LONSURF Drug Patent Profile

When do Lonsurf patents expire, and when can generic versions of Lonsurf launch?

Lonsurf is a drug marketed by Taiho Oncology and is included in one NDA. There are six patents protecting this drug and one Paragraph IV challenge.

This drug has one hundred and eighteen patent family members in thirty-three countries.

The generic ingredient in LONSURF is tipiracil hydrochloride; trifluridine. There are two drug master file entries for this compound. One supplier is listed for this compound. Additional details are available on the tipiracil hydrochloride; trifluridine profile page.

DrugPatentWatch^® Litigation and Generic Entry Outlook for Lonsurf

A generic version of LONSURF was approved as tipiracil hydrochloride; trifluridine by NATCO on June 13^th, 2023.

Summary for LONSURF

International Patents:	118
US Patents:	6
Applicants:	1
NDAs:	1
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	13
Clinical Trials:	55
Patent Applications:	552
Drug Prices:	Drug price information for LONSURF
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for LONSURF
What excipients (inactive ingredients) are in LONSURF?	LONSURF excipients list
DailyMed Link:	LONSURF at DailyMed

See drug prices for LONSURF

Recent Clinical Trials for LONSURF

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

Sponsor	Phase
Yonsei University	Phase 1/Phase 2
Taiho	Phase 2
Amgen	Phase 3

See all LONSURF clinical trials

Pharmacology for LONSURF

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

Paragraph IV (Patent) Challenges for LONSURF

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 LONSURF

LONSURF is protected by ten US patents and one FDA Regulatory Exclusivity.

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	207981-001	Sep 22, 2015	AB	RX	Yes	No	RE46284
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-001	Sep 22, 2015	AB	RX	Yes	No	10,456,399
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-001	Sep 22, 2015	AB	RX	Yes	No	9,943,537
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-002	Sep 22, 2015	AB	RX	Yes	Yes	RE46284
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-002	Sep 22, 2015	AB	RX	Yes	Yes	10,457,666		Y	Y
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-002	Sep 22, 2015	AB	RX	Yes	Yes	9,943,537
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-002	Sep 22, 2015	AB	RX	Yes	Yes	9,527,833		Y	Y

Expired US Patents for LONSURF

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-001	Sep 22, 2015	5,744,475
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-002	Sep 22, 2015	5,744,475
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-001	Sep 22, 2015	6,479,500
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-002	Sep 22, 2015	6,479,500

International Patents for LONSURF

When does loss-of-exclusivity occur for LONSURF?

Based on analysis by DrugPatentWatch, the following patents block generic entry in the countries listed below:

Australia

Brazil

Canada

China

Croatia

Cyprus

Denmark

European Patent Office

Georgia, Republic of

Hong Kong

Hungary

Japan

Lithuania

Malaysia

Mexico

Morocco

New Zealand

Philippines

Poland

Portugal

Russian Federation

Serbia

Singapore

Slovenia

South Korea

Spain

Taiwan

Ukraine

Generics may enter earlier, or later, based on new patent filings, patent extensions, patent invalidation, early generic licensing, generic entry preferences, and other factors.

See the table below for additional patents covering LONSURF around the world.

Country	Patent Number	Title	Estimated Expiration
Australia	2017208215	Stable crystal form of tipiracil hydrochloride and crystallization method for the same
Australia	772486
Japan	6882205
Russian Federation	2727598	СПОСОБ ЛЕЧЕНИЯ БОЛЬНЫХ РАКОМ С ТЯЖЕЛОЙ ПОЧЕЧНОЙ НЕДОСТАТОЧНОСТЬЮ (METHOD OF TREATING PATIENTS WITH CANCER WITH SEVERE RENAL INSUFFICIENCY)
Spain	2203683
Taiwan	201536319	Antitumor agent and antitumor effect enhancer
World Intellectual Property Organization (WIPO)	2014203877

Supplementary Protection Certificates for LONSURF

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
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
1849470	1790063-0	Sweden		PRODUCT NAME: TRIFLURIDINE IN COMBINATION WITH TIPIRACIL HYDROCHLORIDE; REG. NO/DATE: EU/1/16/1096 20160427
1849470	17C1028	France		PRODUCT NAME: TRIFLURIDINE/TIPIRACIL; REGISTRATION 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	300889	Netherlands		PRODUCT NAME: TRIFLURIDINE IN COMBINATIE MET TIPIRACILHYDROCHLORIDE; REGISTRATION NO/DATE: EU/1/16/1096 20160427
1849470	34/2017	Austria		PRODUCT NAME: TRIFLURIDIN / TIPIRACIL ODER DEREN PHARMAZEUTISCH WIRKSAMEN SALZE; REGISTRATION NO/DATE: EU/1/16/1096 (MITTEILUNG) 20160427
1849470	PA2017024,C1849470	Lithuania		PRODUCT NAME: TRIFLURIDINAS/TIPIRACILAS; REGISTRATION NO/DATE: EU/1/16/1096 20160425

Market Dynamics and Financial Trajectory for LONSURF (Trifluridine/Tipiracil)

Introduction to LONSURF

LONSURF, a combination of trifluridine (FTD) and tipiracil (TPI), is an oral anticancer drug developed by Taiho Pharmaceutical Co., Ltd. It is designed to treat various types of cancer, including metastatic colorectal cancer (mCRC) and metastatic gastric cancer.

Mechanism of Action and Clinical Indications

LONSURF's dual mechanism involves FTD, an antineoplastic nucleoside analogue, which is incorporated into DNA to interfere with its function, and TPI, which inhibits the FTD-degrading enzyme thymidine phosphorylase, thereby maintaining the blood concentration of FTD[1].

Approval and Licensing

LONSURF has received significant regulatory approvals. It was approved for the treatment of mCRC in the United States in 2015, and later for metastatic gastric cancer in the U.S. in February 2019, in Japan in August 2019, and in the EU in September 2019[1].

Global Market Presence

As of August 2019, LONSURF has been approved for advanced mCRC in 72 countries and regions worldwide. It is marketed by Taiho Pharmaceutical in Japan, by Taiho Oncology, Inc. in the United States, and by Servier in Europe and other countries outside of the U.S., Canada, Mexico, and Japan/Asia[1].

Financial Performance of Servier

Servier, the partner responsible for the commercialization of LONSURF in many regions, has seen significant financial growth. For the 2022-2023 financial year, Servier's consolidated revenue increased by 9.2% to €5.327 billion, driven by a 9.4% growth in brand-name medicine sales, which includes LONSURF. The group's EBITDA margin improved to 19.1%, reflecting higher sales and tight cost control[2].

Revenue Contribution of LONSURF

While specific revenue figures for LONSURF are not detailed in the overall financial reports, the drug's approval and expanding indications have contributed to the growth of Servier's brand-name medicine sales. The international revenue, particularly from the American continent, has been a significant driver, with the U.S. subsidiary being the group's leading entity[2].

Economic and Cost-Effectiveness Assessments

The Canadian Agency for Drugs and Technologies in Health (CADTH) conducted an economic assessment of LONSURF plus bevacizumab. The assessment found that while the combination improved overall survival (OS) and progression-free survival (PFS), it did not provide good value for the healthcare system at the public list price. A price reduction was recommended to achieve a more favorable cost-effectiveness ratio[3][4].

Patient Needs and Clinical Benefits

LONSURF plus bevacizumab has met some patient needs by extending life with manageable treatment side effects. However, the clinical benefit of the evidence remains uncertain, and the combination's high cost poses a significant challenge for healthcare systems[3][4].

Market Expansion and Future Prospects

The approval of LONSURF for additional indications, such as metastatic gastric cancer, has expanded its market potential. Servier's strategic plans, including its 2025 and 2030 ambitions, involve further transformation and growth, which could positively impact LONSURF's market presence and financial performance[2].

Regional Market Dynamics

In regions like the EU and Japan, LONSURF's approvals have opened up new markets. In the U.S., the drug's performance is part of Servier's overall growth strategy, with the U.S. subsidiary being a key contributor to the group's revenue[1][2].

Challenges and Opportunities

Despite its clinical benefits, LONSURF faces challenges related to cost-effectiveness and pricing. However, its unique mechanism of action and expanding indications present opportunities for continued market growth and financial success.

Conclusion

LONSURF's market dynamics are influenced by its regulatory approvals, global market presence, and the financial performance of its commercial partners. While it faces economic challenges, its clinical benefits and expanding indications position it for continued growth in the oncology market.

Key Takeaways

• Regulatory Approvals: LONSURF has been approved for mCRC and metastatic gastric cancer in several regions.
• Global Presence: Approved in 72 countries and regions for mCRC.
• Financial Performance: Contributes to Servier's brand-name medicine sales growth.
• Economic Assessments: High cost poses challenges for healthcare systems.
• Clinical Benefits: Improves OS and PFS with manageable side effects.
• Future Prospects: Expanding indications and Servier's strategic growth plans.

FAQs

What is LONSURF used for?

LONSURF is used for the treatment of metastatic colorectal cancer (mCRC) and metastatic gastric cancer, including adenocarcinoma of the gastroesophageal junction (GEJ).

Who are the key partners involved in the commercialization of LONSURF?

Taiho Pharmaceutical Co., Ltd., and Servier are the key partners involved in the commercialization of LONSURF.

What are the unique features of LONSURF's mechanism of action?

LONSURF combines trifluridine (FTD) and tipiracil (TPI), where FTD is incorporated into DNA to interfere with its function, and TPI inhibits the FTD-degrading enzyme thymidine phosphorylase.

How has LONSURF impacted Servier's financial performance?

LONSURF has contributed to the growth of Servier's brand-name medicine sales, which increased by 9.4% in the 2022-2023 financial year.

What are the economic challenges faced by LONSURF?

The high cost of LONSURF, particularly when combined with bevacizumab, poses significant challenges for healthcare systems, requiring price reductions to achieve a favorable cost-effectiveness ratio.

Cited Sources

1. Taiho Pharmaceutical Co., Ltd. - LONSURF® (trifluridine/tipiracil) Receives Marketing Authorization in Europe for Previously Treated Metastatic Gastric Cancer[1].
2. Servier - Servier confirms its 2025 trajectory to achieve its 2030 ambition[2].
3. CADTH - Trifluridine-Tipiracil (Lonsurf) - Canada's Drug Agency[3].
4. NCBI Bookshelf - Trifluridine-Tipiracil (Lonsurf)[4].