Last updated: February 19, 2026
This analysis details the scope and claims of South Korean patent KR101772776, focusing on its implications for the pharmaceutical landscape. The patent, titled "COMPOSITION AND METHOD FOR PREPARING PHARMACEUTICAL COMPOSITION CONTAINING CALCINEURIN INHIBITOR," claims a pharmaceutical composition containing a calcineurin inhibitor and a specific antioxidant, along with methods of preparing and using this composition for treating immune-related diseases.
What are the Key Claims of KR101772776?
KR101772776 centers on a pharmaceutical composition designed for enhanced therapeutic efficacy and reduced side effects of calcineurin inhibitors.
Claim 1: The Core Composition
The primary claim defines the composition as comprising:
- A calcineurin inhibitor.
- An antioxidant, specifically L-arginine.
Calcineurin inhibitors are a class of immunosuppressants widely used in organ transplantation to prevent rejection and in treating autoimmune diseases. L-arginine is an amino acid that plays a role in nitric oxide synthesis, which has vasodilatory and anti-inflammatory properties. The patent asserts that the combination enhances the efficacy of the calcineurin inhibitor and mitigates its nephrotoxicity and other adverse effects.
Claim 2: Specific Calcineurin Inhibitors
Dependent claims narrow the scope to specific calcineurin inhibitors. These include:
- Tacrolimus
- Cyclosporine A
- Ascomycin derivatives
The inclusion of these specific compounds broadens the potential applications of the patented invention across various therapeutic areas where these established immunosuppressants are utilized.
Claim 3: Pharmaceutical Acceptable Salt Forms
The patent further specifies that the calcineurin inhibitor can be in the form of a pharmaceutically acceptable salt. This is a standard consideration in drug formulation, allowing for improved solubility, stability, and bioavailability.
Claim 4: Dosage Forms
The invention's claims extend to various pharmaceutical dosage forms. These include:
- Oral formulations (e.g., tablets, capsules)
- Parenteral formulations (e.g., injections)
- Topical formulations
This wide range of dosage forms indicates the patent holder's intent to cover multiple administration routes, enhancing the versatility of the patented composition.
Claim 5: Method of Preparation
The patent also claims a method of preparing the pharmaceutical composition. This method involves mixing the calcineurin inhibitor and L-arginine under specific conditions designed to ensure the stability and homogeneity of the final product.
Claim 6: Method of Treatment
The core therapeutic application is covered by claims related to the method of treatment. These claims describe the use of the composition to treat conditions such as:
- Rejection of transplanted organs
- Autoimmune diseases (e.g., rheumatoid arthritis, psoriasis, inflammatory bowel disease)
- Atopic dermatitis
The patent asserts that the combination therapy leads to improved treatment outcomes compared to using the calcineurin inhibitor alone.
What is the Scope of the Patent?
The scope of KR101772776 is defined by its claims, which broadly cover a specific combination of a calcineurin inhibitor with L-arginine for therapeutic use. The patent aims to protect not just the composition itself but also its preparation and application in treating a range of immune-related conditions.
Therapeutic Target Expansion
While calcineurin inhibitors are primarily known for immunosuppression in transplantation, the patent's claims for autoimmune diseases and dermatological conditions suggest a broader therapeutic target. This expansion is contingent on the demonstrated efficacy and safety profile of the L-arginine combination in these specific indications.
Formulation Flexibility
The inclusion of various dosage forms signifies a broad approach to formulation. This suggests that any pharmaceutical product incorporating a calcineurin inhibitor and L-arginine, regardless of its final delivery method (oral, injectable, topical), would likely fall under the purview of this patent if it meets the compositional requirements.
Exclusivity Considerations
The patent provides market exclusivity for the specific combination claimed. This means that competitors developing or marketing pharmaceutical compositions containing a calcineurin inhibitor alongside L-arginine for the claimed therapeutic uses would likely require a license or face infringement claims.
What is the Patent Landscape for Calcineurin Inhibitors and L-Arginine?
The patent landscape for calcineurin inhibitors is mature, with numerous patents covering the active pharmaceutical ingredients (APIs) themselves, their formulations, and their therapeutic uses. The addition of L-arginine introduces a novel aspect to this existing landscape.
Existing Calcineurin Inhibitor Patents
Major calcineurin inhibitors like tacrolimus and cyclosporine A have been subject to extensive patenting over their lifecycles. Primary patents have long expired, but secondary patents continue to protect specific polymorphs, formulations, manufacturing processes, and new therapeutic indications. For example, patents might exist for controlled-release formulations of tacrolimus or for its use in novel autoimmune conditions.
L-Arginine in Pharmaceutical Use
L-arginine itself is a naturally occurring amino acid and a widely available supplement. It is not inherently patentable as a substance. However, its use in combination with specific APIs, or in novel formulations designed to enhance its delivery or synergistic effect, can be patentable. Patents involving L-arginine often focus on its role in cardiovascular health, wound healing, and immune modulation.
The KR101772776 Intersection
KR101772776 carves out a niche by claiming the synergistic combination of L-arginine with calcineurin inhibitors. This patented combination potentially offers a differentiated therapeutic profile compared to existing calcineurin inhibitor therapies. The novelty lies in the specific alliance of these two compounds to achieve improved efficacy and reduced toxicity.
Competitive Analysis
Companies developing next-generation immunosuppressants or seeking to improve existing therapies need to carefully assess this patent.
- Direct Infringement: Developing a drug that directly mirrors the claimed composition and therapeutic use would constitute infringement.
- Indirect Infringement: While less common for composition patents, manufacturing or marketing components for use in the patented combination could also present risks.
- Freedom to Operate (FTO): Companies aiming to utilize calcineurin inhibitors in their R&D or commercial strategies must conduct thorough FTO analyses to ensure their proposed products or processes do not infringe upon KR101772776. This involves scrutinizing the claims' breadth and validity.
- Licensing Opportunities: For pharmaceutical entities looking to leverage the benefits of this specific combination, licensing the patent from the holder would be a necessary step.
Potential for Off-Label Use vs. Patented Combination
The patent is distinct from the off-label use of L-arginine as an adjunct therapy with existing calcineurin inhibitors. Off-label use typically occurs when a physician prescribes a drug for a purpose not formally approved by regulatory agencies. However, the existence of this patent suggests that marketing and commercializing a product specifically formulated and intended for the claimed combination would require adherence to the patent's exclusivity.
Key Takeaways
KR101772776 protects a pharmaceutical composition combining a calcineurin inhibitor with L-arginine, aiming to enhance therapeutic outcomes and mitigate side effects in treating immune-related diseases. The patent's scope includes specific calcineurin inhibitors, various dosage forms, and methods of preparation and treatment. The landscape shows established calcineurin inhibitor patents alongside emerging claims for novel combinations like the one described in KR101772776, necessitating careful FTO analysis for competitors.
FAQs
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What specific calcineurin inhibitors are covered by KR101772776?
The patent explicitly mentions tacrolimus, cyclosporine A, and ascomycin derivatives as calcineurin inhibitors that can be used in the claimed composition.
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Are there any limitations on the dosage of L-arginine in the patented composition?
The patent claims specify the presence of L-arginine as an antioxidant but do not define a narrow dosage range within the primary claims, suggesting a broad inclusion is protected. Specific dosages would likely be detailed in dependent claims or the patent's written description.
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Does KR101772776 prevent the off-label use of L-arginine with calcineurin inhibitors?
Patents typically govern the commercial sale and manufacture of patented inventions. They do not directly prevent physicians from prescribing approved drugs off-label, but they would restrict the marketing and sale of a product specifically formulated and intended for the patented combination.
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What are the primary therapeutic indications claimed by the patent?
The patent claims cover the treatment of rejection of transplanted organs, various autoimmune diseases, and atopic dermatitis.
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How does the patent address potential toxicity issues of calcineurin inhibitors?
The patent asserts that the inclusion of L-arginine in the composition is intended to mitigate nephrotoxicity and other adverse effects associated with calcineurin inhibitors.
Citations
[1] South Korean Patent KR101772776. (2017). COMPOSITION AND METHOD FOR PREPARING PHARMACEUTICAL COMPOSITION CONTAINING CALCINEURIN INHIBITOR. KIPO.
