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Trifluridine/Tipiracil

Phase 3

Refractory Metastatic Colorectal Cancer | Small molecule | Oncology |Tango Therapeutics, Inc.|Last Updated: Sep 19, 2025

Success Probability

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Market & Valuation

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Trial Design

RandomizedACTIVE_CONTROLLEDDMCBiomarker
Total Trials1
Total Enrollment492

FDA Designations

No designations recorded

Clinical trial landscape

Trifluridine/Tipiracil · 3 trials · 6 indications

Phase 3 1Phase 2 2
NCT04737187Phase III Study of Trifluridine/Tipiracil With and Without Bevacizumab in Refractory Metastatic Colorectal Cancer PatientsRefractory Metastatic Colorectal Cancer
COMPLETED492 Analytics
PHASE3COMPLETED
Phase III Study of Trifluridine/Tipiracil With and Without Bevacizumab in Refractory Metastatic Colorectal Cancer Patients
Refractory Metastatic Colorectal CancerUnlock trial analytics

Study Endpoints

Primary Endpoints

Overall Survival (OS)
From date of randomization to the death due to any cause or cut-off date, whichever comes first (maximum duration: up to 20 months)

Overall survival defined as the observed time elapsed between the date of randomization and the date of death due to any cause. The primary estimand of interest was defined to assess the effect of the randomized treatments on the survival duration in all participants regardless of whether or not intercurrent events had occurred (treatment policy strategy). Analysis was performed using Kaplan- Meier method.

Survival Probability at 6 Months
From date of randomization until 6 months post treatment

Overall survival defined as the observed time elapsed between the date of randomization and the date of death due to any cause. The primary estimand of interest was defined to assess the effect of the randomized treatments on the survival duration in all participants regardless of whether or not intercurrent events had occurred (treatment policy strategy). Analysis was performed using Kaplan- Meier method. In this outcome measure, data of survival probability at 6 months was reported.

Survival Probability at 12 Months
From date of randomization until 12 months post treatment

Overall survival defined as the observed time elapsed between the date of randomization and the date of death due to any cause. The primary estimand of interest was defined to assess the effect of the randomized treatments on the survival duration in all participants regardless of whether or not intercurrent events had occurred (treatment policy strategy). Analysis was performed using Kaplan- Meier method. In this outcome measure, data of survival probability at 12 months was reported.

Survival Probability at 18 Months
From date of randomization until 18 months post treatment

Overall survival defined as the observed time elapsed between the date of randomization and the date of death due to any cause. The primary estimand of interest was defined to assess the effect of the randomized treatments on the survival duration in all participants regardless of whether or not intercurrent events had occurred (treatment policy strategy). Analysis was performed using Kaplan- Meier method. In this outcome measure, data of survival probability at 18 months was reported.

Progression free-survival
From randomization to disease progression or death up to 5 years

The progression-free survival (PFS) is the length of time during and after the treatment of a disease that a patient lives with the disease but it does not get worse.

Progression-free survival
8 weeks

Response rate CR/PR

Secondary Endpoints

Progression Free Survival (PFS)
From randomization to the date of radiological tumour progression or death due to any cause or data cut-off date whichever comes first (i.e., up to 20 months)
Probability of Participants With Progression Free Survival at 3, 6, 9 and 12 Months
From randomization until 3, 6, 9, and 12 months post treatment
Overall Response Rate (ORR)
From the date of randomization to the date of documentation of progression or death due to any cause or data cut-off, whichever occurred first (i.e., up to 20 months)
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Trifluridine/Tipiracil + BevacizumabEXPERIMENTALParticipants were administered 35 milligrams per square meter per dose (mg/m²/dose) trifluridine/tipiracil (FTD/TPI) orally twice a day (BID), within 1 hour after completion of morning and evening meals, 5 days on (Day 1 to 5 and Day 8 to 12) with 2 days off (Day 6 to 7 an Day 13 to 14), over 2 weeks, followed by a 14-day rest; with bevacizumab (5 milligrams per kilogram \[mg/kg\], intravenous \[IV\] infusion administered every 2 weeks (Day 1 and Day 15). This treatment cycle was repeated every 4 weeks.
Trifluridine/TipiracilACTIVE_COMPARATORParticipants were administered 35 mg/m²/dose of FTD/TPI orally BID, within 1 hour after completion of morning and evening meals, 5 days on (Day 1 to 5 and Day 8 to 12) with 2 days off (Day 6 to 7 and Day 13 to 14), over 2 weeks, followed by a 14-day rest. This treatment cycle was repeated every 4 weeks.
Trifluridine/Tipiracil + Oxaliplatin ± nivolumabEXPERIMENTALTrifluridine/Tipiracil will be administered with a 14-day schedule (35 mg/m² twice-daily \[BID\] for 5 days followed by 9 days of recovery) until disease progression or intolerable toxicity. Oxaliplatin will be administered intravenously on day 1 of each treatment cycle (infusion duration: 2 hours), every 2 weeks. The first cycle will be administered at level -1 (70 mg/m²) and then increased to 85 mg/m² (if feasible) from the cycle 2 to 8 or until disease progression, whatever occurs first. In case of limiting-oxaliplatin neuropathy and in all cases after 8 cycles, oxaliplatin will be stopped and Trifluridine/Tipiracil will be continued alone until disease progression or intolerable toxicity. ± nivolumab 240 mg (infusion duration 30 minutes, every 2 weeks) until disease progression or intolerable toxicity for a maximum of 2 years.
FOLFOX ± nivolumabACTIVE_COMPARATORFolinic Acid 400 mg/m² (or 200 mg/m² if L-folinic acid) + oxaliplatin 85 mg/m² (infusion duration: 2 hours) followed by 5-FU bolus 400 mg/m² and then 5-FU 2400 mg/m² as a 46-hour continuous infusion. Treatment repeated every 14 days. In case of limiting-oxaliplatin neuropathy and in all cases after 8 cycles, oxaliplatin will be stopped and 5-FU (simplified LV5FU2 regimen) or capecitabine (1000 mg/m² BID during 2 weeks every 3 weeks) will be continued alone until disease progression or intolerable toxicity. ± nivolumab 240 mg (infusion duration 30 minutes, every 2 weeks) until disease progression or intolerable toxicity for a maximum of 2 years.
TreatmentEXPERIMENTALTreatment with TAS102

Interventions

NameTypeDescription
Trifluridine/TipiracilDRUGTaken by mouth two times a day, 5 days on/2 days off, over 2 weeks, followed by a 14-day rest
BevacizumabDRUGadministered every 2 weeks (Day 1 and Day 15)
OxaliplatinDRUGOxaliplatin will be administered intravenously on day 1 of each treatment cycle (infusion duration: 2 hours), every 2 weeks. The first cycle will be administered at level -1 (70 mg/m²) and then increased to 85 mg/m² (if feasible) from the cycle 2 to 8 or until disease progression, whatever occurs first. In case of limiting-oxaliplatin neuropathy and in all cases after 8 cycles, oxaliplatin will be stopped and Trifluridine/Tipiracil will be continued alone until disease progression or intolerable toxicity.
FOLFOX regimenDRUGFolinic Acid 400 mg/m² (or 200 mg/m² if L-folinic acid) + oxaliplatin 85 mg/m² (infusion duration: 2 hours) followed by 5-FU bolus 400 mg/m² and then 5-FU 2400 mg/m² as a 46-hour continuous infusion. Treatment repeated every 14 days. In case of limiting-oxaliplatin neuropathy and in all cases after 8 cycles, oxaliplatin will be stopped and 5-FU (simplified LV5FU2 regimen) or capecitabine (1000 mg/m² BID during 2 weeks every 3 weeks) will be continued alone until disease progression or intolerable toxicity.
NivolumabDRUGNivolumab 240 mg (infusion duration 30 minutes, every 2 weeks) until disease progression or intolerable toxicity for a maximum of 2 years
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites99

Inclusion Criteria: 1. Has histologically confirmed unresectable adenocarcinoma of the colon or rectum (all other histological types are excluded). 2. RAS status must have been previously determined (mutant or wild-type) based on local assessment of tumor biopsy. 3. Has received a maximum of 2 prio...

Countries:United StatesAustriaBelgiumBrazilDenmarkFranceGermanyHungaryItalyPolandPuerto RicoRussiaSpainUkraineNetherlands
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Competitive Landscape -Colorectal Cancer 258 trials (matched to "Refractory Metastatic Colorectal Cancer")

Frequently asked questions about Trifluridine/Tipiracil

What is Trifluridine/Tipiracil used for?

Trifluridine/Tipiracil is an investigational oral small molecule being studied in oncology. It is being evaluated for refractory metastatic colorectal cancer, gastric adenocarcinoma, and ER-positive, HER2-negative advanced breast cancer. It is also studied in combination with other agents for gastroesophageal junction adenocarcinoma.

Who makes Trifluridine/Tipiracil?

Trifluridine/Tipiracil is being developed by Tango Therapeutics, Inc. (NASDAQ: TNGX). The company is conducting clinical trials of the drug across multiple cancer indications.

What phase is Trifluridine/Tipiracil in?

Trifluridine/Tipiracil is in Phase 2 and Phase 3 clinical trials. It is investigational and not yet approved by the FDA. The drug is being studied in breast cancer, refractory metastatic colorectal cancer, and gastric adenocarcinoma.

What clinical trials is Trifluridine/Tipiracil in?

Trifluridine/Tipiracil is being studied in several trials. NCT04489173 is a Phase 2 trial in ER-positive, HER2-negative advanced breast cancer. NCT04737187 is a completed Phase 3 trial in refractory metastatic colorectal cancer. NCT05476796 is a Phase 2 trial in gastric, esophageal, and gastroesophageal junction cancer.

Is Trifluridine/Tipiracil the same as TAS102?

Yes, Trifluridine/Tipiracil is also known as TAS102. The Phase 2 breast cancer trial NCT04489173 is titled 'TAS102 in Patients With ER-positive, HER2-negative Advanced Breast Cancer', confirming the alternative name.