United States Patent 8,168,209: A Detailed Analysis
Overview of the Patent
United States Patent 8,168,209, titled "Method and composition for administering an NMDA receptor antagonist to a subject," is a significant patent in the field of neuropharmacology. This patent, issued to Forest Laboratories, Inc., pertains to the administration of NMDA receptor antagonists, particularly memantine, for treating various central nervous system (CNS) related conditions.
Claims of the Patent
The patent includes several key claims that define its scope and protection:
Claim 1: Composition and Administration
Claim 1 describes a solid pharmaceutical composition comprising an extended release formulation of an NMDA receptor antagonist, such as memantine, in a dose range of 5 to 40 mg. This claim is crucial as it specifies the dosage form and the amount of the active ingredient[4].
Claim Specifics: Dosage and Release
The claims detail the release profile of the NMDA receptor antagonist, stating that the rate of release is less than 80%, 70%, 60%, 50%, 40%, 30%, 20%, or 10% of the rate for an immediate release (IR) formulation over various time periods (1, 2, 4, 6, 8, 10, or 12 hours). This ensures a controlled and sustained release of the drug, reducing the need for dose escalation and minimizing side effects[4].
Non-Dose Escalating Formulations
The patent emphasizes non-dose escalating formulations, which can be administered once or twice daily. This is a significant advancement as it simplifies the treatment regimen and improves patient compliance[4].
Scope of Protection
Therapeutic Applications
The patent covers a wide range of therapeutic applications, including the treatment of conditions associated with deregulation in NMDA receptor activity. These conditions include neurodegenerative diseases (such as Alzheimer's disease and Parkinson's disease), seizure disorders, pain syndromes, dementias, cerebrovascular conditions, movement disorders, brain trauma, and various neuropathies[4].
Combination Therapies
While the patent primarily focuses on memantine, it also suggests the potential for combination therapies with other agents, such as acetylcholinesterase inhibitors (ACheI), to enhance therapeutic effects. This is evident from related patents that describe combinations of NMDA receptor antagonists with ACheIs for treating CNS-related conditions[1].
Patent Landscape and Litigation
Litigation History
The patent has been involved in several litigation cases, particularly regarding generic drug approvals. For instance, Forest Laboratories, Inc. has taken legal action against generic drug manufacturers, such as Teva Pharmaceuticals, to protect the patent's exclusivity. These cases often revolve around the validity and enforceability of the patent claims[2][5].
Generic Challenges
Generic drug manufacturers have challenged the patent by filing Abbreviated New Drug Applications (ANDAs) with the FDA, alleging that the patent claims are invalid, unenforceable, or not infringed by their generic products. These challenges highlight the ongoing battles in the pharmaceutical industry to protect intellectual property while facilitating generic competition[2].
Technological and Pharmaceutical Significance
Extended Release Formulations
The patent's focus on extended release formulations is technologically significant. These formulations allow for a more controlled release of the drug, reducing the peak concentration and thus minimizing side effects. This is particularly important for drugs like memantine, which can have significant CNS side effects if not managed properly[4].
Patient Compliance
The once or twice daily dosing regimen facilitated by these extended release formulations improves patient compliance. Simplified treatment regimens are crucial for managing chronic conditions, as they reduce the burden on patients and caregivers[4].
Economic and Market Impact
Market Protection
The patent provides Forest Laboratories, Inc. with significant market protection, allowing the company to maintain exclusivity over the extended release memantine formulations. This protection is critical in the pharmaceutical industry, where billions of dollars are invested in research and development[3].
Generic Competition
The expiration of this patent would open the market to generic competition, potentially reducing the cost of treatment for patients. However, the ongoing litigation and challenges to the patent's validity indicate that the exclusivity period may be extended or contested[2].
Key Takeaways
- Extended Release Formulations: The patent covers extended release formulations of memantine, which provide a controlled and sustained release of the drug.
- Therapeutic Applications: The patent applies to a broad range of CNS-related conditions, including neurodegenerative diseases and pain syndromes.
- Litigation and Challenges: The patent has been involved in several litigation cases, particularly regarding generic drug approvals and challenges to its validity.
- Technological Significance: The extended release formulations are technologically significant, improving patient compliance and reducing side effects.
- Market Impact: The patent provides significant market protection, but its expiration could lead to generic competition and reduced treatment costs.
Frequently Asked Questions (FAQs)
Q: What is the primary focus of United States Patent 8,168,209?
A: The primary focus is on methods and compositions for administering an NMDA receptor antagonist, specifically memantine, in extended release formulations.
Q: What are the therapeutic applications covered by this patent?
A: The patent covers various CNS-related conditions, including neurodegenerative diseases, seizure disorders, pain syndromes, and other neuropathies.
Q: Why are extended release formulations important in this patent?
A: Extended release formulations reduce the need for dose escalation, minimize side effects, and improve patient compliance by allowing once or twice daily dosing.
Q: Has this patent been involved in any litigation?
A: Yes, the patent has been involved in several litigation cases, particularly regarding generic drug approvals and challenges to its validity.
Q: What is the economic impact of this patent?
A: The patent provides significant market protection, allowing Forest Laboratories, Inc. to maintain exclusivity over the extended release memantine formulations, which is crucial for the company's market strategy and revenue.
Cited Sources
- US8580858B2 - Compositions for the treatment of CNS-related conditions - Google Patents
- IN THE UNITED STATES DISTRICT COURT FOR THE DISTRICT ... - Insight.RPXcorp.com
- Eviscerating Patent Scope - DigitalCommons@NYLS
- US8168209B2 - Method and composition for administering an NMDA receptor antagonist to a subject - Google Patents
- Forest Labs., Inc. v. Teva Pharms. USA, Inc. - Casetext
