OnCo
drugsProductApproved2015🇪🇺🇬🇧🇯🇵🇨🇳🇦🇺

Trifluridine/tipiracil

An oral chemotherapy pill for bowel cancer that has stopped responding to everything else; with bevacizumab it extends life by about three months.

Trifluridine is incorporated into DNA; tipiracil blocks its breakdown. RECOURSE (2015) showed OS 7.1 vs 5.3 months alone; SUNLIGHT (2023) showed 10.8 vs 7.5 months with bevacizumab. Also approved in gastric cancer (TAGS). Neutropenia is the main toxicity; works even after 5-FU resistance because of a different mechanism.

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Trifluridine
PubChem
Mechanism, step by step
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1.Tipiracil blocks the enzyme that would destroy trifluridine, keeping blood levels up

Modality
Cytotoxic chemotherapy (oral nucleoside)
Mechanism
Trifluridine misincorporation into DNA causes strand dysfunction; tipiracil inhibits thymidine phosphorylase to maintain exposure.
Brand / code
Lonsurf · TAS-102
Dosing & schedule
Route
Oral
Schedule
35 mg/m² twice daily on days 1-5 and 8-12 of a 28-day cycle
Dose modifications
Delay for neutrophils <1,500 or platelets <75,000
Monitoring
Complete blood count before each cycle and on day 15

Source: www.accessdata.fda.gov/drugsatfda_docs/label/2023/207981s012lbl.pdf. Doses are for orientation; the current label governs.

Medicare
Part D (self-administered)

Oral, self-administered, so it is a Part D drug: covered through a stand-alone Part D plan or Medicare Advantage drug benefit, usually on the specialty tier with 25 to 33% coinsurance until the annual cap ($2,000 in 2025, $2,100 in 2026).

Commercial insurance
covered with prior authorisation

Covered for FDA-labelled and NCCN-listed uses, but almost always behind prior authorisation confirming diagnosis, biomarker and line of therapy; dispensed through a specialty pharmacy. Plans require prior fluoropyrimidine, oxaliplatin and irinotecan for colorectal use.

Assistance programmes

Part D out-of-pocket capped at $2,000 (2025) / $2,100 (2026). Medicare patients cannot use manufacturer co-pay cards; charity funds (PAN, HealthWell, CancerCare) and the Extra Help subsidy are the routes.

Sources: Medicare.gov: Drug coverage (Part D) · Medicare.gov: Costs for Medicare drug coverage (annual out-of-pocket cap). Not medical or financial advice; verify with your plan.

NICE recommendedNICE TA405 · 2016SMC: accepted
Appraised for
Metastatic colorectal cancer after standard therapies
Notes
Metastatic gastric or GOJ cancer after 2 or more therapies: TA669 (2021). With bevacizumab (SUNLIGHT) appraised 2024.
NHS England
Routinely funded for the appraised indication (or via managed access)

Sources: NICE TA405 · SMC advice: trifluridine-tipiracil. Funding decisions are indication-specific and change monthly; verify with NICE and your treating team.

Regulatory

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  1. Sept 2015ApprovalUS

    RECOURSE

  2. Aug 2023ApprovalUS

    SUNLIGHT combination

Approvals

RegionYearIndication
US2015Refractory metastatic colorectal cancer
US2019Refractory metastatic gastric/GEJ cancer (TAGS)
US2023Refractory mCRC with bevacizumab

Safety

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Toxicity profile
Adverse event
Neutropenia
Anaemia
Nausea, fatigue

Most common grade 3-4 event; febrile neutropenia uncommon. Events listed without rates were not read from a primary source; see the label. Blank cells mean the figure was not sourced, not that it is zero.

Trials

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ClinicalTrials.gov · phase 2/3
refreshed 2026-09-09
141 studies25 recruiting74 Phase 227 Phase 3
Search “Trifluridine” on ClinicalTrials.gov →
Counts are from a name search and may include unrelated studies; up to 100 studies are summarised.

Recruiting now (live from ClinicalTrials.gov)

Recruiting trials near you · live from ClinicalTrials.gov
Trifluridine/tipiracil
intervention: Trifluridine
Open on ClinicalTrials.gov →

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Landmark trials in OnCo

Latest papers

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Literature trend91 papers in the last 12 months0% vs prior 12How this is computed
Latest papers · live from Europe PMC
Open in Europe PMC

Query for this drug: (TITLE:"Trifluridine/tipiracil" OR ABSTRACT:"Trifluridine/tipiracil" OR TITLE:"Lonsurf" OR ABSTRACT:"Lonsurf" OR TITLE:"TAS-102" OR ABSTRACT:"TAS-102") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Trifluridine/tipiracil, not a curated reading list.

Connected

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