METHYLNALTREXONE BROMIDE - Generic Drug Details

What are the generic sources for methylnaltrexone bromide and what is the scope of patent protection?

Methylnaltrexone bromide is the generic ingredient in two branded drugs marketed by Actavis Llc, Mylan Labs Ltd, Salix Pharms, and Salix, and is included in four NDAs. There are twelve patents protecting this compound and three Paragraph IV challenges. Additional information is available in the individual branded drug profile pages.

Methylnaltrexone bromide has one hundred and twenty-three patent family members in thirty-six countries.

There are three drug master file entries for methylnaltrexone bromide. One supplier is listed for this compound. There is one tentative approval for this compound.

Summary for METHYLNALTREXONE BROMIDE

International Patents:	123
US Patents:	12
Tradenames:	2
Applicants:	4
NDAs:	4
Drug Master File Entries:	3
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	36
Clinical Trials:	17
Patent Applications:	449
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for METHYLNALTREXONE BROMIDE
What excipients (inactive ingredients) are in METHYLNALTREXONE BROMIDE?	METHYLNALTREXONE BROMIDE excipients list
DailyMed Link:	METHYLNALTREXONE BROMIDE at DailyMed

Recent Clinical Trials for METHYLNALTREXONE BROMIDE

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

Sponsor	Phase
University of Alabama at Birmingham	N/A
Bausch Health Americas, Inc.	Phase 2/Phase 3
Karolinska University Hospital	Phase 4

See all METHYLNALTREXONE BROMIDE clinical trials

Generic filers with tentative approvals for METHYLNALTREXONE BROMIDE

Applicant	Application No.	Strength	Dosage Form
		12MG/0.6ML	SOLUTION;SUBCUTANEOUS

The 'tentative' approval signifies that the product meets all FDA standards for marketing, and, but for the patents / regulatory protections, it would approved.

Pharmacology for METHYLNALTREXONE BROMIDE

Drug Class	Opioid Antagonist
Mechanism of Action	Opioid Antagonists

Anatomical Therapeutic Chemical (ATC) Classes for METHYLNALTREXONE BROMIDE

A06AH	Peripheral opioid receptor antagonists
A06A	DRUGS FOR CONSTIPATION
A06	DRUGS FOR CONSTIPATION
A	Alimentary tract and metabolism

N07BB	Drugs used in alcohol dependence
N07B	DRUGS USED IN ADDICTIVE DISORDERS
N07	OTHER NERVOUS SYSTEM DRUGS
N	Nervous system

Paragraph IV (Patent) Challenges for METHYLNALTREXONE BROMIDE

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
RELISTOR	Tablets	methylnaltrexone bromide	150 mg	208271	1	2016-09-06
RELISTOR	Injection	methylnaltrexone bromide	8 mg/0.4 mL, Single Dose Prefilled Syringe	021964	1	2015-09-08
RELISTOR	Injection	methylnaltrexone bromide	12 mg/0.6 mL, Single Dose Vial	021964	1	2015-07-22

US Patents and Regulatory Information for METHYLNALTREXONE BROMIDE

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Salix Pharms	RELISTOR	methylnaltrexone bromide	SOLUTION;SUBCUTANEOUS	021964-001	Apr 24, 2008		RX	Yes	Yes	8,822,490		Y
Salix Pharms	RELISTOR	methylnaltrexone bromide	SOLUTION;SUBCUTANEOUS	021964-001	Apr 24, 2008		RX	Yes	Yes	12,303,592		Y
Salix Pharms	RELISTOR	methylnaltrexone bromide	SOLUTION;SUBCUTANEOUS	021964-001	Apr 24, 2008		RX	Yes	Yes	8,420,663

Expired US Patents for METHYLNALTREXONE BROMIDE

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Salix	RELISTOR	methylnaltrexone bromide	TABLET;ORAL	208271-001	Jul 19, 2016	6,559,158
Salix Pharms	RELISTOR	methylnaltrexone bromide	SOLUTION;SUBCUTANEOUS	021964-003	Sep 27, 2010	9,669,096
Salix Pharms	RELISTOR	methylnaltrexone bromide	SOLUTION;SUBCUTANEOUS	021964-002	Sep 27, 2010	10,376,584

EU/EMA Drug Approvals for METHYLNALTREXONE BROMIDE

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
Bausch Health Ireland Limited	Relistor	methylnaltrexone bromide	EMEA/H/C/000870Treatment of opioid-induced constipation in advanced-illness patients who are receiving palliative care when response to usual laxative therapy has not been sufficient.	Authorised	no	no	no	2008-07-01

International Patents for METHYLNALTREXONE BROMIDE

Country	Patent Number	Title	Estimated Expiration
South Africa	201808498	ORAL FORMULATIONS AND LIPOPHILIC SALTS OF METHYLNALTREXONE
Ukraine	111717	СКЛАД ДЛЯ ПЕРОРАЛЬНОГО ВВЕДЕННЯ І ЛІПОФІЛЬНІ СОЛІ МЕТИЛНАЛТРЕКСОНУ
Russian Federation	2008138266	СОСТАВЫ ДЛЯ ПАРЕНТЕРАЛЬНОГО ВВЕДЕНИЯ ЛЕКАРСТВ И ИХ ПРИМЕНЕНИЯ

Market Dynamics and Financial Trajectory for Methylnaltrexone Bromide

Last updated: July 27, 2025

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Introduction

Methylnaltrexone Bromide, a peripherally acting opioid antagonist, has gained prominence in the management of opioid-induced constipation (OIC), a common adverse effect in opioid therapy. The drug's pharmacological profile, regulatory landscape, and evolving market dynamics shape its commercial trajectory. This analysis provides an in-depth view of the market factors influencing Methylnaltrexone Bromide's financial prospects, outlining industry drivers, challenges, and emerging opportunities.

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Pharmacological Profile and Therapeutic Indications

Methylnaltrexone Bromide is a derivative of naltrexone, formulated for peripherally restricted activity. Its primary indication is the treatment of OIC in patients undergoing opioid therapy for chronic pain or palliative care. Its selectivity limits central nervous system (CNS) penetration, reducing opioid withdrawal symptoms and dependence-related concerns.

The drug's efficacy, safety profile, and ease of oral administration position it as a preferred choice among physicians managing OIC, especially in oncology, hospice, and pain management settings. Its approval in various markets hinges on demonstrating superior safety and tolerability compared to existing options such as methylnaltrexone and naloxegol.

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Market Drivers

1. Rising Prevalence of Chronic Pain and Opioid Usage

The global surge in chronic pain conditions, driven by aging populations and increasing incidences of cancer, correlates directly with higher opioid prescriptions. According to the CDC, approximately 20% of adults in the U.S. suffer from chronic pain, with opioids frequently prescribed for management [1]. Consequently, the incidence of OIC has escalated, underscoring the need for effective management strategies.

2. Growing Awareness and Clinical Guidelines

Expanded awareness among healthcare providers about the adverse effects of opioids, including constipation, has led to endorsed therapeutic guidelines. Organizations like the American Society of Clinical Oncology recommend proactive management of OIC, fostering demand for targeted treatments like Methylnaltrexone Bromide.

3. Patent Expirations and Development of Orally Administered Agents

With some competitors nearing patent expiry, pharmaceutical companies are further investing in developing and commercializing orally available, non-invasive formulations, positioning Methylnaltrexone Bromide favorably in the market.

4. Regulatory Approvals and Reimbursement Policies

The approval of Methylnaltrexone Bromide by key regulatory agencies and favorable reimbursement policies significantly influence market penetration. In the U.S., the FDA’s approval and coverage decisions, along with European Medicines Agency (EMA) endorsements, enhance market confidence and access.

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Market Challenges

1. Competition from Established Agents

Methylnaltrexone Bromide faces competition from well-established drugs such as Methylnaltrexone (Relistor/Relistor SubQ) and Naloxegol (Movantik). These competitors have broad clinical acceptance, extensive post-marketing data, and entrenched provider familiarity.

2. Pricing and Cost-Effectiveness Concerns

Cost considerations play a critical role in formulation adoption. Drugs priced significantly higher than existing therapies may face reimbursement hurdles, especially in cost-sensitive healthcare settings.

3. Limited Awareness in Developing Markets

While the drug enjoys strong recognition in mature markets, awareness remains limited in developing regions. Challenges include regulatory delays, distribution logistics, and healthcare infrastructure constraints.

4. Regulatory Hurdles and Labeling

Additional clinical trials to expand indications or strengthen safety profiles are often necessary. Stringent regulatory processes may delay market entry or expansion in certain jurisdictions.

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Financial Trajectory

1. Revenue Trends and Sales Forecasts

Based on current market penetration, regional adoption, and competitive positioning, Methylnaltrexone Bromide's sales are projected to grow at a Compound Annual Growth Rate (CAGR) of approximately 8-12% over the next five years. North America remains the dominant market, accounting for over 60% of global sales, driven by the high prevalence of opioid therapy and reimbursement support [2].

2. Pricing Strategies

Pharmaceutical firms are adopting tiered pricing models to enhance access in emerging markets. Premium pricing in developed economies compensates for high development costs and regulatory investments, potentially limiting immediate widespread adoption but supporting sustainable revenues.

3. Market Entry and Expansion

Expansion into Europe, Japan, and emerging markets offers substantial growth potential. Strategic partnerships, licensing agreements, and local manufacturing are pivotal for accelerating market penetration and increasing revenue streams.

4. R&D and Pipeline Development

Investments in formulation improvements, such as extended-release variants and combination therapies, could expand the drug’s indications and improve patient adherence. Success in clinical trials for new indications or patient populations can significantly impact revenue trajectories.

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Key Market Segments

a. Hospital and Specialty Clinics

High prescription volume due to inpatient opioid use and cancer care. These providers prioritize efficacy and safety, favoring drugs with proven clinical data.

b. Long-term Care and Palliative Settings

Growing in importance with aging populations, these settings demand effective OIC management solutions, supporting steady demand.

c. Outpatient and Primary Care

As awareness grows, prescribing in outpatient settings increases, although market competition remains intense.

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Regulatory and Market Outlook

The regulatory landscape is increasingly supportive, emphasizing evidence-based use. Pending drug approvals or label expansions will further influence financial outcomes. However, the market's vanguard depends on demonstrating cost-benefit advantages over generics and off-label use.

In conclusion, while Methylnaltrexone Bromide’s market is poised for steady growth, its success hinges on competitive positioning, pricing strategies, and ongoing clinical validation. Companies that leverage regional expansion, clinical differentiation, and strategic alliances can optimize long-term financial gains.

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Key Takeaways

• Demand for Methylnaltrexone Bromide is driven by the rising prevalence of opioid therapy and associated constipation.
• Market growth is robust in North America, with significant expansion potential in Europe and emerging markets.
• Competition from established agents remains a primary challenge, necessitating differentiation through clinical data and pricing.
• Regulatory approvals and reimbursement policies heavily influence revenue trajectories.
• Innovation in formulations and indications can unlock new revenue streams and extend market dominance.

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FAQs

1. How does Methylnaltrexone Bromide differentiate itself from other opioid antagonists?
It is selectively peripherally acting, minimizing central side effects like opioid withdrawal, which differentiates it from other antagonists that might cross the blood-brain barrier.

2. What factors influence the pricing and reimbursement of Methylnaltrexone Bromide?
Regulatory approval, clinical efficacy, safety profile, competitive landscape, and healthcare payer policies determine pricing and reimbursement decisions.

3. What is the outlook for market competition in this therapeutic area?
The landscape is competitive, with multiple agents approved. Differentiation relies on clinical data, ease of administration, safety, and cost-effectiveness.

4. Are there new indications or formulations under development for Methylnaltrexone Bromide?
Yes, ongoing research aims to develop extended-release formulations and explore additional indications such as opioid dependence complications.

5. How might global regulatory trends impact the future market for Methylnaltrexone Bromide?
Stringent regulatory standards require extensive clinical data, but supportive policies can facilitate market entry and expansion, enhancing financial trajectories.

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References

[1] Centers for Disease Control and Prevention (CDC). (2022). Opioid Prescriptions in the US.
[2] MarketsandMarkets. (2021). Opioid-Induced Constipation Pharmacological Market Forecasts.