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Trifluridine-Tipiracil

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Trifluridine-Tipiracil, Trifluridine, Lonsurf

  • See Also
  1. Topical Fluorouracil
  2. Antimetabolite Chemotherapy
  3. Chemotherapy
  • Indications
  1. Colorectal Cancer (metastatic)
  2. Gastric or gastroesophageal junction adenocarcinoma (metastatic, refractory)
  • 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
  • Medications
  1. Trifluridine/Tipiracil Tablets: 15 mg/6.14 mg and 20 mg/8.19 mg
  • Dosing
  1. See other references for disease specific dosing protocols
  • Pharmacokinetics
  1. Trifluridine is metabolized by Thymidine phosphorylase
  • Adverse Effects
  1. Myelosuppression (severe)
  • 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
  • Resources
  1. Trifluridine-Tipiracil Tablets (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f5beed22-d71d-4c0d-8dca-2c7317d65d85