LONSURF (tipiracil hydrochloride)
Lonsurf (trifluridine and tipiracil) is indicated for adult patients with metastatic colorectal cancer (mCRC) as a single agent or in combination with bevacizumab for those previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and an anti-EGFR therapy (if RAS wild-type). It is also indicated as a single agent for metastatic gastric or gastroesophageal junction (GEJ) adenocarcinoma in patients previously treated with at least two prior lines of chemotherapy—including a fluoropyrimidine, a platinum, and either a taxane or irinotecan—and HER2/neu-targeted therapy, if appropriate.
How LONSURF Works
Lonsurf is an antineoplastic combination of trifluridine, a thymidine-based nucleoside metabolic inhibitor, and tipiracil, a thymidine phosphorylase (TP) inhibitor. Tipiracil increases systemic exposure of trifluridine by inhibiting its metabolism by TP. Once trifluridine is taken up into cancer cells, it is incorporated into DNA, which interferes with DNA synthesis and inhibits cellular proliferation.
Development Insights
Details
- Status
- Prescription
- First Approved
- 2015-09-22
- Patent Cliff
- 2037
- Routes
- ORAL
- Dosage Forms
- TABLET
LONSURF Approval History
What LONSURF Treats
3 indicationsLONSURF is approved for 3 conditions since its original approval in 2015. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Metastatic Colorectal Cancer
- Metastatic Gastric Cancer
- Gastroesophageal Junction Adenocarcinoma
LONSURF Target & Pathway
ProTarget
LONSURF Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
Indication competitors
Same indication, different mechanism — what else might this patient receive?
Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
What's emerging in LONSURF's indications
See all emerging drugs →Phase 3 candidates targeting molecules with no FDA-approved drug, in indications LONSURF treats. First-in-class if their pivotal trials read out positive.
Drugs Similar to LONSURF
3 of 18FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
Clinical Trial Registry
3 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT06245356 TRIFLUOX-DP | PRODIGE 91 - UCGI 46 | Ph 2 | recruiting | Safety of Trifluridine/Tipiracil in Patients With Dihydropyrimidine Dehydrogenase Deficiency Diagnosed With Metastatic Colorectal or Gastroesophageal Cancer |
| NCT04046887 | IUSCC-0664 | Ph 1 | terminated | Study of Lonsurf in Combination With Gemcitabine and Nab-Paclitaxel in Patients With Advanced (PDAC) |
| NCT03616574 | HS-CA102N-101 | Ph 1 | completed | First-in-human Study of CA102N Monotherapy and CA102N Combined With Trifluridine/Tipiracil (LONSURF) in Subjects With Advanced Solid Tumors |
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
LONSURF FDA Label Details
Indications & Usage
FDA Label (PDF)LONSURF is indicated for the treatment of Metastatic Colorectal Cancer; Metastatic Gastric Cancer; Gastroesophageal Junction Adenocarcinoma.
LONSURF Patents & Exclusivity
Patents (6 active)
Exclusivity
Pro Intelligence Preview
Deep insights for LONSURF
Revenue Insights
- • Quarterly revenue tracking
- • Historical trend analysis
Patent Timeline
- • Cliff: 2037
- • 40 active patents
Trial Analysis
- • 3 total trials
- • Stage: Stable
Competitive Landscape
- • 18 similar drugs
- • Same target/indication analysis
Full approval history • All patents • Revenue trends • Competitor analysis
Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.
How We Calculate These Metrics
Trial Activity Stage
Measures the current development activity pattern based on trial phases, status, and trends. Important: This measures R&D activity, not commercial lifecycle.
Trial statuses: "Active" means recruiting or ongoing. "Completed" means reached planned endpoint. "Terminated" means stopped early—often due to safety, efficacy, or business reasons.
- Growth: High proportion of early-phase trials (Phase 1/2), active development
- Expansion: Significant Phase 3 activity, approaching or pursuing approvals
- Mature: Substantial Phase 4 post-marketing studies
- Stable: Mixed phase distribution, steady development
- Declining: Low active trial ratio, reduced R&D investment