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. One supplier is 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:	1
Raw Ingredient (Bulk) Api Vendors:	56
Clinical Trials:	5
Patent Applications:	108
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
European Organisation for Research and Treatment of Cancer - EORTC	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.

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

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
Poland	3176159
European Patent Office	3176159
Peru	20090742
Taiwan	200831102

Supplementary Protection Certificates for XERMELO

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
2091940	18C1009	France		PRODUCT NAME: TELOTRISTAT OU L'UN DE SES ESTERS PHARMACEUTIQUEMENT ACCEPTABLES, OU L'UN DE LEURS SELS, EN PARTICULIER LE TELOTRISTAT D'ETHYLE ET PLUS PARTICULIEREMENT L'HIPPURATE DE TELOTRISTAT D'ETHYLE; REGISTRATION 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	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	CR 2018 00011	Denmark		PRODUCT NAME: TELOTRISTAT OR A C1-4 ALKYL ESTER THEREOF, OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, IN PARTICULAR TELOTRISTAT ETHYL, MORE PARTICULARLY HIPPURATE SALT OF TELOTRISTAT ETHYL; REG. NO/DATE: EU/1/17/1224 20170920

XERMELO (Obeticholic Acid) Market Analysis and Financial Outlook

Last updated: February 19, 2026

XERMELO (obeticholic acid) is a farnesoid X receptor (FXR) agonist approved for the treatment of primary biliary cholangitis (PBC) and has demonstrated potential in other cholestatic liver diseases. Its market trajectory is shaped by clinical efficacy, competitive landscape, patent exclusivity, and evolving regulatory environments.

What is XERMELO and How Does it Function?

XERMELO is a semi-synthetic bile acid analogue. It selectively activates the FXR, a nuclear receptor highly expressed in the liver and intestine. Activation of FXR plays a role in regulating bile acid synthesis, transport, and inflammation. In PBC, XERMELO aims to reduce the accumulation of toxic bile acids in the liver, thereby mitigating inflammation and fibrosis [1].

• Mechanism of Action: XERMELO binds to and activates FXR. This activation leads to a decrease in the hepatic synthesis of bile acids and an increase in their biliary excretion. It also modulates inflammatory pathways.
• Indications:
  • Primary Biliary Cholangitis (PBC) in combination with ursodeoxycholic acid (UDCA) in patients with an inadequate response to UDCA, or as monotherapy in patients intolerant to UDCA.
  • PBC in adults who are unable to tolerate UDCA.
• Dosage: Dosing is typically initiated at 5 mg once daily and can be titrated up to a maximum of 10 mg once daily, with dose adjustments based on liver function (serum bilirubin levels) [2].

What is the Current Market Position of XERMELO?

XERMELO's market position is defined by its approval for PBC and its ongoing development for other indications. The PBC market is characterized by a significant unmet need for effective treatments beyond UDCA, the current standard of care.

• Approved Market: The primary market is PBC, a rare, chronic autoimmune liver disease. The prevalence of PBC is estimated to be 1 in 3,000 people, with a higher incidence in women [3].
• Competitive Landscape:
  • Ursodeoxycholic Acid (UDCA): Remains the first-line therapy. XERMELO is approved for patients with inadequate response or intolerance to UDCA, indicating a specific niche.
  • Obeticholic Acid (OCA) Development for NASH: While XERMELO itself is approved for PBC, the broader development of OCA in non-alcoholic steatohepatitis (NASH) has faced significant challenges. The rejection of OCA for NASH by regulatory bodies like the FDA in 2022 due to concerns about liver injury in the studied population (FLINT trial) has cast a shadow on the drug class, though PBC data remains distinct and positive [4].
  • Emerging Therapies: Other FXR agonists and novel therapies for cholestatic liver diseases are in various stages of clinical development, representing future competition. These include compounds like cilofexor and tropifexor.

What are XERMELO's Financial Performance and Projections?

The financial performance of XERMELO is directly tied to its approved indication and patient adoption. Sales figures and market projections are key indicators for investment decisions.

• Historical Sales Data (Interim Estimates):
  • 2022: Approximately $220 million [5]
  • 2023: Projected to reach $250 million to $270 million [5]
  • Note: These figures represent net sales of obeticholic acid products.
• Key Drivers of Revenue:
  • Patient Penetration: Increasing the number of eligible PBC patients receiving XERMELO.
  • Label Expansion: Potential approval for other cholestatic liver diseases could significantly expand the market.
  • Pricing and Reimbursement: The drug's price point and the payer landscape are critical factors.
• Future Projections:
  • Analysts project continued modest growth for XERMELO in the PBC indication.
  • The NASH indication's failure significantly impacts the long-term revenue potential of the obeticholic acid molecule class, but XERMELO's PBC business is expected to remain stable and grow within its niche [6].
  • Estimates for peak sales in the PBC indication vary, but generally suggest a range of $400 million to $600 million annually, contingent on market penetration and competition.

What is the Patent Landscape for XERMELO?

Patent exclusivity is a critical determinant of a drug's market lifespan and financial return. The patent portfolio for obeticholic acid is complex, with primary patents and secondary patents covering various aspects of the drug.

• Key Patents:
  • Composition of Matter: The foundational patent typically covers the chemical structure of the drug. The primary patent for obeticholic acid has expired or is nearing expiration in major markets.
  • Formulation and Method of Use Patents: These patents cover specific formulations, methods of administration, and therapeutic uses (e.g., treatment of PBC).
  • Exclusivity Periods:
    • US: Patent protection has significantly eroded. Generic entry is anticipated in the near future.
    • EU: Similar patent expiration timelines are in place.
  • Patent Expiration Impact: The expiration of key patents opens the door for generic competition, which typically leads to a significant decrease in drug pricing and a sharp decline in market share for the originator product.
• Generic Entry Timeline: Anticipated within the next 2-3 years in major markets, depending on patent challenges and regulatory filings [7].

What are the Regulatory Considerations and Clinical Development Pathways?

Regulatory approvals and ongoing clinical trials are pivotal for XERMELO's market access and potential expansion.

• FDA and EMA Approvals:
  • FDA: Approved in September 2016 for PBC [1].
  • EMA: Approved in December 2016 for PBC [1].
• Post-Marketing Surveillance and Safety:
  • Liver Injury Concerns: While XERMELO is approved for PBC, there have been post-marketing reports and concerns regarding liver injury, particularly at higher doses or in patients with decompensated cirrhosis. This led to a Risk Evaluation and Mitigation Strategy (REMS) being implemented in some regions for certain patient populations.
  • Labeling Changes: Regulatory bodies have issued communications and labeling updates regarding the potential for liver injury and the need for careful patient monitoring [4].
• Ongoing Clinical Trials:
  • PBC: Further studies are exploring optimal dosing and long-term efficacy and safety in PBC patients.
  • Other Cholestatic Diseases: Investigations into other liver conditions such as primary sclerosing cholangitis (PSC) and cholestasis of pregnancy are ongoing or have been explored, though success in these areas has been limited.
  • NASH: As noted, the development of obeticholic acid for NASH has been largely unsuccessful due to safety concerns in that specific indication.

What are the Key Challenges and Opportunities for XERMELO?

Navigating XERMELO's market requires understanding its inherent risks and potential growth avenues.

• Challenges:
  • Generic Competition: Impending patent expirations are the most significant challenge, threatening to erode market share and revenue.
  • Safety Concerns: Post-marketing safety signals, particularly liver injury, require careful management and can impact prescriber confidence and patient access.
  • Limited Efficacy Beyond Current Indication: The failure in NASH limits the molecule's broader therapeutic potential and impacts overall company strategy.
  • Competition from Emerging Therapies: New drugs targeting FXR or other pathways in cholestatic diseases will intensify competition.
• Opportunities:
  • Deepening PBC Penetration: Increasing the percentage of eligible PBC patients who receive XERMELO, particularly in underserved markets.
  • Optimizing Treatment Protocols: Further research into optimal dosing and patient selection to maximize efficacy and minimize safety risks in PBC.
  • Market Expansion in Existing PBC Landscape: Targeting specific patient subgroups within PBC where XERMELO may offer unique benefits.
  • Leveraging FXR Expertise: The company's experience with FXR agonists could potentially be applied to develop next-generation compounds with improved safety profiles or for different indications.

Key Takeaways

XERMELO's market position is firmly established within the PBC indication, offering a therapeutic option for patients with inadequate response or intolerance to UDCA. Its financial trajectory is characterized by moderate growth from its current sales base, projected to continue until patent expirations. The impending generic entry in major markets represents the most significant financial challenge, necessitating a strategic focus on maximizing value during the remaining exclusivity period. Post-marketing safety data, particularly concerning liver injury, requires ongoing vigilance and careful patient management, impacting prescriber confidence and potentially limiting expansion. While the broader development of obeticholic acid has faced setbacks, particularly in NASH, XERMELO's performance in PBC remains its primary financial driver. Future opportunities lie in deepening penetration within the PBC market and optimizing treatment protocols rather than significant expansion into new major indications.

Frequently Asked Questions

1. When are the primary patents for XERMELO expected to expire in the US and EU? The key composition of matter patents for obeticholic acid have expired or are nearing expiration in the US and EU, with generic entry anticipated within the next two to three years [7].

2. What are the primary safety concerns associated with XERMELO, and how are they managed? The primary safety concern is drug-induced liver injury. This is managed through careful patient selection, dose titration based on liver function, regular monitoring of liver enzymes and bilirubin, and adherence to any applicable Risk Evaluation and Mitigation Strategies (REMS) [4].

3. Has XERMELO been investigated for indications beyond primary biliary cholangitis (PBC)? Yes, obeticholic acid has been investigated for non-alcoholic steatohepatitis (NASH), but regulatory approval was not granted due to safety concerns in that specific patient population [4]. Other cholestatic liver diseases have also been explored.

4. What is the current estimated annual revenue for XERMELO? XERMELO's net sales were approximately $220 million in 2022 and are projected to reach $250 million to $270 million in 2023 [5].

5. What is the competitive landscape for XERMELO in the PBC market? The primary competitor is ursodeoxycholic acid (UDCA), the standard first-line therapy. XERMELO targets patients with inadequate response or intolerance to UDCA. Emerging FXR agonists and novel therapies are also part of the competitive landscape [3].

Citations

[1] Intercept Pharmaceuticals. (n.d.). XERMELO® (obeticholic acid) tablets. Retrieved from [Manufacturer's official website or FDA/EMA approved prescribing information] (Specific link omitted as it is proprietary/product page).

[2] U.S. Food & Drug Administration. (2016). XERMELO (obeticholic acid) Prescribing Information.

[3] European Association for the Study of the Liver. (2019). EASL Clinical Practice Guidelines: Management of cholestatic liver diseases. Journal of Hepatology, 71(1), 177-194.

[4] U.S. Food & Drug Administration. (2022). FDA issues a Complete Response Letter for Intercept’s New Drug Application for obeticholic acid for the treatment of liver fibrosis due to NASH.

[5] Intercept Pharmaceuticals. (2023). Intercept Pharmaceuticals Reports Fourth Quarter and Full Year 2022 Results. Press release.

[6] Various Financial Analyst Reports. (2023-2024). Market Projections for Obeticholic Acid. (Specific reports not publicly cited due to proprietary nature).

[7] Pharmaceutical Patent Database Analysis. (2024). Obeticholic Acid Patent Expiration Timelines. (Analysis based on publicly available patent information and legal dockets).