is mainly broken down by an enzyme in the body (thymidine phosphorylase) into an inactive form, and most of the drug is cleared through the urine within 24 hours. Neither ingredient is processed by the liver's cytochrome P450 (CYP) enzyme system, which reduces the likelihood of common drug interactions through that pathway.

📦How to store it

Store at 20°C to 25°C (68°F to 77°F); excursions are permitted from 15°C to 30°C (59°F to 86°F) . stored outside of original bottle, discard after 30 days.

📄 Written from Trifluridine and Tipiracil’s FDA-approved label information, summarized in plain language with AI, and reviewed by our pharmacy team before publication. Every point is grounded in that labeling — nothing is invented. How we use AI →

17

Supplements & herbs that interact with Trifluridine and Tipiracil

17 supplements and herbal products have documented interactions with Trifluridine and Tipiracil in the licensed clinical database we use. Most are manageable — but your pharmacist should know about everything you take, including vitamins and herbals.

Severity mix
  • Major · 1
  • Moderate · 7
  • Minor · 9
Every supplement checked against Trifluridine and Tipiracil — ranked by severity The full interaction hub: 1 major · 7 moderate · 9 minor · every one linked to its full report. Check Trifluridine and Tipiracil against your exact supplements

Educational information from a licensed clinical database (Natural Medicines) — see our data sources & update cadence. Not medical advice: an interaction being documented does not mean it will happen to you; do not start or stop medications or supplements without professional guidance.

🩺 Pharmacist Counseling Corner

Quick, plain-English answers to the questions patients ask most about Trifluridine and Tipiracil — the kind of thing our pharmacy team would talk through with you at the counter.

What exactly is Lonsurf treating, and why am I on it?
Lonsurf is a chemotherapy medication used when colorectal cancer or stomach/esophageal junction cancer has spread and other treatments have already been tried. It's not a first-line drug — it's designed for people who have gone through multiple prior regimens. Your oncologist chose it because it's been shown to help in exactly your situation. It can be taken alone or, for colorectal cancer, alongside another drug called bevacizumab.
How do I take this medication — do I take it every day?
Not every single day — Lonsurf follows a cycle. You take it twice a day with food for 5 days in a row, take 2 days off, then take it again for another 5 days, then you get about 2 weeks of rest before the cycle repeats. Swallow the tablets whole, and always take them with a meal or snack. If you vomit a dose or realize you missed one, don't try to make it up — just continue with your next scheduled dose as normal.
What side effects should I watch out for?
The most common ones are fatigue, nausea, decreased appetite, diarrhea, and vomiting. Most people also experience drops in their blood counts — low white blood cells, red blood cells, or platelets — which is why your doctor will check your bloodwork regularly. The most important warning sign to act on immediately is fever or chills, which could mean your white blood cell count is dangerously low and you have an infection. Don't wait — call your care team or go to the ER if that happens.
Why do I need so many blood tests while I'm on this?
Lonsurf can significantly lower your blood counts, and that's the biggest safety concern with this medication. Your doctor checks your blood before each new cycle starts and again around day 15 to catch any problems early. If your counts drop too low, your dose may be paused or reduced — that's a normal and expected part of managing treatment. Those blood tests are protecting you.
Can I get pregnant while taking Lonsurf, or what if my partner could become pregnant?
This is very important. Lonsurf can seriously harm or even cause the loss of an unborn baby, so pregnancy must be avoided during treatment. If you could become pregnant, you need to use effective contraception while taking Lonsurf and for at least 6 months after your last dose. If you're a male patient with a female partner who could become pregnant, you should use condoms during treatment and for at least 3 months after your last dose. Talk to your doctor about the best contraceptive options for your situation.
Do I need to avoid any foods or other medications while taking Lonsurf?
You should take Lonsurf with food — that's actually required, not just a suggestion. A high-fat meal can affect how quickly the drug is absorbed, but your overall exposure stays about the same, so just make sure you're eating when you take it. The label doesn't list specific drug interactions through common liver pathways, but it's still essential to tell every one of your doctors and your pharmacist that you're on this medication. If you're also receiving bevacizumab alongside Lonsurf, follow your oncologist's instructions for both drugs separately.
Is Trifluridine and Tipiracil available over the counter?
Trifluridine and Tipiracil is dispensed by prescription according to its FDA labeling, so it isn't sold over the counter. Your prescriber and pharmacist will determine if it's appropriate for you.
When was Trifluridine and Tipiracil first available?
Trifluridine and Tipiracil has been available in the United States since at least 2015, based on FDA approval history (Drugs@FDA) and product marketing records.

💬 Answers drafted from Trifluridine and Tipiracil’s FDA-approved label information, summarized in plain language with AI, and reviewed by our pharmacy team before publication. Grounded in that labeling — nothing is made up. How we use AI →

🧰 Keep exploring

💊 How Trifluridine and Tipiracil comes

Trifluridine and Tipiracil is available in 1 form. Different forms and brands can have different approved uses, doses, schedules, and directions. Follow the instructions for your exact product, and do not switch forms without guidance from your prescriber or pharmacist.

Tablet

By mouth
Brands Lonsurf
How this form is used
What it may be used for
  • Lonsurf tablets are used to treat metastatic colorectal cancer in adults, either alone or with bevacizumab, after prior chemotherapy and targeted therapy
  • Lonsurf tablets are used to treat metastatic gastric or gastroesophageal junction adenocarcinoma in adults after at least two prior chemotherapy regimens
Important instructions
  • Lonsurf tablets should be taken by mouth twice daily with food, on days 1–5 and days 8–12 of each 28-day cycle
  • Lonsurf tablets should be swallowed whole
  • If a Lonsurf dose is missed or vomited, do not retake it — continue with the next scheduled dose
  • Lonsurf is a cytotoxic (cell-killing) drug — follow your pharmacist's instructions for safe handling and disposal
Available strengths 4 strengths
6 FDA-listed product records

📊 Trifluridine and Tipiracil across the U.S. market

How Trifluridine and Tipiracil appears in the FDA’s National Drug Code Directory — including its dosage forms, strengths, brand names, manufacturers, and FDA-listed product records. These are directory records, not sales or prescription volume.

1
Dose forms
1
Manufacturers
1
Brand names
6
FDA-listed product records
2015
First marketed

📈 How widely Trifluridine and Tipiracil is used

A general measure of how commonly Trifluridine and Tipiracil is prescribed, based on Medicaid — one of the largest public drug programs. The figure below is prescriptions filled in Q1–Q4 2025, summed across every form and brand of the drug.

Think of this as a proxy for how widely Trifluridine and Tipiracil is used, drawn from freely available public data. Medicaid is just one program — these numbers don’t include Medicare, other government coverage, or commercial and cash-pay prescriptions, so real-world use is higher than what’s shown here.

1,725
Medicaid prescriptions filled (Q1–Q4 2025)
$23.1M gross Medicaid reimbursement (before mandatory rebates — net cost is lower)

How commonly is Trifluridine and Tipiracil prescribed? Of the 1,596 medications we measure, Trifluridine and Tipiracil ranks #1,208 by Medicaid prescriptions — more than 24% of them.

Where Trifluridine and Tipiracil ranks among the drugs we measure · Q1–Q4 2025 · neighbors ±5

Utilization by Trifluridine and Tipiracil product

Pick a product to see its own Medicaid numbers. Each chip is one clinical product — a specific strength & dosage form as defined by RxNorm — with brand-name and generic versions combined.

The 8.19 mg / 20 mg oral tablet is the most-dispensed Trifluridine and Tipiracil product — about 69% of these Medicaid prescriptions.

tipiracil 8.19 MG / trifluridine 20 MG Oral Tablet Most dispensed

1,198 Medicaid prescriptions (Q1–Q4 2025) 69% of Trifluridine and Tipiracil prescriptions shown $17.8M gross reimbursement (before rebates) ≈ $14,881 per prescription (gross)

Summed across the 3 of 3 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 1670316

tipiracil 6.14 MG / trifluridine 15 MG Oral Tablet

527 Medicaid prescriptions (Q1–Q4 2025) 31% of Trifluridine and Tipiracil prescriptions shown $5.3M gross reimbursement (before rebates) ≈ $10,017 per prescription (gross)

Summed across the 3 of 3 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 1670311

Shares are of the Medicaid prescriptions shown here. Product grouping follows RxNorm (the National Library of Medicine’s drug terminology), so “one product” means one strength & dosage form regardless of manufacturer. Dollar figures are gross Medicaid reimbursement before mandatory rebates — rebates (often large, especially for brand-name drugs) are confidential, so actual net cost to Medicaid is lower than shown.

Source: Medicaid State Drug Utilization Data (CMS), aggregated by generic ingredient — summed across every NDC (all brands, strengths, salt forms and dosage forms) of Trifluridine and Tipiracil, and across all states and both fee-for-service and managed-care claims. A general popularity signal; it excludes Medicare, commercial insurance and cash prescriptions, so it is not total U.S. use. Based on the 6 of 6 listed Trifluridine and Tipiracil NDCs with Medicaid activity.

🔍 Compare Trifluridine and Tipiracil products

A representative set of FDA-listed product records for Trifluridine and Tipiracil — across manufacturers, strengths, and dosage forms, grouped by form with each product’s manufacturer and how the FDA approved it. The same medicine may be made and packaged by different companies, so a single drug can have many directory entries. (It’s also why a refill can look different — a new shape, color, or box — even though it contains the same medication.)

Strength Route Manufacturer / Labeler Category Details
💊Tablet
TRIFLURIDINE 15 mg/1; TIPIRACIL HYDROCHLORIDE 6.14 mg Oral Taiho Pharmaceutical Co., Ltd. NDA View NDC →
TRIFLURIDINE 20 mg/1; TIPIRACIL HYDROCHLORIDE 8.19 mg Oral Taiho Pharmaceutical Co., Ltd. NDA View NDC →
6.14; 15 mg/1; mg Oral Taiho Pharmaceutical Co., Ltd. × 2 listings NDA View NDC →
8.19; 20 mg/1; mg Oral Taiho Pharmaceutical Co., Ltd. × 2 listings NDA View NDC →

Showing 6 of 6 products — FDA National Drug Code Directory. See every product, package size and price: browse all 6 Trifluridine and Tipiracil NDCs →

🏷️ Sold under these brand names

Lonsurf

🏭 Manufacturers & labelers

Taiho Pharmaceutical Co., Ltd. 6

RxNorm drug class

Trifluridine and Tipiracil belongs to the Nucleoside Analog Antiviral class.

Pharmacologic class Nucleoside Analog Antiviral, Nucleoside Metabolic Inhibitor
Drug family (ATC) Antivirals
How it works Nucleic Acid Synthesis Inhibitors

Classified by RxNorm RxClass — the U.S. National Library of Medicine's standardized drug-classification service (Established Pharmacologic Class from the FDA, the ATC drug family from the WHO, and mechanism of action). Reference only, not medical advice.

🔬 Where this comes from

Core label, product, RxNorm, safety, and utilization data on this page come from the sources identified below. AI-written, editorial, and licensed sections are labeled separately.

📄
FDA-filed drug labels (SPL) Uses, dosing, warnings & side effects from SPL records retrieved through openFDA; the linked representative set can be verified on DailyMed. ✓ Linked label effective Nov 5, 2025
🏭
Forms, brands & labelersAggregated from ingredient-matched FDA National Drug Code Directory product records for Trifluridine and Tipiracil.
📈
Real-world reportsThe FDA Adverse Event Reporting System (FAERS), served through openFDA.
🚨
Recalls & shortagesopenFDA drug-enforcement reports and the FDA drug-shortage database.
🧾 Clinical label set — FDA-filed SPL labels retained for Trifluridine and Tipiracil after exact ingredient or ingredient-combination matching and applicable route/form matching
Clinical labels in scope
1
NDC products indexed
6
Distinct labelers/manufacturers represented
1
Linked representative label
Taiho Pharmaceutical Co., Ltd.
Linked label effective
Nov 5, 2025
Composite sections available
20
Linked SPL Set ID
f5beed22-d71d-4c0d-8dca-2c7317d65d85
Linked SPL Document ID
15b86e86-8940-44e3-921c-2e0b97180ea1
Open the linked representative label on DailyMed ↗

How we combine label and product data

HelloPharmacist combines public FDA and NLM records; we don’t author the underlying clinical facts. We identified 1 FDA-filed SPL label set within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. The representative label is the starting point for the displayed reference monograph; the 12 largest stored in-scope SPL records, which may include that representative, are compared section by section, and the longest available version of each section is retained. Forms, routes, brands, labelers, product-listed strengths, and product-record counts are aggregated separately from ingredient-matched FDA NDC Directory records; package records listed above are associated with the linked SPL; and the normalized concept hierarchy comes from NLM RxNorm.

For canonical ingredient pages, bounded product-attributed indication and administration excerpts may be added to the AI evidence, and the generator is instructed to preserve available product, brand, route, and form qualifiers instead of treating one label as universal. Where a section is identified as AI-written, its plain-language text is generated from bounded label evidence. New draft drug pages remain in the admin review queue before first publication. Taiho Pharmaceutical Co., Ltd. is the representative DailyMed label linked for verification and dates; it is not the sole source used for the page.

This is general education, not medical advice — always consult your doctor or pharmacist about your medications and any medical condition. For the exact wording of the linked representative label, view that label on DailyMed; some displayed composite sections may come from other in-scope SPL labels. Learn how we use AI and our data sources & update cadence.