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Trifluridine-tipiracil
Trifluridine-tipiracil is a thymidine kinase 1 inhibitor that also has a thymidylate synthase inhibitor component, which works by interfering with DNA synthesis in cancer cells.
Trifluridine-tipiracil is a thymidine kinase 1 inhibitor that also has a thymidylate synthase inhibitor component, which works by interfering with DNA synthesis in cancer cells. Used for Metastatic colorectal cancer.
At a glance
| Generic name | Trifluridine-tipiracil |
|---|---|
| Sponsor | The Methodist Hospital Research Institute |
| Drug class | Nucleoside analog |
| Target | Thymidine kinase 1 |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
Trifluridine-tipiracil is a combination of trifluridine and tipiracil. Trifluridine is a thymidine analog that inhibits thymidine kinase 1, which is necessary for DNA synthesis. Tipiracil is a thymidylate synthase inhibitor that helps to increase the levels of trifluridine in the body. This combination works synergistically to inhibit DNA synthesis in cancer cells, ultimately leading to cell death.
Approved indications
- Metastatic colorectal cancer
Common side effects
- Diarrhea
- Fatigue
- Nausea
- Vomiting
- Abdominal pain
Key clinical trials
- Bioequivalence Study of Trifluridine and Tipiracil Hydrochloride Tablets on Fasting and Fed in Humans (NA)
- Fruquintinib Plus Checkpoint Inhibitor Combined or Sequential TAS-102 in Colorectal Cancer Patients Who Progressed on Second-line Standard Therapy: a Prospective, Multi-cohort, Single-centered, Phase Ib/II Study (PHASE1, PHASE2)
- Phase 2, Single-arm Trial of BMS-986340 in Association With Nivolumab, Trifluridine/Tipiracil and Bevacizumab for Patients Refractory to Standard of Care Treatment and With Microsatellite-stable Colorectal Cancer (PHASE2)
- A Clinical Study to Evaluate Injection TQB2102 for the Treatment of Patients With HER2 IHC3+ Advanced Colorectal Cancer Who Progressed After Treatment With Oxaliplatin, Irinotecan and Fluoropyrimidine-Based Drugs (PHASE3)
- Sequential TAS-OX Alternating With TAS-IRI Plus Bevacizumab for Late-Line Metastatic Colorectal Cancer (PHASE2)
- A Randomized Phase 2 Trial of Fruquintinib and TAS-102 as Compared to Fruquintinib in Patients With Refractory Advanced/Metastatic Colorectal Cancer (PHASE2)
- Evaluation of the Safety and Efficacy of Treatment w/High Dose Melphalan Given Directly Into the Liver Followed by Treatment w/Approved Cancer Treatment or Approved Cancer Treatment Alone in Patients w/ Metastatic Colorectal Cancer w/Liver Dominant Disease (PHASE2)
- Study of TAS-102 Plus Radiation Therapy for the Treatment of the Liver in Patients With Hepatic Metastases From Colorectal Cancer (PHASE1, PHASE2)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Trifluridine-tipiracil CI brief — competitive landscape report
- Trifluridine-tipiracil updates RSS · CI watch RSS
- The Methodist Hospital Research Institute portfolio CI