Last reviewed · How we verify
Trifluridine and Tipiracil
Trifluridine is a nucleoside analog that inhibits thymidylate synthase and gets incorporated into DNA to damage cancer cells, while tipiracil is a thymidine phosphorylase inhibitor that enhances trifluridine bioavailability.
Trifluridine is a nucleoside analog that inhibits thymidylate synthase and gets incorporated into DNA to damage cancer cells, while tipiracil is a thymidine phosphorylase inhibitor that enhances trifluridine bioavailability. Used for Metastatic colorectal cancer (previously treated), Metastatic gastric cancer (previously treated).
At a glance
| Generic name | Trifluridine and Tipiracil |
|---|---|
| Also known as | Lonsurf |
| Sponsor | Amgen |
| Drug class | Antimetabolite combination; thymidylate synthase inhibitor |
| Target | Thymidylate synthase; thymidine phosphorylase |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
Mechanism of action
Trifluridine acts as a thymidylate synthase inhibitor and antimetabolite that incorporates into DNA, causing strand breaks and cell death in rapidly dividing cancer cells. Tipiracil inhibits thymidine phosphorylase, which normally degrades trifluridine, thereby increasing systemic exposure and efficacy of the active drug. This combination allows lower doses of trifluridine to achieve therapeutic effect while reducing toxicity.
Approved indications
- Metastatic colorectal cancer (previously treated)
- Metastatic gastric cancer (previously treated)
Common side effects
- Neutropenia
- Anemia
- Thrombocytopenia
- Nausea
- Fatigue
- Diarrhea
- 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 and Tipiracil CI brief — competitive landscape report
- Trifluridine and Tipiracil updates RSS · CI watch RSS
- Amgen portfolio CI