Detailed Analysis of the Scope and Claims of United States Patent 10,188,663
Introduction to Fulvestrant and Patent 10,188,663
Fulvestrant, marketed under the brand name Faslodex, is a medication used for the treatment of hormone receptor-positive metastatic breast cancer in postmenopausal women, particularly those who have experienced disease progression following anti-estrogen therapy[4].
United States Patent 10,188,663, titled "Fulvestrant formulations," is one of the key patents protecting this drug. Here, we will delve into the details of this patent, including its scope, claims, and the broader patent landscape.
Patent Overview
Publication and Ownership
The patent was issued on January 29, 2019, and is owned by Fresenius Kabi USA LLC[5].
Patent Expiry
The patent is set to expire on February 14, 2034, although this date may be subject to change based on various legal activities such as patent term extensions or amendments to the claims[5].
Scope of the Patent
Therapeutic Use
The patent covers formulations of fulvestrant, which are specifically designed for the treatment of breast cancer. These formulations are intended for parenteral administration, typically through intramuscular injection[1].
Composition
The patent describes a fulvestrant composition that includes:
- Fulvestrant as the active ingredient.
- A pharmaceutically acceptable alcohol.
- Polysorbate 80.
- An antioxidant.
- Castor oil or other ricinoleate vehicles.
These components are crucial for stabilizing the fulvestrant and ensuring its solubility and stability in the formulation[1].
Formulation Stability
A key aspect of this patent is the stability of the fulvestrant formulation. The composition is designed to be storage stable, even at room temperature, which is a significant improvement over earlier formulations that required refrigeration. This stability is achieved through the combination of the mentioned ingredients, particularly the use of antioxidants to prevent oxidative degradation of fulvestrant[1].
Claims of the Patent
Independent Claims
The patent includes several independent claims that define the scope of the invention. These claims cover:
- The composition itself, including the specific ingredients and their concentrations.
- The method of preparing the composition.
- The containers and delivery systems, such as vials, ampoules, cartridges, and syringes, which are sterile and suitable for parenteral administration[1].
Dependent Claims
Dependent claims further specify the details of the composition, such as the concentration of fulvestrant (at least 40 mg/mL), the type of non-aqueous ester solvents used (e.g., benzyl benzoate), and the presence of antioxidants to prevent degradation[1].
Patent Landscape
Related Patents
Fulvestrant is protected by a series of patents, including US9271990 and US9833459, all of which are set to expire around the same time as US10188663. These patents cover various aspects of fulvestrant formulations, including different modes of administration and stability enhancements[5].
Generic Applications
Several generic applications for fulvestrant have been approved, with the first generic version approved on March 4, 2019. However, these generics will not enter the market until the expiration of the relevant patents, estimated to be around May 17, 2034[2].
International Protection
While the focus here is on U.S. patents, fulvestrant is also protected by patents in multiple countries. Understanding the global patent landscape is crucial for strategizing market entry and identifying potential generic launch points in regions with weaker patent protection[5].
Recent Legal Activities
Maintenance Fees and Issue Notifications
Recent activities on US10188663 include the payment of maintenance fees and issue notifications. For instance, the payment of the 4th-year maintenance fee was recorded on July 29, 2022, and various issue notifications were sent in January 2019[5].
Patent Scope and Stability
The patent scope has been refined through the examination process, ensuring that the claims are clear and valid. The stability of the formulation, as described in the patent, has been a key focus, with the inclusion of antioxidants and specific solvents to prevent degradation[1].
Key Takeaways
- Composition and Stability: The patent covers a specific composition of fulvestrant that includes a nonionic surfactant, a pharmaceutically acceptable alcohol, an antioxidant, and castor oil, ensuring stability and solubility.
- Parenteral Administration: The formulation is designed for intramuscular injection and is presented in sterile containers such as vials, ampoules, cartridges, or syringes.
- Patent Expiry: The patent is set to expire on February 14, 2034, subject to changes based on legal activities.
- Generic Launch: Generic versions of fulvestrant are expected to enter the market after the patent expiry, with several generic applications already approved.
- Global Protection: Fulvestrant is protected by patents in multiple countries, requiring a comprehensive understanding of the global patent landscape for market entry strategies.
FAQs
What is the primary use of Fulvestrant?
Fulvestrant is used for the treatment of hormone receptor-positive metastatic breast cancer in postmenopausal women who have experienced disease progression following anti-estrogen therapy[4].
What are the key components of the Fulvestrant formulation described in US10188663?
The formulation includes fulvestrant, a pharmaceutically acceptable alcohol, polysorbate 80, an antioxidant, and castor oil or other ricinoleate vehicles[1].
When is the patent US10188663 set to expire?
The patent is set to expire on February 14, 2034, although this date may be subject to change based on legal activities[5].
Are there any generic versions of Fulvestrant approved?
Yes, several generic versions of fulvestrant have been approved, but they will not enter the market until the relevant patents expire around May 17, 2034[2].
What is the significance of the stability of the Fulvestrant formulation?
The stability of the formulation ensures that the drug remains effective and safe for use over a long period, even when stored at room temperature, which is a significant improvement over earlier formulations[1].
Sources
- US10188663B2 - Fulvestrant formulations - Google Patents
- Drug Patents containing Fulvestrant - Pharsight
- Patent Claims and Patent Scope - Hoover Institution
- Fulvestrant: Uses, Interactions, Mechanism of Action - DrugBank
- Fulvestrant patent expiration - Pharsight
