Trifluridine and Tipiracil

What is Trifluridine and Tipiracil combination medicine

Trifluridine and tipiracil is a combination product that is FDA approved for the treatment of metastatic colorectal cancer and metastatic gastric or gastroesophageal junction cancer after progression on several previous lines of therapy.

Trifluridine was initially developed in the 1960s but was abandoned due to a lack of objective responses and very short half-life (12 minutes) when administered by intravenous injection.

Trifluridine is rapidly inactivated by thymidine phosphorylase after administration; tipiracil inhibits thymidine phosphorylase, preventing this rapid degradation and increasing trifluridine exposure.

Trifluridine; tipiracil can cause severe myelosuppression. Monitor complete blood counts as an interruption of therapy or dose reduction may be necessary.

Brand Name



  • colorectal cancer
  • gastric cancer

For the treatment of metastatic colorectal cancer in patients who have previously been treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF biologic therapy, and if RAS wild-type, an anti-EGFR therapy

Side Effects

  1. abdominal pain
  2. alopecia
  3. anemia
  4. anorexia
  5. asthenia
  6. bone marrow suppression
  7. diarrhea
  8. dysgeusia
  9. fatigue
  10. fever
  11. infection
  12. nausea
  13. neutropenia
  14. pneumonitis
  15. pulmonary embolism
  16. QT prolongation
  17. stomatitis
  18. thrombocytopenia
  19. vomiting

Monitoring Parameters

  • CBC with differential
  • pregnancy testing


  • anemia
  • bone marrow suppression
  • breast-feeding
  • chemotherapy
  • children
  • contraception requirements
  • fever
  • geriatric
  • infants
  • infection
  • male-mediated teratogenicity
  • neutropenia
  • pregnancy
  • pregnancy testing
  • radiation therapy
  • reproductive risk
  • thrombocytopenia


  • Palifermin
  • Penicillamine
  • Tuberculin Purified Protein Derivative, PPD

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