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Trifluridine and Tipiracil

Phase 1

Advanced Malignant Solid Neoplasm | Small molecule | Oncology |Pfizer, Inc.|Last Updated: May 4, 2026

Target and mechanism

ModalitySmall molecule

Also known as Trifluridine and Tipiracil Hydrochloride

Success Probability

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Market & Valuation

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Trial Design

UNCONTROLLEDDMCBiomarker
Total Trials1
Total Enrollment45

FDA Designations

No designations recorded

Clinical trial landscape

Trifluridine and Tipiracil · 1 trial · 29 indications

Phase 1 1
NCT04511039Trifluridine/Tipiracil and Talazoparib for the Treatment of Patients With Locally Advanced or Metastatic Colorectal or Gastroesophageal CancerAdvanced Malignant Solid Neoplasm
RECRUITING45 Analytics
PHASE1RECRUITING
Trifluridine/Tipiracil and Talazoparib for the Treatment of Patients With Locally Advanced or Metastatic Colorectal or Gastroesophageal Cancer
Advanced Malignant Solid NeoplasmUnlock trial analytics

Study Endpoints

Primary Endpoints

Incidence of Adverse Events
after each cycle of treatment ( 1 cycle = 14 days)

All adverse events will be evaluated using Common Terminology Criteria for All Adverse Events (CTCAE) version (v.) 5.

Maximum tolerated dose/ recommended phase II dose
Up to 14 days

Will utilize the keyboard design - a novel model- assisted dose-finding method to find the maximum tolerated dose

Secondary Endpoints

Plasma Concentration (Cmax)
Day -13 post dose
Overall Response Rate (ORR)
Up to 3 years
CEA response rate (colorectal cancer patients)
Up to 3 years
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Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelSINGLE_GROUP
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Treatment ArmEXPERIMENTALPatients receive trifluridine/tipiracil PO BID and talazoparib tosylate PO QD on days 1-5. Cycles repeat every 14 days in the absence of disease progression or unacceptable toxicity.

Interventions

NameTypeDescription
Trifluridine and Tipiracil HydrochlorideDRUGGiven PO
Talazoparib TosylateDRUGGiven PO
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites1

Inclusion Criteria: * Histologically or cytologically confirmed CRC or EGC adenocarcinoma that is locally advanced or metastatic (Cohort A); histologically or cytologically confirmed p53mt/RASonc (Cohort B1) or p53mt/RASwt CRC (Cohort B2) that is locally advanced or metastatic. Patients with adenoc...

Countries:United States
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Frequently asked questions about Trifluridine and Tipiracil

What is Trifluridine and Tipiracil used for?

Trifluridine and Tipiracil is an investigational small molecule being studied for the treatment of advanced malignant solid neoplasms, including locally advanced or metastatic colorectal cancer and gastroesophageal junction adenocarcinoma. It is currently in Phase 1 clinical development for these indications.

What does Trifluridine and Tipiracil target?

Trifluridine and Tipiracil is a small molecule combination therapy. Trifluridine is a thymidine-based nucleoside analog that incorporates into DNA, disrupting DNA synthesis, while tipiracil inhibits thymidine phosphorylase, preventing the breakdown of trifluridine. This combination is being studied for its antitumor activity.

Who makes Trifluridine and Tipiracil?

Trifluridine and Tipiracil is being developed by Pfizer, Inc., a biopharmaceutical company traded on the New York Stock Exchange under the ticker symbol PFE.

What phase is Trifluridine and Tipiracil in?

Trifluridine and Tipiracil is currently in Phase 1 clinical development. It is an investigational drug and has not yet been approved by regulatory authorities for the treatment of advanced malignant solid neoplasms.

What clinical trials is Trifluridine and Tipiracil in?

Trifluridine and Tipiracil is being studied in a Phase 1 clinical trial with the identifier NCT04511039. This trial is evaluating the combination of trifluridine/tipiracil and talazoparib in patients with locally advanced or metastatic colorectal or gastroesophageal cancer. The trial is currently recruiting participants in the United States.

Is Trifluridine and Tipiracil the same as Trifluridine and Tipiracil Hydrochloride?

Yes, Trifluridine and Tipiracil is also known as Trifluridine and Tipiracil Hydrochloride. Both names refer to the same investigational drug combination being developed by Pfizer, Inc.