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Trifluridine/Tipiracil + Regorafenib
Trifluridine/Tipiracil + Regorafenib is a Nucleoside analog + multikinase inhibitor combination Small molecule drug developed by Second Affiliated Hospital, School of Medicine, Zhejiang University. It is currently in Phase 3 development for Metastatic colorectal cancer (Phase 3 trial).
This combination pairs a nucleoside analog that inhibits thymidylate synthase with a multikinase inhibitor targeting angiogenesis and tumor growth pathways.
This combination pairs a nucleoside analog that inhibits thymidylate synthase with a multikinase inhibitor targeting angiogenesis and tumor growth pathways. Used for Metastatic colorectal cancer (Phase 3 trial).
At a glance
| Generic name | Trifluridine/Tipiracil + Regorafenib |
|---|---|
| Sponsor | Second Affiliated Hospital, School of Medicine, Zhejiang University |
| Drug class | Nucleoside analog + multikinase inhibitor combination |
| Target | Thymidylate synthase (trifluridine/tipiracil); VEGFR, FGFR, KIT, RET, BRAF (regorafenib) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
Trifluridine/tipiracil (TAS-102) is a nucleoside analog that incorporates into DNA and inhibits thymidylate synthase, disrupting DNA synthesis in cancer cells. Regorafenib is a multikinase inhibitor that blocks VEGFR, FGFR, and other kinases involved in angiogenesis and tumor cell proliferation. The combination leverages complementary mechanisms: direct cytotoxicity plus anti-angiogenic and anti-proliferative effects.
Approved indications
- Metastatic colorectal cancer (Phase 3 trial)
Common side effects
- Neutropenia
- Anemia
- Thrombocytopenia
- Diarrhea
- Fatigue
- Hand-foot skin reaction
- Hypertension
Key clinical trials
- 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)
- 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
- Sotorasib and Panitumumab Versus Investigator's Choice for Participants With Kirsten Rat Sarcoma (KRAS) p.G12C Mutation (PHASE3)
- Study of Lenvatinib (MK-7902/E7080) in Combination With Pembrolizumab (MK-3475) Versus Standard of Care in Participants With Metastatic Colorectal Cancer (MK-7902-017/E7080-G000-325/LEAP-017) (PHASE3)
- Phase Ib/II Study of QL1706 + Fruquintinib + SCRT vs. Standard Third-Line Therapy in Unresectable Liver-Metastatic pMMR/MSS Colorectal Cancer: Safety, Tolerability, and Efficacy. (PHASE2)
- Circulating Cell-Free Tumor DNA Testing in Guiding Treatment for Patients With Advanced or Metastatic Colorectal Cancer (PHASE2)
- A Study of Coformulated Favezelimab/Pembrolizumab (MK-4280A) Versus Standard of Care in Subjects With Previously Treated Metastatic PD-L1 Positive Colorectal Cancer (MK-4280A-007)-China Extension Study (PHASE3)
- An Observational Study Called STAR-T to Learn More About the Sequential Treatment With Regorafenib and TAS-102 in Adults With Metastatic Colorectal Cancer Under Real World Conditions
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 + Regorafenib CI brief — competitive landscape report
- Trifluridine/Tipiracil + Regorafenib updates RSS · CI watch RSS
- Second Affiliated Hospital, School of Medicine, Zhejiang University portfolio CI
Frequently asked questions about Trifluridine/Tipiracil + Regorafenib
What is Trifluridine/Tipiracil + Regorafenib?
How does Trifluridine/Tipiracil + Regorafenib work?
What is Trifluridine/Tipiracil + Regorafenib used for?
Who makes Trifluridine/Tipiracil + Regorafenib?
What drug class is Trifluridine/Tipiracil + Regorafenib in?
What development phase is Trifluridine/Tipiracil + Regorafenib in?
What are the side effects of Trifluridine/Tipiracil + Regorafenib?
What does Trifluridine/Tipiracil + Regorafenib target?
Related
- Drug class: All Nucleoside analog + multikinase inhibitor combination drugs
- Target: All drugs targeting Thymidylate synthase (trifluridine/tipiracil); VEGFR, FGFR, KIT, RET, BRAF (regorafenib)
- Manufacturer: Second Affiliated Hospital, School of Medicine, Zhejiang University — full pipeline
- Therapeutic area: All drugs in Oncology
- Indication: Drugs for Metastatic colorectal cancer (Phase 3 trial)
- Compare: Trifluridine/Tipiracil + Regorafenib vs similar drugs
- Pricing: Trifluridine/Tipiracil + Regorafenib cost, discount & access