United States Drug Patent 8,680,144: Scope, Claims, and Landscape Analysis

United States Patent 8,680,144, granted on March 25, 2014, to Amgen Inc., covers novel substituted cyclic peptides and their use in treating hypercholesterolemia. The patent's claims define specific chemical structures and their therapeutic application, establishing a distinct intellectual property barrier. The patent landscape reveals limited direct competition within its core claims, but adjacent intellectual property and ongoing research in PCSK9 inhibition present potential indirect challenges.

What is the Core Invention of Patent 8,680,144?

The central invention of U.S. Patent 8,680,144 is a class of substituted cyclic peptides. These peptides are characterized by specific structural modifications designed to enhance their biological activity and pharmacokinetic properties. The patent's disclosure details the chemical structure of these compounds, which are designed to inhibit proprotein convertase subtilisin/kexin type 9 (PCSK9). PCSK9 is a protein that regulates the number of LDL receptors on liver cells. By inhibiting PCSK9, these peptides increase the number of LDL receptors, leading to a reduction in circulating low-density lipoprotein cholesterol (LDL-C).

The specification defines the general structure of the claimed peptides, including a cyclic core and specific substituent groups at defined positions. These substituents are critical for the observed biological activity and are meticulously described in the patent's chemical definitions. The patent further claims the pharmaceutical compositions containing these peptides, along with methods of treating conditions associated with elevated LDL-C, such as hypercholesterolemia and cardiovascular disease.

What are the Key Claims of Patent 8,680,144?

Patent 8,680,144 contains a series of independent and dependent claims that define the scope of the invention. The primary claims focus on the chemical structure of the substituted cyclic peptides and their pharmaceutical use.

Claim 1, the broadest independent claim, defines the core chemical structure of the substituted cyclic peptide. It specifies a defined cyclic peptide core with a series of substituents designated by variables (e.g., R1, R2, R3, R4). These variables are further elaborated in dependent claims and the specification, detailing specific functional groups, amino acid residues, and their connectivity. The claim outlines a precise arrangement of atoms and bonds that collectively define the patented molecular entities.

Dependent claims further narrow the scope by providing specific examples of substituents and structural variations. These claims can cover:

Specific amino acid sequences within the cyclic peptide core.
Particular types of substitutions at defined positions (e.g., halogenation, alkylation, amidation).
Stereochemical configurations of chiral centers within the molecule.
Salts and prodrug forms of the claimed peptides.

Other independent claims address:

Pharmaceutical Compositions: Claims directed to formulations comprising the substituted cyclic peptides and pharmaceutically acceptable carriers, diluents, or excipients. These claims cover the delivery aspect of the invention.
Methods of Treatment: Claims for methods of treating hypercholesterolemia or reducing LDL-C levels in a subject. These claims define the therapeutic application and are crucial for market exclusivity. The methods typically involve administering an effective amount of the claimed peptide.

The precise wording of these claims dictates the boundaries of Amgen's exclusive rights. Infringement occurs if a competitor makes, uses, sells, offers for sale, or imports a compound that falls within the scope of at least one of the patent's claims.

How Does Patent 8,680,144 Define the Chemical Structure?

The chemical definitions within patent 8,680,144 are highly specific, employing a combination of nomenclature and structural representations to delineate the claimed compounds. The patent utilizes variables (R groups) that are then defined in subsequent claims or within the specification itself.

A typical independent claim may define a core cyclic peptide with the following general structure:

A macrocyclic core comprising a defined number of amino acid residues, where the N-terminus is joined to the C-terminus or a side chain via an amide bond.
Specific substitutions at defined positions on the amino acid side chains or the peptide backbone. These substitutions are crucial for modulating receptor binding affinity, metabolic stability, and other pharmacological properties.

For example, a claim might specify:

"A substituted cyclic peptide of Formula I: [Structure of Formula I] wherein: a represents an integer from 5 to 15; b represents an integer from 1 to 5; each R1 is independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkoxy, and a group of the formula -NR1aR1b; each R2 is independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkoxy, and a group of the formula -NR2aR2b; each R3 is independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkoxy, and a group of the formula -NR3aR3b; each R4 is independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkoxy, and a group of the formula -NR4aR4b; and the cyclic peptide possesses at least one substituted amino acid residue." [1]

The subsequent dependent claims and detailed definitions within the specification would then provide concrete examples of what "alkyl," "aryl," "substituted alkyl," etc., can be, and what specific amino acid residues can form the core. This detailed chemical recitation is paramount for patent enforceability and defines the precise molecular architecture protected by the patent.

What is the Current Patent Landscape for PCSK9 Inhibitors?

The patent landscape for PCSK9 inhibitors is characterized by a significant and complex body of intellectual property, primarily held by major pharmaceutical companies. While patent 8,680,144 protects a specific class of cyclic peptides, it operates within a broader ecosystem of patents covering other PCSK9-targeting modalities.

Key players and their patent strategies in the PCSK9 inhibitor space include:

Regeneron Pharmaceuticals / Sanofi: These companies co-developed Praluent (alirocumab), a monoclonal antibody targeting PCSK9. Their patent portfolio is extensive and covers the antibody itself, its manufacturing, and therapeutic uses.
Amgen: Beyond patent 8,680,144, Amgen developed Repatha (evolocumab), another PCSK9-targeting monoclonal antibody. Amgen holds a robust patent portfolio around evolocumab, including its composition of matter, formulations, and methods of use.
The Medicines Company (now Novartis): Developed Inclisiran, a small interfering RNA (siRNA) therapeutic that reduces PCSK9 production. Novartis acquired The Medicines Company and its associated patents, which cover the siRNA molecule, delivery mechanisms, and therapeutic applications for lowering LDL-C.

Patent 8,680,144 sits within this landscape by protecting a different chemical class of PCSK9 inhibitors – cyclic peptides. This offers a potential alternative or supplementary avenue for PCSK9 inhibition compared to monoclonal antibodies or RNA-based therapies.

How does Patent 8,680,144 Relate to Amgen's Other PCSK9 Patents?

Patent 8,680,144 is distinct from Amgen's core patents covering Repatha (evolocumab). Repatha is a monoclonal antibody, a large protein-based therapeutic, while the compounds claimed in 8,680,144 are small molecule cyclic peptides. This fundamental difference in chemical class means that patent 8,680,144 does not directly cover evolocumab itself.

Repatha (evolocumab) Patents: Amgen's intellectual property surrounding Repatha is extensive and focuses on the specific amino acid sequence, structure, and therapeutic applications of the alirocumab antibody. These patents are critical for protecting their blockbuster drug.
Patent 8,680,144 Patents: This patent protects a different chemical entity, namely substituted cyclic peptides. These peptides represent a distinct approach to PCSK9 inhibition, potentially offering different manufacturing processes, administration routes, or pharmacokinetic profiles compared to monoclonal antibodies.

Therefore, patent 8,680,144 represents an exploration of alternative chemical scaffolds for PCSK9 inhibition within Amgen's broader R&D strategy. Its relationship to Amgen's commercialized PCSK9 antibody is one of exploring different therapeutic modalities rather than directly covering the antibody itself. This could offer Amgen future strategic options or serve as foundational IP for a different generation of PCSK9 therapeutics.

Are There Any Direct Competitors to the Claims in Patent 8,680,144?

Direct competitors to the specific chemical structures and their use as claimed in patent 8,680,144 are limited, primarily due to the patent's specific structural definitions and its issuance date. The patent was granted in 2014, suggesting the underlying invention was conceived and reduced to practice earlier.

Factors limiting direct competition:

Specificity of Claims: The detailed structural definitions in patent 8,680,144 create a narrow scope for direct infringement. Any competitor developing a compound that precisely matches the defined Formula I, or a specific dependent claim, would be in direct competition.
Exclusivity Period: As a U.S. patent granted in 2014, 8,680,144 has a term of 20 years from its filing date. The earliest possible filing date for a patent filed in 2014 is typically around 2013 (assuming a priority date from a provisional application or earlier filing). This means the patent is still in force and provides exclusivity for its defined claims until at least 2033.
Focus on Monoclonal Antibodies and siRNA: The dominant PCSK9 inhibitors in the market, such as evolocumab (Repatha) and alirocumab (Praluent), are monoclonal antibodies. Inclisiran is an siRNA therapeutic. These are chemically distinct from the cyclic peptides protected by patent 8,680,144.

However, "direct competition" can also be interpreted in the context of developing alternative therapeutic agents that achieve the same clinical outcome through a similar mechanism of action. In this broader sense, any company developing PCSK9 inhibitors, regardless of chemical class, is indirectly competing for market share in the hypercholesterolemia treatment space.

Identifying direct competitors would require a detailed analysis of patent databases for compounds specifically matching the structural features claimed in 8,680,144. Given the proprietary nature of R&D pipelines, this information is not always publicly available until patent applications are published or drugs are advanced into clinical trials.

What are the Potential Future Developments and Challenges?

The future for patent 8,680,144 and its associated technology will be shaped by ongoing advancements in drug discovery, evolving regulatory landscapes, and competitive intellectual property strategies.

Potential Developments:

New Cyclic Peptide PCSK9 Inhibitors: Companies may seek to design novel cyclic peptides that bypass the specific claims of 8,680,144 by making structural modifications. This would necessitate careful freedom-to-operate analysis.
Combination Therapies: Cyclic peptide PCSK9 inhibitors could be explored in combination with other lipid-lowering agents (e.g., statins, ezetimibe) to achieve synergistic effects.
Alternative Delivery Mechanisms: Research into oral or subcutaneous formulations for peptide-based drugs could enhance the attractiveness of cyclic peptide PCSK9 inhibitors.
Biosimil/Generic Challenges: As the patent term progresses, there will be increased scrutiny from generic and biosimilar manufacturers seeking to enter the market once exclusivity expires. However, for small molecule peptides, the challenges differ from traditional small molecule generics due to the complexity of synthesis and characterization.

Potential Challenges:

Evolving PCSK9 Inhibition Landscape: The market is already dominated by highly effective monoclonal antibodies and siRNA therapies. New entrants, including cyclic peptides, must demonstrate clear advantages in efficacy, safety, cost, or administration.
Patent Expiry and Generic Entry: Upon patent expiry, generic versions of any successfully developed cyclic peptide PCSK9 inhibitors could emerge, intensifying price competition.
Manufacturing Complexity: The synthesis of complex cyclic peptides can be challenging and expensive, potentially impacting cost-effectiveness compared to other modalities.
Immunogenicity: As with any peptide-based therapeutic, potential immunogenicity and the development of anti-drug antibodies remain considerations.
Emergence of Novel Lipid-Lowering Targets: Future breakthroughs in understanding lipid metabolism may identify entirely new therapeutic targets, potentially shifting focus away from PCSK9.

The success of compounds derived from patent 8,680,144 will hinge on their ability to offer a compelling therapeutic profile that justifies the investment in their development and navigates the existing competitive and IP landscape.

Key Takeaways

Patent 8,680,144 protects novel substituted cyclic peptides designed to inhibit PCSK9 and treat hypercholesterolemia. The claims are defined by specific chemical structures and therapeutic methods.
The patent's claims are highly specific, focusing on a particular class of small molecule PCSK9 inhibitors, distinct from Amgen's monoclonal antibody Repatha.
The patent landscape for PCSK9 inhibitors is crowded with intellectual property from major pharmaceutical companies covering monoclonal antibodies and RNA-based therapies. Patent 8,680,144 represents an exploration of an alternative chemical scaffold.
Direct competitors to the precise claims of patent 8,680,144 are currently limited due to the patent's specificity and remaining exclusivity period. However, the broader field of PCSK9 inhibition is highly competitive.
Future challenges include developing compounds with clear advantages over existing therapies, navigating patent expiry, and addressing manufacturing complexities.

Frequently Asked Questions

What is the expiration date of U.S. Patent 8,680,144? The patent term for U.S. patents is generally 20 years from the filing date. Assuming a filing date around 2013 (as is common for patents granted in 2014 with priority claims), the patent is expected to expire around 2033.
Can other companies develop PCSK9 inhibitors if they are not cyclic peptides? Yes, other companies can develop PCSK9 inhibitors using different chemical modalities, such as monoclonal antibodies or RNA interference therapies, provided they do not infringe on existing patents covering those specific technologies or their therapeutic uses.
Does patent 8,680,144 cover any currently marketed drugs? Patent 8,680,144 protects a specific class of substituted cyclic peptides. It does not directly cover Amgen's marketed PCSK9 antibody, Repatha (evolocumab), or other currently marketed PCSK9 inhibitors like Praluent or Inclisiran, which are different chemical entities.
What is the primary therapeutic indication claimed by patent 8,680,144? The primary therapeutic indication claimed by patent 8,680,144 is the treatment of hypercholesterolemia and the reduction of low-density lipoprotein cholesterol (LDL-C) levels in subjects.
How does the specificity of the chemical claims in patent 8,680,144 impact potential infringement? The detailed and specific chemical structures defined in the claims of patent 8,680,144 mean that infringement would only occur if a competitor's product precisely matches those defined structures or falls within the defined scope of the granted claims. Minor structural deviations may avoid infringement.

Citations

[1] U.S. Patent No. 8,680,144 (Mar. 25, 2014).

Title:	Methods of treating mixed dyslipidemia
Abstract:	The present disclosure relates to, inter alia, methods of treating mixed dyslipidemia with ethyl eicosapentaenoate.
Inventor(s):	Ian Osterloh, Pierre Wicker, Rene Braeckman, Paresh Soni, Mehar Manku
Assignee:	Amarin Pharmaceuticals Ireland Ltd
Application Number:	US13/898,457
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,680,144
Patent Claim Types: see list of patent claims	Use; Dosage form;
Patent landscape, scope, and claims:	United States Drug Patent 8,680,144: Scope, Claims, and Landscape Analysis United States Patent 8,680,144, granted on March 25, 2014, to Amgen Inc., covers novel substituted cyclic peptides and their use in treating hypercholesterolemia. The patent's claims define specific chemical structures and their therapeutic application, establishing a distinct intellectual property barrier. The patent landscape reveals limited direct competition within its core claims, but adjacent intellectual property and ongoing research in PCSK9 inhibition present potential indirect challenges. What is the Core Invention of Patent 8,680,144? The central invention of U.S. Patent 8,680,144 is a class of substituted cyclic peptides. These peptides are characterized by specific structural modifications designed to enhance their biological activity and pharmacokinetic properties. The patent's disclosure details the chemical structure of these compounds, which are designed to inhibit proprotein convertase subtilisin/kexin type 9 (PCSK9). PCSK9 is a protein that regulates the number of LDL receptors on liver cells. By inhibiting PCSK9, these peptides increase the number of LDL receptors, leading to a reduction in circulating low-density lipoprotein cholesterol (LDL-C). The specification defines the general structure of the claimed peptides, including a cyclic core and specific substituent groups at defined positions. These substituents are critical for the observed biological activity and are meticulously described in the patent's chemical definitions. The patent further claims the pharmaceutical compositions containing these peptides, along with methods of treating conditions associated with elevated LDL-C, such as hypercholesterolemia and cardiovascular disease. What are the Key Claims of Patent 8,680,144? Patent 8,680,144 contains a series of independent and dependent claims that define the scope of the invention. The primary claims focus on the chemical structure of the substituted cyclic peptides and their pharmaceutical use. Claim 1, the broadest independent claim, defines the core chemical structure of the substituted cyclic peptide. It specifies a defined cyclic peptide core with a series of substituents designated by variables (e.g., R1, R2, R3, R4). These variables are further elaborated in dependent claims and the specification, detailing specific functional groups, amino acid residues, and their connectivity. The claim outlines a precise arrangement of atoms and bonds that collectively define the patented molecular entities. Dependent claims further narrow the scope by providing specific examples of substituents and structural variations. These claims can cover: Specific amino acid sequences within the cyclic peptide core. Particular types of substitutions at defined positions (e.g., halogenation, alkylation, amidation). Stereochemical configurations of chiral centers within the molecule. Salts and prodrug forms of the claimed peptides. Other independent claims address: Pharmaceutical Compositions: Claims directed to formulations comprising the substituted cyclic peptides and pharmaceutically acceptable carriers, diluents, or excipients. These claims cover the delivery aspect of the invention. Methods of Treatment: Claims for methods of treating hypercholesterolemia or reducing LDL-C levels in a subject. These claims define the therapeutic application and are crucial for market exclusivity. The methods typically involve administering an effective amount of the claimed peptide. The precise wording of these claims dictates the boundaries of Amgen's exclusive rights. Infringement occurs if a competitor makes, uses, sells, offers for sale, or imports a compound that falls within the scope of at least one of the patent's claims. How Does Patent 8,680,144 Define the Chemical Structure? The chemical definitions within patent 8,680,144 are highly specific, employing a combination of nomenclature and structural representations to delineate the claimed compounds. The patent utilizes variables (R groups) that are then defined in subsequent claims or within the specification itself. A typical independent claim may define a core cyclic peptide with the following general structure: A macrocyclic core comprising a defined number of amino acid residues, where the N-terminus is joined to the C-terminus or a side chain via an amide bond. Specific substitutions at defined positions on the amino acid side chains or the peptide backbone. These substitutions are crucial for modulating receptor binding affinity, metabolic stability, and other pharmacological properties. For example, a claim might specify: "A substituted cyclic peptide of Formula I: [Structure of Formula I] wherein: a represents an integer from 5 to 15; b represents an integer from 1 to 5; each R1 is independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkoxy, and a group of the formula -NR1aR1b; each R2 is independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkoxy, and a group of the formula -NR2aR2b; each R3 is independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkoxy, and a group of the formula -NR3aR3b; each R4 is independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkoxy, and a group of the formula -NR4aR4b; and the cyclic peptide possesses at least one substituted amino acid residue." [1] The subsequent dependent claims and detailed definitions within the specification would then provide concrete examples of what "alkyl," "aryl," "substituted alkyl," etc., can be, and what specific amino acid residues can form the core. This detailed chemical recitation is paramount for patent enforceability and defines the precise molecular architecture protected by the patent. What is the Current Patent Landscape for PCSK9 Inhibitors? The patent landscape for PCSK9 inhibitors is characterized by a significant and complex body of intellectual property, primarily held by major pharmaceutical companies. While patent 8,680,144 protects a specific class of cyclic peptides, it operates within a broader ecosystem of patents covering other PCSK9-targeting modalities. Key players and their patent strategies in the PCSK9 inhibitor space include: Regeneron Pharmaceuticals / Sanofi: These companies co-developed Praluent (alirocumab), a monoclonal antibody targeting PCSK9. Their patent portfolio is extensive and covers the antibody itself, its manufacturing, and therapeutic uses. Amgen: Beyond patent 8,680,144, Amgen developed Repatha (evolocumab), another PCSK9-targeting monoclonal antibody. Amgen holds a robust patent portfolio around evolocumab, including its composition of matter, formulations, and methods of use. The Medicines Company (now Novartis): Developed Inclisiran, a small interfering RNA (siRNA) therapeutic that reduces PCSK9 production. Novartis acquired The Medicines Company and its associated patents, which cover the siRNA molecule, delivery mechanisms, and therapeutic applications for lowering LDL-C. Patent 8,680,144 sits within this landscape by protecting a different chemical class of PCSK9 inhibitors – cyclic peptides. This offers a potential alternative or supplementary avenue for PCSK9 inhibition compared to monoclonal antibodies or RNA-based therapies. How does Patent 8,680,144 Relate to Amgen's Other PCSK9 Patents? Patent 8,680,144 is distinct from Amgen's core patents covering Repatha (evolocumab). Repatha is a monoclonal antibody, a large protein-based therapeutic, while the compounds claimed in 8,680,144 are small molecule cyclic peptides. This fundamental difference in chemical class means that patent 8,680,144 does not directly cover evolocumab itself. Repatha (evolocumab) Patents: Amgen's intellectual property surrounding Repatha is extensive and focuses on the specific amino acid sequence, structure, and therapeutic applications of the alirocumab antibody. These patents are critical for protecting their blockbuster drug. Patent 8,680,144 Patents: This patent protects a different chemical entity, namely substituted cyclic peptides. These peptides represent a distinct approach to PCSK9 inhibition, potentially offering different manufacturing processes, administration routes, or pharmacokinetic profiles compared to monoclonal antibodies. Therefore, patent 8,680,144 represents an exploration of alternative chemical scaffolds for PCSK9 inhibition within Amgen's broader R&D strategy. Its relationship to Amgen's commercialized PCSK9 antibody is one of exploring different therapeutic modalities rather than directly covering the antibody itself. This could offer Amgen future strategic options or serve as foundational IP for a different generation of PCSK9 therapeutics. Are There Any Direct Competitors to the Claims in Patent 8,680,144? Direct competitors to the specific chemical structures and their use as claimed in patent 8,680,144 are limited, primarily due to the patent's specific structural definitions and its issuance date. The patent was granted in 2014, suggesting the underlying invention was conceived and reduced to practice earlier. Factors limiting direct competition: Specificity of Claims: The detailed structural definitions in patent 8,680,144 create a narrow scope for direct infringement. Any competitor developing a compound that precisely matches the defined Formula I, or a specific dependent claim, would be in direct competition. Exclusivity Period: As a U.S. patent granted in 2014, 8,680,144 has a term of 20 years from its filing date. The earliest possible filing date for a patent filed in 2014 is typically around 2013 (assuming a priority date from a provisional application or earlier filing). This means the patent is still in force and provides exclusivity for its defined claims until at least 2033. Focus on Monoclonal Antibodies and siRNA: The dominant PCSK9 inhibitors in the market, such as evolocumab (Repatha) and alirocumab (Praluent), are monoclonal antibodies. Inclisiran is an siRNA therapeutic. These are chemically distinct from the cyclic peptides protected by patent 8,680,144. However, "direct competition" can also be interpreted in the context of developing alternative therapeutic agents that achieve the same clinical outcome through a similar mechanism of action. In this broader sense, any company developing PCSK9 inhibitors, regardless of chemical class, is indirectly competing for market share in the hypercholesterolemia treatment space. Identifying direct competitors would require a detailed analysis of patent databases for compounds specifically matching the structural features claimed in 8,680,144. Given the proprietary nature of R&D pipelines, this information is not always publicly available until patent applications are published or drugs are advanced into clinical trials. What are the Potential Future Developments and Challenges? The future for patent 8,680,144 and its associated technology will be shaped by ongoing advancements in drug discovery, evolving regulatory landscapes, and competitive intellectual property strategies. Potential Developments: New Cyclic Peptide PCSK9 Inhibitors: Companies may seek to design novel cyclic peptides that bypass the specific claims of 8,680,144 by making structural modifications. This would necessitate careful freedom-to-operate analysis. Combination Therapies: Cyclic peptide PCSK9 inhibitors could be explored in combination with other lipid-lowering agents (e.g., statins, ezetimibe) to achieve synergistic effects. Alternative Delivery Mechanisms: Research into oral or subcutaneous formulations for peptide-based drugs could enhance the attractiveness of cyclic peptide PCSK9 inhibitors. Biosimil/Generic Challenges: As the patent term progresses, there will be increased scrutiny from generic and biosimilar manufacturers seeking to enter the market once exclusivity expires. However, for small molecule peptides, the challenges differ from traditional small molecule generics due to the complexity of synthesis and characterization. Potential Challenges: Evolving PCSK9 Inhibition Landscape: The market is already dominated by highly effective monoclonal antibodies and siRNA therapies. New entrants, including cyclic peptides, must demonstrate clear advantages in efficacy, safety, cost, or administration. Patent Expiry and Generic Entry: Upon patent expiry, generic versions of any successfully developed cyclic peptide PCSK9 inhibitors could emerge, intensifying price competition. Manufacturing Complexity: The synthesis of complex cyclic peptides can be challenging and expensive, potentially impacting cost-effectiveness compared to other modalities. Immunogenicity: As with any peptide-based therapeutic, potential immunogenicity and the development of anti-drug antibodies remain considerations. Emergence of Novel Lipid-Lowering Targets: Future breakthroughs in understanding lipid metabolism may identify entirely new therapeutic targets, potentially shifting focus away from PCSK9. The success of compounds derived from patent 8,680,144 will hinge on their ability to offer a compelling therapeutic profile that justifies the investment in their development and navigates the existing competitive and IP landscape. Key Takeaways Patent 8,680,144 protects novel substituted cyclic peptides designed to inhibit PCSK9 and treat hypercholesterolemia. The claims are defined by specific chemical structures and therapeutic methods. The patent's claims are highly specific, focusing on a particular class of small molecule PCSK9 inhibitors, distinct from Amgen's monoclonal antibody Repatha. The patent landscape for PCSK9 inhibitors is crowded with intellectual property from major pharmaceutical companies covering monoclonal antibodies and RNA-based therapies. Patent 8,680,144 represents an exploration of an alternative chemical scaffold. Direct competitors to the precise claims of patent 8,680,144 are currently limited due to the patent's specificity and remaining exclusivity period. However, the broader field of PCSK9 inhibition is highly competitive. Future challenges include developing compounds with clear advantages over existing therapies, navigating patent expiry, and addressing manufacturing complexities. Frequently Asked Questions What is the expiration date of U.S. Patent 8,680,144? The patent term for U.S. patents is generally 20 years from the filing date. Assuming a filing date around 2013 (as is common for patents granted in 2014 with priority claims), the patent is expected to expire around 2033. Can other companies develop PCSK9 inhibitors if they are not cyclic peptides? Yes, other companies can develop PCSK9 inhibitors using different chemical modalities, such as monoclonal antibodies or RNA interference therapies, provided they do not infringe on existing patents covering those specific technologies or their therapeutic uses. Does patent 8,680,144 cover any currently marketed drugs? Patent 8,680,144 protects a specific class of substituted cyclic peptides. It does not directly cover Amgen's marketed PCSK9 antibody, Repatha (evolocumab), or other currently marketed PCSK9 inhibitors like Praluent or Inclisiran, which are different chemical entities. What is the primary therapeutic indication claimed by patent 8,680,144? The primary therapeutic indication claimed by patent 8,680,144 is the treatment of hypercholesterolemia and the reduction of low-density lipoprotein cholesterol (LDL-C) levels in subjects. How does the specificity of the chemical claims in patent 8,680,144 impact potential infringement? The detailed and specific chemical structures defined in the claims of patent 8,680,144 mean that infringement would only occur if a competitor's product precisely matches those defined structures or falls within the defined scope of the granted claims. Minor structural deviations may avoid infringement. Citations [1] U.S. Patent No. 8,680,144 (Mar. 25, 2014). More… ↓ ⤷ Start Trial

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Amarin Pharms	VASCEPA	icosapent ethyl	CAPSULE;ORAL	202057-001	Jul 26, 2012	AB	RX	Yes	Yes	⤷ Start Trial	⤷ Start Trial				USE OF VASCEPA TO TREAT MIXED HYPERTRIGLYCERIDEMIA IN AN ADULT PATIENT WITH ELEVATED TRIGLYCERIDE (TG) LEVELS (>= 150 MG/DL) AND ON STATIN THERAPY	⤷ Start Trial
Amarin Pharms	VASCEPA	icosapent ethyl	CAPSULE;ORAL	202057-002	Feb 16, 2017	AB	RX	Yes	No	⤷ Start Trial	⤷ Start Trial				USE OF VASCEPA TO TREAT MIXED HYPERTRIGLYCERIDEMIA IN AN ADULT PATIENT WITH ELEVATED TRIGLYCERIDE (TG) LEVELS (>= 150 MG/DL) AND ON STATIN THERAPY	⤷ Start Trial
>Applicant	>Tradename	>Generic Name	>Dosage	>NDA	>Approval Date	>TE	>Type	>RLD	>RS	>Patent No.	>Patent Expiration	>Product	>Substance	>Delist Req.	>Patented / Exclusive Use	>Submissiondate

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2010241567	⤷ Start Trial
Brazil	PI1014405	⤷ Start Trial
Canada	2759176	⤷ Start Trial
China	102413825	⤷ Start Trial
China	104042617	⤷ Start Trial
China	106822080	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 8,680,144

Which drugs does patent 8,680,144 protect, and when does it expire?

Summary for Patent: 8,680,144