II. Indications

  1. Colorectal Cancer (metastatic)
  2. Gastric or gastroesophageal junction adenocarcinoma (metastatic, refractory)

III. Mechanism

  1. Trifluridine
    1. Fluorinated thymidine analog with both antineoplastic and Antiviral activity
    2. As a thymidine analog, Trifluridine is incorporated into DNA
      1. Inhibits thymidylate synthase
      2. Inhibits DNA synthesis and Protein synthesis
  2. Tipiracil
    1. Thymidine phosphorylase inhibitor
    2. Thymidine is added to Trifluridine, to slow its metabolism, and potentiate its activity

IV. Medications

  1. Trifluridine/Tipiracil Tablets: 15 mg/6.14 mg and 20 mg/8.19 mg

V. Dosing

  1. See other references for disease specific dosing protocols

VI. Pharmacokinetics

  1. Trifluridine is metabolized by Thymidine phosphorylase

VII. Adverse Effects

  1. Myelosuppression (severe)

VIII. Safety

  1. Avoid in Lactation
  2. Avoid in pregnancy (all trimesters)
    1. Use reliable Contraception
  3. Monitoring
    1. Complete Blood Count (CBC)
      1. Obtain prior to dosing and again on Day 15 of Chemotherapy cycle

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Related Studies

Cost: Medications

trifluridine (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
TRIFLURIDINE 1% EYE DROPS Generic $19.43 per ml

Ontology: Trifluridine (C0040987)

Definition (NCI) A fluorinated thymidine analog with potential antineoplastic activity. Trifluridine is incorporated into DNA and inhibits thymidylate synthase, resulting in inhibition of DNA synthesis, inhibition of protein synthesis, and apoptosis. This agent also exhibits antiviral activity. (NCI04)
Definition (MSH) An antiviral derivative of THYMIDINE used mainly in the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to HERPES SIMPLEX virus. (From Martindale, The Extra Pharmacopoeia, 30th ed, p557)
Definition (PDQ) A fluorinated thymidine analog with potential antineoplastic activity. Trifluridine is incorporated into DNA and inhibits thymidylate synthase, resulting in inhibition of DNA synthesis, inhibition of protein synthesis, and apoptosis. This agent also exhibits antiviral activity. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39240&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39240&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C905" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Nucleic Acid, Nucleoside, or Nucleotide (T114)
MSH D014271
SnomedCT 58892008, 373512003
English 5 Trifluoromethyl 2' deoxyuridine, 5-Trifluoromethyl-2'-deoxyuridine, Trifluoridine, Trifluorothymidine, Trifluridine, Thymidine, alpha,alpha,alpha-trifluoro-, 2'-Deoxy-5-trifluoromethyluridine, F3 T, F<sub>3</sub>T, F3T - trifluorothymidine, F3TdR, Trifluridine [Chemical/Ingredient], TRIFLURIDINE, trifluridine, 2'-deoxy-5-(trifluoromethyl)uridine, F>3<T, Trifluridine (product), Trifluridine (substance), triflorothymidine, Triflorothymidine
German Trifluoridin, Trifluorthymidin, Trifluridin
Swedish Trifluridin
Czech trifluorothymidin, trifluridin
Finnish Trifluridiini
Russian TRIFTORURIDIN, TRIFTORTIMIDIN, ТРИФТОРТИМИДИН, ТРИФТОРУРИДИН
Japanese トリフルオロチミジン, ビロプチック, ビロプティック, トリフルリジン
Polish Trifluorotymidyna, Trójfluorotymidyna, Triflurydyna
Spanish trifluorotimidina, trifluridina (producto), trifluridina (sustancia), trifluridina, Trifluorotimidina, Trifluridina
French Trifluorothymidine
Italian Trifluoridina
Portuguese Trifluorotimidina, Trifluridina