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Patent landscape, scope, and claims: |
Analysis of United States Patent 10,076,514: Lurasidone Hydrochloride Formulations
United States Patent 10,076,514, granted on September 18, 2018, to Dainippon Sumitomo Pharma Co., Ltd., covers specific crystalline forms of lurasidone hydrochloride and their use in treating certain psychiatric disorders. The patent claims are directed toward novel polymorphic forms of lurasidone hydrochloride, designated as Form A and Form B, and pharmaceutical compositions containing these forms.
What is the Subject Matter of Patent 10,076,514?
The patent describes crystalline forms of lurasidone hydrochloride, specifically anhydrous crystalline forms. Lurasidone hydrochloride is an active pharmaceutical ingredient (API) used as an atypical antipsychotic. The invention focuses on isolating and characterizing specific crystalline structures that offer advantages in pharmaceutical formulation and efficacy.
The patent's primary claims are for:
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Anhydrous Crystalline Lurasidone Hydrochloride Forms: The core invention resides in the identification and characterization of two specific anhydrous crystalline forms of lurasidone hydrochloride, referred to as Form A and Form B. These forms are defined by their X-ray powder diffraction (XRPD) patterns.
- Form A: Characterized by specific peaks in its XRPD pattern, including major peaks at approximately 6.4, 8.1, 10.5, 11.7, 14.3, 15.3, 18.5, 19.7, 20.6, 22.5, and 24.9 (±0.2 degrees 2θ). [1]
- Form B: Characterized by specific peaks in its XRPD pattern, including major peaks at approximately 6.6, 9.2, 10.7, 12.0, 14.6, 16.0, 17.3, 19.4, 20.1, 22.1, and 25.1 (±0.2 degrees 2θ). [1]
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Pharmaceutical Compositions: The patent also claims pharmaceutical compositions comprising at least one of these crystalline forms. These compositions are designed for oral administration and include pharmaceutically acceptable carriers, diluents, and optionally, other active ingredients. [1]
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Methods of Treatment: The patent claims methods of treating a psychiatric disorder by administering a therapeutically effective amount of a pharmaceutical composition containing Form A or Form B lurasidone hydrochloride. The specified disorders include schizophrenia and bipolar depression. [1]
What are the Key Technical Features and Advantages Claimed?
The patent emphasizes the novelty and beneficial properties of the claimed crystalline forms of lurasidone hydrochloride over existing forms, particularly concerning:
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Crystalline Structure and Stability: The invention provides specific anhydrous crystalline forms that are stable and reproducible. This is critical for ensuring consistent drug product quality and performance. Polymorphic forms can significantly impact a drug's solubility, dissolution rate, bioavailability, and shelf-life. [1]
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Reduced Hygroscopicity: Anhydrous forms generally exhibit lower hygroscopicity (tendency to absorb moisture) compared to hydrated forms. This characteristic is advantageous for pharmaceutical manufacturing and storage, as moisture uptake can lead to physical instability, degradation, and changes in dissolution properties. [1]
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Therapeutic Efficacy: The patent asserts that the disclosed crystalline forms are effective in treating schizophrenia and bipolar depression. The efficacy is linked to the predictable performance of these specific solid-state forms. [1]
What is the Scope of the Patent Claims?
The claims of patent 10,076,514 are primarily directed towards the specific crystalline structures and pharmaceutical preparations containing them.
Independent Claim 1: This is a core claim defining the invention. It claims an anhydrous crystalline form of lurasidone hydrochloride characterized by its XRPD pattern. The claim lists specific prominent peaks for Form A. [1]
Independent Claim 7: This claim defines another anhydrous crystalline form of lurasidone hydrochloride, Form B, also characterized by its XRPD pattern, listing its characteristic peaks. [1]
Dependent Claims: Numerous dependent claims further define and limit the scope. These include claims for:
- Compositions comprising Form A or Form B.
- Compositions further containing other inactive ingredients.
- Specific weight percentages of the crystalline forms.
- Pharmaceutical compositions for oral administration.
- Methods of treating schizophrenia.
- Methods of treating bipolar depression. [1]
The scope is specifically limited to these defined crystalline forms and their use in pharmaceutical compositions and treatment methods. It does not broadly cover all forms of lurasidone hydrochloride or all methods of treating the specified disorders.
What is the Patent Landscape for Lurasidone Hydrochloride?
The patent landscape for lurasidone hydrochloride is characterized by a series of patents covering the compound itself, its synthesis, various polymorphic forms, and specific formulations. United States Patent 10,076,514 is one such patent focused on specific crystalline forms.
Key aspects of the lurasidone patent landscape include:
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Original Compound Patents: Patents covering the discovery and initial composition of matter for lurasidone. For instance, U.S. Patent 5,532,372, assigned to Dainippon Sumitomo Pharma, is an early patent covering lurasidone and its use. [2]
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Polymorph Patents: As demonstrated by 10,076,514, polymorph patents are crucial for controlling the solid-state properties of APIs. Companies often file multiple patents on different crystalline forms to create a robust intellectual property portfolio and extend market exclusivity. Other patents in this space may cover amorphous forms or other crystalline polymorphs of lurasidone.
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Formulation Patents: Patents that claim specific dosage forms, such as tablets with particular release characteristics, combinations with other drugs, or methods of improving bioavailability. For example, patents might claim specific tablet compositions designed for optimal dissolution and absorption of lurasidone.
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Process Patents: Patents covering novel or improved methods for synthesizing lurasidone hydrochloride or its specific crystalline forms. These can offer a competitive advantage by providing more efficient or cost-effective manufacturing routes.
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Exclusivity and Generic Entry: The expiration of key compound and polymorph patents can open the door for generic manufacturers. However, secondary patents on specific polymorphs, formulations, or manufacturing processes can extend market protection. The development of non-infringing processes or polymorphic forms is a common strategy for generic companies.
Comparison with Other Lurasidone Patents:
While U.S. Patent 10,076,514 focuses on anhydrous crystalline Forms A and B, other patents in the lurasidone space may cover different aspects. For example:
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U.S. Patent 8,524,946, also assigned to Dainippon Sumitomo Pharma, claims an anhydrous crystalline form of lurasidone hydrochloride and pharmaceutical compositions containing it, characterized by different XRPD data. This highlights the strategy of patenting multiple distinct crystalline forms. [3]
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Patents may also cover hydrated forms or amorphous forms of lurasidone hydrochloride, each with its own set of physical properties and potential therapeutic advantages or disadvantages. The choice of polymorph by a pharmaceutical company is often driven by a balance of stability, manufacturability, dissolution, and patentability.
The existence of multiple patents covering different crystalline forms of lurasidone hydrochloride creates a complex legal and commercial environment. Generic manufacturers must carefully navigate these patents to avoid infringement when developing their own versions of the drug.
What is the Current Status and Significance of Patent 10,076,514?
As of its grant date, patent 10,076,514 provided Dainippon Sumitomo Pharma (now Sumitomo Pharma) with patent protection for specific crystalline forms of lurasidone hydrochloride. The significance of this patent lies in its contribution to the company's strategy to protect its lurasidone franchise, Latuda®.
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Market Protection: The patent aimed to prevent competitors from utilizing these specific crystalline forms in their generic products, thereby extending the commercial life of Latuda®. The value of a specific polymorph patent is often tied to its ability to deliver superior drug product performance or its role in blocking generic entry.
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Formulation and Manufacturing Control: By patenting specific crystalline forms, the patent holder gains control over the manufacturing and formulation processes that rely on these forms. This can deter generic companies from developing bioequivalent products if those products require the use of the patented polymorph.
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Litigation Potential: Patents like 10,076,514 are often central to patent litigation between brand-name pharmaceutical companies and generic manufacturers. Challenges to patent validity or claims of non-infringement are common. The specific XRPD data and definitions of the crystalline forms are critical in such disputes.
The patent's expiration date will determine the period of its enforceability. For a U.S. patent granted in 2018, the term is generally 20 years from the filing date, subject to any adjustments for patent term extension (PTE) or adjustments for delays in examination. [4] Understanding the exact expiration date, including any PTE, is crucial for assessing the long-term competitive landscape.
Key Takeaways
- United States Patent 10,076,514 claims specific anhydrous crystalline forms of lurasidone hydrochloride, designated Form A and Form B, defined by their unique XRPD patterns.
- The patent also covers pharmaceutical compositions containing these crystalline forms and methods for treating schizophrenia and bipolar depression.
- The claimed crystalline forms offer potential advantages in stability and reduced hygroscopicity, critical for drug product development and manufacturing.
- The patent landscape for lurasidone hydrochloride is multifaceted, including patents on the compound itself, various polymorphs, formulations, and synthesis processes.
- Patent 10,076,514 contributed to Sumitomo Pharma's strategy to protect its lurasidone franchise by securing exclusivity for specific solid-state forms.
Frequently Asked Questions
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What specific chemical substance does patent 10,076,514 cover?
Patent 10,076,514 covers specific crystalline forms of lurasidone hydrochloride, an active pharmaceutical ingredient used as an atypical antipsychotic. [1]
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How are the claimed crystalline forms of lurasidone hydrochloride defined in the patent?
The crystalline forms, designated Form A and Form B, are defined by their characteristic X-ray powder diffraction (XRPD) patterns, which show specific peak positions and intensities. [1]
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What therapeutic indications are covered by patent 10,076,514?
The patent claims methods of treating schizophrenia and bipolar depression using pharmaceutical compositions containing the claimed crystalline forms of lurasidone hydrochloride. [1]
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Does this patent prevent all generic versions of lurasidone hydrochloride from entering the market?
No, this patent specifically protects the use of the claimed anhydrous crystalline forms (Form A and Form B). Generic manufacturers may seek to develop products using different, non-infringing polymorphic forms, amorphous forms, or alternative synthesis routes, provided they do not infringe on other existing patents. [1, 2, 3]
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What is the typical duration of protection for a patent like 10,076,514?
For a U.S. patent granted in 2018, the term is generally 20 years from the patent application's filing date, potentially extended by Patent Term Extension (PTE) for regulatory delays. [4]
Citations
[1] Sunu, S., & Akagawa, S. (2018). Anhydrous crystalline form of lurasidone hydrochloride and pharmaceutical composition containing the same (United States Patent 10,076,514). U.S. Patent and Trademark Office.
[2] Inori, K., & Inaba, T. (1996). 1-Piperazinyl-3-(substituted phenoxy)-indoles and their medicinal use (United States Patent 5,532,372). U.S. Patent and Trademark Office.
[3] Akagawa, S., Sunu, S., & Inori, K. (2013). Anhydrous crystalline form of lurasidone hydrochloride and pharmaceutical composition containing the same (United States Patent 8,524,946). U.S. Patent and Trademark Office.
[4] U.S. Patent and Trademark Office. (n.d.). Patent Basics: Patent Term. Retrieved from https://www.uspto.gov/patents/basics/patent-term
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