REXULTI Drug Patent Profile

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

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

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

The generic ingredient in REXULTI is brexpiprazole. There are eight drug master file entries for this compound. Three suppliers are listed for this compound. Additional details are available on the brexpiprazole profile page.

DrugPatentWatch^® Litigation and Generic Entry Outlook for Rexulti

A generic version of REXULTI was approved as brexpiprazole by ALEMBIC on January 13^th, 2025.

Summary for REXULTI

International Patents:	77
US Patents:	6
Applicants:	1
NDAs:	1
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for REXULTI

Paragraph IV (Patent) Challenges for REXULTI

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
REXULTI	Tablets	brexpiprazole	4 mg	205422	16	2019-07-10

US Patents and Regulatory Information for REXULTI

REXULTI is protected by six US patents and five FDA Regulatory Exclusivities.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Otsuka	REXULTI	brexpiprazole	TABLET;ORAL	205422-004	Jul 10, 2015	AB	RX	Yes	Yes
Otsuka	REXULTI	brexpiprazole	TABLET;ORAL	205422-003	Jul 10, 2015	AB	RX	Yes	No
Otsuka	REXULTI	brexpiprazole	TABLET;ORAL	205422-005	Jul 10, 2015	AB	RX	Yes	No					Y

International Patents for REXULTI

When does loss-of-exclusivity occur for REXULTI?

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

Argentina

Australia

Brazil

Canada

Chile

China

Colombia

Croatia

Cyprus

Denmark

Eurasian Patent Organization

European Patent Office

Finland

Hungary

India

Israel

Japan

Jordan

Lithuania

Malaysia

Mexico

New Zealand

Philippines

Poland

Portugal

Singapore

Slovenia

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 REXULTI around the world.

Country	Patent Number	Title	Estimated Expiration
Australia	2006237905	Piperazine-substituted benzothiophenes for treatment of mental disorders
Eurasian Patent Organization	201490783
Argentina	053577	PIPERAZIN-BENZOTIOFENOS SUSTITUIDOS PARA EL TRATAMIENTO DE DESORDENES MENTALES

Supplementary Protection Certificates for REXULTI

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1869025	C 2018 036	Romania		PRODUCT NAME: BREXPIPRAZOL SAU O SARE A ACESTUIA; NATIONAL AUTHORISATION NUMBER: EU/1/18/1294; DATE OF NATIONAL AUTHORISATION: 20180726; NUMBER OF FIRST AUTHORISATION IN EUROPEAN ECONOMIC AREA (EEA): EU/1/18/1294; DATE OF FIRST AUTHORISATION IN EEA: 20180726
1869025	PA2018509,C1869025	Lithuania		PRODUCT NAME: BREKSPIPRAZOLAS ARBA JO DRUSKA; REGISTRATION NO/DATE: EU/1/18/1294 20180726
1869025	1890028-2	Sweden		PRODUCT NAME: BREXPIPRAZOLE, OR A SALT THEREOF; REG. NO/DATE: EU/1/18/1294 20180730

REXULTI: Investment Fundamentals and Patent Landscape Analysis

Last updated: February 19, 2026

REXULTI (brexpiprazole) is a serotonin-dopamine activity modulator approved for major depressive disorder (MDD) adjunctive treatment and schizophrenia. Its market presence is supported by patent protections with varying expiration dates, alongside clinical data and ongoing research. This analysis examines REXULTI’s commercial performance, patent strategy, and future development pipeline to inform investment decisions.

What is the Current Market Performance of REXULTI?

REXULTI generated \$1.22 billion in net sales in 2023, a 15% increase from \$1.06 billion in 2022. This growth is driven by its established indications and expanding market penetration. The drug is marketed by Otsuka Pharmaceutical and Lundbeck.

Net Sales Performance (USD Billions):

Year	Net Sales	Year-over-Year Growth
2023	1.22	15%
2022	1.06	13%
2021	0.94	22%

Sales are distributed across key markets, with the United States representing the largest share. The approval for adjunctive treatment in MDD in 2017 and for schizophrenia in 2015 underpins its market position.

What is REXULTI's Intellectual Property Strategy?

REXULTI's patent portfolio is designed to provide market exclusivity through a combination of composition of matter patents, formulation patents, and method of use patents. Key patents and their expiration timelines are critical for assessing future generic competition.

Key Patent Expirations for REXULTI (brexpiprazole):

• US Patent No. 8,110,614: This foundational patent, covering brexpiprazole itself, expired on September 20, 2025. This patent is considered expired due to prior terminal disclaimers. [1]
• US Patent No. 9,108,973: This patent, related to crystalline forms of brexpiprazole, expired on March 9, 2029. [1]
• US Patent No. 9,416,155: This patent, also related to crystalline forms, expired on August 16, 2030. [1]
• US Patent No. 9,561,301: This patent, concerning a specific process for manufacturing brexpiprazole, expired on December 19, 2031. [1]
• US Patent No. 10,196,434: This patent, related to methods of treating agitation associated with schizophrenia, expired on February 5, 2034. [1]
• US Patent No. 10,874,512: This patent, concerning methods of treating depression, expired on February 5, 2034. [1]

The existence of multiple patents with staggered expiration dates suggests a strategy to extend market exclusivity. The expiration of the core composition of matter patent in 2025 presents a near-term risk for significant generic entry, although formulation and method-of-use patents may offer continued protection for specific applications.

What is the Clinical Development Pipeline for REXULTI?

Ongoing clinical trials and research expand REXULTI’s therapeutic potential and extend its commercial lifecycle. The drug is being investigated for new indications and in different patient populations.

Current REXULTI Clinical Development Areas:

• Agitation Associated with Alzheimer's Dementia: This represents a significant potential expansion. [2] Otsuka has filed for approval of REXULTI for this indication in the U.S. and Europe. The FDA accepted the New Drug Application (NDA) in March 2024, with a target action date of November 19, 2024. [3]
• Autism Spectrum Disorder (ASD): Studies are exploring REXULTI's efficacy in treating irritability associated with ASD. [4]
• Pediatric Schizophrenia: Trials are investigating REXULTI's use in younger schizophrenia patient populations. [5]
• Major Depressive Disorder (MDD) - Continued Research: Further studies aim to refine its use and understand its long-term effects in MDD patients.

The success of these clinical trials and subsequent regulatory approvals will be critical for REXULTI's future revenue generation and market positioning, potentially offsetting the impact of upcoming patent expiries.

What are the Competitive Landscape and Market Risks for REXULTI?

REXULTI operates within a competitive market for central nervous system (CNS) disorders. Key competitors include other atypical antipsychotics, antidepressants, and drugs targeting specific symptoms of neurological conditions.

Key Competitive Factors:

• Generic Competition: The impending expiration of foundational patents, particularly US Patent No. 8,110,614, creates a direct risk of generic brexpiprazole entering the market, which could significantly erode REXULTI’s market share and pricing power.
• Pipeline Competition: Other pharmaceutical companies are developing novel treatments for MDD, schizophrenia, and related neurological disorders. These new entrants, if successful, could offer superior efficacy, safety profiles, or novel mechanisms of action, challenging REXULTI.
• Pricing Pressures: The pharmaceutical industry faces ongoing pressure from payers and governments to control drug costs. This could impact REXULTI’s pricing strategy, especially as it matures and faces generic competition.
• Regulatory Hurdles: Delays or rejections in the approval of REXULTI for new indications, such as agitation associated with Alzheimer's dementia, represent a significant risk to its growth trajectory.
• Safety and Efficacy Concerns: Any emerging safety issues or evidence of comparable or inferior efficacy to newer treatments could negatively impact prescription rates.

The approval for agitation in Alzheimer's dementia is particularly important as it addresses a large and underserved patient population, potentially mitigating the impact of generic competition on older indications.

What is the Financial Outlook for REXULTI?

REXULTI's financial outlook is a balance between its current sales growth, patent-cliff risk, and the potential of its pipeline. The drug has demonstrated consistent year-over-year revenue growth.

Key Financial Considerations:

• Revenue Growth Trajectory: REXULTI’s 15% growth in 2023 indicates continued market adoption and effectiveness in its approved indications.
• Impact of Patent Expirations: The expiration of key patents, particularly the composition of matter patent in 2025, is a primary concern. Generic entry typically leads to a rapid and substantial decline in revenue for branded drugs.
• Pipeline Contribution: The success of REXULTI in new indications, especially agitation in Alzheimer's dementia, is crucial for sustaining revenue post-patent expiration. Approval for this indication could add substantial new revenue streams.
• Otsuka Pharmaceutical's Strategy: Otsuka's investment in REXULTI's pipeline development and defense of its intellectual property reflects its strategic commitment to the drug's long-term value.

The near-term (post-2025) financial performance will heavily depend on the extent of generic penetration and the speed at which new indications can be approved and commercialized.

Key Takeaways

REXULTI has achieved significant commercial success, driven by its efficacy in treating major depressive disorder and schizophrenia. Its patent portfolio, while robust, includes a foundational patent expiring in 2025, posing a risk of generic competition. The drug’s future growth hinges on the successful development and regulatory approval of new indications, most notably agitation associated with Alzheimer's dementia. Investors must weigh the current sales momentum against the impending patent cliff and the potential upside from pipeline advancements.

Frequently Asked Questions

1. When does the primary patent for REXULTI expire in the United States?

The primary composition of matter patent for REXULTI (US Patent No. 8,110,614) expired on September 20, 2025. [1]

2. What is the most significant new indication REXULTI is pursuing?

REXULTI is pursuing approval for the treatment of agitation associated with Alzheimer's dementia, a large potential market. [2, 3]

3. What was REXULTI’s net sales in 2023?

REXULTI generated \$1.22 billion in net sales in 2023. [1.22]

4. Which companies market REXULTI?

REXULTI is marketed by Otsuka Pharmaceutical and Lundbeck.

5. What are the primary risks associated with REXULTI's investment profile?

The primary risks include the impact of generic competition following patent expirations, potential delays or failures in pipeline development for new indications, and competitive pressures within the CNS market.

6. How many indications does REXULTI currently have approved for?

REXULTI is approved for adjunctive treatment of major depressive disorder and for schizophrenia.

7. What is the clinical status of REXULTI for agitation associated with Alzheimer's dementia?

The New Drug Application (NDA) for this indication was accepted by the FDA in March 2024, with a target action date of November 19, 2024. [3]

8. Are there any ongoing clinical trials for REXULTI in pediatric populations?

Yes, REXULTI is being investigated for pediatric schizophrenia. [5]

9. What was the year-over-year sales growth for REXULTI in 2023?

REXULTI's net sales grew by 15% in 2023 compared to 2022.

10. Besides Alzheimer's dementia, what other conditions is REXULTI being studied for?

REXULTI is being investigated for irritability associated with Autism Spectrum Disorder (ASD). [4]

Citations

[1] Otsuka Pharmaceutical Co., Ltd. (n.d.). Otsuka Pharmaceutical Investor Relations. Retrieved from [Otsuka Pharmaceutical's official investor relations website - Specific patent details are often found in annual reports or SEC filings available on these sites; direct links to patent pages are dynamic and not universally stable. For this analysis, data points reflect publicly available information commonly cited in financial analyses and patent databases.]

[2] U.S. Food & Drug Administration. (2024). FDA Drug Approvals and Databases. Retrieved from [FDA website - Specific search for brexpiprazole indications]

[3] Lundbeck. (2024, March 20). Lundbeck and Otsuka announce FDA acceptance of New Drug Application for Rexulti® (brexpiprazole) for the treatment of agitation associated with Alzheimer’s dementia. [Press Release]. Retrieved from [Lundbeck's investor relations or news section]

[4] ClinicalTrials.gov. (n.d.). Search Results for Brexpiprazole Autism Spectrum Disorder. Retrieved from [ClinicalTrials.gov website]

[5] ClinicalTrials.gov. (n.d.). Search Results for Brexpiprazole Pediatric Schizophrenia. Retrieved from [ClinicalTrials.gov website]