APLENZIN Drug Patent Profile

When do Aplenzin patents expire, and what generic alternatives are available?

Aplenzin is a drug marketed by Bausch and is included in one NDA. There are eight patents protecting this drug and three Paragraph IV challenges.

This drug has fifty-two patent family members in eighteen countries.

The generic ingredient in APLENZIN is bupropion hydrobromide. There are thirty-eight drug master file entries for this compound. One supplier is listed for this compound. Additional details are available on the bupropion hydrobromide profile page.

DrugPatentWatch^® Generic Entry Outlook for Aplenzin

By analyzing the patents and regulatory protections it appears that the earliest date for generic entry will be June 27, 2026. This may change due to patent challenges or generic licensing.

There are three Paragraph IV patent challenges for this drug. This may lead to patent invalidation or a license for generic production.

There is one tentative approval for the generic drug (bupropion hydrobromide), which indicates the potential for near-term generic launch.

Indicators of Generic Entry

Summary for APLENZIN

International Patents:	52
US Patents:	8
Applicants:	1
NDAs:	1
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	20
Clinical Trials:	2
Patent Applications:	101
Drug Prices:	Drug price information for APLENZIN
Drug Sales Revenues:	Drug sales revenues for APLENZIN
What excipients (inactive ingredients) are in APLENZIN?	APLENZIN excipients list
DailyMed Link:	APLENZIN at DailyMed

See drug prices for APLENZIN

See drug sales revenues for APLENZIN

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

NDA:

022108

Dosage:

TABLET, EXTENDED RELEASE;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 APLENZIN

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

Sponsor	Phase
Valeant Pharmaceuticals International, Inc.	Phase 4
Bausch Health Americas, Inc.	Phase 4
Stanford University	Phase 4

See all APLENZIN clinical trials

Pharmacology for APLENZIN

Drug Class	Aminoketone
Mechanism of Action	Dopamine Uptake Inhibitors Norepinephrine Uptake Inhibitors
Physiological Effect	Increased Dopamine Activity Increased Norepinephrine Activity

Paragraph IV (Patent) Challenges for APLENZIN

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
APLENZIN	Extended-release Tablets	bupropion hydrobromide	522 mg	022108	1	2009-12-24
APLENZIN	Extended-release Tablets	bupropion hydrobromide	174 mg	022108	1	2009-09-28
APLENZIN	Extended-release Tablets	bupropion hydrobromide	348 mg	022108	1	2009-09-24

US Patents and Regulatory Information for APLENZIN

APLENZIN is protected by eight 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
Bausch	APLENZIN	bupropion hydrobromide	TABLET, EXTENDED RELEASE;ORAL	022108-001	Apr 23, 2008		RX	Yes	No
Bausch	APLENZIN	bupropion hydrobromide	TABLET, EXTENDED RELEASE;ORAL	022108-003	Apr 23, 2008		RX	Yes	Yes			Y
Bausch	APLENZIN	bupropion hydrobromide	TABLET, EXTENDED RELEASE;ORAL	022108-003	Apr 23, 2008		RX	Yes	Yes			Y
Bausch	APLENZIN	bupropion hydrobromide	TABLET, EXTENDED RELEASE;ORAL	022108-001	Apr 23, 2008		RX	Yes	No			Y

International Patents for APLENZIN

When does loss-of-exclusivity occur for APLENZIN?

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

Australia

Canada

China

Colombia

Costa Rica

Ecuador

European Patent Office

Hong Kong

Israel

Japan

Mexico

New Zealand

Nicaragua

Russian Federation

Singapore

South Africa

South Korea

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 APLENZIN around the world.

Country	Patent Number	Title	Estimated Expiration
South Korea	20100055402	BUPROPION HYDROBROMIDE AND THERAPEUTIC APPLICATIONS
Japan	2008546841
South Africa	201003036	BUPROPION HYDROBROMIDE AND THERAPEUTIC APPLICATIONS
World Intellectual Property Organization (WIPO)	2007002597

Supplementary Protection Certificates for APLENZIN

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
2316456	LUC00054	Luxembourg		PRODUCT NAME: NALTREXONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, IN PARTICULAR NALTREXONE HYDROCHLORIDE, AND BUPROPION OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, IN PARTICULAR BUPROPION HYDROCHLORIDE; AUTHORISATION NUMBER AND DATE: EU/1/14/988 20150330
2316456	CA 2017 00062	Denmark		PRODUCT NAME: NALTREXON ELLER ET FARMACEUTISK ACCEPTABELT SALT DERAF, ISAER NALTREXONHYDROCHLORID, OG BUPROPION ELLER ET FARMACEUTISK ACCEPTABELT SALT DERAF, ISAER BUPROPIONHYDROCHLORID; REG. NO/DATE: EU/1/14/988 20150330
2316456	1790064-8	Sweden		PRODUCT NAME: NALTREXONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, IN PARTICULAR NALTREXONE HYDROCHLORIDE, AND BUPROPION OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, IN PARTICULAR BUPROPION HYDROCHLORIDE; REG. NO/DATE: EU/1/14/988 20150330
2316456	SPC/GB17/078	United Kingdom		PRODUCT NAME: NALTREXONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, IN PARTICULAR NALTREXONE HYDROCHLORIDE, AND BUPROPION OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, IN PARTICULAR BUPROPION HYDROCHLORIDE.; REGISTERED: UK EU/1/14/988 20150330; UK PLGB 50742/0001 20150330

Market Dynamics and Financial Trajectory for Aplenzin

Introduction

Aplenzin, a bupropion hydrobromide extended-release tablet, is a significant player in the treatment of major depressive disorder (MDD) and seasonal affective disorder (SAD). Here, we delve into the market dynamics and financial trajectory of Aplenzin, exploring its unique positioning, market performance, and the factors influencing its success.

Unique Positioning of Aplenzin

Aplenzin stands out due to its unique formulation. It is the only FDA-approved single-tablet, once-daily treatment equivalent to 450 mg of bupropion HCl therapy, which typically requires two or three tablets daily[1].

• This convenience is particularly beneficial for patients who need higher doses to manage their MDD, as it simplifies their medication regimen.

Clinical Efficacy and Side Effects

Aplenzin has demonstrated clinical efficacy comparable to other antidepressants like fluoxetine, an SSRI. It also has a low incidence of certain side effects, such as weight gain and orgasm dysfunction, which are common with other antidepressants[1][4].

• In clinical trials, Aplenzin showed a low incidence of weight gain, with only 3% of patients gaining more than 5 lbs, compared to 4% on placebo[4].

Market Performance

Revenue Growth

Aplenzin, along with its counterpart Wellbutrin, has seen significant revenue growth. In the fourth quarter of 2021, combined revenue for Wellbutrin and Aplenzin grew by 16% compared to the same period in 2020[2].

• In the third quarter of 2023, Aplenzin revenue grew by 6%, although the total prescriptions (TRx) declined by 10%[5].

Competitive Landscape

The antidepressant market is highly competitive, with various generic and branded options available. Aplenzin's unique once-daily dosing and low side effect profile help it stand out in this crowded market.

• However, the market is also subject to generic competition, which can impact sales. For instance, Sanofi-Aventis faced layoffs due to generic competition affecting some of its key brands, including Aplenzin[3].

Financial Impact on Parent Companies

Sanofi-Aventis

Sanofi-Aventis, the initial marketer of Aplenzin, faced significant restructuring due to market pressures. The company laid off employees and adjusted its sales force in response to generic competition and declining sales of some of its key products, including Aplenzin[3].

Bausch Health

After Sanofi-Aventis licensed Aplenzin to Biovail Corporation (later acquired by Valeant Pharmaceuticals, now Bausch Health), Bausch Health has been responsible for its marketing and sales.

• Bausch Health has reported solid revenue growth from Aplenzin, contributing to the overall performance of its pharmaceutical segment. Despite some fluctuations, Aplenzin remains a valuable asset in their portfolio[2][5].

Market Trends and Challenges

Generic Competition

Generic competition remains a significant challenge for branded drugs like Aplenzin. The expiration of patents and the introduction of generic alternatives can erode market share and revenue.

• For example, the generic competition faced by Ambien CR, another once-blockbuster drug, has been cited as a factor in Sanofi-Aventis's restructuring efforts[3].

Regulatory Environment

The regulatory environment plays a crucial role in the financial trajectory of pharmaceuticals. FDA approvals and changes in regulatory policies can impact the market dynamics of drugs like Aplenzin.

• Aplenzin's FDA approval in 2008 marked a significant milestone, but ongoing regulatory scrutiny and potential changes in healthcare policies can influence its market position[1].

Consumer and Physician Preferences

Convenience and Compliance

The once-daily dosing of Aplenzin is a significant selling point, enhancing patient compliance and convenience.

• As Dr. Prakash Masand noted, "Aplenzin offers patients and physicians an alternative option which only requires one tablet, once a day at the highest bupropion dose. This provides a simple, convenient option for patients that currently need to take two to three tablets daily"[1].

Side Effect Profile

The low incidence of weight gain and other side effects makes Aplenzin an attractive option for both patients and physicians.

• Clinical trials have consistently shown that Aplenzin has a favorable side effect profile, which is a key factor in its market appeal[4].

Financial Projections and Outlook

Revenue Projections

Bausch Health's financial reports indicate that Aplenzin continues to contribute positively to their revenue. Despite some fluctuations, the overall trend suggests stable to growing revenue from this product.

• For the third quarter of 2023, Bausch Health reported a 6% revenue growth for Aplenzin, although with a decline in total prescriptions[5].

Market Expansion

The company is focusing on expanding its market reach, particularly in international markets. Strong demand in regions like Asia Pacific and Latin America has driven revenue growth for Bausch Health's pharmaceutical segment, including Aplenzin[5].

Key Takeaways

• Unique Formulation: Aplenzin's once-daily dosing and unique HBr salt extended-release formulation set it apart in the antidepressant market.
• Clinical Efficacy: Aplenzin has demonstrated efficacy comparable to other antidepressants with a favorable side effect profile.
• Market Performance: Despite challenges from generic competition, Aplenzin has shown revenue growth and remains a valuable asset for Bausch Health.
• Regulatory and Market Trends: The regulatory environment and market trends, including consumer and physician preferences, continue to influence Aplenzin's financial trajectory.
• Financial Projections: Stable to growing revenue projections indicate a positive outlook for Aplenzin.

FAQs

Q: What is the unique selling point of Aplenzin?

A: Aplenzin is the only FDA-approved single-tablet, once-daily treatment equivalent to 450 mg of bupropion HCl therapy, which typically requires two or three tablets daily.

Q: How does Aplenzin compare to other antidepressants in terms of side effects?

A: Aplenzin has a low incidence of weight gain and orgasm dysfunction compared to other antidepressants, making it a favorable option for patients.

Q: Which company is currently responsible for marketing and sales of Aplenzin?

A: Bausch Health is currently responsible for the marketing and sales of Aplenzin after it was licensed from Sanofi-Aventis.

Q: What are the main challenges facing Aplenzin in the market?

A: Generic competition and changes in the regulatory environment are significant challenges facing Aplenzin.

Q: How has Aplenzin performed in terms of revenue growth?

A: Aplenzin has shown revenue growth, with a 6% increase in the third quarter of 2023, although with a decline in total prescriptions.

Sources

1. Sanofi-aventis U.S. - "Aplenzin™, The Only Single Tablet Once-Daily Treatment for Major Depressive Disorder, Now Available in the United States" - PR Newswire.
2. Bausch Health Companies Inc. - "4Q & FY 2021 - Financial Results" - Bausch Health IR.
3. Pharmaceutical Executive - "Sanofi-Aventis Cuts 400 Jobs" - Pharmaceutical Executive.
4. Aplenzin - "Clinical Experience in MDD & SAD for Healthcare Professionals" - Aplenzin.
5. Bausch Health Companies Inc. - "Q3 2023 Earnings Presentation" - Bausch Health IR.