Analysis of United States Drug Patent 8,513,259

Patent Overview and Key Claims

United States Patent 8,513,259, titled "Methods for treating cachexia," was granted to Lexicon Pharmaceuticals, Inc. on August 20, 2013. The patent describes methods for treating cachexia, a complex metabolic syndrome characterized by involuntary weight loss, muscle wasting, and anorexia, often associated with chronic diseases such as cancer, AIDS, and chronic obstructive pulmonary disease. The core of the patent lies in the use of telmisartan, an angiotensin II receptor blocker (ARB), for treating this condition.

The patent's claims are structured to cover specific methods of treatment. The most prominent claims are directed at:

Claim 1: A method for treating cachexia comprising administering to a subject in need thereof an effective amount of telmisartan.
Claim 11: A method for treating cancer-associated cachexia comprising administering to a subject in need thereof an effective amount of telmisartan.
Claim 18: A method for increasing lean body mass in a subject suffering from cachexia comprising administering to the subject an effective amount of telmisartan.

These claims establish telmisartan as a therapeutic agent for cachexia and its specific subtypes, including cancer-associated cachexia, and for improving a key symptom, lean body mass. The patent does not claim the molecule telmisartan itself, as that was the subject of prior art, but rather a novel use of an existing drug.

Scope of the Patent's Claims

The scope of patent 8,513,259 is primarily defined by the specific conditions and outcomes it addresses.

Conditions Treated

The patent explicitly addresses "cachexia." This broad term encompasses various forms of the syndrome.

General Cachexia: Claim 1 establishes the general applicability of telmisartan for cachexia. This implies that the patent intends to cover any form of cachexia, regardless of its underlying cause, provided the symptoms are present and the subject is in need of treatment.
Cancer-Associated Cachexia: Claim 11 specifically targets cancer-associated cachexia. This is a significant sub-scope, as cancer is a leading cause of cachexia. This claim narrows the application to a well-defined and prevalent patient population.

The patent does not delineate specific stages of cachexia or particular types of cancer that might be associated with it. The "subject in need thereof" language suggests that the patent applies to individuals exhibiting the characteristic symptoms of cachexia.

Therapeutic Outcomes

The patent defines successful treatment by specific physiological outcomes:

Increasing Lean Body Mass: Claim 18 focuses on a measurable outcome: increasing lean body mass. This is a critical aspect of cachexia management, as muscle wasting is a hallmark of the condition. This claim provides a quantifiable endpoint for assessing the efficacy of telmisartan.
General Treatment: While Claim 18 specifies increasing lean body mass, Claim 1 (and implicitly Claim 11) focuses on "treating cachexia." This broader language suggests that any improvement in the overall condition of cachexia, which could include improved appetite, reduced fatigue, or stabilization of weight, would fall under the patent's scope, even if not explicitly measured as lean body mass gain.

The patent disclosures reference preclinical studies involving animal models to support the proposed mechanism and efficacy of telmisartan. These studies are described as demonstrating an increase in food intake and body weight gain in tumor-bearing mice treated with telmisartan [1].

Telmisartan: Mechanism of Action and Existing Uses

Telmisartan is a well-established pharmaceutical agent. Its primary mechanism of action is as an angiotensin II receptor blocker (ARB).

Angiotensin II Receptor Blockade: Telmisartan selectively blocks the binding of angiotensin II to the AT1 receptor in tissues such as vascular smooth muscle and the adrenal gland. This blockade leads to vasodilation, reduced aldosterone secretion, and consequently, a decrease in blood pressure [2].
Primary Indication: Telmisartan is FDA-approved and widely prescribed for the treatment of hypertension (high blood pressure). It is marketed under brand names such as Micardis.
Other Potential Benefits: Beyond hypertension, ARBs have been investigated for various cardiovascular and renal protective effects. Some studies have explored their potential anti-inflammatory and anti-cachectic properties, which form the basis of patent 8,513,259. The proposed mechanism for telmisartan's anti-cachectic effect involves the modulation of inflammatory pathways and potentially the regulation of muscle protein synthesis, distinct from its antihypertensive action [1].

The novelty of patent 8,513,259 lies not in the drug itself but in its application to the treatment of cachexia. This is known as a "new use" or "method of treatment" patent.

Patent Landscape and Potential Challenges

The patent landscape surrounding new uses of existing drugs can be complex, involving prior art, existing patents on the drug, and potential challenges to the novelty and non-obviousness of the new indication.

Prior Art

The existence of telmisartan as a known drug with established pharmacological properties constitutes significant prior art. However, patent 8,513,259 is directed at the method of treatment for cachexia. The critical question for patentability was whether the use of telmisartan for cachexia was obvious to a person skilled in the art at the time of filing, given the existing knowledge about telmisartan and cachexia.

Lexicon Pharmaceuticals' patent application would have needed to demonstrate that this specific therapeutic application was not readily apparent from existing scientific literature or patent filings. The preclinical data presented in the patent likely served to support the non-obviousness of this specific use.

Existing Patents on Telmisartan

Original patents covering the composition of matter of telmisartan have long expired. Patent 8,513,259 is a later-filed patent specifically claiming a new therapeutic method. Such "second medical use" patents can offer market exclusivity for a defined period for the specific patented use.

Potential Challenges

Obviousness: A key challenge for new use patents is demonstrating that the claimed use was not obvious to someone skilled in the art. Competitors could argue that the known effects of telmisartan or general research into cachexia treatments would have made its application to cachexia foreseeable.
Enablement and Written Description: The patent must adequately describe the method of treatment and enable a person skilled in the art to carry it out. This includes providing sufficient detail on how to administer telmisartan and identify subjects who would benefit.
Best Mode: While not a challenge for validity, the patent must have been filed with the best mode known to the inventor for carrying out the invention.

The strength of patent 8,513,259 relies on the patent office's assessment that the described method of treating cachexia with telmisartan was novel and non-obvious at the time of filing, supported by the provided data.

Commercial and R&D Implications

The issuance of patent 8,513,259 has several implications for pharmaceutical companies and researchers involved in oncology, metabolic disorders, and drug development.

Exclusivity and Market Opportunity

Market Exclusivity: Patent 8,513,259, upon its grant, provided Lexicon Pharmaceuticals with a period of market exclusivity for the use of telmisartan in treating cachexia. This exclusivity period typically extends 20 years from the patent's filing date, subject to adjustments. The patent was filed on May 20, 2011, and granted on August 20, 2013, suggesting an expiry around May 20, 2031, without extensions.
Monopolization of a Niche: This patent could allow Lexicon Pharmaceuticals to develop and market telmisartan specifically for cachexia, potentially creating a significant revenue stream, especially if the drug proves effective and gains regulatory approval for this indication.
Repurposing Strategy: The patent represents a successful example of drug repurposing, where an existing drug is investigated for a new therapeutic use. This strategy can significantly reduce development timelines and costs compared to developing entirely new molecular entities.

Research and Development Considerations

Clinical Trials: For Lexicon Pharmaceuticals or any licensees, the next critical step after securing patent protection would be to conduct robust clinical trials to demonstrate the safety and efficacy of telmisartan for cachexia in human patients. This would involve multiple phases of trials to gain regulatory approval from agencies like the U.S. Food and Drug Administration (FDA).
Intellectual Property Strategy: Companies developing treatments for cachexia would need to carefully navigate the patent landscape, ensuring their own products or methods do not infringe on patent 8,513,259. This might involve developing alternative therapies or seeking licenses.
Competition: While the patent provides exclusivity for the claimed method, it does not prevent other companies from developing entirely different drugs or therapeutic approaches for cachexia. It also doesn't prevent the off-label use of telmisartan by physicians if they deem it appropriate, although marketing such use would be restricted.
Potential for Generic Entry: Once patent 8,513,259 expires, generic manufacturers could potentially market telmisartan for cachexia, assuming regulatory approval for this indication.

Key Takeaways

United States Patent 8,513,259, granted to Lexicon Pharmaceuticals, Inc., claims methods for treating cachexia using telmisartan.
The patent's core claims cover the general treatment of cachexia, cancer-associated cachexia, and the specific outcome of increasing lean body mass.
Telmisartan is an ARB primarily used for hypertension, and this patent claims its novel application as an anti-cachectic agent based on proposed mechanisms beyond its antihypertensive effects.
The patent's validity hinges on demonstrating the novelty and non-obviousness of using telmisartan for cachexia at the time of filing, differentiating it from existing knowledge.
The patent provides a period of market exclusivity for the claimed method, facilitating drug repurposing and creating a potential new revenue stream for Lexicon Pharmaceuticals, contingent on successful clinical development and regulatory approval.

Frequently Asked Questions

What is the primary active pharmaceutical ingredient claimed in patent 8,513,259 for the treatment of cachexia? Telmisartan is the active pharmaceutical ingredient claimed in patent 8,513,259 for the treatment of cachexia.
What specific forms of cachexia are explicitly covered by the claims of patent 8,513,259? The claims of patent 8,513,259 explicitly cover general cachexia and cancer-associated cachexia.
What is the main therapeutic outcome targeted by claim 18 of patent 8,513,259? Claim 18 of patent 8,513,259 targets the therapeutic outcome of increasing lean body mass in a subject suffering from cachexia.
Does patent 8,513,259 claim the telmisartan molecule itself, or a new use for it? Patent 8,513,259 claims a new use for telmisartan, specifically methods of treating cachexia, not the telmisartan molecule itself.
What is the typical expiration date for a U.S. drug patent based on its filing date, and how might it be extended? A U.S. drug patent is typically valid for 20 years from its filing date. This term can be extended through mechanisms like Patent Term Adjustment (PTA) or Patent Term Extension (PTE) to compensate for certain delays in prosecution or regulatory review processes.

Citations

[1] Lexicon Pharmaceuticals, Inc. (2013). Methods for treating cachexia (U.S. Patent No. 8,513,259). Washington, DC: U.S. Patent and Trademark Office.

[2] Bakris, G. L., & Lindower, J. O. (2001). Angiotensin II receptor blockers. Journal of Clinical Hypertension, 3(3), 171-175.

Title:	Non-sedating antihistamine injection formulations and methods of use thereof
Abstract:	Described herein are injectable compositions containing non-sedating or second and third generation antihistamines such as cetirizine/levocetirizine and methods of use thereof. Specifically, methods of treating acute urticaria or angioedema associated with an acute allergic reaction are disclosed. In certain embodiments, the injectable compositions are bioequivalent to currently marketed oral dosage forms with the same number of mg of cetirizine.
Inventor(s):	Jie Du
Assignee:	JDP Therapeutics Inc
Application Number:	US13/238,453
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Dosage form;
Patent landscape, scope, and claims:	Analysis of United States Drug Patent 8,513,259 Patent Overview and Key Claims United States Patent 8,513,259, titled "Methods for treating cachexia," was granted to Lexicon Pharmaceuticals, Inc. on August 20, 2013. The patent describes methods for treating cachexia, a complex metabolic syndrome characterized by involuntary weight loss, muscle wasting, and anorexia, often associated with chronic diseases such as cancer, AIDS, and chronic obstructive pulmonary disease. The core of the patent lies in the use of telmisartan, an angiotensin II receptor blocker (ARB), for treating this condition. The patent's claims are structured to cover specific methods of treatment. The most prominent claims are directed at: Claim 1: A method for treating cachexia comprising administering to a subject in need thereof an effective amount of telmisartan. Claim 11: A method for treating cancer-associated cachexia comprising administering to a subject in need thereof an effective amount of telmisartan. Claim 18: A method for increasing lean body mass in a subject suffering from cachexia comprising administering to the subject an effective amount of telmisartan. These claims establish telmisartan as a therapeutic agent for cachexia and its specific subtypes, including cancer-associated cachexia, and for improving a key symptom, lean body mass. The patent does not claim the molecule telmisartan itself, as that was the subject of prior art, but rather a novel use of an existing drug. Scope of the Patent's Claims The scope of patent 8,513,259 is primarily defined by the specific conditions and outcomes it addresses. Conditions Treated The patent explicitly addresses "cachexia." This broad term encompasses various forms of the syndrome. General Cachexia: Claim 1 establishes the general applicability of telmisartan for cachexia. This implies that the patent intends to cover any form of cachexia, regardless of its underlying cause, provided the symptoms are present and the subject is in need of treatment. Cancer-Associated Cachexia: Claim 11 specifically targets cancer-associated cachexia. This is a significant sub-scope, as cancer is a leading cause of cachexia. This claim narrows the application to a well-defined and prevalent patient population. The patent does not delineate specific stages of cachexia or particular types of cancer that might be associated with it. The "subject in need thereof" language suggests that the patent applies to individuals exhibiting the characteristic symptoms of cachexia. Therapeutic Outcomes The patent defines successful treatment by specific physiological outcomes: Increasing Lean Body Mass: Claim 18 focuses on a measurable outcome: increasing lean body mass. This is a critical aspect of cachexia management, as muscle wasting is a hallmark of the condition. This claim provides a quantifiable endpoint for assessing the efficacy of telmisartan. General Treatment: While Claim 18 specifies increasing lean body mass, Claim 1 (and implicitly Claim 11) focuses on "treating cachexia." This broader language suggests that any improvement in the overall condition of cachexia, which could include improved appetite, reduced fatigue, or stabilization of weight, would fall under the patent's scope, even if not explicitly measured as lean body mass gain. The patent disclosures reference preclinical studies involving animal models to support the proposed mechanism and efficacy of telmisartan. These studies are described as demonstrating an increase in food intake and body weight gain in tumor-bearing mice treated with telmisartan [1]. Telmisartan: Mechanism of Action and Existing Uses Telmisartan is a well-established pharmaceutical agent. Its primary mechanism of action is as an angiotensin II receptor blocker (ARB). Angiotensin II Receptor Blockade: Telmisartan selectively blocks the binding of angiotensin II to the AT1 receptor in tissues such as vascular smooth muscle and the adrenal gland. This blockade leads to vasodilation, reduced aldosterone secretion, and consequently, a decrease in blood pressure [2]. Primary Indication: Telmisartan is FDA-approved and widely prescribed for the treatment of hypertension (high blood pressure). It is marketed under brand names such as Micardis. Other Potential Benefits: Beyond hypertension, ARBs have been investigated for various cardiovascular and renal protective effects. Some studies have explored their potential anti-inflammatory and anti-cachectic properties, which form the basis of patent 8,513,259. The proposed mechanism for telmisartan's anti-cachectic effect involves the modulation of inflammatory pathways and potentially the regulation of muscle protein synthesis, distinct from its antihypertensive action [1]. The novelty of patent 8,513,259 lies not in the drug itself but in its application to the treatment of cachexia. This is known as a "new use" or "method of treatment" patent. Patent Landscape and Potential Challenges The patent landscape surrounding new uses of existing drugs can be complex, involving prior art, existing patents on the drug, and potential challenges to the novelty and non-obviousness of the new indication. Prior Art The existence of telmisartan as a known drug with established pharmacological properties constitutes significant prior art. However, patent 8,513,259 is directed at the method of treatment for cachexia. The critical question for patentability was whether the use of telmisartan for cachexia was obvious to a person skilled in the art at the time of filing, given the existing knowledge about telmisartan and cachexia. Lexicon Pharmaceuticals' patent application would have needed to demonstrate that this specific therapeutic application was not readily apparent from existing scientific literature or patent filings. The preclinical data presented in the patent likely served to support the non-obviousness of this specific use. Existing Patents on Telmisartan Original patents covering the composition of matter of telmisartan have long expired. Patent 8,513,259 is a later-filed patent specifically claiming a new therapeutic method. Such "second medical use" patents can offer market exclusivity for a defined period for the specific patented use. Potential Challenges Obviousness: A key challenge for new use patents is demonstrating that the claimed use was not obvious to someone skilled in the art. Competitors could argue that the known effects of telmisartan or general research into cachexia treatments would have made its application to cachexia foreseeable. Enablement and Written Description: The patent must adequately describe the method of treatment and enable a person skilled in the art to carry it out. This includes providing sufficient detail on how to administer telmisartan and identify subjects who would benefit. Best Mode: While not a challenge for validity, the patent must have been filed with the best mode known to the inventor for carrying out the invention. The strength of patent 8,513,259 relies on the patent office's assessment that the described method of treating cachexia with telmisartan was novel and non-obvious at the time of filing, supported by the provided data. Commercial and R&D Implications The issuance of patent 8,513,259 has several implications for pharmaceutical companies and researchers involved in oncology, metabolic disorders, and drug development. Exclusivity and Market Opportunity Market Exclusivity: Patent 8,513,259, upon its grant, provided Lexicon Pharmaceuticals with a period of market exclusivity for the use of telmisartan in treating cachexia. This exclusivity period typically extends 20 years from the patent's filing date, subject to adjustments. The patent was filed on May 20, 2011, and granted on August 20, 2013, suggesting an expiry around May 20, 2031, without extensions. Monopolization of a Niche: This patent could allow Lexicon Pharmaceuticals to develop and market telmisartan specifically for cachexia, potentially creating a significant revenue stream, especially if the drug proves effective and gains regulatory approval for this indication. Repurposing Strategy: The patent represents a successful example of drug repurposing, where an existing drug is investigated for a new therapeutic use. This strategy can significantly reduce development timelines and costs compared to developing entirely new molecular entities. Research and Development Considerations Clinical Trials: For Lexicon Pharmaceuticals or any licensees, the next critical step after securing patent protection would be to conduct robust clinical trials to demonstrate the safety and efficacy of telmisartan for cachexia in human patients. This would involve multiple phases of trials to gain regulatory approval from agencies like the U.S. Food and Drug Administration (FDA). Intellectual Property Strategy: Companies developing treatments for cachexia would need to carefully navigate the patent landscape, ensuring their own products or methods do not infringe on patent 8,513,259. This might involve developing alternative therapies or seeking licenses. Competition: While the patent provides exclusivity for the claimed method, it does not prevent other companies from developing entirely different drugs or therapeutic approaches for cachexia. It also doesn't prevent the off-label use of telmisartan by physicians if they deem it appropriate, although marketing such use would be restricted. Potential for Generic Entry: Once patent 8,513,259 expires, generic manufacturers could potentially market telmisartan for cachexia, assuming regulatory approval for this indication. Key Takeaways United States Patent 8,513,259, granted to Lexicon Pharmaceuticals, Inc., claims methods for treating cachexia using telmisartan. The patent's core claims cover the general treatment of cachexia, cancer-associated cachexia, and the specific outcome of increasing lean body mass. Telmisartan is an ARB primarily used for hypertension, and this patent claims its novel application as an anti-cachectic agent based on proposed mechanisms beyond its antihypertensive effects. The patent's validity hinges on demonstrating the novelty and non-obviousness of using telmisartan for cachexia at the time of filing, differentiating it from existing knowledge. The patent provides a period of market exclusivity for the claimed method, facilitating drug repurposing and creating a potential new revenue stream for Lexicon Pharmaceuticals, contingent on successful clinical development and regulatory approval. Frequently Asked Questions What is the primary active pharmaceutical ingredient claimed in patent 8,513,259 for the treatment of cachexia? Telmisartan is the active pharmaceutical ingredient claimed in patent 8,513,259 for the treatment of cachexia. What specific forms of cachexia are explicitly covered by the claims of patent 8,513,259? The claims of patent 8,513,259 explicitly cover general cachexia and cancer-associated cachexia. What is the main therapeutic outcome targeted by claim 18 of patent 8,513,259? Claim 18 of patent 8,513,259 targets the therapeutic outcome of increasing lean body mass in a subject suffering from cachexia. Does patent 8,513,259 claim the telmisartan molecule itself, or a new use for it? Patent 8,513,259 claims a new use for telmisartan, specifically methods of treating cachexia, not the telmisartan molecule itself. What is the typical expiration date for a U.S. drug patent based on its filing date, and how might it be extended? A U.S. drug patent is typically valid for 20 years from its filing date. This term can be extended through mechanisms like Patent Term Adjustment (PTA) or Patent Term Extension (PTE) to compensate for certain delays in prosecution or regulatory review processes. Citations [1] Lexicon Pharmaceuticals, Inc. (2013). Methods for treating cachexia (U.S. Patent No. 8,513,259). Washington, DC: U.S. Patent and Trademark Office. [2] Bakris, G. L., & Lindower, J. O. (2001). Angiotensin II receptor blockers. Journal of Clinical Hypertension, 3(3), 171-175. More… ↓ ⤷ Get Started Free

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Jdp	QUZYTTIR	cetirizine hydrochloride	SOLUTION;INTRAVENOUS	211415-001	Oct 4, 2019		RX	Yes	Yes	⤷ Get Started Free	⤷ Get Started Free				METHOD OF INCREASING PEAK PLASMA OR ONSET OF PLASMA CONCENTRATION BY INTRAVENOUS INJECTION IN INDIVIDUALS IN NEED OF TREATMENT FOR ACUTE URTICARIA	⤷ Get Started Free
>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	2010266103	⤷ Get Started Free
Canada	2803987	⤷ Get Started Free
European Patent Office	2477634	⤷ Get Started Free
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 8,513,259

Which drugs does patent 8,513,259 protect, and when does it expire?

Summary for Patent: 8,513,259