trifluridine/tipiracil

High Alert

Metastatic colorectal cancer in patients previously treated with fluoropyrimidine-, oxalplatin- or irinotecan-based chemotherapies, an anti-VEGF based biological, and (if RAS wild-type positive) an anti-EGFR agent (as monotherapy or in combination with bevacizumab).
Metastatic gastric or gastroesophageal junction adenocarcinoma previously treated with ≥2 lines of chemotherapy including a fluoropyrimidine, a platinum, either a taxane or irinotecan, and, if appropriate, a HER2/neu-targeted therapy.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

ANC <1500/mm³ or platelets <75,000/mm³;
Moderate to severe hepatic impairment;
End-stage renal disease;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Severe renal impairment (↓ dose);
Rep: Women of reproductive potential or men with female partners of reproductive potential;
Geri: ↑risk and severity of myelosuppression in older adults.

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:

None reported.

Availability ⬆ ⬇

Tablets: trifluridine 15 mg/tipiracil 6.14 mg; trifluridine 20 mg/tipiracil 8.19 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 35 mg/m²/dose (max dose = 80 mg) (based on trifluridine content rounded to the nearest 5 mg) twice daily on Days 1–5 and 8–12 of each 28-day cycle; continue until disease progression or unacceptable toxicity.

Renal Impairment

PO (Adults ): CCr 15–29 mL/min: 20 mg/m²/dose (based on trifluridine content rounded to the nearest 5 mg) twice daily on Days 1–5 and 8–12 of each 28-day cycle; may ↓ dose to 15 mg/m²/dose if unable to tolerate dose of 20 mg/m²; continue until disease progression or unacceptable toxicity.

US Brand Names ⬆ ⬇

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.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: nucleoside metabolic inhibitors, thymidine phosphorylase inhibitors

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)

ROUTE	ONSET	PEAK	DURATION
PO	1–2 mo	unknown	unknown

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.

Pronunciation ⬆ ⬇

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

Code ⬆

NDC Code

64842- Taiho Pharmaceutical Co., Ltd.
- 64842-1020- LONSURF
  - 64842-1020-1- 20 TABLET, FILM COATED in 1 BOTTLE (64842-1020-1)

64842- Taiho Pharmaceutical Co., Ltd.
- 64842-1020- LONSURF
  - 64842-1020-2- 40 TABLET, FILM COATED in 1 BOTTLE (64842-1020-2)

64842- Taiho Pharmaceutical Co., Ltd.
- 64842-1020- LONSURF
  - 64842-1020-3- 60 TABLET, FILM COATED in 1 BOTTLE (64842-1020-3)

64842- Taiho Pharmaceutical Co., Ltd.
- 64842-1025- LONSURF
  - 64842-1025-1- 20 TABLET, FILM COATED in 1 BOTTLE (64842-1025-1)

64842- Taiho Pharmaceutical Co., Ltd.
- 64842-1025- LONSURF
  - 64842-1025-2- 40 TABLET, FILM COATED in 1 BOTTLE (64842-1025-2)

64842- Taiho Pharmaceutical Co., Ltd.
- 64842-1025- LONSURF
  - 64842-1025-3- 60 TABLET, FILM COATED in 1 BOTTLE (64842-1025-3)

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Indications ⬇