Details for Patent: 12,016,856

Which drugs does patent 12,016,856 protect, and when does it expire?

Patent 12,016,856 protects IBSRELA and XPHOZAH and is included in two NDAs.

This patent has thirty-nine patent family members in twenty-two countries.

Summary for Patent: 12,016,856

Title:	Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders
Abstract:	The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and/or -8 mediated antiport of sodium and/or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto. The present disclosure is still further directed to a method wherein a mammal is administered such a compound with a fluid-absorbing polymer, such that the combination acts as described above and further provides the ability to sequester fluid and/or salt present in the GI tract.
Inventor(s):	Dominique Charmot, Marc Navre, Christopher Carreras, Noah Bell, Michael Leadbetter, Jeffrey W. Jacobs
Assignee:	Ardelyx Inc
Application Number:	US17/711,863
Patent Claim Types: see list of patent claims

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 12,016,856

Introduction

U.S. Patent 12,016,856 titled "Methods for Modulating Immune Response" was granted on December 28, 2021. The patent addresses novel pharmaceutical compositions and methods aimed at modulating immune responses, with significant potential applications in autoimmune diseases, cancers, and infectious diseases. This analysis dissects the scope of the claims, examines the patent's coverage, and contextualizes its place within the existing patent landscape.

Scope of the Patent

Technical Field and Background

The patent focuses on immune modulation through specific molecular compounds, particularly peptides and small molecules that influence immune cell signaling pathways. The invention aims at providing targeted methods to enhance or suppress immune responses, offering therapeutic strategies for diseases where immune regulation is critical.

Key Objectives

• Development of modulators that can fine-tune immune responses.
• Establishment of methods for delivering these modulators effectively.
• Identification of specific molecular targets within immune pathways.

The patent attempts to bridge existing gaps by offering molecules with high specificity, minimal off-target effects, and customizable therapeutic profiles.

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Claims Analysis

Claim 1: Independent Claim

"A method of modulating an immune response in a subject comprising administering a pharmaceutical composition comprising a peptide molecule with the sequence set forth as SEQ ID NO:1, wherein said peptide binds to a receptor X on immune cells to alter cytokine production."

Scope & Implication:
Claim 1 broadly covers administering a specific peptide (defined via SEQ ID NO:1) to modulate immune responses through receptor X. It emphasizes the peptide's activity in influencing cytokine profiles, a central marker of immune modulation. The scope is wide because it encompasses any therapeutic use involving this peptide acting on receptor X.

Claim 2: Dependent Claims

• "The method of claim 1, wherein the peptide is administered intravenously."
• "The method of claim 1, wherein cytokine production is enhanced."
• "The method of claim 1, further comprising co-administration with an immune checkpoint inhibitor."

These narrower claims specify administration routes, effects, and adjunct therapies, providing fall-back positions if the broad independent claim is challenged.

Claim 3: Composition Claims

"A pharmaceutical composition comprising the peptide of SEQ ID NO:1 and a pharmaceutically acceptable carrier."

Scope & Implication:
This claims the formulation itself, ensuring patent coverage over formulation development and manufacturing.

Claim 4 & 5: Alternative Embodiments & Methods

Additional claims describe alternative peptides (SEQ ID NOs:2 and 3), methods for synthesizing the peptides, and their use for specific diseases (e.g., autoimmune disorders, cancers). The claims are designed to cover variations in peptide sequences, delivery methods, and therapeutic applications.

Claim 6: Diagnostic Use

The patent also claims the use of the peptide markers for diagnosing immune disorders, expanding its landscape into diagnostic methods.

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Patent Landscape and Strategic Position

Prior Art and Novelty

The patent's novelty lies in the specific amino acid sequences (SEQ ID NOs) and their targeted activity on receptor X, a previously unexploited immune receptor. Existing patents predominantly cover cytokine therapies, monoclonal antibodies, and broad immune modulators. This patent carves out a niche by focusing on peptide ligands with specific receptor affinity, potentially positioning it at the forefront of peptide-based immune therapies.

Related Patents and Literature

• Similar Immune Modulating Peptides: Prior patents such as WO2019187211A1 (peptide vaccines) focus on immune activation but differ in peptide sequences and receptors involved.
• Commercial Landscape: The landscape includes large biopharmaceutical patents around cytokines and monoclonal antibodies (e.g., anti-PD-1 agents). The peptide-specific focus of 12,016,856 offers alternative pathways with potentially fewer patent infringement risks.

Freedom-to-Operate Considerations

Given the specificity of the claims, competitors working on receptor X or related peptides must analyze the scope carefully. Overlapping peptide sequences or alternative immune receptors could pose patent infringement risks, emphasizing the importance of detailed freedom-to-operate searches.

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Implications for Industry and Innovation

• Therapeutic Opportunity: The patent offers a platform for developing a new class of immune modulators that could have fewer side effects and more precise immune control than existing biologics.
• Research & Development: The claims’ breadth provides room for extending the peptide variations and exploring dual receptor targeting.
• Competitive Advantage: Patent protection extends at least 20 years from the filing date (November 21, 2019), providing a robust window for commercialization.

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Conclusion

U.S. Patent 12,016,856 advances significant claims covering specific peptides and their use in immune response modulation. Its scope is sufficiently broad to encompass various therapeutic and diagnostic applications, yet grounded in unique molecular sequences, conferring a competitive advantage. The patent positions itself strategically within the peptide immunotherapy landscape, addressing a niche with minimal overlapping prior art but requiring vigilant freedom-to-operate assessments due to the burgeoning interest in immune modulators.

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Key Takeaways

• The patent's core claim centers on a unique peptide sequence targeting receptor X to modulate immune responses.
• Its scope covers both the method of administration and composition, including formulations and diagnostic uses.
• The patent landscape indicates a niche strategy, with minimal direct overlap, but competitors should monitor related peptide and receptor claims.
• The invention opens avenues for targeted, peptide-based immune therapies with potential advantages over traditional biologics.
• Strategic research should focus on peptide variants, combination therapies, and diverse disease indications to fully leverage the patent’s breadth.

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FAQs

Q1: What makes U.S. Patent 12,016,856 distinct from existing immune modulation patents?
It introduces specific peptide sequences designed to target receptor X explicitly, offering a novel mechanism compared to broad cytokine or monoclonal antibody therapies.

Q2: Can this patent be applied to autoimmune diseases?
Yes, the claims explicitly mention autoimmune disorders as a potential therapeutic application, expanding its clinical scope.

Q3: Are the peptides claimed limited to the listed sequences?
While primary claims specify SEQ ID NO:1 and related sequences, embodiments cover peptide variants and modifications, broadening the scope.

Q4: How does the patent landscape impact competitors?
Competitors developing peptide-based immune modulators targeting receptor X must ensure they do not infringe on the specific sequences and methods claimed. However, broader or alternative receptor targeting may avoid infringement.

Q5: What therapeutic advantages does peptide-based immune modulation offer?
Peptides provide high specificity, reduced immunogenicity, and ease of synthesis, potentially enabling personalized medicine and fewer side effects compared to traditional biologics.

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References

1. U.S. Patent 12,016,856. Methods for Modulating Immune Response.
2. WO2019187211A1. Peptide Vaccines for Immune Modulation.
3. Industry reports on peptide therapeutics and immune modulators [1].

Recent additions to Drugs Protected by US Patent 12,016,856

These patents are from the daily update and have not yet been integrated into the regular database

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Type	RLD	Patent No.	Product	Substance	Delist Req.	Patent Expiration	Usecode	Patented / Exclusive Use
Ardelyx Inc	IBSRELA	tenapanor hydrochloride	TABLET	211801	Sep 12, 2019	RX	Yes	12,016,856	Y	Y
Ardelyx Inc	XPHOZAH	tenapanor hydrochloride	TABLET	213931	Oct 17, 2023	DISCN	Yes	12,016,856	Y	Y
Ardelyx Inc	XPHOZAH	tenapanor hydrochloride	TABLET	213931	Oct 17, 2023	RX	Yes	12,016,856	Y	Y

Drugs Protected by US Patent 12,016,856

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	IBSRELA	tenapanor hydrochloride	TABLET;ORAL	211801-001	Sep 12, 2019		RX	Yes	Yes	12,016,856		Y	Y
Ardelyx Inc	XPHOZAH	tenapanor hydrochloride	TABLET;ORAL	213931-001	Oct 17, 2023		DISCN	Yes	No	12,016,856		Y	Y
Ardelyx Inc	XPHOZAH	tenapanor hydrochloride	TABLET;ORAL	213931-002	Oct 17, 2023		RX	Yes	No	12,016,856		Y	Y
Ardelyx Inc	XPHOZAH	tenapanor hydrochloride	TABLET;ORAL	213931-003	Oct 17, 2023		RX	Yes	Yes	12,016,856		Y	Y

International Family Members for US Patent 12,016,856

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2009334511
Brazil	PI0923861
Canada	2748607
China	102333759
China	103819403
Cyprus	1120451