United States Patent 7,932,273: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 7,932,273, assigned to Boehringer Ingelheim International GmbH, is a significant patent in the pharmaceutical industry, particularly in the field of anticoagulant therapy. This patent protects the compound dabigatran etexilate mesylate, marketed under the brand name Pradaxa. Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.
Patent Overview
Invention Description
The patent US7932273B2 describes the compound ethyl 3-[(2-{[4-(hexyloxycarbonylaminoiminomethyl)phenylamino]methyl}-1-methyl-1H-benzimidazol-5-carbonyl)pyridin-2-ylamino]propionic acid ethylester methanesulfonate, commonly known as dabigatran etexilate mesylate. This compound is a prodrug that is converted into its active form, dabigatran, in the body. The primary applications of this compound include post-operative prophylaxis of deep vein thrombosis and the prevention of stroke[1].
Scope of the Patent
Claims
The patent includes several claims that define the scope of the invention. These claims cover:
- The chemical structure of the compound itself.
- The use of the compound as a medicament.
- Specific formulations and methods of preparation.
- The stability and storage conditions of the pharmaceutical compositions to ensure the integrity of the active substance[1].
Physicochemical Requirements
The patent emphasizes the importance of the pharmaceutical active substance having high stability under various environmental conditions. This includes stability during the preparation of the pharmaceutical formulation and in the final compositions. The compound should be only slightly hygroscopic to prevent the absorption of moisture, which can reduce the content of the active substance[1].
Patent Landscape
Expiration Dates
The patent US7932273B2 is set to expire on September 7, 2025. This expiration date marks the end of the exclusive rights granted to Boehringer Ingelheim International GmbH to manufacture and market dabigatran etexilate mesylate[2][4].
Related Patents
Several other patents are associated with dabigatran etexilate mesylate, including:
- US9034822: This patent relates to antibody molecules against anticoagulants, particularly dabigatran, and their use as antidotes. It is set to expire on January 20, 2031[2].
- US7866474: This patent covers other aspects of the drug, such as dosage and mode of administration, and has already had maintenance fees paid up to certain years[4].
Generic Availability
With the patent expiration approaching, generic versions of Pradaxa are being approved. However, the commercial availability of these generics is not guaranteed immediately upon patent expiration[2].
Drug Exclusivity
In addition to patent protection, dabigatran etexilate mesylate has benefited from various exclusivity periods granted by the FDA. These include New Chemical Entity (NCE) exclusivity, New Indication exclusivity, and Pediatric Exclusivity, among others. These exclusivities have helped extend the market exclusivity period for the drug beyond the patent expiration dates[4].
Stability and Storage
The patent highlights the importance of stability in the pharmaceutical formulation. The compound has different polymorphic forms with specific melting points, and its stability is crucial to maintain its pharmacological potency. Storage conditions must protect the drug from moisture to prevent degradation[1].
Clinical Applications
Dabigatran etexilate mesylate is used in clinical settings for several critical applications:
- Post-operative Prophylaxis: It is used to prevent deep vein thrombosis in patients undergoing surgery.
- Stroke Prevention: It is also used to prevent stroke in patients with atrial fibrillation[1].
Regulatory Considerations
The FDA has approved dabigatran etexilate mesylate under the brand name Pradaxa, and it has been designated as a Reference Listed Drug (RLD) for generic equivalents. Any generic version must demonstrate bioequivalence to the RLD to gain approval[2].
Economic and Market Impact
The expiration of the patent and the subsequent entry of generic versions are expected to significantly impact the market. Generic competition can reduce the price of the drug, making it more accessible to patients. However, it also means that Boehringer Ingelheim will lose its exclusive market share for dabigatran etexilate mesylate[2][4].
Patent Quality and Scope
The debate on patent quality and scope is relevant here. The patent claims for dabigatran etexilate mesylate are specific and well-defined, which is crucial for maintaining patent quality. The scope of the patent is narrowed to ensure clarity and avoid overly broad claims that could impede innovation[3].
Key Takeaways
- Patent Expiration: The patent US7932273B2 expires on September 7, 2025.
- Generic Availability: Generic versions of Pradaxa are being approved but may not be immediately commercially available.
- Stability and Storage: The compound must be stored under conditions that protect it from moisture to maintain its stability.
- Clinical Applications: Dabigatran etexilate mesylate is used for post-operative prophylaxis and stroke prevention.
- Regulatory Considerations: The drug is an RLD, and generics must demonstrate bioequivalence.
FAQs
What is the primary use of dabigatran etexilate mesylate?
Dabigatran etexilate mesylate is primarily used for the post-operative prophylaxis of deep vein thrombosis and the prevention of stroke in patients with atrial fibrillation.
When does the patent for dabigatran etexilate mesylate expire?
The patent US7932273B2 for dabigatran etexilate mesylate is set to expire on September 7, 2025.
What are the implications of patent expiration for Boehringer Ingelheim?
The expiration of the patent means that Boehringer Ingelheim will lose its exclusive rights to manufacture and market dabigatran etexilate mesylate, allowing generic versions to enter the market.
How does the FDA regulate generic versions of Pradaxa?
Generic versions of Pradaxa must demonstrate bioequivalence to the Reference Listed Drug (RLD) to gain FDA approval.
What are the storage requirements for dabigatran etexilate mesylate?
The drug must be stored under conditions that protect it from moisture to prevent degradation and maintain its stability.
Cited Sources
- US7932273B2 - Google Patents
- Generic Pradaxa Availability - Drugs.com
- Patent Claims and Patent Scope - Hoover Institution
- Pradaxa patent expiration - Pharsight - GreyB
