Trifluridine 1% eye drops preservative free
Prescription only
Requires a prescription from a doctor or prescriber
Trifluridine is a fluorinated pyrimidine nucleoside that is structurally related to [idoxuridine] [A35271].
Active ingredients:
Trifluridine
Formulation:No preservatives — preferred for sensitive patients
Preservative-free
1 safety notice
Safety information for pregnancy and breastfeeding
Pregnancy
Based on the findings from animal studies, trifluridine may cause fetal toxicity when administered to pregnant patients F649.
Always consult your doctor or midwife before taking any medicine during pregnancy or while breastfeeding. Source: DrugBank (CC BY-NC 4.0).
Official documents, adverse reaction reporting, and safety monitoring
Report a side effect
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Official medicine documents
Source: MHRA Products DatabaseOGL 3.0
Updated 3 months ago(16 Jan 2026)Safety monitoring data
Yellow Card reports
MHRA
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
View Drug Analysis Profile
Suspected adverse reactions reported for Trifluridine
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Submit a Yellow Card report to the MHRA
Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
EMA
The European Medicines Agency (EMA) collects suspected adverse reaction reports from across the EU/EEA through the EudraVigilance system. Search for safety data on this medicine.
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Suspected adverse reactions reported for Trifluridine
About EudraVigilance
Learn about EU pharmacovigilance and safety monitoring
EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.
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Same BNF section
Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
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Clinical guidelines and formulary information
British National Formulary
Trifluridine
BNF
Drug monograph — bnf.nice.org.ukSource: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
NICE clinical guidance(9)
Trifluridine–tipiracil for previously treated metastatic colorectal cancer (TA405)
TA405
Technology appraisal
Updated Aug 2016Trifluridine–tipiracil for treating metastatic gastric cancer or gastro-oesophageal junction adenocarcinoma after 2 or more treatments (TA852)
TA852
Technology appraisal
Updated Dec 2022Fruquintinib for previously treated metastatic colorectal cancer (TA1079)
TA1079
Technology appraisal
Updated Jul 2025Trifluridine–tipiracil with bevacizumab for treating metastatic colorectal cancer after 2 systemic treatments (TA1008)
TA1008
Technology appraisal
Updated Sept 2024Regorafenib for previously treated metastatic colorectal cancer (TA866)
TA866
Technology appraisal
Updated Feb 2023Encorafenib plus cetuximab for previously treated BRAF V600E mutation-positive metastatic colorectal cancer (TA668)
TA668
Technology appraisal
Updated Jan 2021Nivolumab with ipilimumab for previously treated metastatic colorectal cancer with high microsatellite instability or mismatch repair deficiency (TA716)
TA716
Technology appraisal
Updated Jul 2021Bevacizumab (originator and biosimilars) with fluoropyrimidine-based chemotherapy for metastatic colorectal cancer (TA1136)
TA1136
Technology appraisal
Updated Feb 2026Colorectal cancer (NG151)
NG151
NICE guideline
Updated Dec 2021Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
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Supply & product information
Official product databases and supply status monitoring
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Codes for healthcare professionals and prescribing systems
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NHS UK identifiers
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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
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Searching UK clinical trials...
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
1.4 hours
Mechanism
The mechanism of action of trifluridine as an antiviral agent has not been fully…
Food interactions
1 warning
Human targets
2 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
57%
After oral administration of LONSURF with [14C]-trifluridine, at least 57% of the administered trifluridine was absorbed.…
Half-life
35 mg/m
After administration of LONSURF 35 mg/m2, the mean elimination and steady-state half-life (t1/2) of trifluridine was 1.4…
Protein binding
96%
In vitro findings suggest that the protein binding of trifluridine in human plasma is greater than 96%, where it is mainly bound to human serum albumin.…
Volume of distribution
35 mg/m
Following a single dose of LONSURF (35 mg/m2) in patients with advanced solid tumours, the apparent volume of distribution (Vd/F) for trifluridine was 21 L.
[L47681]…
[L47681]…
Metabolism
Trifluridine is not metabolized by cytochrome P450 (CYP) enzymes.…
Elimination
60 mg
After single oral administration of LONSURF (60 mg) with [14C]-trifluridine, the total cumulative excretion of radioactivity was 60% of the administered dose.…
Clearance
35 mg/m
Following a single dose of LONSURF (35 mg/m2) in patients with advanced solid tumours, the oral clearance (CL/F) for trifluridine was 10.5…
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Small molecule
About this compound
Trifluridine is a fluorinated pyrimidine nucleoside that is structurally related to [idoxuridine] [A35271]. It is an active antiviral agent in ophthalmic solutions used mainly in the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus. It displays effective antiviral activity against Herpes simplex virus type 1 and 2 [A35271].
The combination product of trifluridine with tipiracil marketed as Lonsurf has been approved in Japan, the United States, and the European Union for the treatment of adult patients with metastatic colorectal cancer who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and if RAS wild-type, an anti-EGFR therapy. In the anticancer therapy, trifluridine acts as a thymidine-based nucleoside metabolic inhibitor that gets incorporated into DNA of cancer cells following cell uptake to aberrate DNA function during cell replication F649.
The combination product of trifluridine with tipiracil marketed as Lonsurf has been approved in Japan, the United States, and the European Union for the treatment of adult patients with metastatic colorectal cancer who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and if RAS wild-type, an anti-EGFR therapy. In the anticancer therapy, trifluridine acts as a thymidine-based nucleoside metabolic inhibitor that gets incorporated into DNA of cancer cells following cell uptake to aberrate DNA function during cell replication F649.
Properties:
View FDA drug labelsolid
Avg. mass: 296.20 Da
DrugBank indication
As a standalone product, trifluridine is used for the ophthalmic treatment of primay keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus, types 1 and 2.
[L47671]
Trifluridine is also available as a combination product with [tipiracil], which is indicated either alone or in combination with [bevacizumab] for the treatment of adult patients with metastatic colorectal cancer who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and if RAS wild-type, an anti-EGFR therapy.
[L47676]
This combination product is also used for adult patients with metastatic gastric or gastroesophageal junction adenocarcinoma and were previously treated with at least two prior lines of chemotherapy that included a fluoropyrimidine, a platinum, either a taxane or irinotecan, and if appropriate, HER2/neu-targeted therapy.
[L47676]
[L47671]
Trifluridine is also available as a combination product with [tipiracil], which is indicated either alone or in combination with [bevacizumab] for the treatment of adult patients with metastatic colorectal cancer who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and if RAS wild-type, an anti-EGFR therapy.
[L47676]
This combination product is also used for adult patients with metastatic gastric or gastroesophageal junction adenocarcinoma and were previously treated with at least two prior lines of chemotherapy that included a fluoropyrimidine, a platinum, either a taxane or irinotecan, and if appropriate, HER2/neu-targeted therapy.
[L47676]
Also known as(59)
5-(Trifluoromethyl)deoxyuridine
5-Trifluoromethyl-2-deoxyuridine
F₃T
TFT
Trifluoromethyldeoxyuridine
Trifluorothymidine
Trifluorothymine deoxyriboside
Trifluridin
Dosage forms(9)
Tablet (Oral)
Tablet, film coated (Oral)
Solution (Ophthalmic) — 10 mg/1mL
Solution / drops (Ophthalmic) — 10 mg/1mL
Ointment (Topical) — 10 mg
Solution / drops (Ophthalmic)
Solution (Conjunctival; Ophthalmic) — 10 mg
Solution (Ophthalmic) — 1 %
Molecular properties(19)
Drug interactions(1178)
Known interactions with other medications. Always consult a healthcare professional.
The risk or severity of adverse effects can be increased when Denosumab is combined with Trifluridine.
Etanercept
Unknown severity
The risk or severity of adverse effects can be increased when Etanercept is combined with Trifluridine.
Peginterferon alfa-2a
Unknown severity
The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Trifluridine.
Interferon alfa-n1
Unknown severity
The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Trifluridine.
Interferon alfa-n3
Unknown severity
The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Trifluridine.
Peginterferon alfa-2b
Unknown severity
The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Trifluridine.
The risk or severity of adverse effects can be increased when Anakinra is combined with Trifluridine.
Interferon gamma-1b
Unknown severity
The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Trifluridine.
Interferon alfa-2a
Unknown severity
The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Trifluridine.
Aldesleukin
Unknown severity
The risk or severity of adverse effects can be increased when Aldesleukin is combined with Trifluridine.
Adalimumab
Unknown severity
The risk or severity of adverse effects can be increased when Adalimumab is combined with Trifluridine.
Gemtuzumab ozogamicin
Unknown severity
The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Trifluridine.
Pegaspargase
Unknown severity
The risk or severity of adverse effects can be increased when Pegaspargase is combined with Trifluridine.
Infliximab
Unknown severity
The risk or severity of adverse effects can be increased when Infliximab is combined with Trifluridine.
Interferon beta-1b
Unknown severity
The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Trifluridine.
Interferon alfacon-1
Unknown severity
The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Trifluridine.
The risk or severity of adverse effects can be increased when Rituximab is combined with Trifluridine.
Basiliximab
Unknown severity
The risk or severity of adverse effects can be increased when Basiliximab is combined with Trifluridine.
The risk or severity of adverse effects can be increased when Muromonab is combined with Trifluridine.
Ibritumomab tiuxetan
Unknown severity
The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Trifluridine.
Tositumomab
Unknown severity
The risk or severity of adverse effects can be increased when Tositumomab is combined with Trifluridine.
Alemtuzumab
Unknown severity
The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Trifluridine.
The risk or severity of adverse effects can be increased when Alefacept is combined with Trifluridine.
Efalizumab
Unknown severity
The risk or severity of adverse effects can be increased when Efalizumab is combined with Trifluridine.
Antithymocyte immunoglobulin (rabbit)
Unknown severity
The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Trifluridine.
Interferon alfa-2b
Unknown severity
The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Trifluridine.
Daclizumab
Unknown severity
The risk or severity of adverse effects can be increased when Daclizumab is combined with Trifluridine.
Phenylalanine
Unknown severity
The risk or severity of adverse effects can be increased when Phenylalanine is combined with Trifluridine.
Flunisolide
Unknown severity
The risk or severity of adverse effects can be increased when Flunisolide is combined with Trifluridine.
Bortezomib
Unknown severity
The risk or severity of adverse effects can be increased when Bortezomib is combined with Trifluridine.
Cladribine
Moderate
Trifluridine may increase the immunosuppressive activities of Cladribine.
Carmustine
Unknown severity
The risk or severity of adverse effects can be increased when Carmustine is combined with Trifluridine.
The risk or severity of adverse effects can be increased when Amsacrine is combined with Trifluridine.
The risk or severity of adverse effects can be increased when Bleomycin is combined with Trifluridine.
Chlorambucil
Unknown severity
The risk or severity of adverse effects can be increased when Chlorambucil is combined with Trifluridine.
Raltitrexed
Unknown severity
The risk or severity of adverse effects can be increased when Raltitrexed is combined with Trifluridine.
The risk or severity of adverse effects can be increased when Mitomycin is combined with Trifluridine.
Bexarotene
Unknown severity
The risk or severity of adverse effects can be increased when Bexarotene is combined with Trifluridine.
The risk or severity of adverse effects can be increased when Vindesine is combined with Trifluridine.
Floxuridine
Unknown severity
The risk or severity of adverse effects can be increased when Floxuridine is combined with Trifluridine.
Indomethacin
Unknown severity
The risk or severity of adverse effects can be increased when Indomethacin is combined with Trifluridine.
Tioguanine
Unknown severity
The risk or severity of adverse effects can be increased when Tioguanine is combined with Trifluridine.
Vinorelbine
Unknown severity
The risk or severity of adverse effects can be increased when Vinorelbine is combined with Trifluridine.
Dexrazoxane
Unknown severity
The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Trifluridine.
Beclomethasone dipropionate
Unknown severity
The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Trifluridine.
The risk or severity of adverse effects can be increased when Sorafenib is combined with Trifluridine.
Streptozocin
Unknown severity
The risk or severity of adverse effects can be increased when Streptozocin is combined with Trifluridine.
Gemcitabine
Unknown severity
The risk or severity of adverse effects can be increased when Trifluridine is combined with Gemcitabine.
Betamethasone
Unknown severity
The risk or severity of adverse effects can be increased when Trifluridine is combined with Betamethasone.
Teniposide
Unknown severity
The risk or severity of adverse effects can be increased when Trifluridine is combined with Teniposide.
Showing 50 of 1178 interactions
Food & lifestyle interactions
Take With Food
Take with food.
Toxicity & overdose
Intravenous LD50 in rat was 2946 mg/kg MSDS. Oral LD50 in rat and mouse were > 4379mg/kg MSDS. Overdosage via ocular instillation is unlikely.
The highest dose of orally-administered Lonsurf, trifluridine in combination with tipiracil, administered in clinical studies was 180 mg/m^2 per day. The primary anticipated complication of an overdose is bone marrow suppression. There is no known antidote for trifluridine overdose: in case of an overdose, management should include customary therapeutic and supportive medical intervention aimed at correcting the presenting clinical manifestations and preventing their possible complications F649.
Based on the findings from animal studies, trifluridine may cause fetal toxicity when administered to pregnant patients F649.
The highest dose of orally-administered Lonsurf, trifluridine in combination with tipiracil, administered in clinical studies was 180 mg/m^2 per day. The primary anticipated complication of an overdose is bone marrow suppression. There is no known antidote for trifluridine overdose: in case of an overdose, management should include customary therapeutic and supportive medical intervention aimed at correcting the presenting clinical manifestations and preventing their possible complications F649.
Based on the findings from animal studies, trifluridine may cause fetal toxicity when administered to pregnant patients F649.
How it works
Mechanism of action
The mechanism of action of trifluridine as an antiviral agent has not been fully elucidated, but appears to involve the inhibition of viral replication. Trifluridine gets incorporated into viral DNA during replication, which leads to the formation of defective proteins and an increased mutation rate. Trifluridine also mediates antineoplastic activities via this mechanism; following uptake into cancer cells, trifluridine is rapidly phosphorylated by thymidine kinase to its active monophosphate form [A35272]. Subsequent phosphorylation produces trifluridine triphosphate [A35272], which is readily incorporated into the DNA of tumour cells in place of thymidine bases to perturb DNA function, DNA synthesis, and tumour cell proliferation [FDA Label]. As trifluridine is subject to rapid degradation by TPase and readily metabolised by a first-pass effect following oral administration, tipiracil is added in the antineoplastic combination product as an inhibitor of TPase to increase the bioavailability of trifluridine F649. Trifluridine monophosphate also reversibly inhibits thymidylate synthetase (TS), an enzyme that is necessary for DNA synthesis and which levels are shown to be elevated different cancer cell lines [A35289]. Up-regulation of the expression of the TS enzyme may also lead to the resistance to antineoplastic therapies, such as 5-fluorouracil (5-FU). [A35289 However, this inhibitory effect is not considered to be sufficient enough to fully contribute to the cytotoxicity in cancer cells. [A35272]
Pharmacodynamics
Trifluridine exhibits an antiviral effect against herpes simplex virus, types 1 and 2 and vacciniavirus both in vitro and in vivo [A35271]. Some strains of adenovirus that contribute to the pathology of keratoconjunctivitis were shown to be susceptible to trifluridine in vitro [A35271]. While there is evidence from a study that cross-resistance may develop between trifluridine and [idoxuridine] or [vidarabine], trifluridine was shown to effective in treating dendritic ulcers in patients with herpetic keratitis who are unresponsive to [idoxuridine] or [vidarabine] based on the results from masked comparative trials [A35271]. In nonclinical studies, trifluridine/tipiracil hydrochloride demonstrated antitumour activity against both 5-fluorouracil (5-FU) sensitive and resistant colorectal cancer cell lines F649. The cytotoxic activity of trifluridine and tipiracil against several human tumour xenografts show high correlation with the amount of trifluridine incorporated into DNA, indicating that the primary mechanism of action of trifluridine involves the direct incorporation into the cancer cell DNA F649. Trifluridine and tipiracil demonstrated anti-tumor activity against KRAS wild-type and mutant human colorectal cancer xenografts in mice [FDA Label].
In clinical studies comprised of patients with previously treated metastatic colorectal cancer, treatment of trifluridine in combination with tipiracil in addition to best supportive care over a 5- or 7-month period resulted in increased progression-free survival (PFS), overall response rate (ORR) and disease control rate (DCR) compared to placebo F649. In an open-label study, administration of trifluridine at the recommended dosage in patients with advanced solid tumors had no clinically relevant effect on QT/QTc prolongation compared with placebo [FDA Label]. Two out of 48 patients displayed had QTc greater than 500 msec and 1 of 42 patients (2.4%) had a QTc increase from baseline greater than 60 msec [FDA Label].
In clinical studies comprised of patients with previously treated metastatic colorectal cancer, treatment of trifluridine in combination with tipiracil in addition to best supportive care over a 5- or 7-month period resulted in increased progression-free survival (PFS), overall response rate (ORR) and disease control rate (DCR) compared to placebo F649. In an open-label study, administration of trifluridine at the recommended dosage in patients with advanced solid tumors had no clinically relevant effect on QT/QTc prolongation compared with placebo [FDA Label]. Two out of 48 patients displayed had QTc greater than 500 msec and 1 of 42 patients (2.4%) had a QTc increase from baseline greater than 60 msec [FDA Label].
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
After oral administration of LONSURF with [14C]-trifluridine, at least 57% of the administered trifluridine was absorbed. Following a single dose of LONSURF (35 mg/m2) in patients with advanced solid tumors, the mean times to peak plasma concentrations (Tmax) of trifluridine was around 2 hours.
[L47681]
Trifluridine area under the concentration-time curve from time 0 to the last measurable concentration (AUC0-last) was approximately 3-fold higher and maximum concentration (Cmax) was approximately 2-fold higher after multiple dose administration (twice daily for 5 days a week with 2 days rest for 2 weeks followed by a 14-day rest, repeated every 4 weeks) than after single-dose administration.
[L47681]
Following a single oral administration of LONSURF at 35 mg/m2 in patients with cancer, the mean time to peak plasma concentration (Tmax) of trifluridine was around 2 hours.
[L47676]
For the ophthalmic formulation, systemic absorption appears to be negligible.
[L47671]
A standardized high-fat, high-calorie meal decreased trifluridine Cmax by approximately 40% but did not change trifluridine AUC compared to those in a fasting state in patients with cancer following administration of a single dose of LONSURF 35 mg/m2.
[L47671]
In a dose finding study (15 to 35 mg/m2 twice daily), the AUC from time 0 to 10 hours (AUC0-10) of trifluridine tended to increase more than expected based on the increase in dose.
[L47681]
[L47681]
Trifluridine area under the concentration-time curve from time 0 to the last measurable concentration (AUC0-last) was approximately 3-fold higher and maximum concentration (Cmax) was approximately 2-fold higher after multiple dose administration (twice daily for 5 days a week with 2 days rest for 2 weeks followed by a 14-day rest, repeated every 4 weeks) than after single-dose administration.
[L47681]
Following a single oral administration of LONSURF at 35 mg/m2 in patients with cancer, the mean time to peak plasma concentration (Tmax) of trifluridine was around 2 hours.
[L47676]
For the ophthalmic formulation, systemic absorption appears to be negligible.
[L47671]
A standardized high-fat, high-calorie meal decreased trifluridine Cmax by approximately 40% but did not change trifluridine AUC compared to those in a fasting state in patients with cancer following administration of a single dose of LONSURF 35 mg/m2.
[L47671]
In a dose finding study (15 to 35 mg/m2 twice daily), the AUC from time 0 to 10 hours (AUC0-10) of trifluridine tended to increase more than expected based on the increase in dose.
[L47681]
Half-life
After administration of LONSURF 35 mg/m2, the mean elimination and steady-state half-life (t1/2) of trifluridine was 1.4 hours and 2.1 hours respectively.
[L47676]
For the ophthalmic formulation, the half-life is significantly shorter, approximately only 12 minutes.
[L47671]
[L47676]
For the ophthalmic formulation, the half-life is significantly shorter, approximately only 12 minutes.
[L47671]
Protein binding
In vitro findings suggest that the protein binding of trifluridine in human plasma is greater than 96%, where it is mainly bound to human serum albumin. Protein binding of trifluridine is independent of drug concentration and presence of tipiracil.
[L47676]
[L47676]
Volume of distribution
Following a single dose of LONSURF (35 mg/m2) in patients with advanced solid tumours, the apparent volume of distribution (Vd/F) for trifluridine was 21 L.
[L47681]
[L47681]
Metabolism
Trifluridine is not metabolized by cytochrome P450 (CYP) enzymes. Trifluridine is mainly eliminated by metabolism via thymidine phosphorylase to form an inactive metabolite, 5-(trifluoromethyl) uracil (FTY). No other major metabolites were detected in plasma or urine.
[L47676]
Other minor metabolites, such as 5-carboxy-2'-deoxyuridine found on the endothelial side of the cornea or 5-carboxyuraci, were also detected, but only at low or trace level in plasma and urine.
[A35307][L47681]
[L47676]
Other minor metabolites, such as 5-carboxy-2'-deoxyuridine found on the endothelial side of the cornea or 5-carboxyuraci, were also detected, but only at low or trace level in plasma and urine.
[A35307][L47681]
Route of elimination
After single oral administration of LONSURF (60 mg) with [14C]-trifluridine, the total cumulative excretion of radioactivity was 60% of the administered dose. The majority of
recovered radioactivity was eliminated into urine (55% of the dose) as FTY and trifluridine glucuronide isomers within 24 hours and the excretion into feces and expired air was <3% for
both. The unchanged trifluridine was <3% of administered dose recovered in the urine and feces.
[L47676]
recovered radioactivity was eliminated into urine (55% of the dose) as FTY and trifluridine glucuronide isomers within 24 hours and the excretion into feces and expired air was <3% for
both. The unchanged trifluridine was <3% of administered dose recovered in the urine and feces.
[L47676]
Clearance
Following a single dose of LONSURF (35 mg/m2) in patients with advanced solid tumours, the oral clearance (CL/F) for trifluridine was 10.5 L/hr.
[L47681]
[L47681]
Drug targets(2)
Proteins and enzymes this drug interacts with in the body
DNA
other/unknown
Thymidylate synthase
TYMS
inhibitor
Specific functionfolic acid binding
Cellular location
Nucleus
General function & pharmacology
Catalyzes the reductive methylation of 2'-deoxyuridine 5'-monophosphate (dUMP) to thymidine 5'-monophosphate (dTMP), using the cosubstrate, 5,10- methylenetetrahydrofolate (CH2H4folate) as a 1-carbon donor and reductant and contributes to the de novo mitochondrial thymidylate biosynthesis pathway
Metabolizing enzymes(2)
Enzymes involved in drug metabolism — important for understanding drug interactions
Enzyme activity key
substrate
inhibitor
inducer
TK1Thymidine kinase, cytosolic
substrate
TYMPThymidine phosphorylase
substrate
Transporters(4)
Proteins that transport this drug across cell membranes
Solute carrier family 22 member 6
SLC22A6
substrate
inhibitor
Specific functionalpha-ketoglutarate transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Secondary active transporter that functions as a Na(+)-independent organic anion (OA)/dicarboxylate antiporter where the uptake of one molecule of OA into the cell is coupled with an efflux of one molecule of intracellular dicarboxylate such as 2-oxoglutarate or glutarate .
PMID:11669456 PMID:11907186 PMID:14675047 PMID:22108572 PMID:23832370 PMID:28534121 PMID:9950961
Mediates the uptake of OA across the basolateral side of proximal tubule epithelial cells, thereby contributing to the renal elimination of endogenous OA from the systemic circulation into the urine .
PMID:9887087
Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins .
PMID:28534121
Transports prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) and may contribute to their renal excretion .
PMID:11907186
Also mediates the uptake of cyclic nucleotides such as cAMP and cGMP .
PMID:26377792
Involved in the transport of neuroactive tryptophan metabolites kynurenate (KYNA) and xanthurenate (XA) and may contribute to their secretion from the brain .
PMID:22108572 PMID:23832370
May transport glutamate .
PMID:26377792
Also involved in the disposition of uremic toxins and potentially toxic xenobiotics by the renal organic anion secretory pathway, helping reduce their undesired toxicological effects on the body .
PMID:11669456 PMID:14675047
Uremic toxins include the indoxyl sulfate (IS), hippurate/N-benzoylglycine (HA), indole acetate (IA), 3-carboxy-4- methyl-5-propyl-2-furanpropionate (CMPF) and urate .
PMID:14675047 PMID:26377792
Xenobiotics include the mycotoxin ochratoxin (OTA) .
PMID:11669456
May also contribute to the transport of organic compounds in testes across the blood-testis-barrier PMID:35307651
PMID:11669456 PMID:11907186 PMID:14675047 PMID:22108572 PMID:23832370 PMID:28534121 PMID:9950961
Mediates the uptake of OA across the basolateral side of proximal tubule epithelial cells, thereby contributing to the renal elimination of endogenous OA from the systemic circulation into the urine .
PMID:9887087
Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins .
PMID:28534121
Transports prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) and may contribute to their renal excretion .
PMID:11907186
Also mediates the uptake of cyclic nucleotides such as cAMP and cGMP .
PMID:26377792
Involved in the transport of neuroactive tryptophan metabolites kynurenate (KYNA) and xanthurenate (XA) and may contribute to their secretion from the brain .
PMID:22108572 PMID:23832370
May transport glutamate .
PMID:26377792
Also involved in the disposition of uremic toxins and potentially toxic xenobiotics by the renal organic anion secretory pathway, helping reduce their undesired toxicological effects on the body .
PMID:11669456 PMID:14675047
Uremic toxins include the indoxyl sulfate (IS), hippurate/N-benzoylglycine (HA), indole acetate (IA), 3-carboxy-4- methyl-5-propyl-2-furanpropionate (CMPF) and urate .
PMID:14675047 PMID:26377792
Xenobiotics include the mycotoxin ochratoxin (OTA) .
PMID:11669456
May also contribute to the transport of organic compounds in testes across the blood-testis-barrier PMID:35307651
Sodium/nucleoside cotransporter 1
SLC28A1
substrate
Specific functionazole transmembrane transporter activity
Cellular location
Cell membrane
General function & pharmacology
Sodium and pyrimidine nucleoside symporter of the plasma membrane that imports uridine, thymidine and cytidine into cells by coupling their transport to the transmembrane sodium electrochemical gradient. Also transports adenosine, an atypical substrate transported with high apparent affinity, but low maximum velocity. Therefore, exhibits the transport characteristics of the nucleoside transport system cit or N2 subtype (N2/cit) .
PMID:10455109 PMID:14701834 PMID:15194733 PMID:21795683 PMID:21998139 PMID:30658162 PMID:32126230 PMID:9124315
Involved in renal nucleoside (re)absorption PMID:30658162
PMID:10455109 PMID:14701834 PMID:15194733 PMID:21795683 PMID:21998139 PMID:30658162 PMID:32126230 PMID:9124315
Involved in renal nucleoside (re)absorption PMID:30658162
Equilibrative nucleoside transporter 1
SLC29A1
substrate
Specific functionadenine transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Uniporter involved in the facilitative transport of nucleosides and nucleobases, and contributes to maintaining their cellular homeostasis .
PMID:10722669 PMID:10755314 PMID:12527552 PMID:14759222 PMID:15037197 PMID:17379602 PMID:21795683 PMID:26406980 PMID:27995448 PMID:35790189 PMID:8986748
Functions as a Na(+)-independent transporter .
PMID:8986748
Involved in the transport of nucleosides such as adenosine, guanosine, inosine, uridine, thymidine and cytidine .
PMID:10722669 PMID:10755314 PMID:12527552 PMID:14759222 PMID:15037197 PMID:17379602 PMID:26406980 PMID:8986748
Also transports purine nucleobases (hypoxanthine, adenine, guanine) and pyrimidine nucleobases (thymine, uracil) .
PMID:21795683 PMID:27995448
Mediates basolateral nucleoside uptake into Sertoli cells, thereby regulating the transport of nucleosides in testis across the blood-testis barrier (By similarity). Regulates inosine levels in brown adipocytes tissues (BAT) and extracellular inosine levels, which controls BAT-dependent energy expenditure PMID:35790189
PMID:10722669 PMID:10755314 PMID:12527552 PMID:14759222 PMID:15037197 PMID:17379602 PMID:21795683 PMID:26406980 PMID:27995448 PMID:35790189 PMID:8986748
Functions as a Na(+)-independent transporter .
PMID:8986748
Involved in the transport of nucleosides such as adenosine, guanosine, inosine, uridine, thymidine and cytidine .
PMID:10722669 PMID:10755314 PMID:12527552 PMID:14759222 PMID:15037197 PMID:17379602 PMID:26406980 PMID:8986748
Also transports purine nucleobases (hypoxanthine, adenine, guanine) and pyrimidine nucleobases (thymine, uracil) .
PMID:21795683 PMID:27995448
Mediates basolateral nucleoside uptake into Sertoli cells, thereby regulating the transport of nucleosides in testis across the blood-testis barrier (By similarity). Regulates inosine levels in brown adipocytes tissues (BAT) and extracellular inosine levels, which controls BAT-dependent energy expenditure PMID:35790189
Equilibrative nucleoside transporter 2
SLC29A2
substrate
Specific functionadenine transmembrane transporter activity
Cellular location
Apical cell membrane
General function & pharmacology
Bidirectional uniporter involved in the facilitative transport of nucleosides and nucleobases, and contributes to maintaining their cellular homeostasis .
PMID:10722669 PMID:12527552 PMID:12590919 PMID:16214850 PMID:21795683 PMID:9396714 PMID:9478986
Functions as a Na(+)-independent, passive transporter .
PMID:9478986
Involved in the transport of nucleosides such as inosine, adenosine, uridine, thymidine, cytidine and guanosine .
PMID:10722669 PMID:12527552 PMID:12590919 PMID:16214850 PMID:21795683 PMID:9396714 PMID:9478986
Also able to transport purine nucleobases (hypoxanthine, adenine, guanine) and pyrimidine nucleobases (thymine, uracil) .
PMID:16214850 PMID:21795683
Involved in nucleoside transport at basolateral membrane of kidney cells, allowing liver absorption of nucleoside metabolites .
PMID:12527552
Mediates apical nucleoside uptake into Sertoli cells, thereby regulating the transport of nucleosides in testis across the blood-testis-barrier .
PMID:23639800
Mediates both the influx and efflux of hypoxanthine in skeletal muscle microvascular endothelial cells to control the amount of intracellular hypoxanthine available for xanthine oxidase-mediated ROS production (By similarity)
PMID:10722669 PMID:12527552 PMID:12590919 PMID:16214850 PMID:21795683 PMID:9396714 PMID:9478986
Functions as a Na(+)-independent, passive transporter .
PMID:9478986
Involved in the transport of nucleosides such as inosine, adenosine, uridine, thymidine, cytidine and guanosine .
PMID:10722669 PMID:12527552 PMID:12590919 PMID:16214850 PMID:21795683 PMID:9396714 PMID:9478986
Also able to transport purine nucleobases (hypoxanthine, adenine, guanine) and pyrimidine nucleobases (thymine, uracil) .
PMID:16214850 PMID:21795683
Involved in nucleoside transport at basolateral membrane of kidney cells, allowing liver absorption of nucleoside metabolites .
PMID:12527552
Mediates apical nucleoside uptake into Sertoli cells, thereby regulating the transport of nucleosides in testis across the blood-testis-barrier .
PMID:23639800
Mediates both the influx and efflux of hypoxanthine in skeletal muscle microvascular endothelial cells to control the amount of intracellular hypoxanthine available for xanthine oxidase-mediated ROS production (By similarity)
Carriers(1)
Proteins that carry this drug through the body
Albumin
ALB
binder
Specific functionantioxidant activity
Cellular location
Secreted
General function & pharmacology
Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc .
PMID:19021548
Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity).
Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity).
Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli .
PMID:6234017
Does not prevent iron uptake by the bacterial siderophore aerobactin PMID:6234017
PMID:19021548
Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity).
Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity).
Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli .
PMID:6234017
Does not prevent iron uptake by the bacterial siderophore aerobactin PMID:6234017
Scientific references(5)
Carmine A.A., Brogden R.N., Heel R.C., Speight T.M., Avery G.S.
Trifluridine.
Drugs
198223(5):329-353. doi: 10.2165/00003495-198223050-00001
Burness C.B., Duggan S.T.
Trifluridine/Tipiracil: A Review in Metastatic Colorectal Cancer.
Drugs
2016 Sep76(14):1393-402. doi: 10.1007/s40265-016-0633-9
Matsuoka K., Nakagawa F., Kobunai T., Takechi T.
Trifluridine/tipiracil overcomes the resistance of human gastric 5-fluorouracil-refractory cells with high thymidylate synthase expression.
Oncotarget
2018 Feb 59(17):13438-13450. doi: 10.18632/oncotarget.24412. eCollection 2018 Mar 2
Pavan-Langston D., Nelson D.J.
Intraocular Penetration of Trifluridine.
American Journal of Ophthalmology
197987(6):814-818. doi: 10.1016/0002-9394(79)90360-x
Altmann S., Brandt C.R., Murphy C.J., Patnaikuni R., Takla T., Toomey M., Nesbit B., McIntyre K., Covert J., Dubielzig R., Leatherberry G., Adkins E., Kodihalli S.
Evaluation of therapeutic interventions for vaccinia virus keratitis.
Journal Infectious Diseases
2011 Mar 1203(5):683-90. doi: 10.1093/infdis/jiq103. Epub 2011 Jan 28
ATC classification(2 codes)
ATC L01BC59
ATC S01AD02
Affected organisms(1)
Human Herpes Virus
International brands(4)
Experimental properties(4)
Commercial products(18)
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Show
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Trifluridine
Additional database identifiers
Drugs Product Database (DPD)
1923
ChemSpider
6020
BindingDB
50132298
ZINC
ZINC000003842753
HUGO Gene Nomenclature Committee (HGNC)
HGNC:12441
GenAtlas
TYMS
GeneCards
TYMS
GenBank Gene Database
X02308
GenBank Protein Database
37479
Guide to Pharmacology
2642
UniProt Accession
TYSY_HUMAN
GenBank Gene Database
J04230
GenBank Protein Database
7537304
UniProt Accession
TYSY_CANAL
HUGO Gene Nomenclature Committee (HGNC)
HGNC:11830
GenAtlas
TK1
GeneCards
TK1
GenBank Gene Database
K02581
GenBank Protein Database
339709
UniProt Accession
KITH_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3148
GenAtlas
ECGF1
GeneCards
TYMP
GenBank Gene Database
M63193
GenBank Protein Database
189701
UniProt Accession
TYPH_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:399
GenAtlas
ALB
GeneCards
ALB
GenBank Gene Database
V00494
GenBank Protein Database
28590
UniProt Accession
ALBU_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10970
GenAtlas
hROAT1
GeneCards
SLC22A6
GenBank Gene Database
AF057039
GenBank Protein Database
3831566
Guide to Pharmacology
1025
UniProt Accession
S22A6_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:11001
GeneCards
SLC28A1
UniProt Accession
S28A1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:11003
GenAtlas
SLC29A1
GeneCards
SLC29A1
GenBank Gene Database
U81375
GenBank Protein Database
1845345
Guide to Pharmacology
1117
UniProt Accession
S29A1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:11004
GeneCards
SLC29A2
UniProt Accession
S29A2_HUMAN
International reference pricing
6 formulations
Reference pricing from DrugBank. Prices are indicative and may not reflect current UK costs.
From $3.41/ml
To $160.07/bottle
Sandoz Trifluridine 1 % Solution
$3.41/ml
Trifluridine 1 % opth soln
$15.21/ml
Viroptic 1% eye drops
$18.63/ml
Trifluridine 1% eye drops
$19.69/ml
Trifluridine 1% Solution 7.5ml Bottle
$153.40/bottle
Source: DrugBank. Used under CC BY-NC 4.0 academic licence for non-commercial purposes.
Patent information
7 active patents, 2 expired
10456399
United States
Approved 29 Oct 2019 · Expires 3 Feb 2037
10y 10m
10960004
United States
Approved 30 Mar 2021 · Expires 3 Feb 2037
10y 10m
9943537
United States
Approved 17 Apr 2018 · Expires 5 Sept 2034
8y 5m
9527833
United States
Approved 27 Dec 2016 · Expires 17 Jun 2034
8y 2m
10457666
United States
Approved 29 Oct 2019 · Expires 17 Jun 2034
8y 2m
The earliest active patent expires December 2026. Generic versions may become available after this date.
Source: DrugBank · CC BY-NC 4.0. Patent data sourced from national patent offices. Expiry dates may not reflect extensions, regulatory exclusivity periods, or legal challenges.
DrugBank citations
If you use DrugBank data in your research, please cite the following publications:
Knox C., Wilson M., Klinger C.M., et al
DrugBank 6.
0: the DrugBank Knowledgebase for 2024
Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
Wishart D.S., Feunang Y.D., Guo A.C., et al
DrugBank 5.
0: a major update to the DrugBank database for 2018
Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
Show earlier publications
Law V., Knox C., Djoumbou Y., et al
DrugBank 4.
0: shedding new light on drug metabolism
Nucleic Acids Res. 2014 Jan 142(1):D1091-7
Knox C., Law V., Jewison T., et al
DrugBank 3.
0: a comprehensive resource for 'omics' research on drugs
Nucleic Acids Res. 2011 Jan39(Database issue):D1035-41
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a knowledgebase for drugs, drug actions and drug targets.
Nucleic Acids Research
2008 Jan36(Database issue):D901-6
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a comprehensive resource for in silico drug discovery and exploration.
Nucleic Acids Research
2006 Jan 134(Database issue):D668-72
Source: go.drugbank.comCC BY-NC 4.0
Updated 26 days ago(8 Mar 2026)