Telotristat etiprate - Generic Drug Details

What are the generic sources for telotristat etiprate and what is the scope of patent protection?

Telotristat etiprate is the generic ingredient in one branded drug marketed by Tersera and is included in one NDA. There are five patents protecting this compound. Additional information is available in the individual branded drug profile pages.

Telotristat etiprate has seventy patent family members in twenty-nine countries.

Two suppliers are listed for this compound.

Summary for telotristat etiprate

International Patents:	70
US Patents:	5
Tradenames:	1
Applicants:	1
NDAs:	1
Finished Product Suppliers / Packagers:	2
Raw Ingredient (Bulk) Api Vendors:	52
Clinical Trials:	15
Patent Applications:	76
DailyMed Link:	telotristat etiprate at DailyMed

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

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 telotristat etiprate

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

Sponsor	Phase
National Cancer Institute (NCI)	Phase 2
Barbara Ann Karmanos Cancer Institute	Phase 2
Ipsen	Phase 1

See all telotristat etiprate clinical trials

Pharmacology for telotristat etiprate

Drug Class	Tryptophan Hydroxylase Inhibitor
Mechanism of Action	Tryptophan Hydroxylase Inhibitors

Anatomical Therapeutic Chemical (ATC) Classes for telotristat etiprate

A16AX	Various alimentary tract and metabolism products
A16A	OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS
A16	OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS
A	Alimentary tract and metabolism

US Patents and Regulatory Information for telotristat etiprate

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				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

International Patents for telotristat etiprate

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

Supplementary Protection Certificates for telotristat etiprate

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

Telotristat etiprate Market Analysis and Financial Projection Experimental

Market Dynamics and Financial Trajectory for Telotristat Ethyl (Xermelo)

Introduction

Telotristat ethyl, marketed under the brand name Xermelo, is a novel oral inhibitor of peripheral serotonin synthesis. It is primarily used to treat carcinoid syndrome diarrhea in patients with neuroendocrine tumors. Here, we delve into the market dynamics and financial trajectory of this drug.

Mechanism of Action

Telotristat ethyl acts by inhibiting tryptophan hydroxylase, the rate-limiting enzyme in the conversion of tryptophan to serotonin. This mechanism is crucial in reducing the gastrointestinal symptoms associated with carcinoid syndrome, such as diarrhea and flushing[4][5].

Clinical Efficacy

Clinical studies have demonstrated the efficacy of telotristat ethyl in reducing gastrointestinal symptoms. A prospective, exploratory study showed that patients experienced a mean decrease of 43.5% in bowel movements per day and a 74.2% mean reduction in urinary 5-hydroxyindoleacetic acid (u5-HIAA), a biomarker of serotonin. These results indicate significant improvements in patient symptoms and support further evaluation in phase 3 studies[5].

Market Position

Telotristat ethyl is positioned as a key product within Lexicon Pharmaceuticals' portfolio, acting as a cash cow due to its consistent revenue generation. In 2022, Xermelo's worldwide revenue reached $52.4 million, highlighting its high market share in the treatment of carcinoid syndrome diarrhea[3].

Patent and Regulatory Landscape

Xermelo is protected by five patents, with seventy patent family members in twenty-nine countries. The earliest date for generic entry is projected to be February 28, 2031, although this may change due to patent challenges or generic licensing agreements[2].

Cost-Effectiveness

Economic evaluations have shown that telotristat ethyl plus somatostatin analogs (SSAs) is a cost-effective treatment compared to SSA monotherapy. A phase 3 study indicated that telotristat ethyl plus SSA resulted in a small increase in quality-adjusted life years (QALYs) and cost savings. Probabilistic sensitivity analyses showed that telotristat ethyl plus SSA has a high probability of being the most cost-effective treatment at various willingness-to-pay thresholds[1].

Budget Impact

The introduction of telotristat ethyl is estimated to have a significant budget impact. While the initial medicine acquisition costs are substantial, the overall 5-year budget impact, including downstream healthcare resource use, is projected to result in cost savings. The company reports potential savings from Year 3 onwards, with a cumulative 5-year budget impact showing a cost-saving trend[1].

Market Size and Growth

The market for treatments targeting carcinoid syndrome is part of the broader neuroendocrine tumor treatment market. This market is expected to grow due to increasing prevalence and advancements in diagnostic techniques. The global oncology market, which includes neuroendocrine tumors, is projected to reach $200 billion by 2026, with a CAGR of 8.2% from 2019 to 2026[3].

Revenue Performance

In the last quarter of 2022, telotristat ethyl sales accounted for $15 million, contributing significantly to Lexicon Pharmaceuticals' operational stability. The annual revenue for Xermelo in 2022 was $52.4 million, indicating its importance in the company's financial performance[3].

Competitive Landscape

Telotristat ethyl faces competition from other treatments for carcinoid syndrome, including somatostatin analogs. However, its unique mechanism of action and clinical efficacy make it a preferred option for many patients. The lack of generic competition until at least 2031 further solidifies its market position[2].

Future Outlook

Given its consistent revenue generation and cost-effectiveness, telotristat ethyl is expected to continue playing a significant role in Lexicon Pharmaceuticals' portfolio. The drug's ability to reduce gastrointestinal symptoms and improve patient quality of life ensures its demand in the market. As the neuroendocrine tumor treatment market grows, Xermelo is well-positioned to capture a substantial share.

Key Takeaways

• Clinical Efficacy: Telotristat ethyl significantly reduces gastrointestinal symptoms in carcinoid syndrome patients.
• Market Position: It is a key cash cow for Lexicon Pharmaceuticals with high market share.
• Cost-Effectiveness: The drug is cost-effective compared to SSA monotherapy.
• Budget Impact: Initial costs are offset by long-term savings in healthcare resource use.
• Market Growth: Part of a growing neuroendocrine tumor treatment market.
• Revenue Performance: Consistent revenue generation supports operational stability.
• Competitive Landscape: Unique mechanism and lack of generic competition until 2031.

FAQs

What is the primary mechanism of action of telotristat ethyl?

Telotristat ethyl acts by inhibiting tryptophan hydroxylase, the rate-limiting enzyme in the conversion of tryptophan to serotonin[4].

How does telotristat ethyl impact the budget in healthcare settings?

The introduction of telotristat ethyl is estimated to result in initial costs, but long-term analysis shows potential cost savings from Year 3 onwards due to reduced downstream healthcare resource use[1].

What is the projected market size for neuroendocrine tumor treatments by 2026?

The global oncology market, which includes neuroendocrine tumors, is projected to reach $200 billion by 2026, with a CAGR of 8.2% from 2019 to 2026[3].

How does telotristat ethyl compare to somatostatin analogs in terms of cost-effectiveness?

Telotristat ethyl plus SSA is considered cost-effective compared to SSA monotherapy, with a small increase in QALYs and cost savings[1].

When is the earliest date for generic entry of telotristat ethyl?

The earliest date for generic entry of telotristat ethyl is projected to be February 28, 2031, subject to patent challenges or generic licensing agreements[2].

Sources

1. AWMSG SECRETARIAT ASSESSMENT REPORT Telotristat ethyl (Xermelo®). AWTTC NHS Wales, 2018.
2. XERMELO Drug Patent Profile. Drug Patent Watch.
3. Lexicon Pharmaceuticals, Inc. (LXRX) BCG Matrix Analysis. dcf.fm.
4. Telotristat etiprate, a novel serotonin synthesis inhibitor, in patients ... European Journal of Endocrinology, 2021.
5. Telotristat etiprate for carcinoid syndrome: a single-arm, multicenter ... PubMed, 2015.