United States Patent 8,545,884: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 8,545,884, titled "Solid pharmaceutical formulations comprising BIBW 2992," is a significant patent in the pharmaceutical industry, particularly for the drug Afatinib. This patent, held by Boehringer Ingelheim, pertains to the formulation and manufacturing process of Afatinib dimaleate, a tyrosine kinase inhibitor used in the treatment of certain types of cancer.
Background of Afatinib
Afatinib, marketed under the brand name Gilotrif, is a potent inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It is used primarily in the treatment of non-small cell lung cancer (NSCLC) with specific EGFR mutations. The drug's efficacy and safety profile have made it a crucial component in the therapeutic arsenal against this type of cancer[2].
Patent Overview
Patent Number and Expiration
The patent number is 8,545,884, and it is set to expire on December 19, 2029. This expiration date is critical for generic manufacturers seeking to enter the market with their own versions of Afatinib[2].
Claims and Scope
The patent claims cover solid pharmaceutical formulations of Afatinib dimaleate, specifically focusing on the manufacturing process and the resulting tablet formulation. Here are some key aspects of the claims:
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Manufacturing Process: The patent describes a method of preparing Afatinib dimaleate tablets using dry granulation via roller compaction. This process involves an intermediate compaction step, which is crucial for achieving the desired tablet properties such as hardness, disintegration time, and dissolution profiles[5].
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Formulation: The claims include specific formulations of Afatinib dimaleate, ensuring that the tablets have adequate hardness, proper disintegration time, and appropriate dissolution profiles. These characteristics are essential for the drug's bioavailability and efficacy[5].
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Stability: The patent also addresses the storage stability of the tablets, ensuring that the formulation remains effective over time[5].
Patent Landscape
Related Patents
The patent landscape surrounding Afatinib includes several other patents that protect different aspects of the drug and its use. Here are some notable patents:
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U.S. Patent Number 8,426,586: This patent, set to expire on October 10, 2029, is another key patent related to Afatinib. It is subject to litigation and paragraph IV certifications by generic manufacturers[2].
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U.S. Patent Number 9,539,258: This method-of-use patent, expiring on November 9, 2026, does not claim any indication or other conditions of use for which generic manufacturers are seeking approval[2].
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U.S. Patent Number 10,004,743: Expiring on July 5, 2030, this patent was submitted after the ANDA (Abbreviated New Drug Application) submission and does not create a statutory stay of approval for generic versions[2].
Litigation and Regulatory Aspects
The patent has been involved in litigation, particularly with Sun Pharmaceutical Industries Limited, which sought to market its own version of Afatinib tablets. The litigation was initiated within the statutory 45-day period, and final approval of the generic version cannot be granted until the patent expires or is found invalid or not infringed by the court[2].
Impact of Proposed USPTO Rule Changes
Although not directly related to this specific patent, proposed rule changes by the USPTO regarding terminal disclaimers could have significant implications for patent portfolios in the pharmaceutical industry. The withdrawn proposal aimed to prevent multiple patents directed to obvious variants of an invention, which could have led to the invalidation of entire groups of patents. This would have had far-reaching consequences for companies holding strategic patent portfolios, including those in the pharmaceutical sector[4].
Challenges and Future Directions
Manufacturing Process Improvements
The current manufacturing process described in the patent involves dry granulation via roller compaction, which is tedious and requires specific equipment. There is a need for more convenient and cost-effective manufacturing processes suitable for large-scale production. Future innovations may focus on developing alternative methods that minimize losses during manufacturing while maintaining the desired tablet properties[5].
Generic Competition
As the patent expiration dates approach, generic manufacturers are preparing to enter the market. The regulatory landscape, including the need for paragraph IV certifications and the resolution of litigation, will play a crucial role in determining when and how these generic versions can be approved and marketed[2].
Key Takeaways
- Patent Expiration: The patent is set to expire on December 19, 2029, which will open the market to generic competition.
- Manufacturing Process: The current process involves dry granulation via roller compaction, but there is a need for more efficient and cost-effective methods.
- Litigation and Regulatory Aspects: Ongoing litigation and regulatory requirements will influence the timing and approval of generic versions.
- Patent Landscape: The patent is part of a broader landscape that includes other related patents protecting different aspects of Afatinib.
FAQs
Q: What is the primary focus of United States Patent 8,545,884?
A: The primary focus is on the solid pharmaceutical formulations of Afatinib dimaleate, including the manufacturing process and resulting tablet formulation.
Q: What is the manufacturing process described in the patent?
A: The process involves dry granulation via roller compaction, which includes an intermediate compaction step.
Q: When is the patent set to expire?
A: The patent is set to expire on December 19, 2029.
Q: What are the implications of the patent expiration for generic manufacturers?
A: The expiration will allow generic manufacturers to enter the market with their own versions of Afatinib, provided they comply with regulatory requirements and resolve any ongoing litigation.
Q: How does the proposed USPTO rule change affect this patent?
A: Although the proposed rule change was withdrawn, it could have had significant implications for patent portfolios in the pharmaceutical industry by potentially invalidating entire groups of patents tied together via terminal disclaimers.
Sources
- US8545884B2 - Solid pharmaceutical formulations comprising BIBW 2992 - Google Patents
- Afatinib Tablets - accessdata.fda.gov
- Patent Claims and Patent Scope - Hoover Institution
- Threat to Many Patent Portfolios Fades as USPTO Withdraws Controversial Proposed Rule - Procopio
- Pharmaceutical compositions comprising Afatinib - Justia Patents
