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Lonsurf (TIPIRACIL)
Lonsurf works by inhibiting the enzyme thymidine phosphorylase, which is involved in the breakdown of certain cancer medications.
Lonsurf (Tipiracil) is a small molecule thymidine phosphorylase inhibitor developed by Taiho Oncology Inc. It targets thymidine phosphorylase, an enzyme involved in the metabolism of certain cancer therapies. Lonsurf is FDA-approved for the treatment of malignant tumors of the colon and stomach. It has a short half-life of 1.4 hours and its commercial status is patented. Key safety considerations include its potential to cause neutropenia, diarrhea, and fatigue.
At a glance
| Generic name | TIPIRACIL |
|---|---|
| Sponsor | Taiho Oncology Inc |
| Drug class | Nucleoside Analog Antiviral [EPC] |
| Target | Thymidine phosphorylase |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2015 |
Mechanism of action
LONSURF consists of thymidine-based nucleoside analog, trifluridine, and the thymidine phosphorylase inhibitor, tipiracil, at molar ratio 1:0.5 (weight ratio, 1:0.471). Inclusion of tipiracil increases trifluridine exposure by inhibiting its metabolism by thymidine phosphorylase. Following uptake into cancer cells, trifluridine is incorporated into DNA, interferes with DNA synthesis and inhibits cell proliferation. Trifluridine/tipiracil demonstrated anti-tumor activity against KRAS wild-type and mutant human colorectal cancer xenografts in mice.
Approved indications
- Malignant tumor of colon
- Malignant tumor of stomach
Common side effects
- Anemia
- Neutropenia
- Asthenia/Fatigue
- Pyrexia
- Nausea
- Diarrhea
- Vomiting
- Abdominal Pain
- Decreased Appetite
- Thrombocytopenia
- Pulmonary Emboli
- Alopecia
Key clinical trials
- Study of TAS-102 or Placebo Plus BSC in Patients With Metastatic Gastric Cancer (PHASE3)
- Study of TAS-102 in Patients With Metastatic Colorectal Cancer Refractory to Standard Chemotherapies (PHASE3)
- 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)
Patents
| Patent | Expiry | Type |
|---|---|---|
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 |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Lonsurf CI brief — competitive landscape report
- Lonsurf updates RSS · CI watch RSS
- Taiho Oncology Inc portfolio CI