Trifluridine and Tipiracil

Trifluridine/tipiracil is a prescription medication used to treat advanced colorectal cancer. It is a single product containing trifluridine and tipiracil. 

Trifluridine belongs to a group of drugs called nucleoside metabolic inhibitor. Tipiracil belongs to a group of drugs called thymidine phosphorylase inhibitor. Together these work to stop the growth and spread of cancer cells.

It is available in tablet form and is typically taken twice a day, within 1 hour of morning and evening meals.  

Common side effects of this medication may include decrease in blood cell counts, fatigue, and nausea.

Trifluridine/tipiracil is a prescription medication used to treat patients with an advanced form of colorectal cancer who are no longer responding to other therapies. These therapies include fluoropyrimidine, oxaliplatin and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and if RAS wild-type, an anti-EGFR therapy. 

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Trifluridine and Tipiracil may be found in some form under the following brand names:

• Lonsurf

Serious side effects have been reported with trifluridine/tipiracil. See the “Trifluridine/tipiracil Precautions” section.

Common side effects include the following:

• anemia (low red blood cell counts)
• neutropenia (low neutrophils)
• fatigue
• nausea
• thrombocytopenia (low platelets)
• decreased appetite
• diarrhea
• vomiting
• abdominal pain
• fever

This is not a complete list of trifluridine/tipiracil side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

No drug interactions have been conducted by the manufacturer. However, you should tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements. Not all drug interactions are known or reported and new drug interactions are continually being reported.

Serious side effects have been reported with trifluridine/tipiracil including the following:

• Bone marrow Suppression (Severe Myelosuppression): Contact your doctor right away if you notice signs or symptoms of infection. Your doctor will monitor your blood counts prior to and on Day 15 of each cycle. Keep all appointments for blood tests. If needed, your doctor may reduce dose and/or hold trifluridine/tipiracil. 
• Gastrointestinal toxicity:  Contact your doctor right away if you experience severe or persistent nausea, vomiting, diarrhea, or abdominal pain.
• Low blood counts. Patients 65 years and older are at a higher risk of having low blood counts after taking trifluridine/tipiracil. 
• Embryo-Fetal Toxicity: Trifluridine/tipiracil can cause fetal harm when administered to a pregnant woman. Females of reproductive potential are recommended to use effective contraception during treatment with trifluridine/tipiracil. 

Medications can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of trifluridine/tipiracil, there are no specific foods that you must exclude from your diet when receiving this medication.

Before taking trifluridine/tipiracil, tell your doctor about all of your medical conditions. Especially tell your doctor if you:

• are allergic to trifluridine, tipiracil or to any of its ingredients
• have liver problems
• have kidney problems
• have or ever had anemia (low red blood cells, neutropenia (low neutrophils) and thrombocytopenia (low platelets) 
• are pregnant or plan to become pregnant
• are breastfeeding or plan to breastfeed

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

Tell your doctor if you are pregnant or plan to become pregnant.

Trifluridine/tipiracil can cause fetal harm when administered to a pregnant woman. Females of reproductive potential are recommended to use effective contraception during treatment with trifluridine/tipiracil. 

Males with female partners of reproductive potential should use condoms during treatment with Lonsurf and for at least 3 months after the final dose.

Tell your doctor if you are breastfeeding or plan to breastfeed.

It is not known whether trifluridine/tipiracil or its metabolites are present in human milk. There are no data to assess the effects of Lonsurf or its metabolites on the breastfed infant or the effects on milk production. Because of the potential for serious adverse reactions in breastfeeding infants, women should not breastfeed during treatment with trifluridine/tipiracil and for one day following the final dose.

Take trifluridine/tipiracil exactly as prescribed.

It is available in tablet form and is typically taken twice a day, within 1 hour of morning and evening meals.  

Anyone else who handles this medication should wear gloves.

If you miss a dose, take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and take your next dose at the regular time. Do not take two doses of trifluridine/tipiracil at the same time.

Take this medication exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

The dose your doctor recommends may be based on the following:

• the condition being treated
• other medical conditions you have
• other medications you are taking
• how you respond to this medication
• your kidney function
• your age

The recommended dose/dose range of Lonsurf (trifluridine and tipiracil) for the treatment of  is 35 mg/m2/dose orally twice daily on Days 1 through 5 and Days 8 through 12 of each 28-day cycle. 

If you take too much trifluridine/tipiracil, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

• Store at 20°C to 25°C (68°F to 77°F).
• Trifluridine/tipiracil is a cytotoxic drug. Follow applicable special handling and disposal procedures.
• Keep this and all medicines out of the reach of children.
• If stored outside of original bottle, discard, following disposal procedures, after 30 days.