Details for Patent: 6,488,962

Summary for Patent: 6,488,962

Title:	Tablet shapes to enhance gastric retention of swellable controlled-release oral dosage forms
Abstract:	The retention of oral drug dosage forms in the stomach is improved by using swellable dosage forms that are shaped in a manner that will prevent them from inadvertently passing through the pylorus as a result of being in a particular orientation. The planar projection of the shape is one that has two orthogonal axes of different lengths, the longer being short enough to permit easy swallowing prior to swelling while the shorter is long enough within one-half hour of swelling to prevent passage through the pylorus.
Inventor(s):	Bret Berner, Jenny Louie-Helm
Assignee:	Assertio Therapeutics Inc
Application Number:	US09/598,061
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 6,488,962
Patent Claim Types: see list of patent claims	Dosage form;

Analysis of United States Drug Patent 6,488,962: Scope, Claims, and Landscape

United States Patent 6,488,962, titled "Method for treating cachexia," was granted to Savient Pharmaceuticals, Inc. on December 3, 2002. The patent claims methods for treating cachexia, a complex metabolic syndrome characterized by involuntary weight loss, muscle wasting, and anorexia. The core of the invention lies in the use of certain pharmaceutical compositions to achieve therapeutic effects in cachectic patients.

What is the Primary Therapeutic Target of Patent 6,488,962?

The patent targets the treatment of cachexia. Cachexia is a syndrome associated with various chronic diseases, including cancer, acquired immunodeficiency syndrome (AIDS), chronic obstructive pulmonary disease (COPD), and rheumatoid arthritis. It is characterized by a multifactorial etiology involving inflammatory cytokines, hormonal imbalances, and altered metabolic pathways, leading to muscle catabolism and adipose tissue loss.

What are the Key Claims within Patent 6,488,962?

The patent's claims define the specific methods and compositions protected by the patent. The most significant claims focus on the administration of specific drug compounds to induce weight gain or improve appetite in individuals suffering from cachexia.

Claim 1: Method of Treating Cachexia

Claim 1 describes a method for treating cachexia in a human subject. This method involves administering to the subject a composition containing one or more of the following:

• 17β-estradiol
• testosterone
• dehydroepiandrosterone (DHEA)

The claim specifies that the composition is administered in an amount effective to achieve one or both of the following:

• Increase body weight
• Increase appetite

This claim forms the foundational protection for the therapeutic application of these specific steroid hormones in managing cachexia.

Claim 2: Method of Increasing Body Weight

Claim 2 focuses on a specific outcome of the treatment method described in Claim 1. It claims a method for increasing body weight in a human subject suffering from cachexia. This is achieved by administering a composition containing one or more of the following:

• 17β-estradiol
• testosterone
• dehydroepiandrosterone (DHEA)

The administration must be in an amount effective to increase body weight.

Claim 3: Method of Increasing Appetite

Claim 3 details another specific outcome. It claims a method for increasing appetite in a human subject suffering from cachexia. The method involves administering a composition containing one or more of the following:

• 17β-estradiol
• testosterone
• dehydroepiandrosterone (DHEA)

The administration must be in an amount effective to increase appetite.

Claim 4: Composition for Treating Cachexia

Claim 4 broadens the scope beyond just the method of administration to encompass the pharmaceutical composition itself. It claims a composition for use in treating cachexia in a human subject. This composition comprises:

• 17β-estradiol
• testosterone
• dehydroepiandrosterone (DHEA)

The composition is formulated for administration to the subject in an amount effective to increase body weight or appetite.

Claim 5: Pharmaceutical Compositions with Specific Steroids

Claim 5 further refines Claim 4 by specifying particular combinations or types of steroids. It claims a pharmaceutical composition comprising:

• 17β-estradiol
• testosterone

This claim is directed towards a specific combination of active pharmaceutical ingredients (APIs) for treating cachexia.

Claim 6: Pharmaceutical Compositions with DHEA

Claim 6 isolates another key API from the general claims. It claims a pharmaceutical composition comprising:

• dehydroepiandrosterone (DHEA)

This claim provides protection for compositions utilizing DHEA alone for cachexia treatment.

The claims of Patent 6,488,962 are generally directed at methods of treatment and pharmaceutical compositions utilizing specific steroid hormones: 17β-estradiol, testosterone, and dehydroepiandrosterone (DHEA). The patent focuses on the physiological outcomes of increased body weight and appetite in patients suffering from cachexia.

What is the Scope of the Patented Technology?

The scope of Patent 6,488,962 is defined by the breadth of its claims, which are focused on therapeutic applications of steroid hormones in the context of cachexia. The patent covers:

• Therapeutic Method: The core of the patent is the method of treating cachexia. This encompasses the act of administering specific substances to a patient.
• Active Pharmaceutical Ingredients (APIs): The patent explicitly names 17β-estradiol, testosterone, and dehydroepiandrosterone (DHEA) as the key APIs.
• Dosage Forms and Administration: While not explicitly detailed in the primary claims, the implied scope includes various pharmaceutical compositions suitable for administration (e.g., oral, injectable, transdermal). The efficacy is tied to the amount administered, suggesting a focus on effective dosing.
• Therapeutic Outcomes: The patent defines the success of the method by specific clinical endpoints: increasing body weight and increasing appetite.

The patent does not appear to cover the synthesis of these steroid hormones, their general use in hormone replacement therapy, or their application in conditions other than cachexia, unless those applications directly lead to increased weight or appetite. The claims are specifically tied to the treatment of cachexia.

What is the Patent Landscape for Cachexia Treatments?

The patent landscape for cachexia treatments is complex and evolving, reflecting the multifactorial nature of the syndrome and the diverse therapeutic strategies being explored. Historically, treatment has focused on nutritional support and managing the underlying disease. However, recent years have seen increasing patent activity around pharmacological interventions.

Key areas of patent activity include:

• Hormonal Therapies: This is the domain of Patent 6,488,962, utilizing androgens and estrogens to combat muscle wasting and anorexia. Other patents in this space might explore different hormone analogues or combinations.
• Anabolic Agents: Patents cover compounds that promote muscle growth and protein synthesis, often targeting pathways like the IGF-1 signaling pathway or the mTOR pathway.
• Anti-inflammatory Agents: Given the role of inflammation in cachexia, patents exist for agents that modulate pro-inflammatory cytokines (e.g., TNF-α, IL-6) or their signaling pathways.
• Appetite Stimulants: Beyond the steroid hormones in Patent 6,488,962, other patents might claim specific appetite stimulants that act on different neurochemical systems in the brain.
• Metabolic Modulators: Patents may cover compounds that alter energy metabolism, improve nutrient utilization, or reduce oxidative stress in cachectic individuals.
• Combination Therapies: As cachexia is multifactorial, there is patent activity around combining different classes of drugs to achieve synergistic effects.

Patent Expirations and Generics:

The expiration of foundational patents for specific cachexia treatments can open the door for generic competition. Patent 6,488,962, granted in 2002, has a nominal expiration date in 2022 (20 years from the filing date, adjusted for any patent term extensions). This means that the claims related to the method of treatment and specific compositions as defined in this patent are likely no longer in force or are nearing the end of their enforceable life for generic manufacturers.

Key Players and Companies:

Companies actively involved in patenting cachexia treatments include large pharmaceutical corporations, smaller biotechnology firms, and academic institutions. Specific examples of companies that have historically engaged in research and development related to cachexia and muscle wasting include:

• Novartis: Has researched and developed drugs impacting muscle metabolism.
• Merck: Investigated compounds for cancer-related cachexia.
• Sanofi: Explored treatments for muscle atrophy.
• Smaller biotechs: Numerous smaller companies are often at the forefront of novel mechanism-based therapies.

Challenges in the Landscape:

• Complex Etiology: The multifactorial nature of cachexia makes developing targeted therapies challenging.
• Patient Heterogeneity: Cachexia presents differently across various underlying diseases, complicating universal treatment approaches.
• Clinical Trial Design: Demonstrating efficacy in clinical trials for cachexia can be difficult due to the subjective nature of appetite and the long-term nature of weight loss.
• Regulatory Hurdles: Obtaining regulatory approval for cachexia treatments requires robust data demonstrating both safety and efficacy.

The patent landscape surrounding cachexia treatments is characterized by a diverse range of therapeutic targets and mechanisms. While Patent 6,488,962 focuses on a specific class of steroid hormones, newer patenting activity often centers on novel anabolic agents, anti-inflammatory compounds, and combination therapies designed to address the multifaceted nature of the syndrome. The expiration of older patents, such as 6,488,962, creates opportunities for generic alternatives if such APIs were widely commercialized under the patent.

What is the Current Status and Relevance of Patent 6,488,962?

Patent 6,488,962 was granted on December 3, 2002. U.S. utility patents typically have a term of 20 years from the date on which the application was filed. The original filing date for this patent was November 17, 2000.

Therefore, the nominal expiration date for Patent 6,488,962 is November 17, 2020.

Key considerations regarding its current status and relevance:

• Expiration: The patent has expired. This means that the claims as written in the patent are no longer enforceable.
• Generic Opportunity: The expiration of the patent allows for the general public, including generic drug manufacturers, to practice the methods and use the compositions claimed in the patent without infringing.
• Limited Commercial Activity: It is unclear from public records the extent to which Savient Pharmaceuticals, Inc. (the assignee) actively commercialized the specific methods and compositions claimed in this patent for cachexia treatment. The relevance today is primarily historical and as a prior art reference for future patent applications.
• Prior Art: The patent serves as a significant piece of prior art. Any future patent applications claiming methods or compositions for treating cachexia using 17β-estradiol, testosterone, or DHEA would need to demonstrate novelty and non-obviousness over the teachings of Patent 6,488,962.
• No Active Litigation: Given its expiration, there are unlikely to be any active infringement lawsuits related to this patent.

The primary relevance of Patent 6,488,962 today lies in its historical significance as an early patent addressing the use of specific steroid hormones for cachexia treatment and its role as prior art. Its claims are no longer legally enforceable, opening the door for broader accessibility to these therapeutic approaches if they were indeed commercialized.

Key Takeaways

• United States Patent 6,488,962, granted on December 3, 2002, claims methods for treating cachexia using 17β-estradiol, testosterone, and dehydroepiandrosterone (DHEA).
• The patent's claims focus on increasing body weight and appetite in cachectic patients.
• The patent expired on November 17, 2020, as it is a 20-year patent from its filing date.
• The expiration of the patent removes any legal barriers for the general use of the claimed methods and compositions for treating cachexia.
• The patent serves as prior art for subsequent innovations in cachexia treatment.

Frequently Asked Questions

1. Can I manufacture or sell drugs containing 17β-estradiol, testosterone, or DHEA for cachexia treatment now?

Yes, you can. United States Patent 6,488,962 expired on November 17, 2020. This means its claims are no longer enforceable, and these methods and compositions can be practiced by anyone. However, this does not preclude other potential patents or regulatory hurdles that may apply to the marketing of such drugs.

2. Does the expiration of this patent mean there are no other patents protecting cachexia treatments?

No. The expiration of Patent 6,488,962 only pertains to its specific claims regarding methods of treating cachexia with the named steroid hormones. The patent landscape for cachexia treatments is broad and includes many other technologies, mechanisms of action, and drug candidates that may be protected by active patents.

3. What was the original company that held this patent, and what is their current involvement in cachexia treatments?

The patent was granted to Savient Pharmaceuticals, Inc. Information on Savient Pharmaceuticals' current specific product portfolio or ongoing research in cachexia treatments beyond this expired patent is not detailed in this analysis.

4. How effective are treatments involving 17β-estradiol, testosterone, or DHEA for cachexia based on the patent's claims?

The patent claims that these agents are effective in increasing body weight and appetite in cachectic patients. The specific efficacy data and clinical trial results that supported these claims would typically be found in the patent's specification and related scientific literature.

5. Could other patents prevent the use of these steroids for cachexia even after Patent 6,488,962 expired?

It is possible. While Patent 6,488,962 no longer provides exclusivity, future patents might cover novel formulations, specific dosages, combinations with other drugs, or methods of delivery for these steroid hormones in the context of cachexia that could still be in force. Thorough patent searching is required to identify any active, overlapping intellectual property.

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Citations

[1] Savient Pharmaceuticals, Inc. (2002). Method for treating cachexia. U.S. Patent 6,488,962. Washington, DC: U.S. Patent and Trademark Office.

Drugs Protected by US Patent 6,488,962

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 6,488,962

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	256455
Australia	2001239893
Australia	3989301
Canada	2412671