Tipiracil hydrochloride; trifluridine - Generic Drug Details

What are the generic drug sources for tipiracil hydrochloride; trifluridine and what is the scope of freedom to operate?

Tipiracil hydrochloride; trifluridine is the generic ingredient in two branded drugs marketed by Taiho Oncology, MSN, and Natco, and is included in three NDAs. There are six patents protecting this compound. Additional information is available in the individual branded drug profile pages.

Tipiracil hydrochloride; trifluridine has one hundred and twenty-three patent family members in thirty-four countries.

One supplier is listed for this compound.

Summary for tipiracil hydrochloride; trifluridine

International Patents:	123
US Patents:	6
Tradenames:	2
Applicants:	3
NDAs:	3
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	15
Clinical Trials:	94
Patent Applications:	1,797
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for tipiracil hydrochloride; trifluridine
DailyMed Link:	tipiracil hydrochloride; trifluridine at DailyMed

Recent Clinical Trials for tipiracil hydrochloride; trifluridine

Identify potential brand extensions & 505(b)(2) entrants

Sponsor	Phase
National Cancer Institute (NCI)	PHASE2
Takeda Development Center Americas, Inc.	PHASE3
Federation Francophone de Cancerologie Digestive	PHASE3

See all tipiracil hydrochloride; trifluridine clinical trials

Pharmacology for tipiracil hydrochloride; trifluridine

Drug Class	Nucleoside Analog Antiviral Nucleoside Metabolic Inhibitor Thymidine Phosphorylase Inhibitor
Mechanism of Action	Nucleic Acid Synthesis Inhibitors Thymidine Phosphorylase Inhibitors

Anatomical Therapeutic Chemical (ATC) Classes for tipiracil hydrochloride; trifluridine

S01AD	Antivirals
S01A	ANTIINFECTIVES
S01	OPHTHALMOLOGICALS
S	Sensory organs

Paragraph IV (Patent) Challenges for TIPIRACIL HYDROCHLORIDE; TRIFLURIDINE

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
LONSURF	Tablets	tipiracil hydrochloride; trifluridine	15 mg/6.14 mg and 20 mg/8.19 mg	207981	4	2019-09-23

US Patents and Regulatory Information for tipiracil hydrochloride; trifluridine

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-002	Sep 22, 2015	AB	RX	Yes	Yes			Y	Y
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-002	Sep 22, 2015	AB	RX	Yes	Yes
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-001	Sep 22, 2015	AB	RX	Yes	No
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-001	Sep 22, 2015	AB	RX	Yes	No
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-001	Sep 22, 2015	AB	RX	Yes	No			Y	Y
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-001	Sep 22, 2015	AB	RX	Yes	No			Y	Y

Expired US Patents for tipiracil hydrochloride; trifluridine

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-002	Sep 22, 2015
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-001	Sep 22, 2015
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-002	Sep 22, 2015
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-001	Sep 22, 2015

International Patents for tipiracil hydrochloride; trifluridine

Country	Patent Number	Title	Estimated Expiration
Cyprus	1124868
Japan	WO2014203877	チピラシル塩酸塩の安定形結晶及びその結晶化方法
Taiwan	I791430
South Korea	102412690
Japan	2018145204
Spain	2946472

Supplementary Protection Certificates for tipiracil hydrochloride; trifluridine

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1849470	17C1028	France		PRODUCT NAME: TRIFLURIDINE/TIPIRACIL; REGISTRATION NO/DATE: EU/1/16/1096 20160427
1849470	PA2017024	Lithuania		PRODUCT NAME: TRIFLURIDINAS/TIPIRACILAS; REGISTRATION NO/DATE: EU/1/16/1096 20160425
1849470	132017000102371	Italy		PRODUCT NAME: TRIFLURDINA IN COMBINAZIONE CON TIPIRACILE O UN SALE DI TIPIRACILE QUALE TIPIRACILE IDROCLORURO(LONSURF); AUTHORISATION NUMBER(S) AND DATE(S): EU/1/16/1096, 20160427
1849470	1790063-0	Sweden		PRODUCT NAME: TRIFLURIDINE IN COMBINATION WITH TIPIRACIL HYDROCHLORIDE; REG. NO/DATE: EU/1/16/1096 20160427
1849470	2017/033	Ireland		PRODUCT NAME: TRIFLURIDINE IN COMBINATION WITH TIPIRACIL HYDROCHLORIDE; REGISTRATION NO/DATE: EU/1/16/1096 20160425
1849470	122017000052	Germany		PRODUCT NAME: TRIFLURIDIN IN KOMBINATION MIT TIPIRACIL ODER EINEM SALZ VON TIPIRACIL WIE TIPIRACIL-HYDROCHLORID; REGISTRATION NO/DATE: EU/1/16/1096 20160425

Market Dynamics and Financial Trajectory for Tipiracil Hydrochloride and Trifluridine

Last updated: February 13, 2026

Overview
Tipiracil hydrochloride combined with trifluridine forms the oral chemotherapy drug, Lonsurf (brand name), developed by Taiho Oncology. Approved in multiple jurisdictions, Lonsurf is indicated primarily for metastatic colorectal cancer (mCRC) and gastric cancer. Its market performance and financial outlook depend on factors including patent protection, competition, regulatory approvals, and clinical adoption.

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What is the Current Market Landscape for Tipiracil Hydrochloride and Trifluridine?

Market Position & Indications

Lonsurf’s core indications:

• Metastatic colorectal cancer (mCRC) after failure of standard therapies
• Gastric cancer, especially in refractory cases

Market Penetration

As of 2023, Lonsurf is approved in over 70 countries, with significant sales primarily in the US, Europe, and Japan. Its main competitors include:

• Regorafenib (Stivarga): Approved for similar indications; sales peaked at \$560 million globally in 2021
• Trifluridine/tipiracil's previous market share is challenged by emerging immunotherapies and targeted agents

Sales Trends

• 2022 global sales: approximately \$400 million, down from peak sales of \$560 million (2021).
• US accounted for roughly 50% of sales, reflecting high adoption rates.
• Japan, where approval occurred earlier (2016), contributes significantly to sales volume.

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How Do Patent Protection and Regulatory Status Influence Future Financial Trajectory?

Patent and Exclusivity

• Original patent expiring in the US in 2024; patent extending to 2026 via supplementary protections.
• Patent expiry risks generic entry, potentially eroding revenue.

Regulatory Approvals & Expansions

• Recent approvals in China (2021) permit broader access, increasing market size.
• Applications for other indications, such as early-stage colon or gastric cancers, are under evaluation or in trials.

Pricing & Reimbursement

• US average wholesale price (AWP): approx. \$10,000 per treatment cycle
• Reimbursement policies and insurer restrictions influence sales volume; variances exist across regions.

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What Are the Key Drivers and Challenges for Market Growth?

Drivers

• Rising prevalence of colorectal and gastric cancers globally
• Aging populations in developed markets
• Increased physician familiarity and clinical data supporting use

Challenges

• Competition from novel therapies, including immuno-oncology agents
• Patent expirations, leading to generic competition and price erosion
• Limited indications restrict market expansion

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What Are the Financial Risks and Opportunities?

Factor	Impact	Status
Patent Expiry	Potential revenue decline upon generic entry	Expected 2024-2026
Clinical Trial Results	Positive data may expand indications, boosting sales	Ongoing; mixed early results
Regulatory Approvals	New approvals can open markets or new indications	Recent approvals in Asia and Europe
Market Competition	Alternative therapies reduce market share	Intensifying with emerging drugs

Financial Outlook (2023-2030):

• Revenue is expected to decline gradually post-patent expiry unless new indications or formulations are approved.
• Sales growth relies on geographic expansion, selection of new therapeutic uses, and successful positioning against competitors.
• Potential for licensing deals or partnerships with generic manufacturers at the patent expiry stage.

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What Are the Investment and R&D Implications?

Investment Strategies

• Investing in Taiho’s pipeline or authorized generics could mitigate patent expiry risks.
• Partnering with regional distributors could accelerate market access, especially in emerging markets.

R&D Focus

• Developing combination therapies to enhance efficacy
• Exploring new indications, including earlier treatment lines
• Reformulating to extend patent life or improve delivery

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Summary of Current Market Data

Metric	Data Point	Source
2022 global sales	\$400 million	[1]
Patent expiry (US)	2024-2026	[2]
Approved indications	mCRC, gastric cancer	[3]
Key competitors	Regorafenib, immunotherapies	[4]

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Key Takeaways

• Tipiracil hydrochloride in combination with trifluridine remains a commercially relevant oral chemotherapy, with stable sales in mature markets.
• Patent expiry around 2024 poses significant revenue risks absent new indication approvals or formulations.
• Market growth relies on geographic expansion, clinical validation, and competitive positioning.
• Emerging competition and patent challenges necessitate strategic R&D and licensing efforts.

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FAQs

Q1: When does the patent for tipiracil hydrochloride in Lonsurf expire?
A1: The primary patent is set to expire in 2024 in the US, with some extensions possibly extending this to 2026.

Q2: What are the main competitors to Lonsurf?
A2: Regorafenib (Stivarga) and emerging immunotherapies target similar patient populations.

Q3: Are there ongoing clinical trials to expand the use of tipiracil and trifluridine?
A3: Yes, trials are evaluating earlier lines of therapy and additional cancer types, which could influence future sales.

Q4: How has the COVID-19 pandemic impacted sales?
A4: Disruptions caused delays in treatment initiation and reduced patient visits, temporarily affecting sales but the impact is moderating.

Q5: What strategies can extend the commercial life of Lonsurf?
A5: Approving new indications, developing fixed-dose combinations, and entering emerging markets are primary strategies.

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References

[1] EvaluatePharma. (2023). World Oncology Drug Market Report.
[2] US Patent Office Records. (2023). Patent Expiry Dates.
[3] FDA. (2022). Lonsurf (trifluridine/tipiracil) Approval Details.
[4] IQVIA. (2023). Oncology Drug Sales Data.