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    DRUG CLASS:

    Thymidine phosphorylase inhibitor

    Related drugs:
    1d
    TAS-102 in ctDNA-defined Minimal Residual Disease in Colorectal Cancer After Completion of Adjuvant Chemotherapy (clinicaltrials.gov)
    P2, N=25, Recruiting, M.D. Anderson Cancer Center | N=15 --> 25 | Trial completion date: May 2024 --> May 2025 | Trial primary completion date: May 2024 --> May 2025
    Enrollment change • Trial completion date • Trial primary completion date • Minimal residual disease • Circulating tumor DNA
    |
    Signatera™
    |
    Lonsurf (trifluridine/tipiracil)
    1d
    TIBET: TAS102 in Patients With ER-positive, HER2-negative Advanced Breast Cancer (clinicaltrials.gov)
    P2, N=52, Active, not recruiting, Borstkanker Onderzoek Groep | Recruiting --> Active, not recruiting | Trial completion date: Jul 2024 --> Dec 2024 | Trial primary completion date: Sep 2023 --> Jan 2024
    Enrollment closed • Trial completion date • Trial primary completion date • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    ER positive • HER-2 negative • PGR positive
    |
    Lonsurf (trifluridine/tipiracil)
    6d
    TAS-102 in Patients With Advanced, Refractory Pancreatic Adenocarcinoma (clinicaltrials.gov)
    P2, N=28, Active, not recruiting, The University of Hong Kong | Recruiting --> Active, not recruiting | Trial completion date: Nov 2023 --> Dec 2024 | Trial primary completion date: May 2023 --> Mar 2024
    Enrollment closed • Trial completion date • Trial primary completion date • Metastases
    |
    Lonsurf (trifluridine/tipiracil)
    7d
    Irinotecan, TAS-102 Plus Bevacizumab as a Third-Line or Beyond Therapy in mCRC Patients (clinicaltrials.gov)
    P2, N=35, Active, not recruiting, Cancer Institute and Hospital, Chinese Academy of Medical Sciences
    New P2 trial • Combination therapy • Metastases
    |
    Avastin (bevacizumab) • irinotecan • Lonsurf (trifluridine/tipiracil)
    18d
    Predictive significance of FGFR4 p.G388R polymorphism in metastatic colorectal cancer patients receiving trifluridine/tipiracil (TAS-102) treatment. (PubMed, J Transl Med)
    This phenotype/genotype investigation suggests that the FGFR4 p.G388R variant may serve as a new marker for identifying patients who are responsive to TAS-102. A mechanistic hypothesis is proposed to interpret these findings.
    Journal • Metastases
    |
    FGFR4 (Fibroblast growth factor receptor 4)
    |
    FGFR4 G388R
    |
    5-fluorouracil • oxaliplatin • irinotecan • Lonsurf (trifluridine/tipiracil)
    22d
    Trifluridine/Tipiracil Combined With Cetuximab in the Treatment of Third-line and Above RAS/BRAF Wild-type mCRC (clinicaltrials.gov)
    P1/2, N=26, Recruiting, Wangxia LV
    New P1/2 trial • Metastases
    |
    BRAF (B-raf proto-oncogene)
    |
    Erbitux (cetuximab) • Lonsurf (trifluridine/tipiracil)
    1m
    Efficacy of Regorafenib and Trifluridine/Tipiracil According to Extended RAS Evaluation in Advanced Metastatic Colorectal Cancer Patients: A Multicenter Retrospective Analysis. (PubMed, Target Oncol)
    Our data demonstrate that RAS mutations do not affect outcome in rego-treated patients as well as TFD/TPI-treated patients. Nevertheless, a trend toward a higher efficacy of rego in RAS-mutated (in particular codon 12, rare RAS mutations, and G12D) patients has been recorded. The rego-TFD/TPI sequence seems to be superior to the reverse sequence in patients carrying an RAS codon 12 mutation, although the impact of other factors as disease burden or performance status cannot be excluded.
    Retrospective data • Journal • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    KRAS mutation • KRAS G12C • BRAF mutation • NRAS mutation • KRAS G12D • KRAS wild-type • RAS mutation • RAS wild-type • KRAS G12 • KRAS exon 2 mutation • NRAS G12D • NRAS G12
    |
    Stivarga (regorafenib) • Lonsurf (trifluridine/tipiracil)
    1m
    TAS 102 in Combination With Ramucirumab in Advanced, Refractory Gastric or Gastroesophageal Junction (GEJ) Adenocarcinoma (clinicaltrials.gov)
    P2, N=23, Active, not recruiting, H. Lee Moffitt Cancer Center and Research Institute | Trial completion date: Mar 2024 --> Jul 2024
    Trial completion date • Combination therapy • Metastases
    |
    Cyramza (ramucirumab) • Lonsurf (trifluridine/tipiracil)
    1m
    Trametinib and Trifluridine and Tipiracil Hydrochloride in Treating Patients With Colon or Rectal Cancer That is Advanced, Metastatic, or Cannot Be Removed by Surgery (clinicaltrials.gov)
    P1, N=26, Completed, City of Hope Medical Center | Active, not recruiting --> Completed | Trial completion date: Dec 2023 --> Jul 2023 | Trial primary completion date: Dec 2023 --> Jul 2023
    Trial completion • Trial completion date • Trial primary completion date • Combination therapy • Surgery • Metastases
    |
    BRAF (B-raf proto-oncogene) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
    |
    BRAF mutation • PIK3CA mutation • BRAF wild-type • RAS mutation • RAS wild-type • RAS wild-type + BRAF wild-type • PIK3CA mutation + PTEN mutation
    |
    Mekinist (trametinib) • Lonsurf (trifluridine/tipiracil)
    1m
    NOTABLE-308: Nimotuzumab Combined With Trifluridine/Tipiracil in the Treatment of Refractory Metastatic Colorectal Cancer (clinicaltrials.gov)
    P3, N=420, Not yet recruiting, Biotech Pharmaceutical Co., Ltd.
    New P3 trial
    |
    EGFR (Epidermal growth factor receptor)
    |
    Lonsurf (trifluridine/tipiracil) • TheraCIM (nimotuzumab)
    1m
    Study of Cabozantinib Plus TAS102 in mCRC as Salvage Therapy (clinicaltrials.gov)
    P1, N=12, Active, not recruiting, University of California, Irvine | Trial completion date: Jan 2024 --> Feb 2025 | Trial primary completion date: Dec 2023 --> Aug 2023
    Trial completion date • Trial primary completion date • Metastases
    |
    RAS wild-type
    |
    Cabometyx (cabozantinib tablet) • Cometriq (cabozantinib capsule) • Lonsurf (trifluridine/tipiracil)
    2ms
    TRITICC: Trifluridine/Tipiracil in Combination With Irinotecan as a Second Line Therapy in Patients With Cholangiocarcinoma (clinicaltrials.gov)
    P2, N=28, Completed, Heinrich-Heine University, Duesseldorf | Active, not recruiting --> Completed | Trial completion date: Nov 2024 --> Jan 2024 | Trial primary completion date: Oct 2024 --> Jan 2024
    Trial completion • Trial completion date • Trial primary completion date • Combination therapy
    |
    irinotecan • Lonsurf (trifluridine/tipiracil)
    2ms
    SHOrt Course Radiation and TASOX (TAS102 Plus Oxaliplatin) Chemotherapy in Operable Rectal Cancer (clinicaltrials.gov)
    P2, N=13, Completed, Providence Health & Services | Active, not recruiting --> Completed
    Trial completion
    |
    oxaliplatin • Lonsurf (trifluridine/tipiracil)
    2ms
    Efficacy of Chemotherapy Rechallenge Versus Regorafenib or Trifluridine/Tipiracil in Third-Line Setting of Metastatic Colorectal Cancer: A Multicenter Retrospective Comparative Study. (PubMed, JCO Glob Oncol)
    This study suggests that chemotherapy rechallenge may provide a survival benefit in the third-line treatment of mCRC. However, patient characteristics, such as sex and ECOG PS, should also be considered in treatment decisions. Further prospective studies are required to confirm our findings.
    Retrospective data • Journal • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS wild-type • RAS wild-type
    |
    Stivarga (regorafenib) • Lonsurf (trifluridine/tipiracil)
    2ms
    Impact of KRASG12 mutations on survival with trifluridine/tipiracil plus bevacizumab in patients with refractory metastatic colorectal cancer: post hoc analysis of the phase III SUNLIGHT trial. (PubMed, ESMO Open)
    The presence of a KRASG12 mutation had no detrimental effect on OS among patients treated in SUNLIGHT. The benefit of FTD/TPI plus bevacizumab over FTD/TPI alone was confirmed independently of KRASG12 status.
    P3 data • Retrospective data • Journal • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • RAS mutation • KRAS G12R • KRAS G12
    |
    Avastin (bevacizumab) • Lonsurf (trifluridine/tipiracil)
    2ms
    LONGBOARD: LONsurf and G-CSF Use: Being On A Right Dose-intensity to Optimize Treatment Efficacy (clinicaltrials.gov)
    P2, N=176, Active, not recruiting, GERCOR - Multidisciplinary Oncology Cooperative Group | Recruiting --> Active, not recruiting | Trial completion date: Jun 2024 --> Nov 2024
    Enrollment closed • Trial completion date
    |
    BRAF (B-raf proto-oncogene)
    |
    BRAF wild-type • RAS wild-type
    |
    Lonsurf (trifluridine/tipiracil)
    2ms
    Study of ctDNA Guided Change in Tx for Refractory Minimal Residual Disease in Colon Adenocarcinomas (clinicaltrials.gov)
    P1; Trial completion date: Jun 2024 --> Dec 2025 | Trial primary completion date: Dec 2023 --> Dec 2024
    Trial completion date • Trial primary completion date • Minimal residual disease • Circulating tumor DNA
    |
    Signatera™
    |
    capecitabine • irinotecan • Lonsurf (trifluridine/tipiracil)
    2ms
    TRITICC: Trifluridine/Tipiracil in Combination With Irinotecan as a Second Line Therapy in Patients With Cholangiocarcinoma (clinicaltrials.gov)
    P2, N=28, Active, not recruiting, Heinrich-Heine University, Duesseldorf | Trial completion date: Apr 2024 --> Nov 2024 | Trial primary completion date: Oct 2023 --> Oct 2024
    Trial completion date • Trial primary completion date • Combination therapy
    |
    irinotecan • Lonsurf (trifluridine/tipiracil)
    3ms
    A Phase II Study of FOLFIRI Plus Ziv-Aflibercept After Trifluridine/Tipiracil Plus Bevacizumab in Patients with Metastatic Colorectal Cancer: WJOG 11018G. (PubMed, Target Oncol)
    This study did not meet the primary endpoint. Hence, FOLFIRI plus AFL should not be used after FTD/TPI plus BEV for metastatic colorectal cancer. Further studies are needed to determine factors not targeted by AFL that may affect the efficacy of the treatment.
    P2 data • Journal • Metastases
    |
    SPP1 (Secreted Phosphoprotein 1) • PGF (Placental Growth Factor)
    |
    Avastin (bevacizumab) • 5-fluorouracil • oxaliplatin • irinotecan • Lonsurf (trifluridine/tipiracil) • leucovorin calcium
    3ms
    SOREGATT: Sequences Of REGorafenib And Trifluridine/Tipiracil in Patients With Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=340, Active, not recruiting, UNICANCER | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    EGFR (Epidermal growth factor receptor)
    |
    Stivarga (regorafenib) • Lonsurf (trifluridine/tipiracil)
    3ms
    Delphi consensus for the third-line treatment of metastatic colorectal cancer. (PubMed, Clin Transl Oncol)
    The experts agreed with most of the proposed items on 3L treatment of mCRC, prioritizing therapeutic options that increase survival and preserve QoL, while facilitating the possibility that patients can continue to be treated later.
    Journal • Metastases
    |
    BRAF (B-raf proto-oncogene) • MSI (Microsatellite instability)
    |
    BRAF V600E • MSI-H/dMMR • BRAF V600
    |
    5-fluorouracil • Stivarga (regorafenib) • Lonsurf (trifluridine/tipiracil)
    3ms
    TAS-102 and Anlotinib in ≥3 Lines mGC (clinicaltrials.gov)
    P2, N=45, Recruiting, Zhejiang University | Trial primary completion date: Dec 2023 --> Dec 2024
    Trial primary completion date • Metastases
    |
    Focus V (anlotinib) • Lonsurf (trifluridine/tipiracil)
    3ms
    FIERCE: TAS-102 With Concurrent Radiation for the Treatment of Untreated Resectable Stage II-III Rectal Cancer (clinicaltrials.gov)
    P1, N=18, Recruiting, OHSU Knight Cancer Institute | Phase classification: P1b --> P1
    Phase classification
    |
    Lonsurf (trifluridine/tipiracil)
    3ms
    BEV-TASIRI: Second-line Treatment of Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=50, Recruiting, Qilu Hospital of Shandong University
    New P2 trial • Combination therapy • Metastases
    |
    Avastin (bevacizumab) • irinotecan • Lonsurf (trifluridine/tipiracil)
    3ms
    TRIFLUOX-DP: Safety of Trifluridine/Tipiracil in Patients With Dihydropyrimidine Dehydrogenase Deficiency Diagnosed With Metastatic Colorectal or Gastroesophageal Cancer (clinicaltrials.gov)
    P2, N=73, Not yet recruiting, UNICANCER
    New P2 trial • Metastases
    |
    Opdivo (nivolumab) • Avastin (bevacizumab) • Herceptin (trastuzumab) • 5-fluorouracil • Vectibix (panitumumab) • capecitabine • oxaliplatin • Lonsurf (trifluridine/tipiracil)
    3ms
    TASKIN: Evaluation of Efficacy of Trifluridine/Tipiracil Plus an Anti-IL-1α True Human Antibody Versus Trifluridine/Tipiracil Plus Placebo in Metastatic Colorectal Cancer Patients After Failure of Oxaliplatin, Irinotecan, Fluoropyrimidine (clinicaltrials.gov)
    P1/2, N=160, Recruiting, Centre Georges Francois Leclerc | Not yet recruiting --> Recruiting | Trial completion date: Mar 2026 --> Oct 2026 | Trial primary completion date: Mar 2024 --> Oct 2026
    Enrollment open • Trial completion date • Trial primary completion date • Metastases
    |
    BRAF (B-raf proto-oncogene) • MSI (Microsatellite instability)
    |
    oxaliplatin • irinotecan • Lonsurf (trifluridine/tipiracil) • Natrunix (vilamakitug)
    3ms
    Chronological improvement of survival in patients with advanced gastric cancer over 15 years. (PubMed, Ther Adv Med Oncol)
    Clinical strategy changes, including gastrectomy, HER2 testing, and approval of new drugs, may be associated with improved OS in patients with AGC. In the last 4 years, a remarkable improvement has been observed in patients with LM.
    Journal • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    Opdivo (nivolumab) • Cyramza (ramucirumab) • Lonsurf (trifluridine/tipiracil)
    3ms
    TAS-102 and Irinotecan in 2L+ Gastric and Gastroesophageal Adenocarcinoma (clinicaltrials.gov)
    P1, N=20, Completed, University of California, Irvine | Active, not recruiting --> Completed
    Trial completion
    |
    irinotecan • Lonsurf (trifluridine/tipiracil)
    4ms
    SHOrt Course Radiation and TASOX (TAS102 Plus Oxaliplatin) Chemotherapy in Operable Rectal Cancer (clinicaltrials.gov)
    P2, N=13, Active, not recruiting, Providence Health & Services | Recruiting --> Active, not recruiting | N=27 --> 13 | Trial completion date: Apr 2025 --> Apr 2024 | Trial primary completion date: Oct 2024 --> Dec 2023
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date
    |
    oxaliplatin • Lonsurf (trifluridine/tipiracil)
    4ms
    Fruquintinib Combined With TAS-102 in Refractory Metastatic Colorectal Cancer (clinicaltrials.gov)
    P=N/A, N=20, Recruiting, Fudan University
    New trial • Metastases
    |
    Fruzaqla (fruquintinib) • Lonsurf (trifluridine/tipiracil)
    4ms
    TAS102 in Combination With NAL-IRI in Advanced GI Cancers (clinicaltrials.gov)
    P1/2, N=64, Recruiting, Emory University | Trial completion date: Nov 2024 --> Nov 2025 | Trial primary completion date: Nov 2023 --> Nov 2024
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    Lonsurf (trifluridine/tipiracil) • Onivyde (nanoliposomal irinotecan)
    4ms
    Irinotecan, TAS-102 Plus Bevacizumab as a Second-Line Therapy in mCRC Patients (clinicaltrials.gov)
    P1/2, N=70, Recruiting, Cancer Institute and Hospital, Chinese Academy of Medical Sciences
    New P1/2 trial • Combination therapy • Metastases
    |
    Avastin (bevacizumab) • irinotecan • Lonsurf (trifluridine/tipiracil)
    4ms
    A Retrospective Study of Trifluridine/Tipiracil with Fruquintinib in Patients with Chemorefractory Metastatic Colorectal Cancer. (PubMed, J Clin Med)
    Our results suggest that TAS-102 combined with fruquintinib has promising clinical efficacy and manageable safety for refractory mCRC patients in a real-world clinical setting. Further prospective trials are warranted to confirm our results.
    Retrospective data • Journal • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    Fruzaqla (fruquintinib) • Lonsurf (trifluridine/tipiracil)
    4ms
    Treatment Options in Late-Line Colorectal Cancer: Lessons Learned from Recent Randomized Studies. (PubMed, Cancers (Basel))
    First- and second-line combinations of 5FU, oxaliplatin, and irinotecan, with or without anti-angiogenic and/or anti-EGFR antibodies, were approved shortly after the turn of the millennium. Further triumphs were not seen for almost 10 years, until the approval of initially regorafenib and shortly after trifluridine/tipiracil...Here, we review the most recent clinical data for late-line treatment options in mCRC, focusing on randomized trials if available. We include recommendations for options in unselected patients and therapies that should only be offered in patients with distinct tumor profiles (e.g., BRAF mutations, KRAS G12C mutations, HER2 amplification, deficient MMR, or NTRK gene fusions).
    Review • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    KRAS mutation • KRAS G12C • BRAF mutation • HER-2 amplification • KRAS G12 • NTRK fusion
    |
    5-fluorouracil • Stivarga (regorafenib) • oxaliplatin • irinotecan • Lonsurf (trifluridine/tipiracil)
    4ms
    Exploratory Biomarker Analysis Using Plasma Angiogenesis-Related Factors and Cell-Free DNA in the TRUSTY Study: A Randomized, Phase II/III Study of Trifluridine/Tipiracil Plus Bevacizumab as Second-Line Treatment for Metastatic Colorectal Cancer. (PubMed, Target Oncol)
    Low baseline plasma concentrations of HGF and IL-8 may predict better DCR and PFS in patients with mCRC receiving FTD/TPI plus bevacizumab, however further studies are warranted.
    P2/3 data • Journal • Metastases
    |
    IL6 (Interleukin 6) • HGF (Hepatocyte growth factor) • CXCL8 (Chemokine (C-X-C motif) ligand 8) • SPP1 (Secreted Phosphoprotein 1) • THBS2 (Thrombospondin 2)
    |
    HGF-L • IL6-L • CXCL8-L • SPP1-L
    |
    Avastin (bevacizumab) • Lonsurf (trifluridine/tipiracil)
    4ms
    A Real-world Study of Trifluridine/Tipiracil Containing Regimen for the Treatment of Patients With mCRC (REFLECT Study) (clinicaltrials.gov)
    P=N/A, N=200, Not yet recruiting, Second Affiliated Hospital, School of Medicine, Zhejiang University
    New trial • Real-world evidence • Real-world • Metastases
    |
    Lonsurf (trifluridine/tipiracil)
    4ms
    Study of Lonsurf in Combination With Gemcitabine and Nab-Paclitaxel in Patients With Advanced (PDAC) (clinicaltrials.gov)
    P1, N=14, Terminated, Patrick Joseph Loehrer Sr. | Trial completion date: Oct 2024 --> Oct 2023 | Active, not recruiting --> Terminated; Unable to proceed due to Neulasta difficulties and other complications.
    Trial completion date • Trial termination • Combination therapy • Metastases
    |
    gemcitabine • albumin-bound paclitaxel • Lonsurf (trifluridine/tipiracil)
    5ms
    Surufatinib Combined With TAS-102 in Third-line and Later-line Therapy of Patients With Advanced Pancreatic Cancer (clinicaltrials.gov)
    P2, N=20, Recruiting, Sun Yat-sen University
    Trial completion date • Trial primary completion date • Metastases
    |
    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
    |
    Lonsurf (trifluridine/tipiracil) • Sulanda (surufatinib)
    5ms
    ERASE-CRC: Exploiting Circulating Tumour DNA to Intensify the Postoperative Treatment Resected Colon Cancer Patients (clinicaltrials.gov)
    P2, N=477, Recruiting, Gruppo Oncologico del Nord-Ovest | N=300 --> 477
    Enrollment change • Circulating tumor DNA
    |
    Herceptin (trastuzumab) • 5-fluorouracil • capecitabine • oxaliplatin • irinotecan • Tukysa (tucatinib) • Lonsurf (trifluridine/tipiracil) • leucovorin calcium
    5ms
    SUNLIGHT: Phase III Study of Trifluridine/Tipiracil With and Without Bevacizumab in Refractory Metastatic Colorectal Cancer Patients (clinicaltrials.gov)
    P3, N=492, Completed, Taiho Oncology, Inc. | Active, not recruiting --> Completed
    Trial completion • Combination therapy • Metastases
    |
    Avastin (bevacizumab) • Lonsurf (trifluridine/tipiracil)
    5ms
    Live-RF: Amplitude Modulated Radiofrequency Electromagnetic Field Treatment Combined With TAS-102 (Lonsurf) and Bevacizumab in Refractory Metastatic Colorectal Cancer (clinicaltrials.gov)
    P=N/A, N=12, Recruiting, Charite University, Berlin, Germany | Trial completion date: May 2026 --> Nov 2026 | Initiation date: Jul 2023 --> Dec 2023 | Trial primary completion date: May 2026 --> Nov 2026
    Trial completion date • Trial initiation date • Trial primary completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene)
    |
    BRAF mutation • KRAS wild-type • RAS wild-type
    |
    Avastin (bevacizumab) • Lonsurf (trifluridine/tipiracil)
    5ms
    TACT-D: Circulating Cell-Free Tumor DNA Testing in Guiding Treatment for Patients With Advanced or Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=100, Active, not recruiting, M.D. Anderson Cancer Center | Recruiting --> Active, not recruiting
    Enrollment closed • Circulating tumor DNA • Metastases
    |
    RAS (Rat Sarcoma Virus)
    |
    RAS wild-type
    |
    Stivarga (regorafenib) • Lonsurf (trifluridine/tipiracil)