• Colorectal and other GI cancers

Lonsurf Generic Name & Formulations

General Description

Trifluridine, tipiracil; 15mg/6.14mg, 20mg/8.19mg; tabs.

Pharmacological Class

Antineoplastic thymidine-based nucleoside analog + thymidine phosphorylase inhibitor.

How Supplied

Tabs—20, 40, 60


Generic Availability


Mechanism of Action

Lonsurf consists of trifluridine, a thymidine-based nucleoside analog, and tipiracil, a thymidine phosphorylase inhibitor. Inclusion of tipiracil increases trifluridine exposure by inhibiting its metabolism by thymidine phosphorylase. Following uptake into cancer cells, trifluridine is incorporated into DNA, interferes with DNA synthesis and inhibits cell proliferation.

Lonsurf Indications


As a single agent or in combination with bevacizumab in patients with 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. Metastatic gastric or gastroesophageal junction adenocarcinoma in patients 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.

Lonsurf Dosage and Administration


Swallow whole. Take with food. 35mg/m2 twice daily on Days 1–5 and 8–12 of each 28-day cycle until disease progression or unacceptable toxicity; max 80mg per dose (based on trifluridine component). Severe renal impairment: 20mg/m2 twice daily on Days 1–5 and 8–12 of each 28-day cycle; if unable to tolerate, may reduce to 15mg/m2 twice daily. Permanently discontinue if unable to tolerate the 15mg/m2 twice daily dose. Dose modifications for adverse reactions: see full labeling. Refer to the Prescribing Information for bevacizumab dosing information.


Not established.

Lonsurf Contraindications

Not Applicable

Lonsurf Boxed Warnings

Not Applicable

Lonsurf Warnings/Precautions


Severe myelosuppression. Obtain CBCs prior to and on Day 15 of each cycle, and as clinically indicated. Do not initiate cycle until ANC ≥1,500/mm3 or febrile neutropenia is resolved, platelets ≥75,000/mm3 or Grade 3/4 non-hematological adverse reactions resolved to Grade 0/1. Withhold dose if ANC <500/mm3 or febrile neutropenia, platelets <50,000/mm3, or Grade 3/4 non-hematological adverse reactions occur; upon recovery, resume at a reduced dose (see full labeling). Moderate or severe hepatic impairment: do not initiate. Severe renal impairment (CrCl <30mL/min): reduce dose. ESRD: not studied. Embryo-fetal toxicity. Use effective contraception during and for ≥6 months (females) or ≥3 months (males w. female partners) after final dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 1 day after final dose).

Lonsurf Pharmacokinetics


Following a single oral administration of Lonsurf at 35 mg/m2 in patients with cancer, the mean time to peak plasma concentration (Tmax) of trifluridine was ~2 hours.


Plasma protein bound: >96% (trifluridine); <8% (tipiracil).


Trifluridine is mainly eliminated by metabolism via thymidine phosphorylase.


Renal, fecal. Half-life (at steady-state): 2.1 hours (trifluridine); 2.4 hours (tipiracil).

Lonsurf Interactions

Not Applicable

Lonsurf Adverse Reactions

Adverse Reactions

Anemia, neutropenia, asthenia/fatigue, nausea, thrombocytopenia, decreased appetite, diarrhea, vomiting, abdominal pain, pyrexia.

Lonsurf Clinical Trials

See Literature

Lonsurf Note

Not Applicable

Lonsurf Patient Counseling

See Literature