trifluridine, combinations

L01BC59

Forms & Strengths

Adult Dosing

Metastatic colorectal cancer: 35 mg/m2 (based on trifluridine component) orally twice daily on Days 1 through 5 and Days 8 through 12 of each 28-day cycle
Metastatic gastric or gastroesophageal junction adenocarcinoma: 35 mg/m2 orally twice daily on Days 1 through 5 and Days 8 through 12 of each 28-day cycle
Maximum dose: 80 mg per dose (based on trifluridine component)

Pediatric Dosing

Indications

Treatment of patients with metastatic colorectal cancer previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and, if RAS wild-type, an anti-EGFR therapy
Treatment of patients with metastatic gastric or gastroesophageal junction adenocarcinoma previously treated with at least two prior lines of chemotherapy that included a fluoropyrimidine, platinum, either a taxane or irinotecan, and if appropriate, HER2/neu-targeted therapy

Mechanism of Action

Trifluridine is a nucleoside metabolic inhibitor incorporated into DNA during DNA synthesis, interfering with DNA function
Tipiracil hydrochloride is a thymidine phosphorylase inhibitor that prevents rapid degradation of trifluridine, increasing its systemic exposure

Contraindications

Adverse Reactions

Drug Interactions

Thymidine kinase inhibitors (e.g., zidovudine) may competitively interfere with the efficacy of trifluridine; avoid concurrent use
Substrates of equilibrative nucleoside transporter 1 (ENT1) or organic cation transporter 2 (OCT2) may have altered pharmacokinetics

Curated Content: Needs Vetting Before Put to Clinical Use