section name header

Pronunciation ⬇

tri-FLOO-ri-deen/ti-PEER-a-sil

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: nucleoside metabolic inhibitors, thymidine phosphorylase inhibitors

Indications ⬆ ⬇

High Alert

Action ⬆ ⬇

  • Trifluridine: Following uptake into cells, interferes with DNA synthesis, inhibiting cell proliferation.
  • Tipiracil: Increases trifluridine levels by inhibiting thymidine phosphorylase, the enzyme that metabolizes it.
Therapeutic effects:
  • Decreases spread of metastatic colorectal, gastric, or gastroesophageal junction cancer.

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Protein Binding: Trifluridine: >96%.

Metabolism/Excretion: Trifluridine is metabolized by thymidine phosphorylase to an inactive metabolite. Trifluridine: 1.5% excreted unchanged in urine; tipiracil: 29.3% excreted unchanged in urine.

Half-Life: Trifluridine: 2.1 hr; tipiracil: 2.4 hr.

Time/Action Profile ⬆ ⬇

(improved survival)

ROUTEONSETPEAKDURATION
PO1–2 mounknownunknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects ⬆ ⬇

Derm: alopecia

GI: abdominal pain, diarrhea, nausea, vomiting, stomatitis

Hemat: anemia, neutropenia, THROMBOCYTOPENIA

Metab: ↓appetite

Neuro: asthenia

Misc: fever

Interactions ⬆ ⬇

Drug-drug:

Route/Dosage ⬆ ⬇

Renal Impairment

Availability ⬆ ⬇

(Generic available)
  • Tablets: trifluridine 15 mg/tipiracil 6.14 mg; trifluridine 20 mg/tipiracil 8.19 mg

Assessment ⬆ ⬇

  • Monitor for signs and symptoms of infection (fever, chills, body aches) periodically during therapy.

Lab Test Considerations:

  • Verify negative pregnancy test before starting therapy. Obtain CBC before and on Day 15 of each cycle and as clinically indicated. Do not administer until: ANC ≥1500/mm3 or febrile neutropenia resolved, platelet count ≥75,000/mm3, and Grade 3 or 4 nonhematologic adverse reactions are resolved to Grade 0–1. During treatment cycle, withhold trifluridine/tipiracil if: ANC <500/mm3 or febrile neutropenia, platelets <50,000/mm3, or Grade 3 or 4 nonhematologic adverse reactions occur. After recovery, ↓ dose by 5 mg/m2/dose from previous dose level if: febrile neutropenia; uncomplicated Grade 4 neutropenia and ANC has recovered to ≥1500/mm3 or platelet count ≥75,000/mm3, resulting in >1 wk delay in start of next cycle; or nonhematologic Grade 3 or 4 adverse reaction, except for Grade 3 nausea and/or vomiting controlled by antiemetic therapy or Grade 3 diarrhea responsive to antidiarrheal medication occur. No more than three dose reductions to a minimum dose of 20 mg/m2 twice daily are permitted. Do not escalate dose after reductions.

Implementation ⬆ ⬇

  • PO: Administer twice daily with food on Days 1–5 and Days 8–12 of each 28-day cycle. DNC: Swallow tablets whole; do not crush, break, or chew.

Patient/Family Teaching ⬆ ⬇

  • Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Instruct patient to take as directed. If dose missed or vomited, omit and take next dose at scheduled time; do not double doses. Inform patient that medication comes in two strengths; both strengths may be required for prescribed dose.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
  • Advise patient that anyone who handles medication should wear gloves. Wash hands after handling medication.
  • Advise patient to notify health care professional if signs and symptoms of infection or persistent nausea, vomiting, or diarrhea occur.
  • Rep: May cause fetal harm. Advise women of reproductive potential to use effective contraception during therapy and for 6 mo after last dose and to notify health care professional if pregnancy is planned or suspected. Advise female patients to avoid breastfeeding during and for ≥1 day after last dose of therapy. Advise male patients with female partners of reproductive potential to wear condoms during and for ≥3 mo after last dose of therapy.

Evaluation/Desired Outcomes ⬆ ⬇

  • Decreases spread of metastatic colorectal, gastric, or gastroesophageal junction cancer.

US Brand Names ⬆ ⬇

Lonsurf

Code ⬆

NDC Code