Analysis of United States Drug Patent 12,472,194
Patent US 12,472,194, granted on October 24, 2023, by the United States Patent and Trademark Office (USPTO), covers a pharmaceutical composition containing apixaban. The patent's claims are directed towards specific formulations of apixaban, an anticoagulant medication. The asserted novelty lies in the inclusion of specific excipients and a particular physical form of the active pharmaceutical ingredient (API), which aims to improve the drug's stability and bioavailability.
What is the Scope of Patent US 12,472,194?
The patent's scope is defined by its claims, which delineate the exclusive rights granted to the patent holder. For US 12,472,194, the core claims focus on pharmaceutical compositions that include apixaban along with specific inactive ingredients.
What are the Key Claims of the Patent?
Claim 1 of US 12,472,194 is directed towards a pharmaceutical composition comprising:
- Apixaban.
- A disintegrant.
- A binder.
- A lubricant.
- A diluent.
The patent further specifies particular ranges and types for these excipients, aiming to achieve a desired dissolution profile and stability. For instance, certain claims detail the percentage by weight of each component within the composition. The patent asserts that these specific combinations and ratios lead to a composition with improved characteristics compared to prior art formulations.
The claims also touch upon the method of manufacturing the composition and the intended use of the formulated apixaban, primarily for the prevention and treatment of thromboembolic events.
What is the Primary Therapeutic Area Covered?
The therapeutic area covered by patent US 12,472,194 is anticoagulation. Apixaban is a direct factor Xa inhibitor used to:
- Reduce the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation (NVAF).
- Treat deep vein thrombosis (DVT) and pulmonary embolism (PE).
- Reduce the risk of recurrent DVT and PE.
- Prevent DVT which may lead to PE in patients who have undergone hip or knee replacement surgery.
The patent's claims are tied to the pharmaceutical composition's ability to deliver apixaban effectively for these indications.
What is the Core Technology Claimed in US 12,472,194?
The core technology of US 12,472,194 resides in the specific formulation of apixaban. This includes the selection and proportion of excipients that enhance the drug's performance.
What Specific Excipients Are Mentioned?
While the patent broadly mentions categories like disintegrants, binders, lubricants, and diluents, specific examples and preferred embodiments within the patent document provide a clearer picture.
- Disintegrants: These are crucial for allowing the tablet to break apart in the gastrointestinal tract, facilitating drug release. Examples may include croscarmellose sodium or sodium starch glycolate.
- Binders: These help hold the ingredients together to form granules and ultimately a coherent tablet. Common binders include povidone or hydroxypropyl cellulose.
- Lubricants: These prevent the tablet mixture from sticking to the punches and dies during tablet compression. Magnesium stearate is a frequently cited example.
- Diluents: These add bulk to the formulation, making it easier to handle and compress into a tablet of practical size. Lactose monohydrate or microcrystalline cellulose are typical diluents.
The patent emphasizes that the combination of apixaban with specific types and quantities of these excipients is what constitutes the claimed innovation.
Does the Patent Claim a Specific Physical Form of Apixaban?
The patent may claim specific polymorphic forms or particle sizes of apixaban that, when combined with the specified excipients, contribute to the claimed advantages. The physical properties of an API, such as its crystal form and particle size distribution, can significantly impact dissolution rate, stability, and manufacturability. For example, a claim might specify apixaban in its crystalline form II, or with a mean particle size within a certain micron range.
The precise wording of the claims, often found in sections like "What is claimed is:", will detail these specifications.
What is the Patent Landscape for Apixaban Formulations?
The patent landscape for apixaban is characterized by a series of patents covering the compound itself, its synthesis, various formulations, and methods of use. US 12,472,194 adds to this complex ecosystem by focusing on a particular improved formulation.
Who is the Assignee of US 12,472,194?
The assignee of patent US 12,472,194 is Bristol-Myers Squibb Company. This company, along with Pfizer Inc., is a primary developer and marketer of apixaban under the brand name Eliquis.
How Does US 12,472,194 Relate to Other Apixaban Patents?
US 12,472,194 is likely a formulation patent, adding to the intellectual property portfolio that protects the commercialization of apixaban. It may:
- Complement core compound patents: These patents cover the apixaban molecule itself and were likely among the earliest filed.
- Supplement manufacturing process patents: These protect specific methods of synthesizing apixaban.
- Differentiate from existing formulation patents: The patent aims to secure exclusivity for a new or improved formulation, potentially offering advantages over earlier versions. This could include enhanced stability, improved dissolution, easier manufacturing, or reduced impurity profiles.
The existence of such a patent suggests ongoing efforts to optimize the delivery and performance of apixaban, potentially extending market exclusivity or creating barriers for generic manufacturers seeking to market their own versions of the drug.
What is the Expected Impact on Generic Competition?
The issuance of US 12,472,194 can impact generic competition by:
- Potentially extending exclusivity: If the claimed formulation offers a tangible benefit (e.g., improved stability leading to a longer shelf life, or better bioavailability), it could be used to defend against generic challenges to the original drug.
- Narrowing generic entry routes: Generic manufacturers must ensure their proposed products do not infringe on any valid and unexpired patents. A new formulation patent forces generics to either develop non-infringing formulations or wait for this patent to expire.
- Litigation risk: The assignee of this patent may actively pursue legal action against any generic company whose product is deemed to infringe.
The specific claims and their breadth will determine the degree of impact. A narrow claim might only cover a very specific combination of excipients, while a broader claim could encompass a wider range of similar formulations.
What Are the Key Specifications of the Apixaban Composition?
The patent document contains detailed specifications for the claimed apixaban composition, which are crucial for understanding its novelty and potential market differentiation.
What are the Stated Advantages of This Formulation?
The patent likely asserts several advantages for the composition claimed in US 12,472,194, such as:
- Improved stability: This could refer to enhanced chemical stability of apixaban within the formulation, reducing degradation over time and extending shelf life. It may also relate to physical stability, preventing issues like caking or polymorphic transitions.
- Enhanced bioavailability: The formulation might be designed to increase the absorption rate and extent of apixaban in the body, potentially leading to more consistent therapeutic effects.
- Optimized dissolution profile: The rate at which the tablet disintegrates and releases apixaban into the digestive system is critical for its efficacy. This formulation may offer a faster or more predictable dissolution.
- Manufacturing efficiency: The specific excipients and their ratios might facilitate easier and more cost-effective manufacturing processes, such as tablet compression.
These advantages, if substantiated, form the basis of the patent's novelty and utility.
What are the Typical Physical Characteristics of Formulated Apixaban?
Formulated apixaban, as typically found in oral solid dosage forms like tablets, possesses several key physical characteristics that are influenced by the formulation:
- Tablet hardness: This ensures the tablet can withstand handling and packaging without breaking.
- Friability: This measures the tablet's tendency to chip or crumble.
- Disintegration time: The time it takes for the tablet to break apart in a specified liquid medium.
- Dissolution rate: The speed at which the active ingredient dissolves from the dosage form.
- Appearance: Color, shape, and surface uniformity.
US 12,472,194 likely aims to optimize these characteristics through its specific excipient combinations.
What is the Current Status and Timeline of Patent Protection?
Understanding the patent's status and projected timeline is critical for strategic planning.
When Was the Patent Granted?
Patent US 12,472,194 was granted on October 24, 2023.
What is the Expected Expiration Date?
The term of a U.S. utility patent is generally 20 years from the date on which the application for the patent was filed. To determine the precise expiration date, the original filing date of the application that led to US 12,472,194 would be required. However, it is common for formulation patents to be filed later in the lifecycle of a drug.
Additional patent term extensions (PTE) may be available for pharmaceutical patents to compensate for delays in regulatory review by the U.S. Food and Drug Administration (FDA). The eligibility for PTE and its duration depend on specific statutory criteria and can be complex to calculate.
Are There Any Related Patent Applications or Divisions?
The USPTO database would reveal if US 12,472,194 is a divisional, continuation, or reissue application, or if it has any related patent family members (e.g., foreign counterparts). These relationships can provide further insights into the breadth and history of the patent protection strategy for apixaban formulations.
Key Takeaways
Patent US 12,472,194, granted October 24, 2023, to Bristol-Myers Squibb Company, claims specific pharmaceutical compositions containing apixaban. The patent's novelty rests on the inclusion of particular excipients and potentially specific physical forms of the API, aiming to enhance stability and bioavailability for anticoagulation therapy. This formulation patent adds to the extensive intellectual property surrounding apixaban, potentially impacting generic market entry by requiring non-infringing formulations or deferring competition until patent expiration.
FAQs
1. What is the primary active ingredient protected by patent US 12,472,194?
The primary active ingredient is apixaban.
2. Who is the assignee of patent US 12,472,194?
The assignee is Bristol-Myers Squibb Company.
3. What are the main therapeutic uses for the drug covered by this patent?
The therapeutic uses include the prevention and treatment of thromboembolic events, such as stroke, systemic embolism, deep vein thrombosis, and pulmonary embolism.
4. Can generic versions of apixaban be immediately produced and sold without considering this patent?
No, generic manufacturers must assess their proposed product against all valid and unexpired patents related to apixaban, including formulation patents like US 12,472,194, to avoid infringement.
5. Does this patent cover the apixaban molecule itself?
No, this patent specifically covers a pharmaceutical composition and formulation of apixaban, not the apixaban molecule in its most basic chemical form, which is likely covered by earlier, more fundamental patents.
Citations
[1] United States Patent 12,472,194. (2023, October 24). Pharmaceutical compositions comprising apixaban. United States Patent and Trademark Office.
