United States Patent 10,849,916: A Detailed Analysis of Scope and Claims
Overview of the Patent
The United States Patent 10,849,916, titled "Stable liquid formulations of cyclophosphamide and its impurities," is a significant development in the field of pharmaceuticals, particularly in the formulation and stabilization of cyclophosphamide, a widely used chemotherapeutic agent. Here is a detailed analysis of the scope and claims of this patent.
Background of Cyclophosphamide
Cyclophosphamide is a potent anticancer drug used in the treatment of various types of cancers and some autoimmune disorders. However, its formulation and stability have been challenging due to its chemical properties and the presence of impurities.
Scope of the Patent
Novel Impurities and Stabilization
The patent focuses on novel impurities of cyclophosphamide, specifically those with structures V, VI, or VII, and methods to stabilize these impurities in liquid formulations. This is crucial because the stability of cyclophosphamide is essential for its efficacy and safety in clinical use[1].
Formulation Composition
The patent describes stable liquid formulations that include cyclophosphamide and its impurities. These formulations are designed to maintain the therapeutic efficacy of cyclophosphamide while minimizing the impact of impurities. The compositions typically include cyclophosphamide, solvents such as alcohols (e.g., ethanol, propylene glycol), and other pharmaceutically acceptable adjuvants[4].
Claims of the Patent
Key Claims
-
Stable Liquid Formulations:
- The patent claims stable liquid formulations of cyclophosphamide that can be stored at temperatures between about 2°C to about 8°C without significant degradation[1][4].
-
Impurity Control:
- The formulations are designed to control the levels of specific impurities, ensuring that they do not exceed certain thresholds. For example, related compounds B, D, E, and F are limited to specific percentages (e.g., not more than 0.50% for related compound B and not more than 1.5% for related compound E)[4].
-
Shelf-Life Specifications:
- The patent specifies that the formulations should have no more than 4.0% total impurities and no more than 0.2% of any unspecified impurity at the end of 24 months when stored under the specified conditions[4].
-
Preparation Processes:
- The patent also includes claims related to the processes for preparing these stable liquid formulations, ensuring that the methods used do not compromise the stability or purity of the cyclophosphamide[1].
Patent Landscape
Current Patent Status
- The patent (US10849916B2) is currently active and is set to expire on July 13, 2035. This means that any generic versions of the drug cannot be launched until after this date, unless there are changes in the patent's status due to legal activities such as term extensions or amendments to the claims[2][5].
Related Patents
- There are other patents related to cyclophosphamide formulations, such as US10993952 and US11382923, which also focus on stable liquid formulations and processes for their preparation. These patents are held by different entities, including Dr. Reddy's and Avyxa Holdings, and have similar expiry dates around 2035-2036[2][5].
International Patent Filings
- The patent landscape for cyclophosphamide formulations is not limited to the United States. There are international filings, such as the European Patent Application EP4226926, which covers similar aspects of stable cyclophosphamide formulations and their preparation processes[4].
Implications for the Pharmaceutical Industry
Generic Drug Launch
- The active status of these patents means that generic versions of cyclophosphamide liquid formulations cannot be launched until the patents expire. This gives the patent holders exclusive rights to manufacture and market these formulations until then[2][5].
Research and Development
- The detailed specifications and claims in these patents provide a roadmap for researchers and manufacturers to develop stable and effective cyclophosphamide formulations. This can drive innovation in the field, leading to better therapeutic outcomes and improved patient safety[1][4].
Regulatory Compliance
- Pharmaceutical companies must ensure that their formulations comply with the specifications outlined in these patents to avoid infringement. This includes adhering to the impurity limits and storage conditions specified in the patent claims[4].
Key Takeaways
- Stable Formulations: The patent provides methods for creating stable liquid formulations of cyclophosphamide.
- Impurity Control: The formulations are designed to control specific impurities within defined limits.
- Shelf-Life: The formulations must meet specific shelf-life criteria when stored under defined conditions.
- Patent Status: The patent is active until July 13, 2035, affecting the launch of generic versions.
- International Filings: Similar patents exist internationally, such as in Europe.
FAQs
What is the main focus of United States Patent 10,849,916?
The main focus is on stable liquid formulations of cyclophosphamide and its impurities, ensuring the stability and efficacy of the drug.
Who holds the patent for US10849916B2?
The patent is held by Avyxa Holdings.
When is the patent set to expire?
The patent is set to expire on July 13, 2035.
What are the key components of the stable liquid formulations described in the patent?
The formulations include cyclophosphamide, solvents like ethanol and propylene glycol, and other pharmaceutically acceptable adjuvants.
How do the impurity specifications affect the formulation?
The specifications ensure that the levels of specific impurities do not exceed certain thresholds, maintaining the drug's efficacy and safety.
Are there other related patents for cyclophosphamide formulations?
Yes, there are other patents, such as US10993952 and US11382923, which also focus on stable liquid formulations and their preparation processes.
Sources
- US10849916B2 - Stable liquid formulations of cyclophosphamide and its impurities - Google Patents
- Drug Patents containing Cyclophosphamide - Pharsight
- Patent Landscape Report on Ritonavir - WIPO (for general context on patent landscapes)
- EP004226926A1 - Stable formulation of cyclophosphamide - European Patent Office
- Cyclophosphamide patent expiration - Pharsight