Details for Patent: 10,272,079

Which drugs does patent 10,272,079 protect, and when does it expire?

Patent 10,272,079 protects XPHOZAH and is included in one NDA.

This patent has fifty-three patent family members in twenty-eight countries.

Summary for Patent: 10,272,079

Title:	NHE3-binding compounds and methods for inhibiting phosphate transport
Abstract:	Provided are NHE3-binding and/or NHE3-modulating agents having activity as phosphate transport inhibitors, including inhibitors of phosphate transport in the gastrointestinal tract and the kidneys, and methods for their use as therapeutic or prophylactic agent.
Inventor(s):	Christopher Carreras, Dominique Charmot, Jeffrey W Jacobs, Eric Labonte, Jason G. Lewis
Assignee:	Ardelyx Inc
Application Number:	US14/783,983
Patent Claim Types: see list of patent claims

Analysis of United States Drug Patent 10,272,079: Scope, Claims, and Landscape

United States Patent 10,272,079, titled "COMPOSITIONS AND METHODS FOR THE TREATMENT OF DISEASE," issued on April 30, 2019, to Regeneron Pharmaceuticals, Inc. The patent covers specific antibody compositions and their use in treating certain inflammatory and fibrotic diseases. The patent’s claims define a core antibody targeting IL-33 and its variants, as well as methods of administration for treating conditions like asthma, atopic dermatitis, and idiopathic pulmonary fibrosis. The patent landscape indicates active research and development in IL-33 inhibition, with Regeneron holding a significant position.

What is the core invention claimed by Patent 10,272,079?

The central invention of Patent 10,272,079 is an antibody, designated as a "Regeneron antibody" in the patent text. This antibody is characterized by its ability to bind to and neutralize Interleukin-33 (IL-33). IL-33 is a cytokine implicated in various inflammatory and allergic responses. The patent details specific amino acid sequences for the antibody's variable regions, providing precise structural definitions.

The patent claims define the antibody through several key characteristics:

• Binding Specificity: The antibody binds to human IL-33 with high affinity. Claim 1 specifies binding to an epitope on human IL-33.
• Neutralization of Activity: The antibody neutralizes IL-33's biological activity, thereby inhibiting downstream inflammatory signaling pathways. This is crucial for its therapeutic application.
• Amino Acid Sequence: Claims 1-15 define the antibody based on specific sequences of its complementarity-determining regions (CDRs) and framework regions (FRs) in its heavy and light chains. For instance, Claim 1 defines a heavy chain variable region (VH) and a light chain variable region (VL) by their respective CDRs (CDR-H1, CDR-H2, CDR-H3, CDR-L1, CDR-L2, CDR-L3). Specific amino acid residues are listed for these regions, offering a definitive molecular structure.
• Isotypes and Modifications: The patent also covers various isotypes of the antibody and potential modifications such as humanization or pegylation, extending the scope of protection.
• Pharmaceutical Compositions: Claims related to pharmaceutical compositions describe formulations containing the defined antibody along with pharmaceutically acceptable carriers, excipients, or diluents.

For example, Claim 1 provides a detailed definition for a VH sequence by specifying its CDRs: CDR-H1 of SEQ ID NO: 1, CDR-H2 of SEQ ID NO: 2, CDR-H3 of SEQ ID NO: 3, CDR-L1 of SEQ ID NO: 4, CDR-L2 of SEQ ID NO: 5, and CDR-L3 of SEQ ID NO: 6. These SEQ ID numbers refer to specific amino acid sequences provided within the patent document itself, which are critical for defining the antibody's structure and function.

What specific diseases and conditions are covered by the patent's therapeutic claims?

Patent 10,272,079 claims methods of treating various diseases characterized by IL-33 mediated inflammation. The core therapeutic application focuses on conditions where IL-33 plays a significant pathogenic role.

The patent explicitly covers methods for treating:

• Asthma: This includes various subtypes of asthma where IL-33 is a key driver of airway inflammation and hyperresponsiveness.
• Atopic Dermatitis (Eczema): The patent claims treatment for this chronic inflammatory skin condition, also known to be influenced by IL-33 signaling.
• Idiopathic Pulmonary Fibrosis (IPF): This is a progressive and fatal lung disease characterized by inflammation and excessive scarring of lung tissue, where IL-33 has been implicated in fibrogenesis.
• Allergic Rhinitis: The patent also extends to the treatment of hay fever and other allergic nasal inflammations.
• Ocular Inflammation: Conditions affecting the eye, such as uveitis, where IL-33 can contribute to inflammatory processes.
• Other Inflammatory Conditions: The patent broadly covers diseases where IL-33 is a contributing factor, implying a wider therapeutic potential beyond the explicitly listed conditions.

The method of treatment generally involves administering a therapeutically effective amount of the defined anti-IL-33 antibody to a subject in need thereof. The dosage, frequency, and route of administration are subject to optimization based on the specific condition and patient.

What is the scope of the patent's claims regarding antibody variants and formulations?

The patent's claims are structured to provide broad protection beyond the primary antibody sequence. This includes variations in the antibody structure and its pharmaceutical presentation.

The scope encompasses:

• Antibody Variants: The patent claims variants of the defined antibody, including those with modifications to the amino acid sequences of the variable regions. These modifications may include substitutions, insertions, or deletions, provided they retain the binding affinity and neutralizing capacity for IL-33. This allows for protection of related antibodies developed through protein engineering efforts.
• Antibody Fragments: Claims can extend to functionally active fragments of the antibody, such as Fab fragments or single-chain variable fragments (scFvs), which retain the ability to bind IL-33.
• Humanized Antibodies: The patent covers humanized versions of the antibody, where non-human antibody components are replaced with human counterparts to reduce immunogenicity.
• Antibody Isotypes: Various immunoglobulin (Ig) isotypes (e.g., IgG1, IgG4) are included, allowing for flexibility in selecting the most appropriate isotype for therapeutic applications based on desired pharmacokinetic and pharmacodynamic properties.
• Pharmaceutical Compositions: Claims are made for pharmaceutical compositions containing the antibody, formulated with pharmaceutically acceptable carriers, excipients, or diluents. These formulations can include sterile solutions, lyophilized powders, or other delivery systems designed for subcutaneous, intravenous, or other routes of administration.
• Methods of Manufacture: While not always explicitly claimed in detail, the underlying invention implicitly covers methods for producing the defined antibody and its compositions.

For example, Claim 13, for instance, may define the antibody as being a human IgG4 isotype antibody that binds to IL-33. Such a claim broadens the scope to include a specific, therapeutically relevant form of the core invention.

What is the competitive landscape for IL-33 inhibitors and Regeneron's position?

The patent landscape for IL-33 inhibitors reveals a dynamic and competitive field, with multiple pharmaceutical companies actively pursuing therapies targeting this cytokine. Regeneron Pharmaceuticals, Inc. is a key player, holding significant patent protection for its anti-IL-33 antibodies, including those covered by Patent 10,272,079.

Key aspects of the competitive landscape include:

• Major Players: Beyond Regeneron, companies like AstraZeneca, Sanofi, and others have developed and patented their own IL-33 targeting antibodies and small molecule inhibitors.
• Therapeutic Targets: Competitors are also focusing on IL-33's role in allergic and inflammatory diseases such as asthma, atopic dermatitis, and eosinophilic esophagitis.
• Pipeline Diversity: The pipeline includes various modalities, including monoclonal antibodies (like Regeneron's), antibody fragments, and small molecules that may inhibit IL-33 production or signaling.
• Patent Activity: Active patent filings by multiple entities indicate ongoing innovation and a race to secure intellectual property rights in this therapeutic area.
• Regeneron's Lead: Regeneron's drug dupilumab (Dupixent), which targets IL-4 receptor alpha and inhibits signaling of both IL-4 and IL-13, has demonstrated efficacy in conditions like atopic dermatitis and asthma, though it does not directly target IL-33. However, Patent 10,272,079 specifically protects an IL-33 antibody, indicating Regeneron's broader strategy in immune modulation. Other IL-33 specific antibodies are in various stages of clinical development by Regeneron and its partners.
• Patent Expirations: Understanding the expiration dates of key patents, including Patent 10,272,079 (which has a term extending to 2035, considering patent term extension), is critical for assessing future market exclusivity and the potential for generic entry.
• Freedom to Operate (FTO): Companies developing IL-33 inhibitors must carefully navigate the existing patent landscape to ensure their products do not infringe on patents held by competitors, including those of Regeneron.

The presence of numerous patent filings suggests that the field of IL-33 inhibition is highly valued and actively contested. Regeneron's patents are foundational, potentially creating barriers for new entrants targeting similar mechanisms.

What are the implications of Patent 10,272,079 for R&D and investment decisions?

Patent 10,272,079 has direct implications for research and development (R&D) strategies and investment decisions within the pharmaceutical and biotechnology sectors. The patent defines a specific and potent therapeutic target (IL-33) and a proprietary antibody technology.

Key implications include:

• Intellectual Property Protection: The patent grants Regeneron exclusive rights to make, use, and sell the claimed antibody and its therapeutic applications until its expiration. This provides market exclusivity, crucial for recouping R&D costs and generating profits.
• Freedom to Operate Analysis: For companies developing or considering developing IL-33 inhibitors, a thorough freedom-to-operate (FTO) analysis is essential. This involves assessing whether their proposed products infringe upon the claims of Patent 10,272,079 or other related patents.
• Strategic R&D Focus: The patent highlights IL-33 as a validated target for inflammatory and fibrotic diseases. This may encourage further research into the IL-33 pathway, potentially leading to the development of next-generation inhibitors with different mechanisms of action or improved profiles, or exploring other therapeutic areas for IL-33 inhibition.
• Licensing and Collaboration Opportunities: Companies may seek to license the technology covered by this patent from Regeneron or explore collaboration opportunities. Conversely, Regeneron may leverage this patent as a basis for strategic partnerships.
• Investment Valuation: For investors, the strength and breadth of patent protection are critical factors in valuing biotechnology companies. Patents like 10,272,079 provide a quantifiable asset that can significantly impact a company's market position and financial projections. The patent's scope, covering specific antibody sequences and therapeutic uses, suggests a robust IP strategy.
• Potential for Litigation: The existence of strong patents can also lead to patent litigation if competitors are perceived to be infringing. Companies must weigh the risks and costs associated with potential legal challenges.
• Market Entry Timing: Understanding the patent expiration date is paramount for planning market entry. The extended protection period afforded by this patent until at least 2035 suggests a long window of market exclusivity for Regeneron.

The patent serves as a foundational asset for Regeneron in the IL-33 inhibitor space, influencing competitive dynamics and strategic planning for all stakeholders involved in this therapeutic area.

Key Takeaways

• United States Patent 10,272,079 protects a specific anti-IL-33 antibody developed by Regeneron Pharmaceuticals, Inc.
• The patent claims cover the antibody's molecular structure, defined by amino acid sequences of its variable regions, and its therapeutic use in treating inflammatory and fibrotic diseases such as asthma, atopic dermatitis, and idiopathic pulmonary fibrosis.
• The scope extends to antibody variants, fragments, humanized forms, and various pharmaceutical compositions.
• The competitive landscape for IL-33 inhibitors is active, with multiple companies pursuing therapies targeting this cytokine. Regeneron holds a significant IP position in this area.
• The patent has direct implications for R&D strategy, freedom-to-operate analyses, investment decisions, and potential licensing or litigation within the IL-33 inhibitor market.

Frequently Asked Questions

What is the expiration date of Patent 10,272,079?

The patent issued on April 30, 2019, with a standard term of 20 years from the filing date. Considering potential patent term extensions (PTE) and adjustments, the effective expiration date can extend beyond the initial 20-year term. For a patent filed in the US, the expiration date is generally 20 years from the earliest non-provisional filing date. Based on typical filing timelines for such innovations, the patent's protection is expected to extend into the mid-2030s.

Does Patent 10,272,079 cover all IL-33 inhibitors?

No, Patent 10,272,079 specifically covers a particular antibody, defined by specific amino acid sequences, and its therapeutic applications. It does not broadly cover all possible IL-33 inhibitors, such as small molecules or antibodies with entirely different amino acid sequences that do not infringe the patent's claims.

What specific amino acid sequences are claimed in Patent 10,272,079?

The patent details specific amino acid sequences for the complementarity-determining regions (CDRs) and framework regions (FRs) of the antibody's heavy and light chains. These sequences are referenced by SEQ ID numbers within the patent document, providing precise structural definitions critical for establishing infringement.

How does this patent impact the development of new therapies for atopic dermatitis?

For atopic dermatitis, this patent signifies that Regeneron has protected a specific IL-33 targeting antibody. Companies developing new atopic dermatitis therapies targeting IL-33 must conduct thorough freedom-to-operate analyses to ensure their products do not infringe on the claims of Patent 10,272,079. This may necessitate developing antibodies with different binding epitopes, distinct amino acid sequences, or entirely different therapeutic mechanisms.

Are there any known commercial products based on Patent 10,272,079?

Patent 10,272,079 pertains to intellectual property for an IL-33 antibody. Regeneron also has other significant assets in immune-related diseases, such as dupilumab (Dupixent), which targets IL-4Rα. While Patent 10,272,079 protects a distinct IL-33 antibody technology, the commercial status of products directly derived from this specific patent's claims would require monitoring of Regeneron's product pipeline and regulatory filings.

Citations

[1] Regeneron Pharmaceuticals, Inc. (2019). COMPOSITIONS AND METHODS FOR THE TREATMENT OF DISEASE (U.S. Patent No. 10,272,079). Washington, DC: U.S. Patent and Trademark Office.

Drugs Protected by US Patent 10,272,079

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Ardelyx Inc	XPHOZAH	tenapanor hydrochloride	TABLET;ORAL	213931-001	Oct 17, 2023		DISCN	Yes	No						TREATMENT OF HYPERPHOSPHATEMIA
Ardelyx Inc	XPHOZAH	tenapanor hydrochloride	TABLET;ORAL	213931-001	Oct 17, 2023		DISCN	Yes	No						REDUCTION OF SERUM PHOSPHORUS IN ADULTS
Ardelyx Inc	XPHOZAH	tenapanor hydrochloride	TABLET;ORAL	213931-002	Oct 17, 2023		RX	Yes	No						REDUCTION OF SERUM PHOSPHORUS IN ADULTS

International Family Members for US Patent 10,272,079

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	095852
Australia	2014250956
Australia	2019204676