United States Patent 11,793,386: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 11,793,386, titled "Analogs of deutetrabenazine, their preparation and use," is a significant patent in the pharmaceutical industry, particularly in the treatment of movement disorders. This patent, assigned to Auspex Pharmaceuticals, Inc., delves into the development and application of deutetrabenazine analogs, which have improved pharmacokinetic properties compared to their non-deuterated counterparts.
Background on Deutetrabenazine
Deutetrabenazine is a vesicular monoamine transporter 2 (VMAT2) inhibitor used primarily for the symptomatic treatment of tardive dyskinesia and chorea associated with Huntington's disease[4]. The original compound has been a subject of extensive research and development, leading to the creation of its deuterated analogs.
Patent Overview
Publication and Assignee
The patent was issued on November 23, 2021, and is assigned to Auspex Pharmaceuticals, Inc. It is part of a series of patents related to deutetrabenazine and its analogs, reflecting the company's ongoing efforts to enhance the therapeutic efficacy and pharmacokinetic profile of this drug.
Patent Expiration Dates
The patent is set to expire on September 15, 2038, which is consistent with the typical 17-year patent term from the date of issuance, considering any potential extensions or adjustments[2].
Scope of the Patent
Claims
The patent includes claims related to the deutetrabenazine analogs, their preparation methods, and their use in pharmaceutical compositions. Here are some key aspects:
- Compounds: The patent describes various deuterium-substituted benzoquinoline compounds, which are analogs of deutetrabenazine. These compounds are designed to have improved pharmacokinetic properties, such as longer half-lives and reduced metabolism rates[1][2].
- Preparation Methods: Detailed methods for synthesizing these analogs are provided, including specific chemical reactions and purification processes. This ensures that the compounds can be consistently produced with high purity and efficacy[1].
- Pharmaceutical Compositions: The patent outlines the formulation of pharmaceutical compositions containing these deutetrabenazine analogs. This includes various dosage forms such as tablets, capsules, and oral solutions, tailored for the treatment of movement disorders[1].
Methods of Use
The patent also covers methods for the treatment of abnormal involuntary movement disorders using these deuterium-substituted compounds. This includes new dosage regimens and administration protocols designed to optimize therapeutic outcomes for conditions like tardive dyskinesia, chorea associated with Huntington's disease, and other movement disorders[2].
Pharmacokinetic Improvements
Deuterium Substitution
The use of deuterium in these analogs is a key innovation. Deuterium substitution can significantly alter the pharmacokinetic profile of a drug, often leading to improved metabolic stability and reduced side effects. This is because deuterium, being a heavier isotope of hydrogen, forms stronger bonds with carbon, thereby slowing down the metabolic breakdown of the drug[1].
Clinical Implications
The improved pharmacokinetics of these analogs can result in more consistent and sustained therapeutic effects, potentially reducing the frequency of dosing and enhancing patient compliance. This is particularly important for chronic conditions where long-term treatment is necessary.
Patent Landscape
Related Patents
Auspex Pharmaceuticals, Inc. has a robust portfolio of patents related to deutetrabenazine and its analogs. Some notable patents include:
- Patent 8,524,733: This patent, issued in 2013, relates to benzoquinoline inhibitors of VMAT2 and their use in treating movement disorders[2].
- Patent 11,357,772: Issued in 2022, this patent covers new dosage regimens for deuterium-substituted benzoquinoline compounds and their application in treating abnormal muscular activity and related conditions[2].
- Patent 11,446,291: Also issued in 2022, this patent details new dosage regimens and methods for treating movement disorders using deuterium-substituted compounds[2].
Generic Availability
As of the current date, there is no therapeutically equivalent generic version of Austedo (deutetrabenazine) or its extended-release formulation, Austedo XR, available in the United States. This underscores the exclusive rights held by Auspex Pharmaceuticals, Inc. under these patents[2][5].
Regulatory and Legal Considerations
Patent Expiration and Extensions
The patent expiration dates for these deutetrabenazine-related patents range from 2031 to 2041, with some patents having pediatric extensions that extend their exclusivity period. This ensures that Auspex Pharmaceuticals, Inc. maintains market exclusivity for these drugs for an extended period[2][4].
Genus Claims and Patent Scope
The patent landscape in the pharmaceutical industry is complex, especially regarding genus claims. Genus claims aim to capture a broad class of compounds rather than specific embodiments. However, recent jurisprudence has made it challenging to obtain robust patent protection for such claims, as they must meet stringent written description and enablement requirements[3].
Clinical and Therapeutic Implications
Indicated Conditions
The deutetrabenazine analogs covered under this patent are indicated for the treatment of tardive dyskinesia and chorea associated with Huntington's disease. These conditions involve involuntary muscular movements that can significantly impact the quality of life for patients[4].
Mechanism of Action
Deutetrabenazine acts by inhibiting the vesicular monoamine transporter 2 (VMAT2), which reduces the amount of monoamines (such as dopamine, serotonin, and norepinephrine) released into the synaptic cleft. This mechanism helps in controlling the abnormal involuntary movements associated with these conditions[4].
Conclusion
The United States Patent 11,793,386 is a critical component of the intellectual property portfolio of Auspex Pharmaceuticals, Inc., focusing on the development and use of deutetrabenazine analogs. These analogs offer improved pharmacokinetic properties, enhancing the therapeutic efficacy and patient compliance in treating movement disorders. The patent landscape surrounding deutetrabenazine is complex, with multiple related patents and stringent regulatory requirements, but it underscores the innovative efforts in pharmaceutical research and development.
Key Takeaways
- Deutetrabenazine Analogs: The patent covers deuterium-substituted benzoquinoline compounds with improved pharmacokinetic properties.
- Pharmaceutical Compositions: Detailed formulations for various dosage forms are provided.
- Methods of Use: New dosage regimens for treating movement disorders are outlined.
- Patent Expiration: The patent expires on September 15, 2038.
- Regulatory Considerations: The patent is part of a broader portfolio with specific regulatory and legal implications.
- Clinical Implications: The analogs are indicated for treating tardive dyskinesia and chorea associated with Huntington's disease.
FAQs
What is the primary use of deutetrabenazine?
Deutetrabenazine is primarily used for the symptomatic treatment of tardive dyskinesia and chorea associated with Huntington's disease.
What is the significance of deuterium substitution in deutetrabenazine analogs?
Deuterium substitution improves the pharmacokinetic profile by enhancing metabolic stability and reducing side effects.
Are there generic versions of Austedo or Austedo XR available?
No, there are currently no therapeutically equivalent generic versions of Austedo or Austedo XR available in the United States.
What is the mechanism of action of deutetrabenazine?
Deutetrabenazine acts by inhibiting the vesicular monoamine transporter 2 (VMAT2), reducing the release of monoamines into the synaptic cleft.
When does the patent for deutetrabenazine analogs expire?
The patent for deutetrabenazine analogs covered under US Patent 11,793,386 expires on September 15, 2038.
Sources
- US Patent 11,793,386: Analogs of deutetrabenazine, their preparation and use.
- Drugs.com: Generic Austedo XR Availability.
- DigitalCommons@NYLS: Eviscerating Patent Scope.
- DrugBank: Deutetrabenazine: Uses, Interactions, Mechanism of Action.
- Drugs.com: Generic Austedo Availability.
