Lonsurf

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Lonsurf

Treatment option: Colorectal Cancer, Cancer

Medically reviewed

Marina Burgos

Last updated on 10/01/2026

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Lonsurf

Quick Facts

Property Description
Active Ingredients Trifluridine and Tipiracil
Form Film-coated tablets
Pharmacological Class Antineoplastic Agent, Antimetabolite, Thymidine Phosphorylase Inhibitor
Route of Administration Oral (Systemic)
Origin Synthetic

What Type of Medicine is Lonsurf?

Lonsurf, officially known by its International Nonproprietary Name (INN) Trifluridine/Tipiracil, is a synthetic chemotherapy agent designated for systemic treatment. It is classified as an antineoplastic agent, meaning its fundamental design is to inhibit the proliferation and growth of malignant cells. This classification as a fixed-dose combination of a nucleoside metabolic inhibitor and a thymidine phosphorylase inhibitor is recognized for providing control in advanced disease stages. The medication is used to slow or stop the growth of cancer cells by interfering with their DNA processes.

Composition: A Fixed-Dose Combination of Trifluridine and Tipiracil

The medicine's identity is rooted in its unique two-component structure, containing two distinct active ingredients: Trifluridine and Tipiracil hydrochloride. Trifluridine is the primary cytotoxic agent, a chemical analogue intended to be mistakenly incorporated into the cancer cell’s DNA, thereby disrupting its ability to divide. The co-dependent component, Tipiracil, functions as an enzyme inhibitor that prevents the body's natural enzymes from rapidly degrading the active Trifluridine component. The addition of Tipiracil increases the systemic exposure of Trifluridine, making the combination functionally unique among antimetabolite therapies. This protective mechanism is engineered to ensure a sustained therapeutic level, enhancing the overall anti-proliferative effect against the target cells. The drug is presented as film-coated tablets suitable for oral administration, and it contains these active components alongside necessary pharmaceutical excipients.

What side effects are possible with Lonsurf ?

Possible side effects and safety information

The safety profile of Lonsurf (trifluridine/tipiracil) is characterized by the potential for adverse effects that are documented in official regulatory labeling. These adverse reactions are classified by frequency and grouped by the body system affected, reflecting the medicine’s activity.

Officially Documented Adverse Reactions

The most frequently observed adverse reactions are primarily related to the blood and lymphatic system and gastrointestinal disorders. The following are documented in regulatory sources:

Frequency Classification Adverse Reactions (Examples)
Very Common (≥ 1 in 10 patients) Neutropenia, Anemia, Thrombocytopenia (low blood counts), Fatigue/Asthenia, Nausea, Decreased Appetite, Diarrhea.
Common (≥ 1 in 100 patients) Vomiting, Abdominal pain, Stomatitis, Pyrexia (fever), Infections, Pulmonary Emboli.
Uncommon (≥ 1 in 1,000 patients) Interstitial Lung Disease, Neutropenic Sepsis.

Serious Safety Considerations

The official labeling notes that the medicine carries a risk of Severe Myelosuppression (Grade 3-4), which may lead to fatal infections such as neutropenic sepsis and septic shock. The drug is documented to pose a risk of Embryo-Fetal Toxicity based on animal studies, necessitating specific contraception requirements for both male and female patients of reproductive potential.

Population-Specific Safety Notes

The regulatory documents specify that Older Adults (aged 65 and older) have demonstrated a higher incidence of Grade 3 or 4 hematological abnormalities compared to younger patients. Additionally, the initiation of Lonsurf is restricted in individuals with baseline moderate or severe hepatic impairment, and breastfeeding is advised against during treatment.

Overdose and Emergency Response

Overdose and When to Seek Help

The official regulatory profile for a Lonsurf overdose is defined by an exacerbation of the drug’s established severe toxicities, primarily severe or life-threatening myelosuppression. This toxicity involves critical reductions in blood cell counts, specifically documented as Grade 3 or 4 neutropenia and thrombocytopenia, along with anemia. These hematological effects increase the documented risk of serious secondary outcomes, such as febrile neutropenia, infection, and subsequent sepsis or septic shock.

Overdose Manifestations Emergency Response
Severe Myelosuppression (Neutropenia, Thrombocytopenia, Anemia) Contact a poison control center or emergency room at once
Risk of Sepsis and Febrile Neutropenia Call emergency services immediately if the person collapses or has trouble breathing

No specific antidote is known for Lonsurf overdose. Due to this constraint, the required medical management is restricted to symptomatic and supportive treatment. This includes frequent monitoring with complete blood counts and potentially administering supportive agents like G-CSF or antimicrobial agents to manage severe neutropenia and infection risk. A higher risk of severe toxicity is officially noted for patients 65 years of age or older and those with severe renal impairment.

Therapeutic Uses of Lonsurf

What Lonsurf Treats: Main Uses and Benefits

Lonsurf (trifluridine/tipiracil) is a medication relevant in the management of conditions presenting with systemic or localized discomfort. It is commonly used across conditions presenting with acute episodes when supportive relief is needed.

It is approved to treat adults with metastatic colorectal cancer (mCRC) and metastatic gastric cancer, including gastroesophageal junction adenocarcinoma (GEJ). It is often used during phases when symptoms become more noticeable, particularly in patients who have been previously treated with other lines of systemic management. The medicine is used in managing conditions associated with acute or disruptive episodes.

In clinical settings, its use provides supportive relief when symptoms interfere with routine activities. It generally contributes to easing the overall symptom burden, helping patients cope more steadily during difficult episodes.

Quick Fact: Supports Management of Symptoms Related to Noticeable Physiological Strain

Eligibility and Restrictions for Use

Lonsurf is indicated for use in adult patients (age 18 and older). Official regulatory documents specify strict criteria for who may and may not receive this medicine.

Contraindicated Populations

Lonsurf is contraindicated and must not be used in the following patient groups:

  • Patients with known hypersensitivity to the active substances (trifluridine, tipiracil) or any of the inactive ingredients.
  • Patients with baseline moderate or severe hepatic impairment (defined as total bilirubin > 1.5 imes the Upper Limit of Normal and any AST).

Use Restrictions and Special Considerations

Eligibility Factor Official Regulatory Rule
Age Safety and effectiveness in pediatric patients have not been established.
Organ Function Dose reduction is required for patients with severe renal impairment ( CrCl = 15 to 29 mL/min). Use is not recommended in end-stage renal disease ( CrCl < 15 mL/min).
Hematologic Status Treatment cannot be started or a new cycle initiated unless the patient's Absolute Neutrophil Count (ANC) is ge 1,500/ mm^3 and Platelets are ge 75,000/ mm^3.
Pregnancy/Lactation Use is prohibited in pregnant women (can cause fetal harm). Women must not breastfeed during treatment and for a period after the final dose.
Contraception Both female patients of reproductive potential (during treatment and for 6 months after the final dose) and male patients with female partners of reproductive potential (during treatment and for 3 months after the final dose) must use adequate contraception.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Interaction Scope

Category Official Regulatory Statement
Medicinal product categories with documented interactions Human Thymidine Kinase (TK) Substrate Antivirals
Specific interacting medicines (if explicitly listed) Bevacizumab (Co-administration is formally approved)
Mechanistic basis of interactions (only if stated in label) Competition for Human Thymidine Kinase activation with TK substrate antivirals
Timing-based interaction rules (if applicable) Lonsurf must be taken with food, specifically within one hour after completion of the morning and evening meals
Population-specific interaction notes (if applicable) Moderate Renal Impairment: Increased AUC of both trifluridine (43%) and tipiracil (65%) is documented
Interaction-related restrictions Use is not recommended in patients with severe renal impairment or severe hepatic impairment due to lack of study data

Interaction Classifications (High-level)

Category Official Regulatory Statement
Interaction severity classification (as defined in official documents) Contraindications: None
Regulatory basis (EMA / FDA / etc.) U.S. Food and Drug Administration Prescribing Information, European Medicines Agency SmPC
Interaction-context constraints (as defined in official documents) Risk of severe myelosuppression is documented when co-administered with Bevacizumab

Resulting Interaction Structure

The regulatory documents establish that the official interaction profile of Lonsurf is primarily defined by pharmacokinetic interactions that alter drug exposure, including a notable effect caused by food, and population-dependent changes related to renal function. These regulatory findings result in mandatory administration timing rules relative to meals and explicit restrictions against use in patients with unstudied severe organ impairment. The profile also formally acknowledges a specific co-administration protocol with Bevacizumab and notes a potential pharmacodynamic competition with certain antiviral agents.

Mechanism of Action

The mechanism involves the fixed combination of two active components, trifluridine (FTD) and tipiracil (TPI), which together disrupt the proliferation processes of rapidly dividing cells.

1. Direct Disruption of DNA Replication

This domain covers the primary cytotoxic action, where trifluridine (FTD), after internal activation, acts as a false nucleoside analogue. It is mistakenly incorporated directly into the rapidly synthesizing DNA strands of the cell, severely compromising the integrity of the genetic code. Additionally, an FTD metabolite inhibits Thymidylate Synthase (TS), cutting off the supply of essential building blocks needed to repair or replicate DNA. The cellular consequence of this combined action is the induction of cell cycle arrest and cytotoxicity (cell death) in the proliferating cell population.


2. Metabolic Shielding for Sustained Action

This vital mechanistic domain is the function of tipiracil (TPI), which acts as a specific inhibitor of the enzyme Thymidine Phosphorylase (TP). Since TP rapidly degrades the cytotoxic component FTD, TPI effectively creates a metabolic shield, preventing this immediate breakdown. By inhibiting TP, the mechanism ensures significantly prolonged and sustained systemic exposure of FTD, which is required to sustain the DNA disruption and cytotoxic cascade.

Dosage and Administration Information

The administration of Lonsurf (Trifluridine/Tipiracil) follows specific, standardized usage principles. The medicine is provided as film-coated tablets for oral administration. Dosing is determined by the patient's Body Surface Area (BSA), with a recommended starting dose of 35 mg/m^2 per dose, calculated based on the Trifluridine component. This calculated dose is rounded to the nearest 5 mg increment and must not exceed 80 mg per dose.

Lonsurf is administered twice daily (BID) following an intermittent 28-day cyclic schedule. Dosing occurs only on Days 1 through 5 and Days 8 through 12 of each cycle, followed by a scheduled rest period. A requirement for use is that the tablets must be swallowed whole and taken with food, specifically within one hour of both morning and evening meals. If a dose is missed or vomited, the dose should not be retaken; the patient proceeds with the next scheduled dose.

The initiation of any new 28-day cycle is conditional, requiring patients to meet predefined laboratory thresholds, such as specific Absolute Neutrophil Count and platelet levels, to proceed. For specific populations, such as patients with severe renal impairment (Creatinine Clearance 15 to 29 mL/min), the starting dose is 20 mg/m^2 twice daily. The overall treatment pattern is continued until disease progression or development of unacceptable toxicity, with a maximum of three dose reductions permitted according to documented adjustment logic.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Lonsurf (Trifluridine/Tipiracil)

According to the scientific and regulatory record, the research foundation for Lonsurf (trifluridine/tipiracil) comes from official clinical studies, primarily large-scale Randomized Controlled Trials (RCTs), which are a primary type of controlled clinical research. These studies were designed to explore patient outcomes in specific conditions compared to either a placebo or best supportive care alone. Evidence contributes to understanding patient outcomes related to systemic or functional imbalance in advanced disease.


Evidence for Use in Metastatic Colorectal Cancer (mCRC)

The research for metastatic colorectal cancer (mCRC) was evaluated in adult patients whose disease had progressed despite prior standard treatments, primarily through major Phase 3 trials. Researchers designed these trials to compare Lonsurf, used either alone (monotherapy) or in combination with bevacizumab, against a comparator group receiving placebo or best supportive care. The core outcomes that researchers monitored were Overall Survival (OS) and Progression-Free Survival (PFS). Findings from these RCTs describe patterns observed in the studies where the measured OS and PFS differed between the group receiving Lonsurf and the control group. The research also described patterns related to the Disease Control Rate (DCR), which includes the proportion of patients who experienced stable disease during the study period.


Evidence for Use in Metastatic Gastric and Gastroesophageal Junction (GEJ) Adenocarcinoma

The evidence for metastatic gastric cancer or GEJ adenocarcinoma was studied for adult patients whose disease progressed after receiving at least two other lines of chemotherapy. The core research was evaluated in a large, global Phase 3, placebo-controlled trial, where Lonsurf plus best supportive care was compared to a control group receiving placebo plus best supportive care. The core outcomes that the research examined were Overall Survival (OS) and Progression-Free Survival (PFS).


Research Gaps and Areas of Uncertainty

The current body of evidence highlights several areas where research is ongoing and more data would be valuable. The existing research mainly provided evidence derived from settings with varying symptom burdens but is constrained by the exclusion of patients with very poor functional health or advanced organ dysfunction, meaning results apply only to the populations studied in the highly controlled setting of the trials. Furthermore, long-term effects are not fully established, particularly concerning the durability of response years after treatment completion. Research on the full range of potential combination strategies for both indications is still uncertain, and data are still emerging in this area.

Frequently Asked Questions (FAQ)

Common questions about Lonsurf (FAQ)

Q: Does Lonsurf work by shrinking tumors or by stopping their growth?

The mechanism of action for Lonsurf is described as disrupting the DNA processes of cancer cells to inhibit their ability to grow and proliferate. This leads to cytotoxicity, or cell death. Clinical studies that support the medicine’s use examine patient outcomes related to Objective Response Rate and Disease Control Rate, which reflect how the cancer is affected.

Q: Can Lonsurf be used alone (monotherapy) or is it always used in combination?

According to official product information, Lonsurf can be used either as a single agent (monotherapy) for specific patients with metastatic gastric or gastroesophageal junction adenocarcinoma, or in combination with the medicine bevacizumab for specific patients with metastatic colorectal cancer. Its use is determined by the patient’s specific condition and prior treatments.

Q: Does Lonsurf typically cause hair loss?

Hair loss, or alopecia, has been reported as a side effect in clinical studies of Lonsurf. Official product information lists this as a common adverse reaction, meaning it occurs in up to 1 in 10 patients.

Q: Can Lonsurf be affected by over-the-counter medicines or supplements?

Regulatory documents explicitly focus on interactions with specific antiviral medicines, as well as the approved combination with bevacizumab. Official guidance indicates that patients should inform their healthcare team of all medicines, including over-the-counter products, supplements, or herbal teas they are taking.

Q: What birth control precautions are described for females taking Lonsurf?

Due to the potential for harm to a developing fetus, women of reproductive potential must use adequate contraception during treatment and for six months after the last dose. However, the core regulatory summary does not specify the particular type of contraception that is considered adequate.

Q: What happens if I need a surgery while on Lonsurf?

Patient resources generally highlight that patients should consult with their healthcare team before receiving any surgery or other medical procedures. This is to ensure the procedures can be timed appropriately around the medicine’s treatment cycles and to manage any potential risks.

Q: What common side effects can lead to a delay in the treatment cycle?

The initiation or continuation of a Lonsurf treatment cycle is conditional upon the patient’s body meeting specific laboratory thresholds for blood cell counts. Because the medicine can cause myelosuppression (low blood counts), side effects like low Absolute Neutrophil Count or low platelets can require a dose interruption or delay the start of the next cycle.

Q: Is Lonsurf described as being for patients who have already tried other treatments?

Yes, official indications state that Lonsurf is for adult patients whose disease has progressed despite prior standard treatments, which include previous rounds of chemotherapy and targeted agents. This means it is generally used after other treatment approaches have been tried.

Q: How does Lonsurf work differently from standard fluoropyrimidine-based treatments?

The active component, trifluridine, is a fluorinated thymidine analogue that directly disrupts DNA function. Official documents explicitly state that trifluridine is not a prodrug of 5-fluorouracil (5-FU), which is the component used in standard fluoropyrimidine chemotherapy. This gives it a distinct functional mechanism.

Q: Are there any dietary restrictions or foods to avoid while on Lonsurf?

Official instructions only mandate that the medicine be taken with food within one hour after completion of both the morning and evening meals. Some patient resources suggest avoiding foods that are overly spicy, salty, or acidic, as these may increase the chance of experiencing gastrointestinal side effects.

Q: What is the storage temperature required for Lonsurf tablets?

According to official regulatory sources, Lonsurf must be stored at controlled room temperature, specifically between 20 C and 25 C (68 F to 77 F). Maintaining the medicine within this temperature range is necessary for proper storage as defined by official labeling.

Q: Can Lonsurf be kept in a pill box or must it stay in its original container?

The tablets must be stored in the original container with the desiccant packet and the cap tightly closed to protect against moisture. Patient education materials recommend that if a pill box is used, it should be a separate, dedicated container and that special handling precautions should be followed when it is being filled.

Q: Does Lonsurf affect fertility?

Based on animal studies, the medicine is known to cause embryo-foetal toxicity, which is why mandatory contraception rules are in place for both men and women. The potential effect on adult human fertility is not fully established in regulatory documents.

Q: Are there different strengths of Lonsurf tablets?

Yes, Lonsurf is available in two different strengths, based on the dose of the trifluridine component: a 15 mg strength and a 20 mg strength. Both strengths contain a fixed ratio of the two active ingredients.

Q: Do patients always use Lonsurf for a full 28-day cycle?

Official documents state that treatment is continued for as long as a clinical benefit is observed or until unacceptable toxicity occurs. Dose interruptions or reductions may be required if specific toxicity thresholds are not met, meaning a full 28-day cycle is not always completed without adjustment.

Q: Can Lonsurf cause changes in liver function blood tests?

Abnormal results in liver function blood tests have been reported as a common side effect, especially when Lonsurf is used in combination with bevacizumab. Due to this risk, the drug is restricted in patients who have pre-existing moderate or severe hepatic impairment.

Q: Why is it important for a caregiver to wear gloves when handling Lonsurf?

Lonsurf is classified as a cytotoxic drug, which means it can be toxic to living cells and requires special handling and disposal procedures. Patient safety instructions often state that a caregiver should wear gloves when handling the tablets to minimize direct exposure.

Q: Is Lonsurf a common or standard first-line treatment for cancer?

The medicine is indicated for patients who have progressed despite prior standard treatments. This means it is typically used later in the course of therapy for patients with metastatic disease, rather than as a standard first-line treatment.

Q: Is it described as normal to feel dizzy after taking Lonsurf?

Dizziness is a symptom that is mentioned in patient safety information as something to monitor. Official information indicates that patients should not drive or operate machinery until they know how the medicine affects them, particularly if they feel dizzy or drowsy.

Q: Does Lonsurf cause a metallic taste in the mouth?

Changes in the sense of taste, known as dysgeusia, are reported as a common side effect in official patient information. This class of side effect includes symptoms like a metallic or altered taste in the mouth.

Q: Can Lonsurf cause a change in skin color or rash?

Skin problems, such as the appearance of a rash, itchy skin, or flaky skin, have been reported as side effects in patient-facing resources. These should be monitored and reported to the healthcare provider if they occur.

Q: Does Lonsurf interact with common pain relievers?

The official interaction profile focuses on specific antivirals and co-administration with bevacizumab. The label does not list common over-the-counter pain relievers as specific interacting medicines, but it is indicated that patients should discuss all products they take with their healthcare provider.

Q: Can Lonsurf affect a patient's ability to drive or operate machinery?

Official patient information states that patients should not drive or operate machinery until they know how the medicine affects them. This precaution is advised particularly if a patient experiences side effects like drowsiness or dizziness.

Q: Is the tablet size the same for all mg strengths?

No, the two available strengths of Lonsurf tablets, 15 mg and 20 mg, are visually distinct. Official documentation states they differ in both size (diameter) and color to help distinguish them.

Q: Can Lonsurf be taken at the same time as all other medications?

The primary administration rule is related to taking the medicine with food within one hour of meals. The regulatory label does not strictly mandate separating the dose from all other medications; only those with known interactions are highlighted for caution.

Q: How long does Lonsurf remain in the body's fluids after the last dose?

Regulatory review documents provide pharmacokinetic information on the two active components. The half-life of trifluridine is approximately 2.1 hours, and the half-life of tipiracil is approximately 2.4 hours.

Q: Are there any known issues with Lonsurf for patients who have lactose intolerance?

According to the Summary of Product Characteristics, Lonsurf tablets contain lactose monohydrate as an inactive ingredient, or excipient. Official information highlights that patients who have lactose intolerance should consult with their healthcare provider regarding this excipient.

How should Lonsurf be stored and disposed of?

How to Store and Dispose of LONSURF

LONSURF (trifluridine/tipiracil) tablets must be stored at controlled room temperature, specifically between 20 C and 25 C (68 F to 77 F). The medicine must be kept out of the sight and reach of children.


Storage Conditions

  • Original Container: Store the tablets only in the original container with the desiccant packet and keep the cap tightly closed to protect against moisture.
  • Stability: Any unused LONSURF tablets must be discarded 30 days after first opening the bottle.

Disposal Requirements

LONSURF is classified as a cytotoxic drug and requires special handling. Do not dispose of the tablets in household trash or pour them into wastewater. Unused or expired medication must be disposed of according to local regulatory requirements for pharmaceutical waste.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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