Search results for "Trifluridine"

showing 10 items of 11 documents

Trifluridine/tipiracil : an emerging strategy for the management of gastrointestinal cancers

2018

Fluoropyrimidines are currently the backbone of treatment for gastrointestinal (GI) cancers but development of resistance to these agents remains a major problem. Trifluridine/tipiracil is an oral chemotherapeutic agent recently approved for third-line treatment of chemorefractory metastatic colorectal cancer. This article reviews the clinical value of trifluridine/tipiracil as a monotherapy, including recent trials in GI cancers, and the potential benefit of combining it with other agents in patients with GI cancers, including the preclinical rationale for combination therapy and recently completed and ongoing clinical trials. Data gathered so far suggest that trifluridine/tipiracil has t…

0301 basic medicineOncologyCancer Researchmedicine.medical_specialtyIndolesPyrrolidinesOrganoplatinum CompoundsCombination therapyColorectal cancerTrifluridineDocetaxelIrinotecanTrifluridine03 medical and health scienceschemistry.chemical_compound0302 clinical medicineInternal medicineAntineoplastic Combined Chemotherapy ProtocolsmedicineHumansGastrointestinal cancerContinuum of careUracilGastrointestinal NeoplasmsTipiracilClinical Trials as Topicbusiness.industryGeneral Medicinemedicine.diseaseBevacizumabOxaliplatinClinical trialDrug Combinations030104 developmental biologyOncologychemistry030220 oncology & carcinogenesisColonic NeoplasmsQuality of LifeClinical valueCamptothecinTaxoidsFluorouracilImmunotherapyHuman medicinebusinessThyminemedicine.drugFuture oncology
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A phase I dose-escalation of trifluridine/tipiracil in combination with oxaliplatin in metastatic colorectal cancer.

2017

TPS3626 Background: Trifluridine/tipiracil, also known as TAS‐102, is a combination of an antineoplastic thymidine‐based nucleoside analogue (trifluridine) and a thymidine phosphorylase inhibitor (tipiracil hydrochloride). The antitumor activity of combined trifluridine/tipiracil and oxaliplatin has been studied in gastrointestinal tumor xenografts, including a 5‐FU resistant subline, using a nude mouse model. This study demonstrated increased antitumor activity for the combination compared to trifluridine/tipiracil or oxaliplatin alone (p < 0.001) (Nukatsuka et al., Anticancer Res 2015). These data support the rationale for clinical use of the combination. We describe a phase 1, intern…

0301 basic medicineOncologyCancer Researchmedicine.medical_specialtyNucleoside analogueColorectal cancerbusiness.industryTrifluridinemedicine.diseaseOxaliplatin03 medical and health scienceschemistry.chemical_compound030104 developmental biology0302 clinical medicineOncologychemistry030220 oncology & carcinogenesisInternal medicinemedicineDose escalationThymidine phosphorylasebusinessThymidinemedicine.drugTipiracilJournal of Clinical Oncology
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Phase I multicenter, open-label study to establish the maximum tolerated dose (MTD) of trifluridine/tipiracil (TAS-102) and oxaliplatin combination i…

2018

816 Background: Preclinical evidence suggests improved efficacy when combining trifluridine/tipiracil with oxaliplatin compared to each monotherapy (Nukatsuka, 2015). The primary objective was to determine the MTD and the safety profile of the doublet among mCRC pts who have progressed after at least one prior line of treatment. Methods: Using a 3+3 design, eligible pts received escalating trifluridine/tipiracil doses from 25, 30 to 35 mg/m² bid, days 1–5 q14, together with a fixed dose of oxaliplatin 85 mg/m² (day 1). An intermediate cohort with a lower dose of oxaliplatin (65 mg/m²) plus 35 mg/m² of trifluridine/tipiracil was also tested. Results: Fifteen of 17 enrolled pts were evaluabl…

0301 basic medicineOncologyCancer Researchmedicine.medical_specialtybusiness.industryColorectal cancerTrifluridinemedicine.diseaseOxaliplatinstomatognathic diseases03 medical and health scienceschemistry.chemical_compound030104 developmental biology0302 clinical medicineOncologyOpen label studychemistry030220 oncology & carcinogenesisMaximum tolerated doseInternal medicinemedicineIn patientbusinessmedicine.drugTipiracilJournal of Clinical Oncology
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Phase I dose-escalation of trifluridine/tipiracil in combination with oxaliplatin in patients with metastatic colorectal cancer

2019

Abstract Background and objectives Pre-clinical data have shown that combining trifluridine/tipiracil with oxaliplatin enhances anti-tumour activity compared with either monotherapy. A phase I dose-escalation study was conducted to determine the maximum tolerated dose (MTD), recommended dose (RD) for phase II and pharmacokinetic profile of this combination in patients with metastatic colorectal cancer (mCRC) who had progressed after at least 1 prior line of treatment. Methods Using a 3 + 3 design, patients received escalating trifluridine/tipiracil doses from 25, then 30 and to 35 mg/m2 twice daily, days 1–5, q14 days, together with a fixed dose of 85 mg/m2 of oxaliplatin day 1, q14 days. A…

AdultMale0301 basic medicineCancer Researchmedicine.medical_specialtyPyrrolidinesMaximum Tolerated DoseNauseaTrifluridineNeutropeniaGastroenterologyTrifluridine03 medical and health scienceschemistry.chemical_compound0302 clinical medicineInternal medicineAntineoplastic Combined Chemotherapy ProtocolsHumansMedicineUracilAdverse effectneoplasmsAgedTipiracilbusiness.industryMiddle Agedmedicine.diseaseOxaliplatinOxaliplatinDrug Combinations030104 developmental biologyOncologychemistry030220 oncology & carcinogenesisVomitingFemalemedicine.symptomColorectal NeoplasmsbusinessThymineFebrile neutropeniamedicine.drugEuropean Journal of Cancer
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A Phase I dose-escalation study of third-line regorafenib with trifluridine/tipiracil in metastatic colorectal cancer

2021

Aim: To determine a recommended Phase II dose of the oral fluoropyrimidine trifluridine/tipiracil (FTD/TPI) combined with the multi-kinase inhibitor regorafenib (REG) in refractory metastatic colorectal cancer patients. Materials & methods: A conventional 3 + 3 dose finding design was used. FTD/TPI was administered on days 1–5 and 8–12 of a 28-day cycle, REG on days 2–22. Two dose levels were used: FTD/TPI 25 mg/m2 b.i.d. + REG 120 mg/d, then escalated to FTD/TPI 35 mg/m2 b.i.d. + REG 120 mg/d. Results: In total, 12 patients were treated at two dose levels. Three dose-limiting toxicities were observed; all were grade 3 hypertension causally attributed to REG. Recommended Phase II dose …

AdultMale0301 basic medicineOncologyCancer Researchmedicine.medical_specialtyPyrrolidinesMaximum Tolerated DosePyridinesColorectal cancerAdministration OralTrifluridineDrug Administration ScheduleTrifluridine03 medical and health scienceschemistry.chemical_compound0302 clinical medicineRefractoryRegorafenibInternal medicineAntineoplastic Combined Chemotherapy ProtocolsmedicineDose escalationHumansResponse Evaluation Criteria in Solid TumorsAgedTipiracilDose-Response Relationship Drugbusiness.industryPhenylurea CompoundsGeneral MedicineMiddle Agedmedicine.diseaseProgression-Free SurvivalDrug Combinations030104 developmental biologyOncologychemistryThird lineDrug Resistance Neoplasm030220 oncology & carcinogenesisHypertensionToxicityFeasibility StudiesFemaleColorectal NeoplasmsbusinessThyminemedicine.drugFuture Oncology
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Efficacy of trifluridine and tipiracil (TAS-102) versus placebo, with supportive care, in a randomized, controlled trial of patients with metastatic …

2016

[Purpose] TAS-102 is a combination of the thymidine-based nucleoside analog trifluridine and the thymidine phosphorylase inhibitor tipiracil. Efficacy and safety of TAS-102 in patients with metastatic colorectal cancer (mCRC) refractory or intolerant to standard therapies were evaluated in the phase 3 RECOURSE trial. Results of RECOURSE demonstrated significant improvement in overall survival (OS) and progression-free survival (PFS) with TAS-102 versus placebo [hazard ratio (HR) = 0.68 and 0.48 for OS and PFS, respectively; both P < 0.001]. The current analysis evaluates efficacy and safety of TAS-102 in the RECOURSE Spanish subgroup.

Male0301 basic medicineOncologyCancer ResearchPyrrolidinesColorectal cancerTrifluridineHelsinki declarationlaw.inventionTrifluridinechemistry.chemical_compound0302 clinical medicineRandomized controlled triallawMedicineAged 80 and overMetastatic colorectal cancerPalliative CareHazard ratioGeneral MedicineMiddle AgedPrognosisTAS-102Survival RateDrug CombinationsOncology030220 oncology & carcinogenesisDrug Therapy CombinationFemaleColorectal NeoplasmsFluoropyrimidineResearch Articlemedicine.drugAdultmedicine.medical_specialtyanimal structuresSubgroup analysisPlaceboAntiviral Agents03 medical and health sciencesDouble-Blind MethodInternal medicineHumansTipiracil hydrochlorideUracilAgedNeoplasm StagingTipiracilbusiness.industrymedicine.diseaseSurgery030104 developmental biologychemistrySpainbusinessThymineFollow-Up StudiesClinical and Translational Oncology
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Trifluridine/tipiracil in earlier lines of chemotherapy for advanced colorectal cancer

2020

Oncologymedicine.medical_specialtyChemotherapyPyrrolidinesbusiness.industrymedicine.medical_treatmentMEDLINEHematologyTrifluridineBevacizumabAdvanced colorectal cancerDrug CombinationsOncologyInternal medicinemedicineHumansColorectal NeoplasmsbusinessThymineAnnals of Oncology
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Prognostic Value of Sarcopenia in Metastatic Colorectal Cancer Patients Treated with Trifluridine/Tipiracil

2021

Sarcopenia is common in metastatic colorectal cancer (mCRC), increases the risk of treatment-related toxicity and reduces survival. Trifluridine/tipiracil (TT) chemotherapy significantly improved survival in refractory mCRC patients, but the prognostic and predictive role of pretherapeutic sarcopenia and variation in the skeletal muscle index (SMI) during this treatment has not been investigated so far. In this retrospective, observational study, clinical data on mCRC patients treated with TT at six cancer centres in Poland were collected. Computed tomography (CT) scans acquired at the time of initiation of TT (CT1) and on the first restaging (CT2), were evaluated. SMI was assessed based on…

Oncologymedicine.medical_specialtyColorectal cancermedicine.medical_treatmentTrifluridineArticletrifluridine/tipiracilsarcopeniachemistry.chemical_compoundCarcinoembryonic antigenInternal medicineMedicineTipiracilChemotherapyPerformance statusbiologybusiness.industrymetastatic colorectal cancerRCancerGeneral Medicinemedicine.diseasechemistrySarcopeniabiology.proteinMedicinebusinessmedicine.drugcancer cachexiaJournal of Clinical Medicine
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TAS-102 in metastatic colorectal cancer (mCRC): efficacy, tolerability, and quality of life in heavily pretreated elderly patients: a real-life study

2020

Background: TAS-102 is an oral monotherapy, combining trifluridine and tipiracil hydrochloride, indicated for the treatment of pretreated metastatic colorectal cancer (mCRC). The aim of this real-life study is to evaluate the efficacy and safety of TAS-102 in heavily pretreated elderly patients with mCRC whose disease has progressed with standard therapies. Methods: In this retrospective observational study, we enrolled 50 elderly patients &gt;70 years of age (median age 78 years) with a diagnosis of mCRC who were previously treated or were not considered candidates for treatment with other available therapies. Patients aged &gt;70 years with advanced colorectal cancer and with an ECOG perf…

Oncologymedicine.medical_specialtyColorectal cancermedicine.medical_treatmentTrifluridineECOG Performance StatusDiseasechemotherapyelderly patientstrifluridine/tipiracilQuality of lifeInternal medicinemedicinelonsurfOriginal ResearchPharmacologyChemotherapybusiness.industrymetastatic colorectal cancertrifluridine/ tipiracillcsh:RM1-950Retrospective cohort studyGeneral Medicinemedicine.diseaselcsh:Therapeutics. PharmacologyTolerabilityquality of lifetas-102Molecular Medicinebusinessmedicine.drugDrugs in Context
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Retrospective Study of Regorafenib Versus TAS-102 Efficacy and Safety in Chemorefractory Metastatic Colorectal Cancer (mCRC) Patients: A Multi-instit…

2021

INTRODUCTION: There have been significant developments in colorectal cancer (CRC) research over the last few years, with the introduction of new agents that have been prolonged median overall survival of metastatic colorectal cancer (mCRC). These therapies have improved patient outcomes; however, despite significant progress in strategies for cancer treatment, their use is limited by development of resistant mechanism. Almost 30% of patients with refractory mCRC will remain good candidates for further treatment. Regorafenib and TAS-102 are novel antitumor agents for patients with refractory mCRC. However, it is unclear which patients may derive a survival benefit from these drugs in real-li…

Oncologymedicine.medical_specialtyPyrrolidinesReal Life Clinical dataPyridinesColorectal cancerTrifluridinechemistry.chemical_compoundRefractoryInternal medicineRegorafenibmedicineHumansUracilRetrospective Studiesbusiness.industryPhenylurea CompoundsGastroenterologyRetrospective cohort studymedicine.diseaseTAS-102Disease controlCancer treatmentClinical trialDrug CombinationsOncologychemistrymCRCCohortchemorefractoryregorafenibColorectal NeoplasmsbusinessThymine
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