pharmacopeia
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/api/v1/drug/trifluridine

Mechanism of action

Sourced from openFDA

Mechanism-of-action classes: Nucleic Acid Synthesis Inhibitors; Thymidylate Synthetase Inhibitors; Unknown Cellular or Molecular Interaction.

Nucleic Acid SynthesisThymidylate Synthetase

Indications

Sourced from openFDA
  • Trifluridine Ophthalmic Solution is indicated for the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus, types 1 and 2.ICD-10: B00.9

Contraindications

Sourced from openFDA
  • Trifluridine Ophthalmic Solution is contraindicated for patients who develop hypersensitivity reactions or chemical intolerance to trifluridine.contraindicated

Dosage & administration

Sourced from openFDA

Instill one drop of Trifluridine Ophthalmic Solution onto the cornea of the affected eye every 2 hours while awake for a maximum daily dosage of nine drops until the cornea ulcer has completely re-epithelialized. Following re-epithelialization, treatment for an additional 7 days of one drop every 4 hours while awake for a minimum daily dosage of five drops is recommended. If there are no signs of improvement after 7 days of therapy or complete re-epithelialization has not occurred after 14 days of therapy, other forms of therapy should be considered. Continuous administration of trifluridine for periods exceeding 21 days should be avoided because of potential ocular toxicity.

Warnings & precautions

Sourced from openFDA

The recommended dosage and frequency of administration should not be exceeded (See DOSAGE AND ADMINISTRATION ).

Adverse reactions

Sourced from openFDA

The most frequent adverse reactions reported during controlled clinical trials were mild, transient burning or stinging upon instillation (4.6%) and palpebral edema (2.8%). Other adverse reactions in decreasing order of reported frequency were superficial punctate keratopathy, epithelial keratopathy, hypersensitivity reaction, stromal edema, irritation, keratitis sicca, hyperemia, and increased intraocular pressure.

Use in specific populations

Sourced from openFDA

Pregnancy: Teratogenic Effects: Trifluridine was not teratogenic at doses up to 5 mg/kg/day (23 times the estimated human exposure) when given subcutaneously to rats and rabbits. However, fetal toxicity consisting of delayed ossification of portions of the skeleton occurred at dose levels of 2.5 and 5 mg /kg /day in rats and at 2.5 mg/kg/day in rabbits. In addition, both 2.5 and 5 mg/kg/day produced fetal death and resorption in rabbits. In both rats and rabbits, 1 mg/kg/day (5 times the estimated human exposure) was a no-effect level. There were no teratogenic or fetotoxic effects after topical application of trifluridine (approximately 5 times the estimated human exposure) to the eyes of rabbits on the 6th through the 18th days of pregnancy. In a non-standard test, trifluridine solution has been shown to be teratogenic when injected directly into the yolk sac of chicken eggs. There are no adequate and well-controlled studies in pregnant women. Trifluridine Ophthalmic Solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Overdosage

Sourced from openFDA

Overdosage by ocular instillation is unlikely because any excess solution should be quickly expelled from the conjunctival sac. Acute overdosage by accidental oral ingestion of trifluridine has not occurred. However, should such ingestion occur, the 75 mg dosage of trifluridine in a 7.5 mL bottle of Trifluridine Ophthalmic Solution is not likely to produce adverse effects. Single intravenous doses of 1.5 to 30 mg/kg/day in children and adults with neoplastic disease produce reversible bone marrow depression as the only potentially serious toxic effect and only after three to five courses of therapy. The acute oral LD 50 in the mouse and rat was 4379 mg/kg or higher.

Approval history

Sourced from openFDA
  • Oct 6, 1995ANDAANDA074311Sandoz
  • Sep 22, 2015NDANDA207981Taiho Oncology

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
10,906 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Death3,11729%
  2. 2Disease Progression1,81217%
  3. 3Fatigue1,39413%
  4. 4Nausea1,17611%
  5. 5Diarrhoea1,0299.4%
  6. 6Decreased Appetite6896.3%
  7. 7Vomiting6355.8%
  8. 8Asthenia4924.5%
  9. 9White Blood Cell Count Decreased4844.4%
  10. 10Drug Ineffective4023.7%
  11. 11Anaemia3713.4%
  12. 12Neutropenia3493.2%
  13. 13Weight Decreased3363.1%
  14. 14Constipation3353.1%
  15. 15Off Label Use3343.1%

Literature

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Recent PubMed references pinned to Trifluridine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 196 ClinicalTrials.gov registrations naming Trifluridine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Trifluridine work?
Mechanism-of-action classes: Nucleic Acid Synthesis Inhibitors; Thymidylate Synthetase Inhibitors; Unknown Cellular or Molecular Interaction.
What is Trifluridine used for?
According to FDA labeling, Trifluridine carries indications including: Trifluridine Ophthalmic Solution is indicated for the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus, types 1 and 2.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Trifluridine?
Trifluridine is classified as Antivirals, Nucleoside Analog Antiviral, Nucleoside Metabolic Inhibitor, Nucleic Acid Synthesis Inhibitors, Thymidylate Synthetase Inhibitors, Unknown Cellular or Molecular Interaction, Decreased DNA Replication, Decreased RNA Replication.
What are the brand names for Trifluridine?
Trifluridine is marketed under brand names including Lonsurf.
What are the contraindications for Trifluridine?
Trifluridine labeling lists contraindications including: Trifluridine Ophthalmic Solution is contraindicated for patients who develop hypersensitivity reactions or chemical intolerance to trifluridine.. Always consult the full prescribing information and a clinician.
Note. Data for trifluridine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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