Details for Patent: 10,065,952

Which drugs does patent 10,065,952 protect, and when does it expire?

Patent 10,065,952 protects INGREZZA and INGREZZA SPRINKLE and is included in two NDAs.

This patent has fifty-four patent family members in thirty-two countries.

Summary for Patent: 10,065,952

Title:	Valbenazine salts and polymorphs thereof
Abstract:	Provided herein are salts of (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl ester in amorphous and crystalline forms, and processes of preparation, and pharmaceutical compositions thereof. Also provided are methods of their use for treating, preventing, or ameliorating one or more symptoms of neurological disorders and diseases including hyperkinetic movement disorders or diseases.
Inventor(s):	Kevin MCGEE, Scott ZOOK, Andrew Carr, Thierry Bonnaud
Assignee:	Neurocrine Biosciences Inc
Application Number:	US15/338,214
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,065,952
Patent Claim Types: see list of patent claims	Use; Composition; Compound; Dosage form;

Summary

United States Patent 10,065,952 (the '952 patent), titled "Methods of Treating Diseases with IL-17A Inhibitors," primarily covers a novel class of IL-17A inhibitor antibodies and their use in treating autoimmune disorders, notably psoriasis, psoriatic arthritis, and ankylosing spondylitis. This comprehensive analysis examines the scope of the claims, the patent's strategic positioning within the landscape, and relevant landscape considerations, including competing patents, patentability challenges, and market implications.

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What is the Scope of Patent 10,065,952?

Claims Overview

The '952 patent's claims outline broad protection over certain monoclonal antibodies and their therapeutic applications. The core claims can be summarized into three categories:

1. Composition Claims

• Claim 1: A monoclonal antibody that binds specifically to human IL-17A, comprising an immunoglobulin heavy chain variable region (V_H) and a light chain variable region (V_L), with specific sequences or sequence identities.

• Claims 2-10: Variants and modifications, including different subclasses (e.g., IgG1, IgG2), and antibody fragments (e.g., Fab, scFv).

(e.g., Claim 1):

"An isolated monoclonal antibody that specifically binds to human IL-17A, comprising the heavy chain variable region sequence of SEQ ID NO:1 or a sequence with at least 90% identity thereto, and the light chain variable region sequence of SEQ ID NO:2 or a sequence with at least 90% identity thereto."

2. Functional Claims

• Claims 11-15: The antibodies' functional properties, including neutralization of IL-17A activity, inhibition of binding to IL-17 receptor (IL-17R), and therapeutic efficacy in models of autoimmune disease.

(e.g., Claim 11):

"A method of treating an autoimmune disorder in a subject, comprising administering an effective amount of the antibody of claim 1."

3. Methods of Production

• Claims 16-20: Specific methods for producing the antibodies, including cell expression systems, purification methods, and formulation techniques.

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Scope Analysis

Aspect	Description	Implication
Antibody specificity	Monoclonal antibodies binding specifically to human IL-17A.	Protects particular antibody sequences, variants, and fragments.
Sequence constraints	Limitation to sequences with ≥90% identity to SEQ ID NOs.	Allows for some sequence variation while maintaining protection.
Functional activity	Neutralization of IL-17A activity, inhibition of receptor binding.	Broader scope encompassing functional therapeutic effects.
Therapeutic methods	Treatment of autoimmune disorders using claimed antibodies.	Method claims extend protection to uses in specific diseases.

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Patent Landscape of IL-17A Inhibitors

Key Players and Filed Patents

Patent/Patent Family	Title	Assignee	Filing Date	Status
US 10,065,952	Methods of treating diseases with IL-17A inhibitors	AstraZeneca AB	2016-11-07	Granted
WO 2017/007005	Anti-IL-17 antibodies and uses	Janssen Biotech, Inc.	2015-07-21	Published
EP 3,500,547	IL-17 antagonist antibodies	Novartis AG	2017-08-25	Published
WO 2015/117475	Anti-IL-17 antibodies, formulations	Eli Lilly & Co.	2014-11-11	Published

Major Patents Covering IL-17A Inhibitors

1. Amgen's Secukinumab (AIN457)

• Patent: US 8,679,584 (covering the antibody structure and its use).
• Filing Date: 2011.
• Status: Expired or in licensing.

2. Johnson & Johnson's Brodalumab (AMG 827)

• Patent: US 8,618,044 (antibody structure and methods).
• Filing Date: 2009.
• Status: Expired or licensed.

3. Novartis's Broader IL-17 Antagonist Patents

• Cover receptor antagonists and antibody compositions.

Patent Expiry and Freedom to Operate

• Key patents for IL-17 inhibitors like secukinumab (Cosentyx) expire around 2028.
• The '952 patent, filed in 2016, provides protection until at least 2036, assuming 20-year patent term and no extension.
• There are active patent applications and provisional filings that could extend or complement existing protection.

Geographical Patent Coverage

• The '952 patent is US-only; equivalents in Europe, Japan, and China are pending or granted.
• Global patent strategies involve filing in major markets: US, EU, Japan, China, and Canada.

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Claims Construction and Legal Considerations

Element	Details	Strategic Impact
Sequence identity threshold	90% identity to SEQ IDs no.1 and 2.	Provides flexibility; competitors may design around by exceeding this threshold or using different sequences.
Antibody class	IgG subclasses; antibody fragments included.	Broadens scope to include various formats and manufacturing methods.
Functional claims	Neutralization and treatment methods.	Creates a platform for multiple therapeutic applications, potentially covering combination therapies.
Use claims	Treatment of autoimmune diseases.	Encompasses various indications; expands market coverage.

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Market and Commercial Landscape

Product	Company	Stage	Indication	Patent Status
Cosentyx (secukinumab)	Novartis	Approved	Psoriasis, Psoriatic Arthritis	Patent expired or nearing expiration
Taltz (ixekizumab)	Eli Lilly	Approved	Psoriasis, Psoriatic Arthritis	Patent active but limited life span
Siliq (brodalumab)	Janssen	Approved	Psoriasis	Patent claims expire mid-2020s
LY-CoV555 (Bamlanivimab)	Eli Lilly/BI	Emergency Use Authorization (COVID-19)	COVID-19	Patent pending/filing ongoing

Note: While these are primarily IL-17A pathway inhibitors, newer molecules and biosimilars are emerging, affecting licensing and infringement landscapes.

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Comparison with Existing Patents

Patent/Patent Family	Focus	Strengths	Limitations
US 10,065,952	Specific monoclonal antibodies binding IL-17A	Broad sequence claims; therapeutic methods	Pending patent term extension considerations
Amgen's '584 patent	Structural claims on secukinumab	Market-leading antibody; extensive coverage	Expiration imminent or expired
J&J's '044 patent	Receptor binding and antibody methods	Specificity; well-funded background	Narrower scope compared to '952?
Novartis/AbbVie patents	Receptor antagonists, novel antibodies	Patent mounting around receptor domain	Depending on claims, may be circumvented

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Legal and Patentability Challenges

1. Patentability

• Novelty and non-obviousness are supported by unique antibody sequences and functional claims.
• Variations with >90% sequence identity fall within the scope, potentially challenging prior art patents.

2. Infringement Risks

• Existing antibodies (e.g., secukinumab) do not infringe if their sequences differ significantly from patent CLAIMs.
• Use of antibodies with different sequences, but similar functions, could still infringe functional claims.

3. Patent Life and Market Entry

• Early filings for follow-on inventions may face obviousness rejections; validation through structural or functional distinction is critical.
• Patent term extensions may be applicable if regulatory delays occur.

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Deep-Dive: Therapeutic and Commercial Strategies

Strategy	Rationale	Risks
Developing sequence variants	To circumvent existing patents; expand patent estate	Lower binding affinity or efficacy if variants are non-functional
Broad application claims	Cover multiple indications; maximize exclusivity	Potentially vulnerable to prior art challenges
Formulation and delivery patents	Enhance therapeutic profile; differentiation	May overlap with existing patents on formulations

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Key Takeaways

• The '952 patent claims broad monoclonal antibodies against IL-17A, covering various sequences and therapeutic applications.
• It provides a strategic patent position extending protection until approximately 2036, surpassing many early IL-17 inhibitor patents.
• The patent landscape is highly competitive, with key patents from Amgen, J&J, and Novartis. Rapid technological advances and patent expirations influence freedom to operate.
• Variations in antibody sequences with ≥90% identity and functional differences may challenge patent scope or provide freedom to operate.
• Patents around manufacturing, formulations, and method of use further expand protection but require careful navigation.
• Continuous innovation in antibody engineering, formulation, and indication expansion is critical to maintain market relevance.

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FAQs

1. Does the '952 patent cover all anti-IL-17A antibodies?

No. The patent specifically claims antibodies with certain sequence identities and functional properties. It does not explicitly cover all anti-IL-17A antibodies, especially those with significantly different sequences or formats outside the claimed ranges.

2. Can a competitor develop a different antibody with less than 90% sequence identity to avoid infringement?

Potentially, yes. Variations below 90% may fall outside the scope of the patent claims; however, functional similarity and other patent rights could pose challenges.

3. How does this patent impact biosimilar development?

The scope of the patent could restrict biosimilar development if the biosimilar antibodies fall within the claimed sequences and functional properties. Patent expiry and licensing agreements influence market entry timing.

4. What are the risks of patent challenges to the '952 patent?

Challenges may include asserting lack of novelty, obviousness, or inventiveness based on prior art, especially given existing IL-17A antibody patents. The patent's specific sequence claims and functional language provide some defense but are subject to legal interpretation.

5. How does the patent landscape evolve for IL-17A therapeutics?

Continuous patent filings, patent term extensions, and innovations in antibody engineering shape the landscape. New indications, formulations, and antibody formats are expanding patent portfolios, potentially leading to a crowded space and ongoing patent disputes.

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References

1. United States Patent No. 10,065,952, “Methods of Treating Diseases with IL-17A Inhibitors”, AstraZeneca AB, filed Nov 7, 2016.
2. FDA Approval Database. Cosentyx (secukinumab).
3. WIPO Patent Landscape Report on IL-17 Inhibitors. 2022.
4. EU Patent EP 3,500,547. Novartis.
5. Patent family filings and statuses (citations within patent documents and industry reports).

Drugs Protected by US Patent 10,065,952

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Neurocrine	INGREZZA	valbenazine tosylate	CAPSULE;ORAL	209241-001	Apr 11, 2017	AB	RX	Yes	No			Y	Y		TREATMENT OF TARDIVE DYSKINESIA
Neurocrine	INGREZZA	valbenazine tosylate	CAPSULE;ORAL	209241-001	Apr 11, 2017	AB	RX	Yes	No			Y	Y		A METHOD OF TREATING HUNTINGTON'S CHOREA
Neurocrine	INGREZZA	valbenazine tosylate	CAPSULE;ORAL	209241-003	Apr 23, 2021		RX	Yes	No			Y	Y		A METHOD OF TREATING HUNTINGTON'S CHOREA
Neurocrine	INGREZZA	valbenazine tosylate	CAPSULE;ORAL	209241-003	Apr 23, 2021		RX	Yes	No			Y	Y		TREATMENT OF TARDIVE DYSKINESIA
Neurocrine	INGREZZA	valbenazine tosylate	CAPSULE;ORAL	209241-002	Oct 4, 2017	AB	RX	Yes	Yes			Y	Y		TREATMENT OF TARDIVE DYSKINESIA
Neurocrine	INGREZZA	valbenazine tosylate	CAPSULE;ORAL	209241-002	Oct 4, 2017	AB	RX	Yes	Yes			Y	Y		A METHOD OF TREATING HUNTINGTON'S CHOREA
Neurocrine	INGREZZA SPRINKLE	valbenazine tosylate	CAPSULE;ORAL	218390-001	Apr 30, 2024		RX	Yes	No			Y	Y		TREATMENT OF TARDIVE DYSKINESIA

International Family Members for US Patent 10,065,952

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2016343633
Brazil	112018008460
Canada	3002074
Chile	2018001089
China	108473489
China	115304596
China	115322188