Trifluridine and tipiracil
Looking up MedlinePlus…
From MedlinePlus, U.S. National Library of Medicine
Handling and access
NIOSH hazardous drug
Table 1This product contains trifluridine, which NIOSH lists as a hazardous drug. AHFS class: 10:00 antineoplastic agents.
- The package insert includes manufacturer's special handling information (MSHI). Follow it when preparing, administering, and disposing of this drug.
Handle with the precautions your facility uses for hazardous drugs (USP <800>). NIOSH's Managing Hazardous Drug Exposures lists controls by drug form and activity.
Nucleoside Analog Antiviral, Nucleoside Metabolic Inhibitor
Dosing in kidney impairment
Recommended Dosage for Renal Impairment Severe Renal Impairment In patients with severe renal impairment [creatinine clearance (CLcr) of 15 to 29 mL/min as determined by the Cockcroft-Gault formula], the recommended dosage is 20 mg/m 2 (based on the trifluridine component) orally twice daily with food on Days 1 through 5 and Days 8 through 12 of each 28-day cycle (Table 2) [see Use in Specific Populations and Clinical Pharmacology ] .
Reduce dose to 15 mg/m 2 twice daily in patients with severe renal impairment who are unable to tolerate a dose of 20 mg/m 2 twice daily (Table 2). Permanently discontinue LONSURF in patients who are unable to tolerate a dose of 15 mg/m 2 twice daily. [See table below.] : Recommended Dosage for Severe Renal Impairment According to BSA BSA (m 2 ) Total daily dose (mg) Dose (mg) administered twice daily Tablets per dose 15 mg 20 mg For a dose of 20 mg/m 2 twice daily: < 1.14 40 20 0 1 1.14 – 1.34 50 25 For a total daily dose of 50 mg, instruct patients to take 1 x 20-mg tablet in the morning and 2 x 15-mg tablets in the evening. 2 in the evening 1 in the morning 1.35 – 1.59 60 30 2 0 1.60 – 1.94 70 35 1 1 1.95 – 2.09 80 40 0 2 2.10 – 2.34 90 45 3 0 ≥ 2.35 100 50 2 1 For a dose of 15 mg/m 2 twice daily: < 1.15 30 15 1 0 1.15 – 1.49 40 20 0 1 1.50 – 1.84 50 25 2 in the evening 1 in the morning 1.85 – 2.09 60 30 2 0 2.10 – 2.34 70 35 1 1 ≥ 2.35 80 40 0 2
| BSA (m2) | Total daily dose (mg) | Dose (mg) administered twice daily | Tablets per dose | |
| 15 mg | 20 mg | |||
| For a dose of 20 mg/m2 twice daily: | ||||
| < 1.14 | 40 | 20 | 0 | 1 |
| 1.14 – 1.34 | 50 | 25For a total daily dose of 50 mg, instruct patients to take 1 x 20-mg tablet in the morning and 2 x 15-mg tablets in the evening. | 2 in the evening | 1 in the morning |
| 1.35 – 1.59 | 60 | 30 | 2 | 0 |
| 1.60 – 1.94 | 70 | 35 | 1 | 1 |
| 1.95 – 2.09 | 80 | 40 | 0 | 2 |
| 2.10 – 2.34 | 90 | 45 | 3 | 0 |
| ≥ 2.35 | 100 | 50 | 2 | 1 |
| For a dose of 15 mg/m2 twice daily: | ||||
| < 1.15 | 30 | 15 | 1 | 0 |
| 1.15 – 1.49 | 40 | 20 | 0 | 1 |
| 1.50 – 1.84 | 50 | 25 | 2 in the evening | 1 in the morning |
| 1.85 – 2.09 | 60 | 30 | 2 | 0 |
| 2.10 – 2.34 | 70 | 35 | 1 | 1 |
| ≥ 2.35 | 80 | 40 | 0 | 2 |
Dosing in liver impairment
Hepatic Impairment No adjustment to the starting dosage of LONSURF is recommended for patients with mild hepatic impairment. Do not initiate LONSURF in patients with baseline moderate or severe (total bilirubin >1.5 times ULN and any AST) hepatic impairment [see Clinical Pharmacology ] .
Contraindications
None. None. ( 4 )
Safety data
Reported adverse events (FAERS)
Liver injury (LiverTox)
LiverTox has no chapter for trifluridine and tipiracil. Check the label's hepatic warnings.
Pregnancy and lactation
Pregnancy
8.1 Pregnancy Risk Summary Based on animal data and its mechanism of action [see Clinical Pharmacology (12.2) ] , LONSURF can cause fetal harm. LONSURF caused embryo-fetal lethality and embryo-fetal toxicity in pregnant rats when given during gestation at doses resulting in exposures lower than or similar to human exposures at the recommended clinical dose (see Data ) . There are no available data on LONSURF use in pregnant women. Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.
Data Animal Data Trifluridine/tipiracil was administered orally once daily to female rats during organogenesis at dose levels of 15, 50, and 150 mg/kg [trifluridine (FTD) equivalent]. Decreased fetal weight was observed at FTD doses ≥50 mg/kg (approximately 0.33 times the FTD exposure at the clinical dose of 35 mg/m 2 twice daily). At the FTD dose of 150 mg/kg (approximately 0.92 times the FTD exposure at the clinical dose of 35 mg/m 2 twice daily) embryolethality and structural anomalies (kinked tail, cleft palate, ectrodactyly, anasarca, alterations in great vessels, and skeletal anomalies) were observed.
For breastfeeding, also see LactMed (National Library of Medicine), which summarizes milk levels and infant effects.
Supply and cost
Drug shortage status
Recalls (last 24 months)
Therapeutic equivalence (Orange Book)
Price ladder
Not the price at the counterThese are not what a patient pays at the pharmacy counter. They are what pharmacies, health plans, and government buyers pay, before manufacturer rebates. A patient's cost depends on their insurance (copay, coinsurance, or deductible) or the pharmacy's cash price.