Tipiracil and Trifluridine

Cytostatic · Thymidine Phosphorylase Inhibitor/Viral DNA Synthesis Inhibitor

Indications

Treatment of adult patients with: (1) Metastatic colorectal cancer who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and if RAS wild-type, an anti-EGFR therapy. (2) Metastatic gastric or gastroesophageal junction adenocarcinoma previously treated with at least 2 prior lines of chemotherapy that included a fluoropyrimidine, a platinum, either a taxane or irinotecan, and if appropriate, HER2/neu-targeted therapy.

Dosage

Adults: Recommended dosage: 35 mg/m2/dose orally twice daily with food on Days 1 through 5 and Days 8 through 12 of each 28-day cycle until disease progression or unacceptable toxicity. Round dose to the nearest 5 mg increment. A maximum of 3 dose reductions are permitted. Permanently discontinue in patients who are unable to tolerate a dose of 20 mg/m2 orally twice daily. Do not escalate dosage after it has been reduced. Children: Not recommended.

Adverse Effects

Anaemia, neutropaenia, fatigue/asthenia, nausea, thrombocytopaenia, reduced appetite, diarrhoea, vomiting and pyrexia.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Baseline moderate or severe hepatic impairment. Absolute neutrophil count (ANC) =1500/mm3 or febrile neutropaenia. Platelets =75000/mm3. Grade 3 or 4 non-haematological adverse reaction. Precautions: Severe myelosuppression; obtain complete blood counts prior to and on Day 15 of each cycle. Withhold and resume at next lower dosage as recommended. Elderly. Severe renal impairment.

Advice to Patient

Swallow whole tablet. Take with meals. Anyone else who handles the medication must wear gloves. Do not retake doses that are vomited or missed and continue with the next scheduled dose. Females of reproductive potential must use effective contraception during treatment and for at least 6 months after the final dose. Because of the potential for genotoxicity, males with female partners of reproductive potential must use protection during treatment and for at least 3 months after the final dose. Lactating mothers must avoid lactation during treatment and for 1 day after the final dose. Immediately report signs or symptoms of infection. Keep all appointments for blood tests. Report severe or persistent nausea, vomiting, diarrhoea, or abdominal pain.

Pharmacokinetics

Absorption: Trifluridine: 2 hrs. Metabolism: Trifluridine: Via thymidine phosphorylase. Excretion: Trifluridine: Urine (55%). Faeces and expired air (<3%). Tipiracil: Urine (27%). Faeces (50%).

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.