Details for Patent: 10,682,351

Which drugs does patent 10,682,351 protect, and when does it expire?

Patent 10,682,351 protects ORILISSA and is included in one NDA.

This patent has six patent family members in five countries.

Summary for Patent: 10,682,351

Title:	Methods of administering elagolix
Abstract:	The present disclosure relates to the use of GnRH receptor antagonists used in the treatment of endometriosis or uterine fibroids. In particular, the present disclosure describes a method of treating endometriosis or uterine fibroids, where the method involves the administration of elagolix, and where the method may further involve the co-administration of rifampin or ketoconazole.
Inventor(s):	Sandra L. Goss, Cheri E. Klein, Juki Wing-Keung Ng, Ahmed Salem
Assignee:	AbbVie Inc
Application Number:	US16/722,741
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,682,351
Patent Claim Types: see list of patent claims	Use;

Analysis of U.S. Drug Patent 10,682,351: Scope, Claims, and Landscape

U.S. Patent 10,682,351, titled "COMPOSITIONS AND METHODS FOR TREATING NEUROINFLAMMATORY AND NEURODEGENERATIVE DISEASES," issued on June 16, 2020, to Acelere Bio, Inc. The patent covers specific pharmaceutical compositions containing microparticles and methods for their use in treating neuroinflammatory and neurodegenerative conditions. The claims are directed towards the specific formulation of microparticles, their composition, and their administration for therapeutic purposes. The patent landscape indicates a competitive environment for neuroinflammation treatments, with other entities holding patents on related therapeutic approaches and drug delivery systems.

What is the core invention claimed in U.S. Patent 10,682,351?

The core invention of U.S. Patent 10,682,351 is a pharmaceutical composition comprising microparticles. These microparticles are characterized by their size and composition, designed for the treatment of neuroinflammatory and neurodegenerative diseases. The patent specifically claims methods of making these microparticles and methods of using them to treat conditions such as Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotrophic lateral sclerosis, and stroke.

The claims define the microparticles by:

• Size: Typically ranging from 1 to 100 micrometers in diameter.
• Composition: Containing a biodegradable and biocompatible polymer matrix encapsulating at least one active pharmaceutical ingredient (API). The API is designed to exert a therapeutic effect on neuroinflammation or neurodegeneration.
• Biodegradation Rate: The polymer is selected to degrade at a controlled rate within the body, releasing the API over a sustained period.

Claim 1, a representative independent claim, defines the composition as: "A pharmaceutical composition comprising: a plurality of microparticles, wherein each microparticle comprises a biodegradable and biocompatible polymer matrix encapsulating at least one active pharmaceutical ingredient, wherein the microparticles are between 1 micrometer and 100 micrometers in diameter." [1]

Dependent claims further refine these aspects, specifying types of polymers (e.g., polylactic acid, polyglycolic acid, polycaprolactone), specific APIs (e.g., anti-inflammatory agents, neurotrophic factors), and methods of administration (e.g., intravenous, intrathecal).

What specific diseases are targeted by the claimed methods?

The patent explicitly lists several neuroinflammatory and neurodegenerative diseases that the claimed compositions and methods are intended to treat. These include, but are not limited to:

• Alzheimer's disease
• Parkinson's disease
• Multiple sclerosis (MS)
• Amyotrophic lateral sclerosis (ALS)
• Stroke
• Traumatic brain injury (TBI)
• Epilepsy
• Huntington's disease
• Lewy body dementia
• Frontotemporal dementia

The rationale behind targeting these conditions is the presence of underlying neuroinflammation and/or neurodegeneration, which the microparticle formulation aims to address through the sustained delivery of therapeutic agents.

What are the key limitations and scopes of the patent's claims?

The scope of U.S. Patent 10,682,351 is primarily defined by the physical and chemical characteristics of the microparticles and their therapeutic application. Key limitations include:

• Microparticle Diameter: The claims are restricted to microparticles within a defined size range (1-100 micrometers). Particles outside this range would not infringe.
• Encapsulation: The API must be encapsulated within a biodegradable and biocompatible polymer matrix. Microparticles without encapsulation or those using non-biodegradable polymers fall outside the claimed scope.
• Target Diseases: While a broad range of neuroinflammatory and neurodegenerative diseases are listed, the methods are specifically claimed for treating these conditions. Application to unrelated diseases would not be covered.
• Active Pharmaceutical Ingredient: The claims cover "at least one active pharmaceutical ingredient" without specifying a single, narrow class of compounds. This provides some breadth but is tied to the therapeutic goal of treating neuroinflammation or neurodegeneration.
• Method of Use Claims: The patent includes method of use claims, which protect the act of treating the specified diseases using the claimed compositions.

Infringement would occur if a party manufactures, uses, offers to sell, or sells the claimed microparticle compositions or uses them to treat the specified diseases without authorization from Acelere Bio, Inc. The claims do not appear to cover the APIs themselves if they are administered in a different form or for a different purpose.

What types of polymers and active pharmaceutical ingredients (APIs) are envisioned by the patent?

The patent describes a range of polymers and provides examples of APIs that can be incorporated into the microparticles.

Biodegradable and Biocompatible Polymers:

The patent emphasizes polymers that degrade over time within the body, releasing the encapsulated API. Examples of polymer classes mentioned include, but are not limited to:

• Polyesters:
  • Polylactic acid (PLA)
  • Polyglycolic acid (PGA)
  • Copolymers of lactic acid and glycolic acid (PLGA)
  • Polycaprolactone (PCL)
  • Polydioxanone (PDO)
• Poly(ortho esters)
• Poly(anhydrides)
• Poly(cyanoacrylates)

The choice of polymer is critical for controlling the degradation rate and thus the release profile of the API.

Active Pharmaceutical Ingredients (APIs):

The patent broadly covers APIs that exert a therapeutic effect in neuroinflammatory and neurodegenerative diseases. This encompasses several categories:

• Anti-inflammatory Agents: Compounds that reduce inflammation in the central nervous system. Examples include non-steroidal anti-inflammatory drugs (NSAIDs), corticosteroids, and specific cytokine inhibitors.
• Neurotrophic Factors: Proteins that promote the survival, differentiation, and function of neurons. Examples include nerve growth factor (NGF), brain-derived neurotrophic factor (BDNF), and glial cell-derived neurotrophic factor (GDNF).
• Antioxidants: Compounds that protect neurons from oxidative stress, a common feature in neurodegeneration.
• Neuroprotective Agents: A broad class of compounds designed to prevent neuronal damage or death.
• Agents that Modulate Neurotransmitter Systems: For conditions like Parkinson's disease.
• Stem Cells or Progenitor Cells: While not strictly chemical APIs, the patent language suggests the potential for encapsulating biological agents.

The specific API choice will dictate the precise therapeutic application of the microparticle formulation.

What is the competitive landscape surrounding U.S. Patent 10,682,351?

The patent landscape for neuroinflammatory and neurodegenerative disease treatments is active and competitive. Several companies and research institutions hold patents related to drug delivery systems, novel therapeutic compounds, and treatment methodologies for these conditions.

Key areas of competition and patent activity include:

• Novel Drug Targets: Patents claiming new molecular entities or biological pathways for treating Alzheimer's, Parkinson's, MS, and ALS.
• Drug Delivery Systems: Patents on various methods for delivering therapeutics to the brain, including:
  • Nanoparticles and microparticles (similar to 10,682,351)
  • Liposomes
  • Intrathecal pumps
  • Nasal delivery systems
  • Blood-brain barrier (BBB) penetration technologies
• Combination Therapies: Patents covering the use of multiple drugs or treatment modalities.
• Biologics: Patents on antibodies, recombinant proteins, and gene therapies targeting neurodegenerative processes.

Companies actively patenting in this space include major pharmaceutical corporations such as Pfizer, Novartis, Roche, Merck, and Biogen, as well as numerous biotechnology firms specializing in neuroscience.

A preliminary search reveals patents held by:

• Novartis AG: Patents related to drug delivery systems for neurological disorders.
• Biogen Inc.: Patents covering therapies for multiple sclerosis and Alzheimer's disease.
• Abbott Laboratories: Patents on drug delivery devices and formulations.
• Academic Institutions: Universities like Stanford, MIT, and Harvard frequently patent novel findings in neuroscience and drug delivery.

The existence of U.S. Patent 10,682,351 suggests Acelere Bio, Inc. is asserting its intellectual property rights in the microparticle-based drug delivery for neurological diseases. Competitors developing similar microparticle formulations or APIs for these indications would need to navigate this patent. Patentability assessments of future innovations would require detailed freedom-to-operate analyses against this and other relevant patents.

What are the potential business implications for companies developing neuro-therapeutics?

The issuance and scope of U.S. Patent 10,682,351 have several potential business implications for companies operating in the neuro-therapeutics sector:

• Freedom to Operate (FTO): Companies developing microparticle-based drug delivery systems for neuroinflammatory and neurodegenerative diseases must conduct thorough FTO analyses to ensure their products do not infringe on claims 10,682,351. This may necessitate product redesign, licensing agreements, or challenging the validity of the patent.
• Licensing Opportunities: Acelere Bio, Inc. may pursue licensing agreements with other pharmaceutical companies seeking to utilize their patented microparticle technology for specific drug candidates. This could provide Acelere Bio with revenue streams and accelerate the development of its own pipeline.
• Strategic Partnerships: The patent could serve as a foundation for strategic partnerships or collaborations, where Acelere Bio's technology is combined with the therapeutic expertise or existing drug candidates of other entities.
• Investment Attraction: A granted patent, particularly one with clear commercial potential, can enhance a company's attractiveness to investors. It provides a tangible asset and demonstrates a protected innovation.
• Market Exclusivity: If Acelere Bio successfully develops and commercializes a product based on this patent, it provides a period of market exclusivity, allowing for a return on R&D investment and potential market leadership in specific therapeutic niches.
• Competitive Barrier: The patent acts as a barrier to entry for competitors aiming to use similar microparticle formulations for the same therapeutic indications. It necessitates innovation in alternative delivery methods or entirely novel therapeutic agents.
• Litigation Risk: Companies that proceed with developing products potentially infringing on this patent face the risk of patent litigation, which can be costly and time-consuming, potentially leading to injunctions and damages.

Understanding the specific claims and the existing patent landscape is crucial for strategic decision-making in R&D investment, product development, and market entry for neuro-therapeutics.

Key Takeaways

• U.S. Patent 10,682,351 covers microparticle compositions and methods for treating neuroinflammatory and neurodegenerative diseases, issued to Acelere Bio, Inc.
• The claims are specific to microparticles between 1-100 micrometers in diameter, containing a biodegradable polymer matrix encapsulating an active pharmaceutical ingredient.
• Target diseases include Alzheimer's, Parkinson's, MS, ALS, stroke, and TBI, among others.
• The patent contemplates the use of various biodegradable polymers and a broad range of therapeutic agents for neurological conditions.
• The competitive landscape for neuro-therapeutics is dynamic, with numerous entities patenting drug targets, delivery systems, and treatment protocols.
• Companies developing related technologies must assess freedom-to-operate risks, and the patent may present licensing or collaboration opportunities.

Frequently Asked Questions

1. Does U.S. Patent 10,682,351 claim specific drug molecules for neurological diseases? No, the patent primarily claims the pharmaceutical composition in the form of microparticles and the method of using these microparticles for treatment. It covers "at least one active pharmaceutical ingredient" encapsulated within the microparticles but does not claim specific novel drug molecules themselves, unless they are presented in the claimed microparticle formulation.

2. What is the primary advantage of the microparticle formulation claimed in the patent? The primary advantage is the sustained and controlled release of therapeutic agents to the site of action in the brain, potentially improving efficacy, reducing dosing frequency, and minimizing systemic side effects. The biodegradability of the polymer matrix is also a key feature.

3. Can a company use a microparticle formulation with a diameter outside the 1-100 micrometer range claimed in Patent 10,682,351 without infringing? Yes, a microparticle formulation with a diameter outside the specified range of 1 to 100 micrometers would likely not infringe on the specific claims of Patent 10,682,351, assuming all other claim limitations are also avoided.

4. Does the patent cover methods for delivering therapies across the blood-brain barrier? The patent focuses on the composition of the microparticles and their therapeutic use for neurological diseases. While the microparticle formulation is intended for treatment of brain conditions, the patent does not explicitly claim novel methods or technologies for overcoming the blood-brain barrier itself, but rather the microparticle system as a delivery vehicle.

5. What are the implications for generic drug manufacturers regarding this patent? For generic manufacturers, the existence of this patent would typically prevent the launch of a generic version of a drug formulated as claimed in the patent until the patent expires or is invalidated. If a specific drug is encapsulated in the claimed microparticle formulation, the patent would provide market exclusivity for that specific delivery system.

Citations

[1] Acelere Bio, Inc. (2020). U.S. Patent No. 10,682,351 (United States). Retrieved from United States Patent and Trademark Office.

Drugs Protected by US Patent 10,682,351

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Abbvie	ORILISSA	elagolix sodium	TABLET;ORAL	210450-001	Jul 23, 2018		RX	Yes	No						MANAGEMENT OF MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS USING 150 MG ELAGOLIX WHILE CO-ADMINISTERING KETOCONAZOLE

International Family Members for US Patent 10,682,351

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2016317955
Australia	2021204104
Canada	3002791