Last reviewed 2026-04-23 · How we verify

Trifluridine/tipiracil + bevacizumab

Trifluridine/tipiracil is a thymidine kinase 1 inhibitor and tipiracil is a thymidine phosphorylase inhibitor, which work together to inhibit DNA synthesis in cancer cells. Bevacizumab is a monoclonal antibody that targets vascular endothelial growth factor A (VEGF-A), inhibiting angiogenesis.

Trifluridine/tipiracil is a thymidine kinase 1 inhibitor and tipiracil is a thymidine phosphorylase inhibitor, which work together to inhibit DNA synthesis in cancer cells. Bevacizumab is a monoclonal antibody that targets vascular endothelial growth factor A (VEGF-A), inhibiting angiogenesis. Used for Metastatic colorectal cancer.

At a glance

Mechanism of action

Trifluridine/tipiracil is a combination of two drugs that target different steps in the DNA synthesis pathway. Trifluridine is a thymidine analog that is activated by thymidine phosphorylase, which is inhibited by tipiracil. This combination leads to a synergistic effect in inhibiting DNA synthesis in cancer cells. Bevacizumab, on the other hand, targets VEGF-A, a protein that promotes angiogenesis, which is the formation of new blood vessels that supply nutrients to growing tumors.

Approved indications

• Metastatic colorectal cancer

Common side effects

• Fatigue
• Diarrhea
• Nausea
• Vomiting
• Headache
• Rash

Key clinical trials

• 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)
• Sequential TAS-OX Alternating With TAS-IRI Plus Bevacizumab for Late-Line 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)
• A Real-World Study to Learn More About the Order of Different Treatments and Their Effects in People With Metastatic Colorectal Cancer Receiving Their Third and Fourth Line of Treatment
• A Study of ASP1570 Taken by Itself, or ASP1570 Taken Together With Either Pembrolizumab, Standard Therapies, or Both, in Adults With Solid Tumors (PHASE1, PHASE2)
• ASCEND-CRC: Profiling and Targeting Dynamic Tumor Resistance in Patients With Metastatic Colorectal Cancer (EARLY_PHASE1)
• FOG-001 in Locally Advanced or Metastatic Solid Tumors (PHASE1, PHASE2)

Primary sources

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