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At a Glance

Lonsurf is an oral chemotherapy approved in adults to treat metastatic colorectal cancer and metastatic gastric or gastroesophageal junction adenocarcinoma that has progressed after, or is not suitable for, standard therapies.
This is a brand drug with no generic or biosimilar.
Active ingredients: Tipiracil Hydrochloride, Trifluridine.
Available as a prescription only.
Administration route: Oral.
In adults, Lonsurf is typically taken by mouth at 35 mg/m² (trifluridine component) twice daily on days 1–5 and 8–12 of a 28-day treatment cycle, with food.

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How It Works

  • Lonsurf contains two medicines: trifluridine, which damages the DNA of cancer cells so they cannot grow or divide, and tipiracil, which helps keep trifluridine levels high in the body.
  • By interfering with DNA building blocks, Lonsurf slows or stops the growth of certain colorectal and stomach cancers.
  • Because it targets fast-growing cells, it can also affect healthy blood and gut cells, leading to some of its side effects.
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Treatment and Efficacy

Approved indications: Lonsurf is FDA-approved for adults with metastatic colorectal cancer and for adults with metastatic gastric or gastroesophageal junction adenocarcinoma who have previously been treated with or are not candidates for standard regimens (including fluoropyrimidine-, platinum-, and taxane-based chemotherapy, anti-VEGF therapy, and anti-EGFR therapy when appropriate).

Off-label uses: Off-label, it may occasionally be considered in other advanced gastrointestinal cancers (for example, some small studies in pancreatic or other GI tumors), but these uses have more limited evidence and are not standard of care.

Efficacy expectations and timing: Lonsurf is generally used in later lines of therapy to help patients live longer and slow disease progression rather than to shrink tumors dramatically; doctors typically assess response after about 2–3 treatment cycles using scans and blood tests.

Clinical outcomes and comparisons: In its approved settings, Lonsurf has been shown to improve overall survival and disease control compared with best supportive care alone, but response rates are modest and it usually offers stabilization of disease rather than cure; compared with other late-line options like regorafenib, its survival benefit is similar, while side-effect profiles differ, so choice often depends on prior treatments, comorbidities, and tolerance.

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Dosage and Administration

Typical dosing and schedule: For adults, the recommended starting dose is 35 mg/m² of the trifluridine component, taken by mouth twice daily on days 1–5 and 8–12 of each 28-day cycle; dosing is based on body surface area and must be calculated and prescribed by the oncology team.

How to take: Swallow tablets whole with water, within 1 hour after the morning and evening meals, at approximately the same times each day; do not crush, chew, or split tablets.

Special dosing instructions: Doses may be reduced, delayed, or temporarily stopped based on blood counts, kidney function, or side effects such as severe diarrhea, nausea, or fatigue; treatment usually continues as long as it is working and side effects are manageable.

Missed dose guidance: If a dose is missed or vomited, do not take an extra dose to make it up; instead, skip that dose and take the next dose at the usual scheduled time, and inform the oncology team if multiple doses are missed.

Overdose: Taking more than the prescribed amount can cause severe bone marrow suppression and other serious side effects; in suspected overdose, contact emergency medical services or poison control immediately and bring the medication container for reference.

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Safety and Side Effects

Common side effects: The most frequent side effects include low white blood cells (neutropenia), low red blood cells (anemia), low platelets, tiredness, nausea, vomiting, diarrhea, decreased appetite, abdominal pain, and fever; blood count drops often occur within the first 2 cycles and can be moderate to severe, so regular lab monitoring is required.

Serious or rare adverse effects: Serious risks include severe neutropenia with infection or sepsis, febrile neutropenia, severe anemia or thrombocytopenia, profound fatigue, severe diarrhea or vomiting leading to dehydration, and acute kidney injury; fever, chills, shortness of breath, uncontrolled bleeding, or difficulty staying hydrated require urgent medical attention.

Warnings and precautions: Lonsurf can cause significant bone marrow suppression, so it may not be appropriate in patients with very low baseline blood counts; it should be used cautiously in people with moderate to severe kidney problems, with dose adjustments as directed, and those with prior heavy chemotherapy exposure.

Pregnancy, breastfeeding, and age considerations: Lonsurf can harm an unborn baby; effective contraception is recommended during treatment and for a period after the last dose (for both people who can become pregnant and those with partners who can become pregnant), and breastfeeding is not recommended during treatment and for a period after the final dose; its safety and effectiveness in children are not established.

Comparative safety: Compared with some other late-line colorectal cancer treatments, Lonsurf tends to cause more bone marrow suppression but less hand-foot skin reaction and less severe liver toxicity; overall tolerability varies by patient and often requires dose adjustments.

Side effect reporting and safety updates: Patients and caregivers can report suspected side effects to the FDA MedWatch program or through their healthcare team, who monitor for ongoing safety information and updated prescribing guidance.

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Interactions and Precautions

Drug interactions: Lonsurf is not heavily metabolized by common liver enzymes, so major interactions with many standard drugs are less frequent, but caution is needed with other medicines that suppress bone marrow (such as other chemotherapies or some immunosuppressants), which can increase the risk of low blood counts and infection.

Other medicines, supplements, and foods: Tell your care team about all prescription and over-the-counter medicines, vitamins, and herbal supplements; while specific food restrictions are not typical, Lonsurf should be taken with food for proper absorption, and alcohol should be limited or avoided if it worsens nausea, liver function, or overall tolerance.

Diagnostic and imaging procedures: There are no common direct interactions with imaging contrast agents or most diagnostic tests, but low blood counts from Lonsurf can affect when invasive procedures or surgeries are safely performed.

Precautions and conditions: Use with caution in patients with existing low blood counts, active infections, moderate to severe kidney impairment, or significant prior chemotherapy toxicity; frequent blood count monitoring and periodic checks of kidney and liver function are typically required, especially during the first few cycles.

Monitoring needs: Complete blood counts are usually obtained before starting each treatment cycle and at least on day 15 of the early cycles, with additional tests as needed; clinicians may adjust the dose or hold treatment based on these results and on symptoms such as fever, bleeding, or severe fatigue.

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Common Questions and Answers

Q: What is Lonsurf used for?
A: Lonsurf is an oral chemotherapy used in adults with metastatic colorectal cancer or metastatic gastric/ge junction adenocarcinoma that has progressed after, or is not suitable for, standard treatments.

Q: How long can I stay on Lonsurf?
A: Treatment usually continues in 28-day cycles as long as the cancer is controlled and side effects are manageable, with your doctor regularly checking scans, blood counts, and symptoms to decide whether to continue.

Q: Will my hair fall out on Lonsurf?
A: Hair loss can occur but is generally less common and less severe than with many IV chemotherapies; low blood counts, fatigue, and digestive symptoms are more typical side effects.

Q: Do I need special blood tests while taking Lonsurf?
A: Yes, your care team will check your blood counts and often your kidney and liver function regularly, especially during the first few cycles, to adjust the dose and reduce the risk of serious side effects.

Q: Can I take Lonsurf with my other medications?
A: Many medicines can be taken with Lonsurf, but because it can lower blood counts and has chemotherapy-type risks, you should review all prescription drugs, over-the-counter products, and supplements with your oncology team before and during treatment.

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Disposal Guidance

Storage: Store Lonsurf tablets at room temperature (usually 68°F to 77°F / 20°C to 25°C), in the original container, tightly closed, away from moisture and heat, and out of reach of children and pets.

Handling: Caregivers should avoid touching broken or crushed tablets with bare hands and wash hands after handling the medication.

Disposal: Do not throw unused tablets in household trash or flush them; instead, use a drug take-back program or follow pharmacist or local guidance for disposing of chemotherapy medicines.

Content last updated on December 11, 2025. Always consult a qualified health professional before making any treatment decisions or taking any medications. Review our Terms of Service for full details.