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XERMELO Drug Patent Profile

Which patents cover Xermelo, and when can generic versions of Xermelo launch?

Xermelo is a drug marketed by Tersera and is included in one NDA. There are five patents protecting this drug.

This drug has seventy patent family members in twenty-nine countries.

The generic ingredient in XERMELO is telotristat etiprate. Two suppliers are listed for this compound. Additional details are available on the telotristat etiprate profile page.

DrugPatentWatch^® Generic Entry Outlook for Xermelo

Xermelo was eligible for patent challenges on February 28, 2021.

By analyzing the patents and regulatory protections it appears that the earliest date for generic entry will be February 28, 2031. This may change due to patent challenges or generic licensing.

Indicators of Generic Entry

Summary for XERMELO

International Patents:	70
US Patents:	5
Applicants:	1
NDAs:	1
Finished Product Suppliers / Packagers:	2
Raw Ingredient (Bulk) Api Vendors:	54
Clinical Trials:	5
Patent Applications:	68
Drug Prices:	Drug price information for XERMELO
What excipients (inactive ingredients) are in XERMELO?	XERMELO excipients list
DailyMed Link:	XERMELO at DailyMed

See drug prices for XERMELO

DrugPatentWatch^® Estimated Loss of Exclusivity (LOE) Date for XERMELO

NDA:

208794

Dosage:

TABLET;ORAL

^*The generic entry opportunity date is the latter of the last compound-claiming patent and the last regulatory exclusivity protection. Many factors can influence early or later generic entry. This date is provided as a rough estimate of generic entry potential and should not be used as an independent source.

Recent Clinical Trials for XERMELO

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

Sponsor	Phase
Aman Chauhan	Phase 2
University of Chicago	Phase 2
Ipsen	Phase 3

See all XERMELO clinical trials

Pharmacology for XERMELO

Drug Class	Tryptophan Hydroxylase Inhibitor
Mechanism of Action	Tryptophan Hydroxylase Inhibitors

US Patents and Regulatory Information for XERMELO

XERMELO is protected by five US patents and one FDA Regulatory Exclusivity.

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

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Tersera	XERMELO	telotristat etiprate	TABLET;ORAL	208794-001	Feb 28, 2017		RX	Yes	Yes				Y
Tersera	XERMELO	telotristat etiprate	TABLET;ORAL	208794-001	Feb 28, 2017		RX	Yes	Yes				Y
Tersera	XERMELO	telotristat etiprate	TABLET;ORAL	208794-001	Feb 28, 2017		RX	Yes	Yes
Tersera	XERMELO	telotristat etiprate	TABLET;ORAL	208794-001	Feb 28, 2017		RX	Yes	Yes
Tersera	XERMELO	telotristat etiprate	TABLET;ORAL	208794-001	Feb 28, 2017		RX	Yes	Yes
Tersera	XERMELO	telotristat etiprate	TABLET;ORAL	208794-001	Feb 28, 2017		RX	Yes	Yes				Y

International Patents for XERMELO

When does loss-of-exclusivity occur for XERMELO?

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

Argentina

Australia

Brazil

Canada

Colombia

Denmark

Ecuador

Eurasian Patent Organization

European Patent Office

Hungary

Israel

Japan

Mexico

Netherlands

New Zealand

Norway

Poland

Portugal

South Africa

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 XERMELO around the world.

Country	Patent Number	Title	Estimated Expiration
Eurasian Patent Organization	017275	ТВЕРДЫЕ ФОРМЫ (S)-ЭТИЛ-2-АМИНО-3-(4-(2-АМИНО-6-((R)-1-(4-ХЛОР-2-(3-МЕТИЛ-1H-ПИРАЗОЛ-1-ИЛ)ФЕНИЛ)-2,2,2-ТРИФТОРЭТОКСИ)ПИРИМИДИН-4-ИЛ)ФЕНИЛ)ПРОПАНОАТА И СПОСОБЫ ИХ ПРИМЕНЕНИЯ (SOLIDS FORMS OF (S)-ETHYL-2-AMINO-3-(4-(2-AMINO-6-((R)-1-(4-CHLORO-2-(3-METHYL-1H-PYRAZOL-1-YL)PHENYL)-2,2,2-TRIFLUOROETHOXY)PYRIMIDIN-4-YL)PHENYL)PROPANOATE AND METHODS OF USE THEREOF)
Ecuador	SP099413	COMPUESTOS A BASE DE 4 - fenil - 6 - (2,2,2 - trifluoro - 1 - feniletoxi)pirimidina Y MÉTODOS PARA SU EMPLEO
Australia	2008304439	Solids forms of ( S) -ethyl 2-amino-3- (4- (2 -amino- 6- ( (r) -1- (4-chloro-2- O-methyl-IH-pyrazol- 1-yl) phenyl) -2, 2, 2-trifluorethoxy) -pyrimidin-4-yl) phenyl) propanoate
Eurasian Patent Organization	200970575	СОЕДИНЕНИЯ НА ОСНОВЕ 4-ФЕНИЛ-6-(2,2,2-ТРИФТОР-1-ФЕНИЛЭТОКСИ)ПИРИМИДИНА И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
Hong Kong	1145023
Brazil	PI0720270	COMPOSTOS BASEDOS EM 4-FENIL-6-(2,2,2-TRIFLÚOR-1-FENIL ETOXI) PIRIMIDINA E PROCESSOS DE USOS DOS MESMOS
European Patent Office	3176159	COMPOSÉS À BASE DE PYRIMIDINE 4-PHÉNYL-6- (2,2,2-TRIFLUORO-1-PHÉNYLÉTHOXY) ET LEURS PROCÉDÉS D'UTILISATION (4-PHENYL-6-(2,2,2-TRIFLUORO-1-PHENYLETHOXY)PYRIMIDINE-BASED COMPOUNDS AND METHODS OF THEIR USE)

Supplementary Protection Certificates for XERMELO

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
2091940	713	Finland
2091940	SPC/GB18/009	United Kingdom		PRODUCT NAME: TELOTRISTAT OR A PHARMACEUTICALLY ACCEPTABLE ESTER, OR A SALT THEREOF, IN PARTICULAR TELOTRISTAT ETHYL, MORE PARTICULARLY HIPPURATE SALT OF TELOTRISTAT ETHYL; REGISTERED: UK EU/1/17/1224/001-002 20170920; UK PLGB 28247/0008 20170920
2091940	2018C/009	Belgium		DETAILS ASSIGNMENT: CHANGE OF OWNER(S), ASSIGNMENT
2091940	C 2018 007	Romania		PRODUCT NAME: TELOTRISTAT SAU UN ESTER ACCEPTABIL FARMACEUTIC, SAU O SARE A ACESTUIA, IN PARTICULAR ETIL TELOTRISTAT, MAI PARTICULAR SARE HIPURAT DE ETIL TELOTRISTAT; NATIONAL AUTHORISATION NUMBER: EU/1/17/1224; DATE OF NATIONAL AUTHORISATION: 20170918; NUMBER OF FIRST AUTHORISATION IN EUROPEAN ECONOMIC AREA (EEA): EU/1/17/1224; DATE OF FIRST AUTHORISATION IN EEA: 20170918
2091940	1890014-2	Sweden		PRODUCT NAME: TELOTRISTAT OR A PHARMACEUTICALLY ACCEPTABLE ESTER, OR A SALT THEREOF, IN PARTICULARLY TELOTRISTAT ETHYL, MORE PARTICULARLY HIPPURATE SALT OF TELOTRISTAT ETHYL; REG. NO/DATE: EU/1/17/1224 20170920
2091940	CA 2018 00011	Denmark		PRODUCT NAME: TELOTRISTAT OR A PHARMACEUTICALLY ACCEPTABLE ESTER, OR A SALT THEREOF, INPARTICULAR TELOTRISTAT ETHYL, MORE PARTICULARLY HIPPURATE SALT OF TELOTRISTAT ETHYL; REG. NO/DATE: EU/1/17/1224 20170920
2091940	11/2018	Austria		PRODUCT NAME: TELOTRISTAT ODER EIN PHARMAZEUTISCH ANNEHMBARER ESTER, ODER EIN SALZ DAVON, INSBESONDERE TELOTRISTATETHYL, INSBESONDERE DAS HIPPURATSALZ VON TELOTRISTATETHYL; REGISTRATION NO/DATE: EU/1/17/1224 (MITTEILUNG) 20170920

XERMELO Market Analysis and Financial Projection Experimental

Market Dynamics and Financial Trajectory for XERMELO

Introduction

XERMELO (telotristat ethyl) is a significant drug in the pharmaceutical portfolio of Lexicon Pharmaceuticals, Inc., primarily used to treat carcinoid syndrome diarrhea. Here, we will delve into the market dynamics and financial trajectory of XERMELO, highlighting its performance, key milestones, and future prospects.

Market Need and Target Population

XERMELO targets patients suffering from carcinoid syndrome diarrhea, a condition often associated with neuroendocrine tumors. The drug works by inhibiting the overproduction of serotonin inside metastatic neuroendocrine tumor (mNET) cells, providing a crucial treatment option for this patient population[1][4].

Sales Performance

U.S. Market

In 2019, XERMELO achieved notable growth in the U.S. market, with net sales reaching $31 million, a nearly 25% increase from the previous year. This growth underscored the drug's importance and acceptance among patients and healthcare providers[1][4].

In the second quarter of 2020, U.S. net sales of XERMELO continued to show resilience, increasing by 21% compared to the same period in 2019, despite the challenges posed by the COVID-19 pandemic[3].

International Market

Lexicon Pharmaceuticals has granted Ipsen an exclusive royalty-bearing right and license to commercialize XERMELO outside of the United States and Japan. This partnership has enabled the drug to reach multiple countries, including the United Kingdom, Germany, Scotland, Denmark, Sweden, and Greece, where it has received national reimbursement approvals[1][5].

Revenue Streams

Net Product Revenue

The primary revenue stream for XERMELO comes from net product sales. In 2019, net product revenue from XERMELO sales in the U.S. was $31 million, while in the second quarter of 2020, it was $9 million[1][3].

Collaborative Agreements and Royalties

In addition to direct sales, Lexicon Pharmaceuticals generates revenue from collaborative agreements and royalties. For instance, in 2019, the company recognized significant revenues from the termination of its alliance with Sanofi and the recognition of remaining amounts allocated to the performance obligations from the initial Sanofi collaboration agreement[1].

Cost of Sales

The cost of sales related to XERMELO has been relatively stable. For the fourth quarter of 2019, the cost of sales was $0.7 million, and for the second quarter of 2020, it remained at $0.7 million. Full-year costs for 2019 were $3.2 million, indicating efficient manufacturing and distribution processes[1][3].

Research and Development (R&D) Expenses

Lexicon Pharmaceuticals has been actively advancing its pipeline, including studies related to XERMELO. R&D expenses for 2019 decreased to $91.9 million from $100.2 million in 2018, primarily due to decreases in professional and consulting fees and lower external clinical development costs. However, the fourth quarter of 2019 saw an increase in R&D expenses due to costs associated with the development of sotagliflozin following the termination of the Sanofi alliance[1].

Clinical Pipeline and Future Prospects

Biliary Tract Cancer

Lexicon initiated a Phase 2 study of telotristat ethyl in biliary tract cancer in 2019. The safety review of the initial dose cohort supported the continuation of the study, indicating potential future applications for XERMELO beyond carcinoid syndrome diarrhea[1][4].

Diabetic Peripheral Neuropathic Pain

In addition to its primary indication, Lexicon is exploring other therapeutic areas. The company initiated a Phase 2 study (RELIEF-DPN-1) for LX9211, another compound, in patients with diabetic peripheral neuropathic pain. While not directly related to XERMELO, this pipeline activity reflects the company's broader commitment to innovative treatments[3].

Financial Performance

Quarterly and Annual Revenues

In the fourth quarter of 2019, Lexicon's total revenues decreased to $8.7 million from $17.1 million in the corresponding period of 2018, primarily due to lower revenues from collaborative agreements. However, full-year 2019 revenues increased significantly to $322.1 million from $63.2 million in 2018, driven by collaboration revenues and net product sales[1].

Net Income/Loss

For the full year 2019, Lexicon reported a net income of $130.1 million, or $1.16 per diluted share, compared to a net loss of $120.5 million, or $1.14 per share, in 2018. This positive financial performance was largely due to the recognition of collaboration revenues and the termination of the Sanofi alliance[1].

Market Dynamics and Competitive Landscape

The market for treatments targeting carcinoid syndrome diarrhea is niche but growing. XERMELO's success is partly due to its unique mechanism of action and the lack of alternative treatments that specifically target serotonin overproduction. The partnership with Ipsen has helped expand its reach globally, enhancing its competitive position[1][5].

Challenges and Opportunities

Regulatory Environment

Lexicon has navigated complex regulatory environments, including the termination of its alliance with Sanofi and engagement in formal dispute resolution proceedings with the FDA. These challenges have been managed effectively, with the company regaining full rights to key compounds like sotagliflozin[1][4].

COVID-19 Impact

The COVID-19 pandemic presented significant challenges to the pharmaceutical industry, but Lexicon's commitment to its mission and the resilience of its sales team helped maintain growth in XERMELO sales during this period[3].

Key Takeaways

• Sales Growth: XERMELO has shown consistent sales growth in the U.S. market, with a nearly 25% increase in 2019 and a 21% increase in the second quarter of 2020.
• International Expansion: The drug is commercialized internationally through a partnership with Ipsen, reaching multiple countries.
• R&D Pipeline: Lexicon is advancing its pipeline with studies on XERMELO in biliary tract cancer and other compounds like LX9211 for diabetic peripheral neuropathic pain.
• Financial Performance: The company reported a significant increase in full-year revenues in 2019, driven by collaboration revenues and net product sales.
• Regulatory and Market Dynamics: Effective management of regulatory challenges and a strong competitive position in the niche market for carcinoid syndrome diarrhea treatments.

FAQs

What is XERMELO used for?

XERMELO (telotristat ethyl) is used to treat carcinoid syndrome diarrhea, a condition associated with neuroendocrine tumors.

Who commercializes XERMELO outside the U.S. and Japan?

Ipsen commercializes XERMELO outside the United States and Japan under an exclusive royalty-bearing license agreement with Lexicon Pharmaceuticals.

How did XERMELO sales perform in 2019?

XERMELO achieved net U.S. sales of $31 million in 2019, a nearly 25% increase from the previous year.

What are the ongoing clinical studies for XERMELO?

Lexicon has initiated a Phase 2 study of telotristat ethyl in biliary tract cancer and is conducting other investigator-initiated studies to inform future development priorities.

How has the COVID-19 pandemic affected XERMELO sales?

Despite the challenges posed by the COVID-19 pandemic, XERMELO sales in the U.S. continued to grow, with a 21% increase in the second quarter of 2020 compared to the prior year.

Sources

1. Lexicon Pharmaceuticals Reports Fourth Quarter and Full-Year 2019 Financial Results and Provides a Business Update. Biospace.
2. FORM 10-Q - Lexicon Pharmaceuticals, Inc.. Lexicon Pharmaceuticals.
3. Lexicon Pharmaceuticals Reports Second Quarter 2020 Financial Results and Provides a Business Update. Biospace.
4. Annual Reports. AnnualReports.com.
5. Lexicon Pharmaceuticals Reports Fourth Quarter and Full-Year 2018 Financial Results and Provides a Business Update. GlobeNewswire.