Last updated: February 19, 2026
Canadian patent CA2613273, titled "FORMULATIONS AND METHODS FOR TREATING DYSLIPIDEMIA AND DIABETES," protects specific pharmaceutical compositions and their use in treating dyslipidemia and diabetes. The patent was filed on December 19, 2005, and granted on November 29, 2011. The claims are directed towards pharmaceutical compositions containing fenofibrate and sitagliptin, and methods of using these compositions.
What is the Core Invention Protected by CA2613273?
The central innovation lies in a fixed-dose combination of two active pharmaceutical ingredients: fenofibrate and sitagliptin. Fenofibrate is a fibrate drug used to lower cholesterol and triglycerides, while sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor used to manage type 2 diabetes. The patent claims formulations that combine these two drugs into a single dosage form, along with methods for their administration.
The patent's claims delineate the specific parameters of these compositions and their therapeutic applications.
Key Claims and Their Scope
The claims of CA2613273 define the boundaries of the protected invention. The primary claims focus on:
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Claim 1: A pharmaceutical composition comprising fenofibrate and sitagliptin, wherein fenofibric acid has a mean particle size of less than about 5 microns. This claim specifies a particle size for fenofibric acid, a metabolite of fenofibrate, which is relevant for bioavailability.
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Claim 2: The pharmaceutical composition of claim 1, further comprising a pharmaceutically acceptable carrier. This broadens the scope to include standard excipients used in drug formulations.
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Claim 3: The pharmaceutical composition of claim 1, wherein the fenofibrate is present in an amount effective to provide a therapeutically effective amount of fenofibric acid. This ties the dosage of fenofibrate to its active form.
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Claim 4: The pharmaceutical composition of claim 1, wherein the sitagliptin is present in an amount effective to provide a therapeutically effective amount of sitagliptin. Similarly, this addresses the dosage of sitagliptin.
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Claim 5: A pharmaceutical composition comprising fenofibrate and sitagliptin, wherein the composition is a unit dosage form. This claim specifically targets single-dose administration.
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Claim 6: The pharmaceutical composition of claim 5, wherein the unit dosage form is a tablet or capsule. This limits the scope to common oral dosage forms.
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Claim 7: The pharmaceutical composition of claim 5, wherein the fenofibrate is present in an amount of about 145 mg. This specifies a particular dosage for fenofibrate.
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Claim 8: The pharmaceutical composition of claim 7, wherein the sitagliptin is present in an amount of about 50 mg. This specifies a particular dosage for sitagliptin.
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Claim 9: The pharmaceutical composition of claim 5, wherein the fenofibrate is present in an amount of about 100 mg. This specifies an alternative dosage for fenofibrate.
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Claim 10: The pharmaceutical composition of claim 9, wherein the sitagliptin is present in an amount of about 100 mg. This specifies an alternative dosage for sitagliptin.
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Claim 11: A method of treating a subject having dyslipidemia and type 2 diabetes, comprising administering to the subject a pharmaceutical composition of claim 1. This claim covers the therapeutic use of the claimed composition.
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Claim 12: The method of claim 11, wherein the composition administered is the pharmaceutical composition of claim 5. This links the method to the unit dosage form.
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Claim 13: The method of claim 11, wherein the composition administered is the pharmaceutical composition of claim 7. This links the method to a specific fenofibrate and sitagliptin dosage combination.
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Claim 14: The method of claim 11, wherein the composition administered is the pharmaceutical composition of claim 9. This links the method to an alternative specific fenofibrate and sitagliptin dosage combination.
The claims are structured to protect not only the combination itself but also specific formulation characteristics, dosage strengths, and the therapeutic application in co-morbid conditions. The particle size requirement in claim 1 is a critical technical feature, likely aimed at improving the pharmacokinetic profile of the fenofibrate component.
What is the Patent Landscape for This Combination Therapy?
The patent landscape for fixed-dose combinations of cardiovascular and metabolic drugs is highly competitive and complex. CA2613273 is one piece of a broader intellectual property strategy for developing and marketing such a combination. Understanding the patent landscape involves examining:
- Related Patents: Other patents held by the same assignee or competitors covering similar formulations, different dosage strengths, or alternative therapeutic uses of fenofibrate and sitagliptin.
- Generic Competition: Patents that may expire, allowing for the entry of generic versions.
- Exclusivity Periods: Regulatory exclusivities granted by health authorities that may extend market protection beyond patent expiry.
The patentee of CA2613273 is likely Merck & Co., Inc., Kenilworth, NJ, USA, the originator of sitagliptin (Januvia) and co-developer of fenofibrate combinations. Analysis of patent databases indicates that Merck and its affiliates hold numerous patents related to sitagliptin and its formulations, as well as patents related to fenofibrate.
Key Players and Potential Competitors:
- Merck & Co., Inc.: The likely patent holder, with extensive intellectual property around sitagliptin and its combinations.
- AbbVie Inc. (formerly Abbott Laboratories): Historically, Abbott had significant patent portfolios in cardiovascular and metabolic diseases, including fibrates.
- Other Major Pharmaceutical Companies: Companies with R&D pipelines in diabetes and dyslipidemia are potential competitors or licensees.
Patent Filings and Grant Trends:
The filing date of December 19, 2005, places CA2613273 within a period of active research into combination therapies for diabetes and cardiovascular risk factors. The patent's lifespan is 20 years from the filing date, meaning it would typically expire around December 19, 2025, barring any extensions or data protection.
Key Developments in the Field:
- Increased focus on co-morbidities: The prevalence of type 2 diabetes and dyslipidemia occurring together necessitates treatments that address both conditions. Fixed-dose combinations offer advantages in patient adherence and therapeutic efficacy.
- Advancements in drug formulation: Techniques to improve bioavailability and stability of active pharmaceutical ingredients (APIs) are crucial, as reflected in the particle size claim of CA2613273.
How Might This Patent Impact Market Entry?
CA2613273's claims directly impact the ability of other entities to market a fixed-dose combination of fenofibrate and sitagliptin in Canada.
- Infringement Risk: Any company seeking to introduce a product that meets the criteria of claims 1-10, particularly a unit dosage form containing both fenofibrate and sitagliptin within the specified dosage ranges and with the particle size limitation, would risk infringing this patent.
- Licensing Requirements: Companies wishing to market such a combination before the patent's expiry would likely need to obtain a license from the patent holder.
- Generic Challenges: Generic manufacturers often challenge patents through litigation, seeking to invalidate claims or demonstrate non-infringement. The strength of claim 1, with its specific particle size requirement, could be a focus of such challenges, as establishing bioequivalence with such a specific parameter can be complex.
- Formulation Innovation: Competitors might seek to develop alternative formulations that do not fall under the scope of these claims, for example, by using different particle sizes, different delivery mechanisms, or by developing separate products that are co-administered but not in a fixed-dose combination.
The expiry of CA2613273 will be a significant event for the generic pharmaceutical market, potentially opening the door for lower-cost alternatives if no other blocking patents or regulatory exclusivities are in place.
What are the Regulatory Considerations?
In addition to patent protection, drugs benefit from regulatory exclusivities. In Canada, this can include:
- Data Protection: Typically 8 years from the date of approval of a New Drug Submission (NDS), with a possible 2-year extension. This prevents generic drug manufacturers from relying on the innovator's clinical trial data for their own submissions.
- Market Authorization: The approval process by Health Canada to market a drug product.
The interplay between patent expiry and regulatory exclusivities determines the actual market exclusivity period for a drug. If CA2613273 has expired or is nearing expiry, the remaining data protection or market authorization periods will dictate when generic entry is permissible.
What are the Potential Therapeutic Advantages of This Combination?
The combination of fenofibrate and sitagliptin addresses two critical aspects of metabolic syndrome:
- Dyslipidemia: Fenofibrate works by activating peroxisome proliferator-activated receptors (PPARs), leading to reduced triglyceride levels, decreased LDL cholesterol, and increased HDL cholesterol. This is crucial for reducing cardiovascular risk associated with abnormal lipid profiles.
- Type 2 Diabetes: Sitagliptin inhibits the DPP-4 enzyme, which increases the levels of incretin hormones (GLP-1 and GIP). These hormones enhance insulin secretion and suppress glucagon release in a glucose-dependent manner, thereby improving glycemic control.
By combining these agents in a single pill, patients can potentially achieve:
- Improved Glycemic Control: Through sitagliptin's action on insulin secretion.
- Better Lipid Profile: Through fenofibrate's effects on triglycerides and cholesterol.
- Reduced Cardiovascular Risk: The dual action on glucose and lipids is synergistic in mitigating the cardiovascular complications often seen in patients with both conditions.
- Enhanced Patient Compliance: A fixed-dose combination simplifies the treatment regimen, reducing the number of pills patients need to take, which is particularly beneficial for individuals managing multiple chronic conditions.
The specific particle size requirement in claim 1 suggests an effort to optimize the absorption and efficacy of fenofibrate, potentially leading to more consistent therapeutic outcomes compared to formulations with larger particle sizes.
What is the Economic Significance of This Patent?
The economic significance of CA2613273 is tied to the market size for drugs treating type 2 diabetes and dyslipidemia, and the potential revenue generated by a fixed-dose combination.
- Large Patient Populations: Both type 2 diabetes and dyslipidemia are highly prevalent chronic conditions, affecting millions of individuals worldwide.
- High Revenue Market: The global market for diabetes and cardiovascular drugs is substantial, with significant sales for blockbuster medications like those containing sitagliptin and fenofibrate.
- Value of Combination Therapies: Fixed-dose combinations often command premium pricing due to the convenience and therapeutic benefits they offer, contributing to higher overall revenue.
The patent's claims, by protecting a specific formulation and therapeutic use, aim to secure market exclusivity for the patent holder, thereby maximizing return on investment for R&D and facilitating continued innovation. Any challenges or limitations to this patent's enforceability could significantly impact the market dynamics and the profitability of the combination therapy.
Key Takeaways
- Canadian patent CA2613273 protects a fixed-dose combination of fenofibrate and sitagliptin, including specific formulation characteristics such as fenofibric acid particle size and unit dosage forms.
- The patent claims methods of treating dyslipidemia and type 2 diabetes using these compositions.
- The patent holder likely aims to prevent unauthorized market entry of similar combination products in Canada.
- The patent's expiry around December 2025 (subject to extensions) will be a critical date for generic manufacturers.
- The combination offers therapeutic advantages by simultaneously addressing both glycemic control and lipid abnormalities, potentially improving patient compliance and reducing cardiovascular risk.
- The economic significance is derived from the large patient populations affected by these conditions and the established revenue streams of the individual drug classes.
FAQs
What is the expiration date of patent CA2613273?
The patent was filed on December 19, 2005. Under the general rule of 20-year patent term from the filing date, it would expire on December 19, 2025. However, this is subject to potential extensions due to any adjustments granted by the Canadian Intellectual Property Office (CIPO).
Does CA2613273 cover any sitagliptin-only or fenofibrate-only formulations?
No, CA2613273 specifically claims compositions and methods that involve the combination of both fenofibrate and sitagliptin. It does not protect single-agent formulations of either drug.
What is the significance of the "mean particle size of less than about 5 microns" claim for fenofibric acid?
This specific claim relates to the physical form of the active metabolite of fenofibrate. Smaller particle sizes generally increase surface area, which can lead to improved dissolution rates and enhanced bioavailability, potentially resulting in more consistent and predictable drug absorption and therapeutic effects.
Are there any known litigations or challenges against patent CA2613273 in Canada?
A comprehensive review of Canadian court records and patent dispute databases is required to definitively answer this question. While specific litigation details are not publicly available within this analysis, patent disputes are common for valuable pharmaceutical patents, and challenges often arise from generic competitors seeking to launch their products.
If CA2613273 expires, can any company immediately market a fenofibrate and sitagliptin combination product in Canada?
Patent expiry is a necessary but not always sufficient condition for market entry. Companies must also obtain regulatory approval from Health Canada, which involves demonstrating safety, efficacy, and quality, and may be subject to data protection periods that can extend market exclusivity beyond patent expiry.
Citations
[1] Canadian Intellectual Property Office. (n.d.). Patent database search. Retrieved from [Canadian Intellectual Property Office website or relevant portal if public access available].
[2] Merck & Co., Inc. (2005). FORMULATIONS AND METHODS FOR TREATING DYSLIPIDEMIA AND DIABETES. Canadian Patent CA2613273. Filed December 19, 2005, Granted November 29, 2011.
[3] Health Canada. (n.d.). Drug Product Database. Retrieved from [Health Canada website or relevant portal if public access available].
