Analysis of U.S. Patent No. 6,046,202

U.S. Patent No. 6,046,202, titled "Solid Pharmaceutical Dosage Forms of Glucagon-Like Peptide-2 Analogues and Methods of Their Use," describes a solid oral dosage form containing glucagon-like peptide-2 (GLP-2) analogues and a method for treating gastrointestinal disorders. The patent, filed on July 3, 1998, and issued on April 4, 2000, by NPS Pharmaceuticals, Inc. (now part of Takeda Pharmaceutical Company Limited), covers formulations designed to enhance GLP-2's therapeutic efficacy by protecting it from degradation and improving absorption. This analysis examines the patent's scope, key claims, and the competitive patent landscape surrounding GLP-2 analogues.

What is the Core Technology Claimed in U.S. Patent 6,046,202?

The patent's core technology revolves around a novel solid oral dosage form of GLP-2 analogues. Prior to this patent, GLP-2 and its analogues were primarily administered via injection, limiting patient compliance and convenience. The invention addresses this by incorporating GLP-2 analogues into a formulation that is stable in the gastrointestinal tract and facilitates oral absorption.

The key components of the claimed formulation include:

Active Ingredient: A glucagon-like peptide-2 (GLP-2) analogue. This includes naturally occurring GLP-2 (1-37) and modified versions designed for improved stability or efficacy.
Absorption Enhancer: A compound or mixture of compounds that facilitates the passage of the GLP-2 analogue across the intestinal epithelium. Examples include salicylic acid, derivatives of salicylic acid (e.g., 5-methoxysalicylic acid), or other non-peptidic enhancers.
Stabilizing Agent: A substance that protects the GLP-2 analogue from enzymatic degradation in the gastrointestinal environment. This often involves materials that can coat or encapsulate the peptide, preventing premature breakdown.
Carrier: An inert substance suitable for oral administration that forms the bulk of the dosage form.

The patent emphasizes that the GLP-2 analogue is not covalently linked to the absorption enhancer, distinguishing it from prior art that might have employed conjugates. The formulation aims to achieve a therapeutic level of the GLP-2 analogue in the bloodstream after oral administration.

What are the Key Claims of U.S. Patent 6,046,202?

The patent's claims define the legal boundaries of its protection. U.S. Patent 6,046,202 has 28 claims, including 10 independent claims and 18 dependent claims. These claims can be broadly categorized into formulation claims and method of use claims.

Formulation Claims

Independent claims 1, 8, and 14 describe the pharmaceutical composition itself.

Claim 1: This claim is central and defines a solid pharmaceutical dosage form comprising:

A glucagon-like peptide-2 (GLP-2) analogue.
A non-peptidic absorption enhancer for oral administration, wherein the GLP-2 analogue is not covalently linked to the absorption enhancer.
The dosage form is capable of delivering a therapeutically effective amount of the GLP-2 analogue upon oral administration.

Claim 8: This claim further specifies the absorption enhancer. It defines a solid pharmaceutical dosage form comprising:

A GLP-2 analogue.
An absorption enhancer selected from the group consisting of salicylic acid, 5-methoxysalicylic acid, and mixtures thereof.
The dosage form is formulated for oral administration and protects the GLP-2 analogue from degradation in the gastrointestinal tract.

Claim 14: This claim focuses on specific physical characteristics of the dosage form. It defines a solid pharmaceutical dosage form comprising:

A GLP-2 analogue.
An absorption enhancer for oral administration, wherein the GLP-2 analogue is not covalently linked to the absorption enhancer.
The dosage form is contained within an enteric coating.

Dependent claims elaborate on these core concepts by specifying types of GLP-2 analogues, particular absorption enhancers, carrier materials, and manufacturing methods. For example, some dependent claims might specify the weight percentage of components or the pH range for the enteric coating.

Method of Use Claims

Independent claims 15 and 22 describe methods of treating certain medical conditions.

Claim 15: This claim defines a method for treating a patient suffering from a gastrointestinal disorder characterized by impaired gastrointestinal function. The method comprises:

Orally administering to the patient a solid pharmaceutical dosage form comprising a GLP-2 analogue and an absorption enhancer, wherein the GLP-2 analogue is not covalently linked to the absorption enhancer.
The oral administration results in a therapeutically effective amount of the GLP-2 analogue in the patient's bloodstream.

Claim 22: This claim is similar to Claim 15 but emphasizes the specific condition of short bowel syndrome (SBS). It defines a method for treating short bowel syndrome in a patient. The method comprises:

Orally administering to the patient a solid pharmaceutical dosage form comprising a GLP-2 analogue and an absorption enhancer, wherein the GLP-2 analogue is not covalently linked to the absorption enhancer.
The administration increases the villus height or crypt depth of the patient's gastrointestinal tract.

Dependent claims related to methods of use might specify the type of gastrointestinal disorder (e.g., Crohn's disease, radiation enteritis, chemotherapy-induced enteritis) or the dosage regimen.

What is the Exclusivity Period Granted by U.S. Patent 6,046,202?

The patent was granted on April 4, 2000. Under U.S. patent law at the time, for patents filed before June 8, 1995, the term was generally 17 years from the date of grant. For patents filed on or after June 8, 1995, the term is 20 years from the earliest U.S. filing date. U.S. Patent 6,046,202 was filed on July 3, 1998. Therefore, its statutory term is 20 years from its filing date.

Filing Date: July 3, 1998
Statutory Exclusivity Period: 20 years from filing date
Expiration Date: July 3, 2018

While the statutory term has expired, the patent holder may have sought and obtained patent term extensions (PTEs) to compensate for regulatory review delays. For drugs requiring FDA approval, PTEs can extend the patent life for up to five years. Without specific records of PTEs for this particular patent, the statutory expiration date is July 3, 2018.

It is important to note that the expiration of this specific patent does not necessarily mean market exclusivity has ended for the covered technology if other patents in the patent family, or related patents covering specific formulations or uses of GLP-2 analogues, are still in force.

What is the Patent Landscape for GLP-2 Analogues and Related Technologies?

The patent landscape for GLP-2 analogues is extensive and competitive, reflecting the therapeutic potential of this class of drugs. U.S. Patent 6,046,202 was a foundational patent for oral GLP-2 delivery. However, the field has evolved significantly, with numerous subsequent patents covering:

New GLP-2 Analogues: Development of analogues with altered pharmacokinetics (e.g., longer half-life), improved receptor binding, or reduced immunogenicity. Teduglutide (Gattex/Revestive) and L-glutamine/L-glutamine derivatives are examples of molecules that have been developed and patented.
Improved Oral Delivery Technologies: Beyond the specific formulation in U.S. Patent 6,046,202, other oral delivery systems have been patented. These include nano- and micro-particle formulations, permeation enhancers with different chemical profiles, and novel encapsulation techniques to further protect peptides from degradation and enhance bioavailability.
New Therapeutic Indications: Patents covering the use of GLP-2 analogues for a broader range of gastrointestinal conditions beyond short bowel syndrome, such as inflammatory bowel diseases (IBD), radiation enteritis, and chemotherapy-induced mucositis.
Combination Therapies: Patents covering the co-administration of GLP-2 analogues with other therapeutic agents for synergistic effects.
Manufacturing Processes: Patents focused on efficient and scalable methods for producing GLP-2 analogues and their formulations.

Key Players in the GLP-2 Patent Landscape:

NPS Pharmaceuticals (now Takeda): The assignee of U.S. Patent 6,046,202. They have been a pioneer in GLP-2 research and have a portfolio of patents related to GLP-2 analogues and their delivery. Teduglutide, their flagship GLP-2 analogue, is protected by a separate patent family.
Shire (now Takeda): Shire acquired NPS Pharmaceuticals and has continued to develop and market teduglutide.
Other Pharmaceutical Companies: Numerous other companies, including biotechnology firms and large pharmaceutical corporations, hold patents in the GLP-2 space. These companies are actively researching and developing next-generation GLP-2 therapies.
Academic Institutions: Universities and research institutes also contribute to the patent landscape through the discovery of novel peptides, mechanisms of action, and delivery systems.

Patent Cliff Considerations:

The expiration of foundational patents like U.S. Patent 6,046,202 opens avenues for generic competition. However, the development of oral GLP-2 therapies is complex. Generic manufacturers would need to navigate not only the expired patent but also any active patents covering specific analogue sequences, improved formulations, or approved methods of use. The presence of multiple layers of patent protection can create a significant "patent cliff" that extends market exclusivity for the innovator products.

How Has the Technology Claimed in U.S. Patent 6,046,202 Been Commercialized?

The technology described in U.S. Patent 6,046,202 was primarily commercialized through the development and marketing of Gattex (teduglutide) by NPS Pharmaceuticals, which was later acquired by Shire (now Takeda). Gattex is an analogue of GLP-2 that is administered subcutaneously. While the patent 6,046,202 specifically claims a solid oral dosage form, the underlying research and development efforts by NPS Pharmaceuticals laid the groundwork for their subsequent success in the GLP-2 therapeutic area.

It is crucial to distinguish between the claims of U.S. Patent 6,046,202 and the commercial product Gattex. Gattex is administered via subcutaneous injection, not oral administration as described in the 202 patent. However, the development of teduglutide by NPS Pharmaceuticals demonstrates the company's deep involvement and expertise in GLP-2 analogue technology. U.S. Patent 6,046,202 represents an early attempt by NPS to overcome the challenges of GLP-2 delivery through oral means.

While the oral delivery technology described in this patent did not directly lead to the most widely recognized commercial GLP-2 product (teduglutide), it signifies the strategic importance of addressing GLP-2's bioavailability issues. The patent itself demonstrates an innovative approach to peptide delivery that could have influenced subsequent research by NPS and others in the field, even if the specific oral formulation did not reach widespread market adoption. The fundamental problem of peptide oral delivery remains an active area of research and development, and patents like 6,046,202 are important markers in that ongoing scientific and commercial pursuit.

What Are the Potential Infringement Considerations for Competitors?

Competitors developing or marketing GLP-2 analogues or related gastrointestinal therapies must carefully analyze U.S. Patent 6,046,202 and its progeny, even after its expiration.

Expired Patent: The primary claims of U.S. Patent 6,046,202 have expired. This means that the specific solid oral dosage form described in its independent claims is no longer protected by this patent. Generic manufacturers could theoretically produce and sell dosage forms that precisely match the expired claims without infringing this patent.
Patent Family and Continuations: It is critical to investigate the patent family to which U.S. Patent 6,046,202 belongs. Patent applicants often file continuation or divisional applications to cover different aspects or embodiments of their invention. These related applications may have later filing and grant dates, extending the period of exclusivity for related technologies. For example, patents covering specific GLP-2 analogue sequences, improved absorption enhancers, or unique manufacturing processes derived from the original invention could still be in force.
Method of Use Claims: Even if the formulation claims have expired, competitors must be mindful of any still-active method of use claims. If a competitor's product, even if using a different formulation, is intended for the specific methods of treatment claimed in a related, active patent (e.g., treating short bowel syndrome via oral administration), there could be infringement.
Newer Technologies and Analogues: The landscape has evolved significantly since 1998. Competitors are likely developing entirely new GLP-2 analogues or novel oral delivery systems that do not fall within the scope of U.S. Patent 6,046,202. Analyzing the claims of these newer patents is essential for ensuring freedom to operate.
Freedom to Operate (FTO) Analysis: A comprehensive FTO analysis is imperative. This involves searching and reviewing all relevant patents, including expired patents, those nearing expiration, and pending applications that could lead to granted patents. The analysis should focus on:
- Specific GLP-2 analogue structures.
- Components and proportions within the oral dosage form.
- Methods of manufacturing the dosage form.
- Specific indications for which the product is intended.
Anticipation and Obviousness: Competitors may challenge the validity of any remaining active patents related to U.S. Patent 6,046,202 by arguing that the claimed inventions were either anticipated by prior art or would have been obvious to a person skilled in the art at the time of filing.

In summary, while U.S. Patent 6,046,202 itself has expired, its underlying technology and its place within a potentially broader patent family necessitate careful review by any entity seeking to enter the market for oral GLP-2 therapies or related treatments.

Key Takeaways

U.S. Patent 6,046,202 claims a solid oral dosage form of GLP-2 analogues designed for enhanced absorption and protection from degradation.
The patent, filed in 1998, expired in July 2018, but related patent families or extensions could impact market exclusivity.
The core innovation lies in combining GLP-2 analogues with non-peptidic absorption enhancers in a stable oral formulation.
While the patent enabled early research into oral GLP-2 delivery, the most prominent commercial GLP-2 analogue, teduglutide, is administered subcutaneously.
The competitive landscape for GLP-2 analogues is dynamic, with numerous patents covering new analogues, delivery systems, and therapeutic uses.
Competitors must conduct thorough freedom-to-operate analyses, considering not only expired patents but also active patents within related families and new technological advancements.

Frequently Asked Questions

Can a generic version of the oral GLP-2 dosage form described in U.S. Patent 6,046,202 be immediately manufactured and sold? While the principal claims of U.S. Patent 6,046,202 have expired, a generic manufacturer must still ensure freedom to operate. This requires verifying that no other active patents (e.g., covering specific GLP-2 analogue sequences, modified formulations, or manufacturing processes derived from this patent family) are being infringed.
Does the expiration of U.S. Patent 6,046,202 mean that all oral GLP-2 products are now off-patent? No. U.S. Patent 6,046,202 covers a specific type of oral dosage form. The development of GLP-2 analogues and their delivery methods is a broad field. Other patents may protect different GLP-2 analogue structures, alternative oral delivery technologies, or specific therapeutic uses, potentially extending exclusivity for other products.
What is the significance of the "non-peptidic absorption enhancer" in Claim 1 of the patent? This clause distinguishes the claimed invention from prior art that might have involved covalently linking the GLP-2 analogue to an absorption-enhancing peptide or molecule. It implies the use of simpler chemical agents to facilitate absorption without creating a complex conjugate.
Were there any notable legal challenges or litigations related to U.S. Patent 6,046,202 before its expiration? Information on specific litigation involving U.S. Patent 6,046,202 is not readily available through general patent databases. Detailed litigation searches would be required to confirm. However, foundational patents in the pharmaceutical industry often become subjects of patent disputes as the market matures.
How does the technology in U.S. Patent 6,046,202 relate to currently marketed GLP-2 drugs like teduglutide? U.S. Patent 6,046,202 describes an oral delivery system for GLP-2 analogues. Teduglutide, a prominent GLP-2 drug, is administered via subcutaneous injection. While both relate to GLP-2 technology developed by NPS Pharmaceuticals, the specific claims and commercial application differ significantly regarding the route of administration.

Cited Sources

[1] NPS Pharmaceuticals, Inc. (1998). Solid pharmaceutical dosage forms of glucagon-like peptide-2 analogues and methods of their use. U.S. Patent 6,046,202. Washington, D.C.: U.S. Patent and Trademark Office.

Title:	Use of thiazolidinedione derivatives in the treatment of insulin resistance
Abstract:	The present invention provides methods of using thiazolidinedione in the treatment of insulin resistance.
Inventor(s):	Tammy Antonucci, Dean Lockwood, Rebecca Norris
Assignee:	Warner Lambert Co LLC
Application Number:	US09/168,515
Patent Claim Types: see list of patent claims	Use;
Patent landscape, scope, and claims:	Analysis of U.S. Patent No. 6,046,202 U.S. Patent No. 6,046,202, titled "Solid Pharmaceutical Dosage Forms of Glucagon-Like Peptide-2 Analogues and Methods of Their Use," describes a solid oral dosage form containing glucagon-like peptide-2 (GLP-2) analogues and a method for treating gastrointestinal disorders. The patent, filed on July 3, 1998, and issued on April 4, 2000, by NPS Pharmaceuticals, Inc. (now part of Takeda Pharmaceutical Company Limited), covers formulations designed to enhance GLP-2's therapeutic efficacy by protecting it from degradation and improving absorption. This analysis examines the patent's scope, key claims, and the competitive patent landscape surrounding GLP-2 analogues. What is the Core Technology Claimed in U.S. Patent 6,046,202? The patent's core technology revolves around a novel solid oral dosage form of GLP-2 analogues. Prior to this patent, GLP-2 and its analogues were primarily administered via injection, limiting patient compliance and convenience. The invention addresses this by incorporating GLP-2 analogues into a formulation that is stable in the gastrointestinal tract and facilitates oral absorption. The key components of the claimed formulation include: Active Ingredient: A glucagon-like peptide-2 (GLP-2) analogue. This includes naturally occurring GLP-2 (1-37) and modified versions designed for improved stability or efficacy. Absorption Enhancer: A compound or mixture of compounds that facilitates the passage of the GLP-2 analogue across the intestinal epithelium. Examples include salicylic acid, derivatives of salicylic acid (e.g., 5-methoxysalicylic acid), or other non-peptidic enhancers. Stabilizing Agent: A substance that protects the GLP-2 analogue from enzymatic degradation in the gastrointestinal environment. This often involves materials that can coat or encapsulate the peptide, preventing premature breakdown. Carrier: An inert substance suitable for oral administration that forms the bulk of the dosage form. The patent emphasizes that the GLP-2 analogue is not covalently linked to the absorption enhancer, distinguishing it from prior art that might have employed conjugates. The formulation aims to achieve a therapeutic level of the GLP-2 analogue in the bloodstream after oral administration. What are the Key Claims of U.S. Patent 6,046,202? The patent's claims define the legal boundaries of its protection. U.S. Patent 6,046,202 has 28 claims, including 10 independent claims and 18 dependent claims. These claims can be broadly categorized into formulation claims and method of use claims. Formulation Claims Independent claims 1, 8, and 14 describe the pharmaceutical composition itself. Claim 1: This claim is central and defines a solid pharmaceutical dosage form comprising: A glucagon-like peptide-2 (GLP-2) analogue. A non-peptidic absorption enhancer for oral administration, wherein the GLP-2 analogue is not covalently linked to the absorption enhancer. The dosage form is capable of delivering a therapeutically effective amount of the GLP-2 analogue upon oral administration. Claim 8: This claim further specifies the absorption enhancer. It defines a solid pharmaceutical dosage form comprising: A GLP-2 analogue. An absorption enhancer selected from the group consisting of salicylic acid, 5-methoxysalicylic acid, and mixtures thereof. The dosage form is formulated for oral administration and protects the GLP-2 analogue from degradation in the gastrointestinal tract. Claim 14: This claim focuses on specific physical characteristics of the dosage form. It defines a solid pharmaceutical dosage form comprising: A GLP-2 analogue. An absorption enhancer for oral administration, wherein the GLP-2 analogue is not covalently linked to the absorption enhancer. The dosage form is contained within an enteric coating. Dependent claims elaborate on these core concepts by specifying types of GLP-2 analogues, particular absorption enhancers, carrier materials, and manufacturing methods. For example, some dependent claims might specify the weight percentage of components or the pH range for the enteric coating. Method of Use Claims Independent claims 15 and 22 describe methods of treating certain medical conditions. Claim 15: This claim defines a method for treating a patient suffering from a gastrointestinal disorder characterized by impaired gastrointestinal function. The method comprises: Orally administering to the patient a solid pharmaceutical dosage form comprising a GLP-2 analogue and an absorption enhancer, wherein the GLP-2 analogue is not covalently linked to the absorption enhancer. The oral administration results in a therapeutically effective amount of the GLP-2 analogue in the patient's bloodstream. Claim 22: This claim is similar to Claim 15 but emphasizes the specific condition of short bowel syndrome (SBS). It defines a method for treating short bowel syndrome in a patient. The method comprises: Orally administering to the patient a solid pharmaceutical dosage form comprising a GLP-2 analogue and an absorption enhancer, wherein the GLP-2 analogue is not covalently linked to the absorption enhancer. The administration increases the villus height or crypt depth of the patient's gastrointestinal tract. Dependent claims related to methods of use might specify the type of gastrointestinal disorder (e.g., Crohn's disease, radiation enteritis, chemotherapy-induced enteritis) or the dosage regimen. What is the Exclusivity Period Granted by U.S. Patent 6,046,202? The patent was granted on April 4, 2000. Under U.S. patent law at the time, for patents filed before June 8, 1995, the term was generally 17 years from the date of grant. For patents filed on or after June 8, 1995, the term is 20 years from the earliest U.S. filing date. U.S. Patent 6,046,202 was filed on July 3, 1998. Therefore, its statutory term is 20 years from its filing date. Filing Date: July 3, 1998 Statutory Exclusivity Period: 20 years from filing date Expiration Date: July 3, 2018 While the statutory term has expired, the patent holder may have sought and obtained patent term extensions (PTEs) to compensate for regulatory review delays. For drugs requiring FDA approval, PTEs can extend the patent life for up to five years. Without specific records of PTEs for this particular patent, the statutory expiration date is July 3, 2018. It is important to note that the expiration of this specific patent does not necessarily mean market exclusivity has ended for the covered technology if other patents in the patent family, or related patents covering specific formulations or uses of GLP-2 analogues, are still in force. What is the Patent Landscape for GLP-2 Analogues and Related Technologies? The patent landscape for GLP-2 analogues is extensive and competitive, reflecting the therapeutic potential of this class of drugs. U.S. Patent 6,046,202 was a foundational patent for oral GLP-2 delivery. However, the field has evolved significantly, with numerous subsequent patents covering: New GLP-2 Analogues: Development of analogues with altered pharmacokinetics (e.g., longer half-life), improved receptor binding, or reduced immunogenicity. Teduglutide (Gattex/Revestive) and L-glutamine/L-glutamine derivatives are examples of molecules that have been developed and patented. Improved Oral Delivery Technologies: Beyond the specific formulation in U.S. Patent 6,046,202, other oral delivery systems have been patented. These include nano- and micro-particle formulations, permeation enhancers with different chemical profiles, and novel encapsulation techniques to further protect peptides from degradation and enhance bioavailability. New Therapeutic Indications: Patents covering the use of GLP-2 analogues for a broader range of gastrointestinal conditions beyond short bowel syndrome, such as inflammatory bowel diseases (IBD), radiation enteritis, and chemotherapy-induced mucositis. Combination Therapies: Patents covering the co-administration of GLP-2 analogues with other therapeutic agents for synergistic effects. Manufacturing Processes: Patents focused on efficient and scalable methods for producing GLP-2 analogues and their formulations. Key Players in the GLP-2 Patent Landscape: NPS Pharmaceuticals (now Takeda): The assignee of U.S. Patent 6,046,202. They have been a pioneer in GLP-2 research and have a portfolio of patents related to GLP-2 analogues and their delivery. Teduglutide, their flagship GLP-2 analogue, is protected by a separate patent family. Shire (now Takeda): Shire acquired NPS Pharmaceuticals and has continued to develop and market teduglutide. Other Pharmaceutical Companies: Numerous other companies, including biotechnology firms and large pharmaceutical corporations, hold patents in the GLP-2 space. These companies are actively researching and developing next-generation GLP-2 therapies. Academic Institutions: Universities and research institutes also contribute to the patent landscape through the discovery of novel peptides, mechanisms of action, and delivery systems. Patent Cliff Considerations: The expiration of foundational patents like U.S. Patent 6,046,202 opens avenues for generic competition. However, the development of oral GLP-2 therapies is complex. Generic manufacturers would need to navigate not only the expired patent but also any active patents covering specific analogue sequences, improved formulations, or approved methods of use. The presence of multiple layers of patent protection can create a significant "patent cliff" that extends market exclusivity for the innovator products. How Has the Technology Claimed in U.S. Patent 6,046,202 Been Commercialized? The technology described in U.S. Patent 6,046,202 was primarily commercialized through the development and marketing of Gattex (teduglutide) by NPS Pharmaceuticals, which was later acquired by Shire (now Takeda). Gattex is an analogue of GLP-2 that is administered subcutaneously. While the patent 6,046,202 specifically claims a solid oral dosage form, the underlying research and development efforts by NPS Pharmaceuticals laid the groundwork for their subsequent success in the GLP-2 therapeutic area. It is crucial to distinguish between the claims of U.S. Patent 6,046,202 and the commercial product Gattex. Gattex is administered via subcutaneous injection, not oral administration as described in the 202 patent. However, the development of teduglutide by NPS Pharmaceuticals demonstrates the company's deep involvement and expertise in GLP-2 analogue technology. U.S. Patent 6,046,202 represents an early attempt by NPS to overcome the challenges of GLP-2 delivery through oral means. While the oral delivery technology described in this patent did not directly lead to the most widely recognized commercial GLP-2 product (teduglutide), it signifies the strategic importance of addressing GLP-2's bioavailability issues. The patent itself demonstrates an innovative approach to peptide delivery that could have influenced subsequent research by NPS and others in the field, even if the specific oral formulation did not reach widespread market adoption. The fundamental problem of peptide oral delivery remains an active area of research and development, and patents like 6,046,202 are important markers in that ongoing scientific and commercial pursuit. What Are the Potential Infringement Considerations for Competitors? Competitors developing or marketing GLP-2 analogues or related gastrointestinal therapies must carefully analyze U.S. Patent 6,046,202 and its progeny, even after its expiration. Expired Patent: The primary claims of U.S. Patent 6,046,202 have expired. This means that the specific solid oral dosage form described in its independent claims is no longer protected by this patent. Generic manufacturers could theoretically produce and sell dosage forms that precisely match the expired claims without infringing this patent. Patent Family and Continuations: It is critical to investigate the patent family to which U.S. Patent 6,046,202 belongs. Patent applicants often file continuation or divisional applications to cover different aspects or embodiments of their invention. These related applications may have later filing and grant dates, extending the period of exclusivity for related technologies. For example, patents covering specific GLP-2 analogue sequences, improved absorption enhancers, or unique manufacturing processes derived from the original invention could still be in force. Method of Use Claims: Even if the formulation claims have expired, competitors must be mindful of any still-active method of use claims. If a competitor's product, even if using a different formulation, is intended for the specific methods of treatment claimed in a related, active patent (e.g., treating short bowel syndrome via oral administration), there could be infringement. Newer Technologies and Analogues: The landscape has evolved significantly since 1998. Competitors are likely developing entirely new GLP-2 analogues or novel oral delivery systems that do not fall within the scope of U.S. Patent 6,046,202. Analyzing the claims of these newer patents is essential for ensuring freedom to operate. Freedom to Operate (FTO) Analysis: A comprehensive FTO analysis is imperative. This involves searching and reviewing all relevant patents, including expired patents, those nearing expiration, and pending applications that could lead to granted patents. The analysis should focus on: Specific GLP-2 analogue structures. Components and proportions within the oral dosage form. Methods of manufacturing the dosage form. Specific indications for which the product is intended. Anticipation and Obviousness: Competitors may challenge the validity of any remaining active patents related to U.S. Patent 6,046,202 by arguing that the claimed inventions were either anticipated by prior art or would have been obvious to a person skilled in the art at the time of filing. In summary, while U.S. Patent 6,046,202 itself has expired, its underlying technology and its place within a potentially broader patent family necessitate careful review by any entity seeking to enter the market for oral GLP-2 therapies or related treatments. Key Takeaways U.S. Patent 6,046,202 claims a solid oral dosage form of GLP-2 analogues designed for enhanced absorption and protection from degradation. The patent, filed in 1998, expired in July 2018, but related patent families or extensions could impact market exclusivity. The core innovation lies in combining GLP-2 analogues with non-peptidic absorption enhancers in a stable oral formulation. While the patent enabled early research into oral GLP-2 delivery, the most prominent commercial GLP-2 analogue, teduglutide, is administered subcutaneously. The competitive landscape for GLP-2 analogues is dynamic, with numerous patents covering new analogues, delivery systems, and therapeutic uses. Competitors must conduct thorough freedom-to-operate analyses, considering not only expired patents but also active patents within related families and new technological advancements. Frequently Asked Questions Can a generic version of the oral GLP-2 dosage form described in U.S. Patent 6,046,202 be immediately manufactured and sold? While the principal claims of U.S. Patent 6,046,202 have expired, a generic manufacturer must still ensure freedom to operate. This requires verifying that no other active patents (e.g., covering specific GLP-2 analogue sequences, modified formulations, or manufacturing processes derived from this patent family) are being infringed. Does the expiration of U.S. Patent 6,046,202 mean that all oral GLP-2 products are now off-patent? No. U.S. Patent 6,046,202 covers a specific type of oral dosage form. The development of GLP-2 analogues and their delivery methods is a broad field. Other patents may protect different GLP-2 analogue structures, alternative oral delivery technologies, or specific therapeutic uses, potentially extending exclusivity for other products. What is the significance of the "non-peptidic absorption enhancer" in Claim 1 of the patent? This clause distinguishes the claimed invention from prior art that might have involved covalently linking the GLP-2 analogue to an absorption-enhancing peptide or molecule. It implies the use of simpler chemical agents to facilitate absorption without creating a complex conjugate. Were there any notable legal challenges or litigations related to U.S. Patent 6,046,202 before its expiration? Information on specific litigation involving U.S. Patent 6,046,202 is not readily available through general patent databases. Detailed litigation searches would be required to confirm. However, foundational patents in the pharmaceutical industry often become subjects of patent disputes as the market matures. How does the technology in U.S. Patent 6,046,202 relate to currently marketed GLP-2 drugs like teduglutide? U.S. Patent 6,046,202 describes an oral delivery system for GLP-2 analogues. Teduglutide, a prominent GLP-2 drug, is administered via subcutaneous injection. While both relate to GLP-2 technology developed by NPS Pharmaceuticals, the specific claims and commercial application differ significantly regarding the route of administration. Cited Sources [1] NPS Pharmaceuticals, Inc. (1998). Solid pharmaceutical dosage forms of glucagon-like peptide-2 analogues and methods of their use. U.S. Patent 6,046,202. Washington, D.C.: U.S. Patent and Trademark Office. 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Details for Patent: 6,046,202

Summary for Patent: 6,046,202