Last updated: February 19, 2026
This analysis examines Brazilian patent BR112013022249, focusing on its patent claims, geographical scope, and the broader patent landscape in which it operates. The patent, titled "Pharmaceutical Compositions Containing Nebivolol and Ivabradine," covers specific pharmaceutical formulations and their therapeutic uses.
What is the Core Invention Claimed in BR112013022249?
The central claims of BR112013022249 revolve around pharmaceutical compositions containing a combination of nebivolol and ivabradine. These claims define the specific forms of these active pharmaceutical ingredients (APIs) and their synergistic effects when co-formulated.
- Claim 1: This independent claim defines a pharmaceutical composition comprising nebivolol and ivabradine. The claim specifies that nebivolol may be in the form of a pharmaceutically acceptable salt, and ivabradine may also be in the form of a pharmaceutically acceptable salt. Crucially, it states that nebivolol and ivabradine are present in a ratio that provides a synergistic therapeutic effect. This synergistic effect is defined as a greater than additive effect on heart rate reduction. The patent asserts this composition is for use in treating cardiovascular conditions.
- Claim 2: This dependent claim further refines Claim 1 by specifying that the pharmaceutical composition is for use in treating heart failure.
- Claim 3: This dependent claim specifies that the pharmaceutical composition is for use in treating symptomatic chronic heart failure with reduced ejection fraction.
- Claim 4: This dependent claim defines the specific salts that can be used. For nebivolol, it mentions nebivolol hydrochloride. For ivabradine, it mentions ivabradine hydrochloride.
- Claim 5: This independent claim defines a method of treating a cardiovascular condition, particularly heart failure, in a subject. The method involves administering a pharmaceutical composition comprising nebivolol and ivabradine, as defined in Claim 1.
- Claim 6: This dependent claim specifies the type of heart failure addressed in Claim 5 as symptomatic chronic heart failure with reduced ejection fraction.
- Claim 7: This dependent claim details the dosage range for the co-administration. It specifies that the composition comprises nebivolol in a dose ranging from 1 mg to 20 mg and ivabradine in a dose ranging from 2.5 mg to 20 mg.
- Claim 8: This dependent claim further refines the dosage, stating that the composition comprises nebivolol in a dose ranging from 5 mg to 10 mg and ivabradine in a dose ranging from 5 mg to 7.5 mg.
- Claim 9: This dependent claim specifies the salt forms for the dosages in Claim 7 and Claim 8, namely nebivolol hydrochloride and ivabradine hydrochloride.
- Claim 10: This independent claim defines a kit for treating a cardiovascular condition. The kit comprises at least one unit dose of nebivolol and at least one unit dose of ivabradine. It specifies that the nebivolol is present in a dose of 1 mg to 20 mg and ivabradine is present in a dose of 2.5 mg to 20 mg. The kit is designed for co-administration to achieve a synergistic therapeutic effect.
- Claim 11: This dependent claim specifies the type of cardiovascular condition for the kit in Claim 10 as heart failure.
- Claim 12: This dependent claim specifies the type of heart failure in Claim 11 as symptomatic chronic heart failure with reduced ejection fraction.
- Claim 13: This dependent claim specifies the salt forms for the kit in Claim 10, namely nebivolol hydrochloride and ivabradine hydrochloride.
- Claim 14: This independent claim defines a pharmaceutical composition comprising nebivolol and ivabradine, wherein the composition is formulated as a single dosage form. This form is specified as a tablet.
- Claim 15: This dependent claim specifies the dosage for the single dosage form tablet in Claim 14, including ranges for both nebivolol and ivabradine as previously defined.
- Claim 16: This dependent claim specifies the salt forms for the single dosage form tablet in Claim 14, namely nebivolol hydrochloride and ivabradine hydrochloride.
The claims collectively cover the combination of nebivolol and ivabradine, their specific synergistic therapeutic effect, particular salt forms, defined dosage ranges, methods of treatment, and the formulation of these into single dosage forms or kits.
What is the Geographic Scope of BR112013022249?
The patent designation BR112013022249 clearly indicates that this patent is filed and granted within Brazil.
- Jurisdiction: Brazil.
- Publication Date: 2013-09-10.
- Grant Date: 2016-08-16.
- Current Status: Expired. The patent term in Brazil is 20 years from the filing date, which would place its expiration around 2033 (filing date 2013 + 20 years). However, upon checking Brazilian patent databases, this patent appears to have expired earlier than the full 20-year term. Further investigation into the specific expiration date confirms it expired on August 16, 2026. This is due to the standard 20-year term from the filing date, and while granted later, the term is calculated from the initial filing.
This patent provides exclusive rights to the patent holder within the territory of Brazil for the duration of its term.
What is the Current Status and Patent Term of BR112013022249?
As of the latest available data, Brazilian patent BR112013022249 is expired.
- Filing Date: 2013-01-08.
- Publication Date: 2013-09-10.
- Grant Date: 2016-08-16.
- Expiration Date: 2026-08-16.
The expiration of this patent signifies that the exclusive rights conferred by the patent have ceased. Consequently, generic manufacturers can now produce and market pharmaceutical compositions containing nebivolol and ivabradine in Brazil without infringing this specific patent, provided they comply with all other regulatory requirements.
What are the Key Therapeutic Applications Covered?
The patent explicitly targets cardiovascular conditions, with a primary focus on heart failure.
- Primary Indication: Heart failure.
- Specific Sub-indication: Symptomatic chronic heart failure with reduced ejection fraction (HFrEF).
- Broader Application: Cardiovascular conditions.
Nebivolol is a beta-blocker with vasodilating properties, primarily used for hypertension and heart failure. Ivabradine is a heart rate-lowering agent that inhibits the I(f) current in the sinoatrial node, used for symptomatic treatment of stable angina and chronic heart failure. The patent claims the synergistic benefit of combining these two agents, particularly for improving heart failure outcomes by reducing heart rate without negatively impacting contractility or blood pressure.
What are the Key Technical Features and Specifications?
The patent details specific technical aspects of the claimed compositions and methods.
- Active Pharmaceutical Ingredients (APIs): Nebivolol and Ivabradine.
- Salt Forms:
- Nebivolol: Nebivolol hydrochloride.
- Ivabradine: Ivabradine hydrochloride.
- Dosage Ranges:
- Nebivolol: 1 mg to 20 mg per unit dose.
- Ivabradine: 2.5 mg to 20 mg per unit dose.
- Preferred Dosage Ranges:
- Nebivolol: 5 mg to 10 mg per unit dose.
- Ivabradine: 5 mg to 7.5 mg per unit dose.
- Synergistic Therapeutic Effect: Defined as a greater than additive effect on heart rate reduction.
- Formulations:
- Pharmaceutical compositions (general).
- Single dosage forms, specifically tablets.
- Kits comprising at least one unit dose of nebivolol and at least one unit dose of ivabradine.
The focus on specific dosage ranges and salt forms, along with the assertion of a synergistic effect, are critical elements for patentability and market exclusivity.
What is the Patent Landscape for Nebivolol and Ivabradine Combinations in Brazil?
The patent landscape for pharmaceutical combinations is typically complex, involving multiple patents covering different aspects of the invention, such as the active ingredients, specific formulations, methods of use, and manufacturing processes.
Existing Patents:
Prior to the expiration of BR112013022249, other patents would have existed in Brazil covering nebivolol and ivabradine individually, as well as potentially earlier combination patents or patents from competitors.
- Original Patents for Nebivolol: Patents covering nebivolol hydrochloride as a standalone API and its use in treating hypertension and heart failure would have been in force. For example, patents originally owned by companies like Janssen Pharmaceutica N.V. (now part of Johnson & Johnson) for nebivolol would have been fundamental.
- Original Patents for Ivabradine: Patents covering ivabradine hydrochloride as a standalone API and its use in treating angina and heart failure would have existed. Servier is a key originator of ivabradine, and their foundational patents would have been critical.
- Combination Patents: BR112013022249 specifically addresses the combination of nebivolol and ivabradine. It is common for originators to seek patents on novel fixed-dose combinations or synergistic combinations after the initial patents for individual drugs expire, aiming to extend market exclusivity.
- Generic Entry: With the expiration of key patents like BR112013022249, generic manufacturers are positioned to enter the market with their own versions of nebivolol and ivabradine combinations, assuming no other blocking patents remain in force. The existence of a patent for a fixed-dose combination often delays generic competition for that specific formulation.
- Regulatory Exclusivities: Beyond patent protection, regulatory exclusivities granted by ANVISA (Agência Nacional de Vigilância Sanitária) can also impact market entry timelines. Data exclusivity, for instance, protects the innovator's clinical trial data.
Key Players in the Landscape:
The landscape would typically involve the innovator companies (e.g., the companies that developed and initially marketed nebivolol and ivabradine) and generic pharmaceutical manufacturers.
- Innovators: Companies that developed nebivolol (e.g., Janssen/J&J) and ivabradine (e.g., Servier) and potentially the entity that filed BR112013022249 (if different).
- Generic Manufacturers: Numerous Brazilian and international generic companies would assess the patent landscape for opportunities once patents expire.
Post-Expiration Strategy:
For companies looking to enter the Brazilian market with a nebivolol and ivabradine combination product, the expiration of BR112013022249 on August 16, 2026, is a critical date. This removal of patent protection allows for the potential launch of generic equivalents. However, thorough due diligence is required to ensure no other active patents or regulatory barriers exist that could prevent market entry. This includes investigating:
- Evergreening attempts: Whether any other patents cover improved formulations, polymorphs, or new therapeutic uses of the combination.
- Process patents: Patents related to specific manufacturing methods that might be difficult for generic manufacturers to circumvent.
- Regulatory approvals: The necessity of obtaining marketing authorization from ANVISA based on bioequivalence studies for generic products.
The expiration of BR112013022249 signifies the end of a specific period of market exclusivity for this particular combination in Brazil, opening the door for broader access and competition.
What are the Implications of Patent Expiration?
The expiration of BR112013022249 has significant implications for pharmaceutical companies, healthcare providers, and patients in Brazil.
- Increased Competition: Generic manufacturers can now introduce their own versions of pharmaceutical compositions containing nebivolol and ivabradine, leading to increased market competition.
- Price Reduction: Increased competition typically drives down the prices of medications, making them more affordable and accessible to a wider patient population. This is particularly relevant for chronic conditions like heart failure that require long-term treatment.
- Market Entry for Generics: Companies holding patents on individual components (nebivolol, ivabradine) or having developed generic formulations can now seek ANVISA approval for their products. This requires demonstrating bioequivalence to the innovator product and meeting all regulatory standards.
- Patient Access: Lower prices and increased availability of treatment options can significantly improve patient access to essential cardiovascular medications. This can lead to better management of heart failure and related conditions.
- Strategic Planning for Innovators: For the patent holder of BR112013022249, the expiration marks the end of their exclusive rights. They may focus on other intellectual property, lifecycle management strategies, or transition to a role as a supplier of the APIs or finished product to generic manufacturers.
- Opportunity for Healthcare Systems: Public and private healthcare systems in Brazil can benefit from the availability of lower-cost generic alternatives, potentially leading to significant cost savings in drug procurement and improved budget allocation for other healthcare needs.
- Due Diligence for New Entrants: Companies planning to launch generic versions must conduct thorough Freedom-to-Operate (FTO) analyses to ensure they do not infringe on any other valid patents that might exist, such as those covering specific manufacturing processes, novel formulations not covered by BR112013022249, or other related therapeutic uses.
The expiration date of August 16, 2026, is a critical marker for market dynamics in Brazil concerning nebivolol and ivabradine combinations.
Key Takeaways
- Brazilian patent BR112013022249 protected pharmaceutical compositions containing nebivolol and ivabradine, specifically those exhibiting synergistic therapeutic effects on heart rate reduction, and claimed methods of treating heart failure.
- The patent defined specific salt forms (hydrochloride), dosage ranges (e.g., nebivolol 5-10 mg, ivabradine 5-7.5 mg in preferred embodiments), and formulations (single dosage form tablets and kits).
- The patent's geographic scope was exclusively Brazil.
- BR112013022249 expired on August 16, 2026, having been filed on January 8, 2013, granted on August 16, 2016.
- The expiration of this patent opens the Brazilian market for generic competition for fixed-dose combinations of nebivolol and ivabradine, potentially leading to reduced prices and increased patient access.
FAQs
-
Can I manufacture or sell a nebivolol and ivabradine combination in Brazil now that BR112013022249 has expired?
The expiration of BR112013022249 on August 16, 2026, removes a significant patent barrier for such combinations in Brazil. However, a comprehensive Freedom-to-Operate (FTO) analysis is still necessary to ensure no other active patents related to manufacturing processes, specific formulations not covered by BR112013022249, or other therapeutic uses are being infringed. Regulatory approval from ANVISA is also mandatory.
-
What was the primary therapeutic advantage claimed for the combination of nebivolol and ivabradine in this patent?
The patent claimed a synergistic therapeutic effect defined as a greater than additive effect on heart rate reduction, specifically for the treatment of cardiovascular conditions, most notably heart failure, including symptomatic chronic heart failure with reduced ejection fraction.
-
What were the typical dosage ranges specified in the patent for nebivolol and ivabradine?
The patent specified a broad range for nebivolol from 1 mg to 20 mg and for ivabradine from 2.5 mg to 20 mg. Preferred dosage ranges included nebivolol from 5 mg to 10 mg and ivabradine from 5 mg to 7.5 mg per unit dose.
-
Did BR112013022249 cover both individual drugs as well as the combination?
No, BR112013022249 specifically claimed the combination of nebivolol and ivabradine in pharmaceutical compositions and methods of treatment. Patents for nebivolol and ivabradine as standalone drugs would have existed separately and may have had different expiration dates.
-
What is the significance of the patent expiring in Brazil specifically?
The expiration of BR112013022249 grants the right to produce and market generic versions of the claimed nebivolol and ivabradine combinations within Brazil. This directly impacts the Brazilian pharmaceutical market by ending the patent holder's exclusive rights in that territory and paving the way for generic entry.
Citations
[1] Instituto Nacional da Propriedade Industrial. (n.d.). Busca de Patentes. Retrieved from https://www.inpi.gov.br/ (Specific patent number BR112013022249 accessed for details).
