United States Patent 9,101,540: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 9,101,540, titled "Nanoparticulate megestrol formulations," is a significant patent in the pharmaceutical industry, particularly in the field of nanoparticulate drug formulations. This patent, held by Par Pharmaceutical, Inc. and Alkermes Pharma Ireland Limited, covers innovative compositions and methods related to megestrol acetate, a drug used for various medical conditions.
Background of the Patent
The patent was granted on August 4, 2015, and it expires on the date specified in the patent documentation, assuming no extensions or adjustments. Megestrol acetate is a synthetic progestin used in the treatment of conditions such as endometriosis, dysmenorrhea, and certain types of cancer, among others[4].
Scope of the Patent
Nanoparticulate Compositions
The patent primarily focuses on nanoparticulate compositions of megestrol, which are designed to enhance the bioavailability and efficacy of the drug. These compositions consist of megestrol particles with an effective average particle size of less than about 2000 nm, often associated with at least one surface stabilizer. This nanoparticulate form improves the solubility of megestrol, a poorly soluble therapeutic agent, thereby enhancing its absorption and therapeutic effectiveness[4].
Surface Stabilizers and Carriers
The patent describes the use of surface stabilizers and pharmaceutically acceptable carriers to stabilize the nanoparticulate megestrol particles. These stabilizers can be contacted with megestrol before, during, or after the size reduction process. The pharmaceutical compositions may also include excipients to further enhance the stability and delivery of the drug[4].
Methods of Treatment
The patent covers methods of treatment using these nanoparticulate compositions for various conditions, including endometriosis, dysmenorrhea, hirsutism, uterine bleeding, neoplastic diseases, appetite enhancement, contraception, and hormone replacement therapy. It also includes methods for treating patients following castration[4].
Claims of the Patent
Composition Claims
The patent includes claims related to the composition of the nanoparticulate megestrol formulations. These claims specify the particle size, the presence of surface stabilizers, and the inclusion of pharmaceutically acceptable carriers and excipients[4].
Method Claims
Method claims cover the processes for preparing these nanoparticulate compositions, including the steps involved in size reduction and the association of surface stabilizers with the megestrol particles. Additionally, method claims encompass the use of these compositions for treating various medical conditions[4].
Patent Landscape
Related Patents
The patent is part of a family of patents related to megestrol acetate formulations. Other patents in this family include U.S. Patent Nos. 9,101,549 and 9,107,827, which also cover aspects of nanoparticulate megestrol compositions and their uses[2][5].
Litigation and Enforcement
The patent has been involved in several patent infringement lawsuits. For instance, Par Pharmaceutical, Inc. and Alkermes Pharma Ireland Limited have filed complaints against Breckenridge Pharmaceutical, Inc. and TWi Pharmaceuticals, Inc. for alleged infringement of this and related patents. These lawsuits highlight the importance of this patent in protecting the intellectual property related to nanoparticulate megestrol formulations[2][5].
Competitive Environment
The patent landscape in the field of nanoparticulate drug formulations is highly competitive. Other companies and research institutions are actively developing similar technologies, which underscores the need for robust patent protection to safeguard innovations in this area.
Economic and Market Impact
Market Value
The nanoparticulate megestrol formulations covered by this patent have significant market value. For example, Megace® ES, a product based on these formulations, generated sales of $81 million, as indicated in a press release by Breckenridge Pharmaceutical, Inc.[2].
Innovation and R&D
This patent contributes to the advancement of pharmaceutical technology by providing more effective and bioavailable formulations of megestrol acetate. It encourages further research and development in the field of nanoparticulate drug delivery systems.
Technical and Scientific Significance
Enhanced Bioavailability
The nanoparticulate form of megestrol acetate enhances the bioavailability of the drug, which is crucial for its therapeutic efficacy. This innovation addresses the challenge of poor solubility associated with traditional megestrol acetate formulations[4].
Clinical Applications
The patent's coverage of various medical conditions highlights its broad clinical applicability. The nanoparticulate compositions can be tailored for different therapeutic needs, making them versatile in clinical practice.
Regulatory Considerations
FDA Approval
Any generic or new formulation of megestrol acetate must comply with FDA regulations and may need to address the patent claims of U.S. Patent 9,101,540. This involves either obtaining a license or demonstrating non-infringement or invalidity of the patent claims[2].
Paragraph IV Certifications
Generic manufacturers often file Paragraph IV certifications with the FDA, alleging that the patents covering the brand drug are invalid, unenforceable, or will not be infringed by their generic product. This was the case with Breckenridge Pharmaceutical, Inc., which filed such a certification regarding the '540 and '576 Patents[2].
Key Takeaways
- Innovative Formulations: The patent covers nanoparticulate megestrol formulations that enhance bioavailability and therapeutic efficacy.
- Broad Clinical Applications: The compositions are used for treating various medical conditions, including endometriosis, dysmenorrhea, and neoplastic diseases.
- Litigation and Enforcement: The patent has been involved in several infringement lawsuits, highlighting its importance in protecting intellectual property.
- Market Value: The formulations have significant market value, as evidenced by the sales figures of related products.
- Regulatory Compliance: Generic manufacturers must navigate the patent landscape and comply with FDA regulations.
Frequently Asked Questions (FAQs)
What is the main focus of U.S. Patent 9,101,540?
The main focus of U.S. Patent 9,101,540 is on nanoparticulate compositions of megestrol acetate, including their preparation and use in treating various medical conditions.
How do nanoparticulate formulations improve the drug's efficacy?
Nanoparticulate formulations enhance the bioavailability of megestrol acetate by improving its solubility, which leads to better absorption and therapeutic effectiveness.
What are some of the medical conditions treated by these formulations?
These formulations are used to treat conditions such as endometriosis, dysmenorrhea, hirsutism, uterine bleeding, neoplastic diseases, and others.
Have there been any significant legal challenges related to this patent?
Yes, there have been several patent infringement lawsuits involving this patent, including cases against Breckenridge Pharmaceutical, Inc. and TWi Pharmaceuticals, Inc.
What is the regulatory impact of this patent on generic manufacturers?
Generic manufacturers must either obtain a license, demonstrate non-infringement, or show invalidity of the patent claims to avoid infringement. They may also need to file Paragraph IV certifications with the FDA.
Cited Sources:
- USPTO Search for Patents: https://www.uspto.gov/patents/search
- IN THE UNITED STATES DISTRICT COURT FOR THE ... - RPX Insight: https://insight.rpxcorp.com/litigation_documents/11728759
- Patent Claims Research Dataset - USPTO: https://www.uspto.gov/ip-policy/economic-research/research-datasets/patent-claims-research-dataset
- US9101540B2 - Nanoparticulate megestrol formulations - Google Patents: https://patents.google.com/patent/US9101540B2/en
- IN THE UNITED STATES DISTRICT COURT FOR THE DISTRICT ... - RPX Insight: https://insight.rpxcorp.com/litigation_documents/11475325
