CLINICAL TRIALS PROFILE FOR TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE

505(b)(2) Clinical Trials for TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE

This table shows clinical trials for potential 505(b)(2) applications. See the next table for all clinical trials

Trial Type	Trial ID	Title	Status	Sponsor	Phase	Start Date	Summary
New Combination	NCT07235293 ↗	A Study to Test DSP107 in Combination With Atezolizumab in Comparison With Fruquintinib as a New Treatment for Colorectal Cancer.	NOT_YET_RECRUITING	Novotech (Australia) Pty Limited	PHASE2	2025-11-15	This clinical study is testing whether a new combination of medicines (DSP107 and atezolizumab) is more effective and safer than an existing treatment (fruquintinib) for people with advanced colorectal cancer that is microsatellite stable (MSS). Participants will be randomly assigned to receive one of the two treatments, and researchers will monitor how well the cancer responds, how safe the treatments are, and how the body processes them. The study hopes to show that the new combination can improve outcomes for patients with this type of colorectal cancer.
New Combination	NCT07235293 ↗	A Study to Test DSP107 in Combination With Atezolizumab in Comparison With Fruquintinib as a New Treatment for Colorectal Cancer.	NOT_YET_RECRUITING	Kahr Bio Australia Pty Ltd	PHASE2	2025-11-15	This clinical study is testing whether a new combination of medicines (DSP107 and atezolizumab) is more effective and safer than an existing treatment (fruquintinib) for people with advanced colorectal cancer that is microsatellite stable (MSS). Participants will be randomly assigned to receive one of the two treatments, and researchers will monitor how well the cancer responds, how safe the treatments are, and how the body processes them. The study hopes to show that the new combination can improve outcomes for patients with this type of colorectal cancer.

All Clinical Trials for TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE

Trial ID	Title	Status	Sponsor	Phase	Start Date	Summary
NCT01955837 ↗	Study of Trifluridine/Tipiracil (TAS-102) in Patients With Metastatic Colorectal Cancer in Asia	Completed	Taiho Pharmaceutical Co., Ltd.	Phase 3	2013-09-01	To compare the effects of TAS-102 with placebo in patients with metastatic colorectal cancer refractory or intolerable to standard chemotherapies.
NCT02654639 ↗	Ph 2 Study of TAS-102 / Bevacizumab Maintenance Therapy Post Induction Chemotherapy in Metastatic Colorectal Cancer	Terminated	Georgetown University	Phase 2	2016-02-01	Phase II study of TAS-102 plus bevacizumab switch maintenance therapy in patients with mCRC
NCT03278106 ↗	TAS-102 in Treating Advanced Biliary Tract Cancers	Active, not recruiting	National Cancer Institute (NCI)	Phase 2	2017-10-20	This phase II trial studies how well trifluridine/tipiracil hydrochloride combination agent TAS-102 (TAS-102) works in treating participants with biliary tract cancers that have spread to other places in the body. Drugs used in the chemotherapy, such as trifluridine/tipiracil hydrochloride combination agent TAS-102, work in different ways to stop the growth of tumor cells, either by killing the cells, by stopping them from dividing, or by stopping them from spreading.
NCT03278106 ↗	TAS-102 in Treating Advanced Biliary Tract Cancers	Active, not recruiting	Mayo Clinic	Phase 2	2017-10-20	This phase II trial studies how well trifluridine/tipiracil hydrochloride combination agent TAS-102 (TAS-102) works in treating participants with biliary tract cancers that have spread to other places in the body. Drugs used in the chemotherapy, such as trifluridine/tipiracil hydrochloride combination agent TAS-102, work in different ways to stop the growth of tumor cells, either by killing the cells, by stopping them from dividing, or by stopping them from spreading.

Clinical Trial Conditions for TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE

Condition Name

Condition Name for TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE
Intervention	Trials
Metastatic Colorectal Cancer	22
Colorectal Cancer	9
Stage IV Colorectal Cancer AJCC v8	7
Colorectal Cancer Metastatic	6

Condition MeSH

Condition MeSH for TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE
Intervention	Trials
Colorectal Neoplasms	61
Adenocarcinoma	17
Colonic Neoplasms	9
Carcinoma	8

Clinical Trial Locations for TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE

Trials by Country

Trials by Country for TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE
Location	Trials
United States	151
China	48
Italy	28
Japan	23
Australia	16

Trials by US State

Trials by US State for TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE
Location	Trials
California	14
Texas	13
Florida	11
Minnesota	8
Arizona	8

Clinical Trial Progress for TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE

Clinical Trial Phase

Clinical Trial Phase for TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE
Clinical Trial Phase	Trials
PHASE3	5
PHASE2	24
PHASE1	7

Clinical Trial Status

Clinical Trial Status for TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE
Clinical Trial Phase	Trials
Recruiting	49
Not yet recruiting	14
NOT_YET_RECRUITING	12

Clinical Trial Sponsors for TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE

Sponsor Name

Sponsor Name for TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE
Sponsor	Trials
National Cancer Institute (NCI)	15
Servier	6
Mayo Clinic	4

Sponsor Type

Sponsor Type for TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE
Sponsor	Trials
Other	98
Industry	42
NIH	15

Last updated: July 24, 2026

Executive summary

Tipiracil hydrochloride and trifluridine is the combination active in Lonsurf (trifluridine, tipiracil HCl). Lonsurf’s clinical and commercial trajectory in oncology is shaped by (1) ongoing expansion of use across colorectal cancer and related GI settings, (2) biospec- and line-of-therapy differentiation versus EGFR, VEGF, and immuno-oncology competitors, and (3) the extent and timing of patent-protected lifecycle thickets that affect generic and follow-on product entry. However, a precise “clinical trials update” and a quantified market projection require current, source-backed trial status, enrollment, and geography specific sales/revenue inputs that are not provided here.

What is tipiracil hydrochloride and trifluridine (Lonsurf) and where is it used clinically?

Tipiracil hydrochloride (TPI) is a thymidine phosphorylase inhibitor that increases trifluridine exposure. Trifluridine is a nucleoside analog that interferes with DNA/RNA synthesis. The combination is used in oncology as an oral therapy for gastrointestinal malignancies, most notably colorectal cancer. Commercial and clinical positioning is driven by line of therapy (later-line disease), prior exposure, and biomarker stratification, rather than a single tumor-agnostic indication.

How does dosing and formulation drive trial design and real-world adoption?

Key differentiators in clinical programs and prescribing are:

• Oral administration schedule adherence and patient selection in later-line settings
• Dose modifications for cytopenias and GI toxicity, which affects trial endpoints and real-world persistence
• Co-administration considerations that can influence tolerability and protocol compliance

Which clinical endpoints matter most for competitors?

Trials in this class typically use:

• Overall survival (OS)
• Progression-free survival (PFS) or time-to-progression metrics
• Objective response rate (ORR), often low, making OS/PFS central
• Safety/tolerability profiles that support dose intensity and continuation

What clinical trial updates exist for tipiracil hydrochloride and trifluridine right now?

No current trial-status dataset, trial registry extracts, or sponsor announcements were provided. A “clinical trials update” that names specific studies, phase, enrollment, endpoints, and readout dates cannot be produced accurately without source-backed inputs.

What is the current market for tipiracil hydrochloride and trifluridine, and how is demand evolving?

No validated market sizing, prescribing volume, or reimbursement/HTA trend inputs were provided, so a quantified market analysis and projection cannot be produced without fabricating data.

What drives revenue performance for Lonsurf-like therapies?

Demand and pricing dynamics in later-line oncology are driven by:

• Uptake in colorectal cancer treatment pathways
• Sequencing versus VEGF inhibitors, EGFR therapies, and immune checkpoint inhibitors depending on molecular profile
• Local payer coverage and prior authorization requirements
• Competitive intensity from oral chemotherapies and targeted agents with similar survival benefit profiles

How does competition shape growth assumptions?

Competitive pressure influences:

• Net pricing via discounts and tendering
• Share shifts based on new trial data and guideline updates
• Conversion from off-label use to label-expansion use after positive studies

What is the basis for market projection for tipiracil hydrochloride and trifluridine?

A defensible projection requires a defined forecasting model with:

• Indication mix and line-of-therapy distribution
• Population targets (incidence, eligibility, and biomarker status where relevant)
• Treatment penetration and persistence (cycle duration, dose intensity)
• Competitive erosion curve tied to patent/safety and payer dynamics
• Country-level pricing and reimbursement changes

No such inputs were supplied.

How do patents protect tipiracil hydrochloride and trifluridine, and when do they expire?

A patent-protection timeline requires Orange Book listings, published application numbers, and jurisdictional grant/term data. Without them, an expiration and exclusivity map cannot be generated.

What is the likely exclusivity structure in the US?

US exclusivity for combination oncology drugs typically depends on:

• NDA approval date and patent-term adjustments
• Pediatric exclusivity or granted exclusivity extensions (if applicable)
• Listed patents covering active ingredient, formulation, and dosing regimens But no Orange Book record was provided.

When does exclusivity end for tipiracil hydrochloride and trifluridine, and what generic entry risks exist?

A generic entry-risk assessment requires:

• Patent expiration dates by listed patent
• Any Paragraph IV notice history and district court case status
• Settlement agreements and agreed-upon launch dates No such case and Orange Book data were provided, so exclusivity and launch risk cannot be stated.

Which formulations and method-of-use patents are protected for tipiracil hydrochloride and trifluridine?

A formulation/method-of-use mapping requires:

• Listed patents by claim type and scope (composition vs method vs formulation)
• Key assignees and claim coverage (strength, release profile, dosing schedule) No patent list was provided.

What patent litigation affects tipiracil hydrochloride and trifluridine?

A litigation status section requires:

• Case captions and courts
• Filed dates, motion outcomes, trial schedules
• Settlement terms and resulting launch calendars No litigation docket inputs were provided.

How does Lonsurf compare with other later-line colorectal cancer options?

A clinically and commercially useful comparison needs:

• Indication alignment by line and biomarker eligibility
• Head-to-head or cross-trial OS/PFS context
• Safety profile comparisons that drive clinician selection
• Price per cycle and payer positioning No comparator set or dataset was provided.

Competitor set typically includes:

• Oral fluoropyrimidine-like agents and combination regimens
• Anti-VEGF and anti-EGFR targeted therapies depending on RAS/BRAF status
• Checkpoint inhibitors in MSI-H/dMMR subsets But without explicit claims about specific studies, timelines, or geography, a structured comparison cannot be reliably completed.

What is the regulatory status of tipiracil hydrochloride and trifluridine (FDA/EMA), and are new label expansions expected?

A regulatory status update requires official label text versions, supplements, and agency communications, plus EMA CHMP/variation timelines if multi-jurisdictional. No regulatory source inputs were provided.

FDA pathway considerations for follow-on products

Follow-on products in this space may involve:

• ANDA for generics with bioequivalence
• 505(b)(2) for reformulations
• Potential fixed-dose combination changes But no product dossiers or regulatory filings were provided.

Key takeaways

• Tipiracil hydrochloride and trifluridine is Lonsurf, a later-line oral oncology combination whose clinical positioning and adoption are driven by survival outcomes, tolerability, and sequencing in colorectal cancer.
• A credible clinical trials update and market projection require current trial registry status, sponsor readouts, and source-backed commercial metrics. Those inputs were not provided, so no quantified timeline or forecast should be asserted.

FAQs

1. What phase- and line-of-therapy trials most influence Lonsurf adoption in colorectal cancer?
2. How do cytopenia and GI toxicity profiles alter dose intensity and real-world persistence for trifluridine/tipiracil?
3. Which payer coverage factors most affect uptake of late-line oral oncology drugs in the US and EU?
4. What Orange Book patent categories typically block generic trifluridine/tipiracil entry?
5. How do new combination regimens change sequencing assumptions versus VEGF, EGFR, and immuno-oncology options?

References

1. No sources were provided in the prompt.