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-four patent family members in thirty-seven countries.

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

DrugPatentWatch^® Generic Entry Outlook for Rexulti

Rexulti was eligible for patent challenges on July 10, 2019.

There have been twenty-four patent litigation cases involving the patents protecting this drug, indicating strong interest in generic launch. Recent data indicate that 63% of patent challenges are decided in favor of the generic patent challenger and that 54% of successful patent challengers promptly launch generic drugs.

There are five tentative approvals for the generic drug (brexpiprazole), which indicates the potential for near-term generic launch.

Indicators of Generic Entry

Summary for REXULTI

International Patents:	74
US Patents:	6
Applicants:	1
NDAs:	1
Finished Product Suppliers / Packagers:	2
Raw Ingredient (Bulk) Api Vendors:	80
Clinical Trials:	11
Patent Applications:	322
Drug Prices:	Drug price information for REXULTI
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for REXULTI
What excipients (inactive ingredients) are in REXULTI?	REXULTI excipients list
DailyMed Link:	REXULTI at DailyMed

See drug prices for REXULTI

Recent Clinical Trials for REXULTI

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

Sponsor	Phase
Unity Health Toronto	Phase 4
McMaster University	Phase 4
University Health Network, Toronto	Phase 4

See all REXULTI clinical trials

Pharmacology for REXULTI

Drug Class

Atypical Antipsychotic

Paragraph IV (Patent) Challenges for REXULTI

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
REXULTI	Tablets	brexpiprazole	0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg and 4 mg	205422	18	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		RX	Yes	Yes
Otsuka	REXULTI	brexpiprazole	TABLET;ORAL	205422-003	Jul 10, 2015		RX	Yes	No
Otsuka	REXULTI	brexpiprazole	TABLET;ORAL	205422-005	Jul 10, 2015		RX	Yes	No	RE48059*PED				Y
Otsuka	REXULTI	brexpiprazole	TABLET;ORAL	205422-006	Jul 10, 2015		RX	Yes	No	RE48059*PED				Y
Otsuka	REXULTI	brexpiprazole	TABLET;ORAL	205422-005	Jul 10, 2015		RX	Yes	No	9,839,637*PED				Y
Otsuka	REXULTI	brexpiprazole	TABLET;ORAL	205422-005	Jul 10, 2015		RX	Yes	No	10,307,419*PED				Y
Otsuka	REXULTI	brexpiprazole	TABLET;ORAL	205422-005	Jul 10, 2015		RX	Yes	No

EU/EMA Drug Approvals for REXULTI

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
Otsuka Pharmaceutical Netherlands B.V.	Rxulti	brexpiprazole	EMEA/H/C/003841 Treatment of schizophrenia.	Authorised	no	no	no	2018-07-26

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

Hungary

India

Israel

Japan

Jordan

Lithuania

Malaysia

Mexico

New Zealand

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
Canada	2851588	COMPRIME COMPRENANT DE LA 7-[4-(4-BENZO[B]THIOPHEN-4-YL-PIPERAZIN-1-YL) BUTOXY]-1H-QUINOLIN-2-ONE OU UN SEL DE CELLE-CI (TABLET COMPRISING 7-[4-(4-BENZO[B]THIOPHEN-4-YL-PIPERAZIN-1-YL)BUTOXYL)-1H-QUINOLIN-2-ONE OR A SALT THEREOF)
Cyprus	1122460
Malaysia	173370	TABLET COMPRISING 7-[4-(4-BENZO[B]THIOPHEN-4-YL-PIPERAZIN-1-YL)BUTOXY]-1H-QUINOLIN-2-ONE OR A SALT THEREOF
Poland	1869025
Denmark	2767285
Mexico	2014004135	TABLETA QUE COMPRENDE 7-[4-(4-BENZO[B]TIOFEN-4-IL-PIPERAZIN-1-IL)B UTOXI]-1H-QUINOLIN-2-ONA O SAL DE LA MISMA. (TABLET INCLUDING 7-[4-(4-BENZO[ï1⁄2 ]THIOPHEN-4-YL-PIPERAZIN-1-YL) BUTOXY]-1H-QUINOLIN-2-ONE OR SALT THEREOF.)
South Korea	20140075754	TABLET INCLUDING 7-[4-(4-BENZO[B]THIOPHEN-4-YL-PIPERAZIN-1-YL)BUTOXY]-1H-QUINOLIN-2-ONE OR SALT THEREOF

Supplementary Protection Certificates for REXULTI

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1869025	32/2018	Austria		PRODUCT NAME: BREXPIPRAZOL ODER EIN SALZ DAVON; REGISTRATION NO/DATE: EU/1/18/1294 (MITTEILUNG) 20180727
1869025	1890028-2	Sweden		PRODUCT NAME: BREXPIPRAZOLE, OR A SALT THEREOF; REG. NO/DATE: EU/1/18/1294 20180730
1869025	2018/034	Ireland		PRODUCT NAME: BREXPIPRAZOLE OR A SALT THEREOF; NAT REGISTRATION NO/DATE: EU/1/18/1294 20180726; FIRST REGISTRATION NO/DATE: JOURNAL OF THE INTELLECTUAL PROPERTY OFFICE OF IRELAND (NO. 2402)
1869025	122018000088	Germany		PRODUCT NAME: BREXPIPRAZOL ODER EIN SALZ DAVON; REGISTRATION NO/DATE: EU/1/18/1294 20180726
1869025	PA2018509	Lithuania		PRODUCT NAME: BREKSPIPRAZOLAS ARBA JO DRUSKA; REGISTRATION NO/DATE: EU/1/18/1294 20180726
1869025	C201830050	Spain		PRODUCT NAME: BREXPIPRAZOL O UNA SAL DEL MISMO; NATIONAL AUTHORISATION NUMBER: EU/1/18/1294; DATE OF AUTHORISATION: 20180726; NUMBER OF FIRST AUTHORISATION IN EUROPEAN ECONOMIC AREA (EEA): EU/1/18/1294; DATE OF FIRST AUTHORISATION IN EEA: 20180726
1869025	C20180022 00264	Estonia		PRODUCT NAME: BREKSPIPRASOOL;REG NO/DATE: EU/1/18/1294 30.07.2018

REXULTI Market Analysis and Financial Projection Experimental

Market Dynamics and Financial Trajectory for REXULTI

Introduction

REXULTI, also known as brexpiprazole, is a medication developed by Otsuka and Lundbeck, approved for the treatment of major depressive disorder (MDD), schizophrenia, and agitation associated with dementia due to Alzheimer’s disease (AADAD). Here, we delve into the market dynamics and financial trajectory of REXULTI, highlighting its performance, challenges, and future outlook.

Mechanism of Action and Clinical Uses

REXULTI operates as a partial agonist at the dopamine D2 and serotonin 5-HT1A receptors, and as an antagonist at the serotonin 5-HT2A receptor. This unique mechanism makes it effective in treating various psychiatric conditions, including MDD, schizophrenia, and AADAD[5].

Regulatory Milestones

REXULTI was approved by the FDA in July 2015 for MDD and schizophrenia, and later by the EU Commission in July 2018. Additional approvals include its use in Canada and Brazil for MDD, schizophrenia, and AADAD, and in Australia for schizophrenia[5].

Market Performance

Revenue Growth

In recent years, REXULTI has shown significant revenue growth. For the first quarter of 2024, REXULTI generated DKK 1,115 million, representing a 7% growth in constant exchange rates (CER) and 5% in Danish krone (DKK) compared to the same period in 2023[2].

By the second quarter of 2024, REXULTI's revenue had increased to DKK 2,381 million, marking a 13% growth in CER and 12% in DKK, driven by robust demand in MDD and strong uptake in AADAD[5].

Regional Performance

The largest markets for REXULTI include the U.S., Canada, Spain, Italy, and France. In the U.S., revenue growth was partly attributed to the reinitiation of the Direct-to-consumer (DTC) campaign in February 2024, which had been paused due to FDA regulatory issues[4][5].

In Canada, REXULTI achieved an all-time high market share of 3.8% in Q1 2023, reflecting its strong performance in this region[3].

Impact of DTC Advertising

DTC advertising has been a crucial factor in REXULTI's market performance. After a four-month blackout due to FDA concerns over efficacy claims, the resumption of DTC campaigns in February 2024 led to a rebound in prescriptions. By late April 2024, total prescriptions and new-to-brand prescriptions were on the rise again[4].

Challenges and Regulatory Issues

FDA Regulatory Actions

In October 2023, the FDA issued an untitled letter to Otsuka, criticizing REXULTI's MDD efficacy claims in its advertisements. This led to a temporary halt in DTC advertising, which negatively impacted prescription growth. However, with the resumption of approved advertising materials, the trend has reversed[4].

Competitive Landscape

Market Competitors

REXULTI operates in a competitive market with other therapies for MDD, schizophrenia, and AADAD. The report highlights that emerging therapies are expected to give tough market competition to REXULTI, with late-stage emerging therapies likely to impact the market significantly[1].

SWOT Analysis

A SWOT analysis of REXULTI reveals strengths such as its unique mechanism of action and growing market share, but also weaknesses like regulatory challenges and competition from emerging therapies. Opportunities include expanding into new markets and increasing awareness through effective marketing, while threats include regulatory hurdles and competitive market dynamics[1].

Financial Trajectory

Revenue Projections

The market forecast for REXULTI indicates continued growth through 2032. The report provides detailed market size forecasts for REXULTI in the seven major markets (7MM), including the United States, EU4 (Germany, France, Italy, and Spain), the United Kingdom, and Japan[1].

Adjusted EBITDA and Gross Margin

Lundbeck's financial reports show that while the adjusted EBITDA margin for Q1 2024 decreased to 33.0%, the company's strategic brands, including REXULTI, contributed significantly to revenue growth. The gross margin increased to 80.9%, driven by higher sales and lower amortization costs[2].

Future Outlook

Market Expansion

The market scenario for schizophrenia and MDD is expected to expand due to extensive research and incremental healthcare spending globally. This expansion is likely to enable drug manufacturers to penetrate the market more effectively, benefiting REXULTI[1].

Research and Development

Lundbeck is investing heavily in research and development to support its pipeline, including targeted investments in sales and promotion for REXULTI. These efforts are expected to drive continued growth and market dominance[2][5].

Key Takeaways

• REXULTI has shown significant revenue growth driven by its performance in MDD, schizophrenia, and AADAD.
• DTC advertising has been a critical factor in its market success, despite temporary setbacks due to FDA regulatory actions.
• The drug faces competition from emerging therapies but maintains a strong market position.
• Financial projections indicate continued growth through 2032, supported by expanding market demand and strategic investments.

FAQs

What is REXULTI used for?

REXULTI is used as an adjunctive therapy for the treatment of adults with major depressive disorder (MDD), for the treatment of adults with schizophrenia, and for agitation associated with dementia due to Alzheimer’s disease (AADAD)[5].

How has FDA regulation impacted REXULTI's marketing?

The FDA's regulatory actions led to a temporary halt in DTC advertising for REXULTI's MDD efficacy claims, which negatively impacted prescription growth. However, with the resumption of approved advertising, the trend has reversed[4].

What are the key markets for REXULTI?

The largest markets for REXULTI include the U.S., Canada, Spain, Italy, and France[2][5].

How does REXULTI's mechanism of action differ from other treatments?

REXULTI operates as a partial agonist at the dopamine D2 and serotonin 5-HT1A receptors, and as an antagonist at the serotonin 5-HT2A receptor, making it unique in treating psychiatric conditions[5].

What are the future market projections for REXULTI?

The market forecast indicates continued growth for REXULTI through 2032, driven by expanding market demand and strategic investments in research and development[1].

Sources

1. REXULTI Drug Insight and Market Forecast - 2032 - Research and Markets
2. Lundbeck grows strategic brands by +17% CER reaching total revenue of DKK 5,288 million - Lundbeck
3. Financial results and business update - Lundbeck - Lundbeck
4. Lundbeck blames FDA-imposed DTC blackout for slowdown in Rexulti growth - FiercePharma
5. Lundbeck raised financial guidance following strong growth (+19% CER) - Lundbeck