Who holds the patent for Axitinib?

Overview of Axitinib

Introduction and Uses 
Axitinib is a potent, small-molecule inhibitor that belongs to the class of tyrosine kinase inhibitors with a primary action in inhibiting vascular endothelial growth factor receptors (VEGFRs). It is widely known for its clinical application in the treatment of various cancers, particularly advanced renal cell carcinoma. Axitinib’s therapeutic utility extends into off-label applications where its mechanism—targeting angiogenesis pathways—also makes it a candidate in other oncologic indications. Its versatility in clinical use has spurred interest in developing novel formulations, delivery systems, and combination therapies to enhance drug delivery, efficacy, and patient compliance.

Mechanism of Action 
Axitinib works primarily by binding to the intracellular ATP-binding domains of VEGFR-1, VEGFR-2, and VEGFR-3. In doing so, it prevents receptor autophosphorylation and downstream signaling necessary for angiogenesis. Inhibition of these receptors disrupts the blood supply to tumors, thus stalling tumor growth and metastatic spread. The precise modulation of angiogenesis also underpins its incorporation in combination therapies, aiming at not just direct tumor suppression but also modifying the tumor microenvironment to improve immune-related responses.

Patent Landscape of Axitinib

Initial Patent and Development 
The chemical entity axitinib (also referred to in literature as AG-013736) represents a significant advancement in targeted cancer therapies. Although our provided references do not explicitly state the full historical chain of custody regarding the original chemical patent, established scientific literature and background knowledge indicate that the initial patents for axitinib were developed and claimed by Pfizer. Pfizer’s extensive research and development efforts led them to secure a series of patents covering the compound’s chemical structure, synthetic routes, and early formulation strategies. These patents served as the foundational intellectual property (IP) that protected the compound’s innovation during its early clinical stages.

Later developments, however, have seen the expansion of the patent landscape into various aspects of formulation, manufacturing processes, and novel therapeutic applications. This expansion reflects the broader trend in pharmaceutical innovation where improvements and new delivery mechanisms are pursued to extend the commercial life of a drug and to address new clinical challenges. Early innovations that were secured by Pfizer provided the initial exclusivity period that allowed for the recovery of R&D investments. As these primary patents have matured, industry players have looked toward optimizing formulations and exploring alternative routes of administration to open up additional markets. The multifaceted nature of these development efforts is evident in the various subsequent patents that have emerged over the years.

Current Patent Holders 
Today, the patent portfolio for axitinib is not held by a single entity. Instead, multiple organizations, including universities, research institutions, and biopharmaceutical companies, have contributed additional layers of IP protection covering diverse aspects of axitinib. The current landscape reflects a distributed network of patents, each focusing on different formulations, methods of production, and new therapeutic uses. A detailed breakdown of the current patent holders is as follows:

1. Wuhan University Zhongnan Hospital 
- This institution holds a patent related to an axitinib pharmaceutical preparation and the associated preparation method. The patent (CN115177594B), published on August 15, 2023, delineates a formulation that includes axitinib combined with excipients such as stabilizers, fillers, and solubilizers. This innovation is aimed at ensuring high stability, quality, and a good dissolution rate for the drug.

2. Fudan University 
- Fudan University has patented the application of axitinib in the preparation of drugs specifically for inhibiting the enterovirus 71 neurotropic virus (EV-A71). The invention, recorded under patent number CN115089582B, highlighiral potential of axitinib beyond its conventional oncological uses and was filed on May 21, 2022, with publication on July 14, 2023. This diversification into antiviral applications represents an innovative repurposing of the compound.

3. Lunan Pharmaceutical Group Co., Ltd.
- This company holds two critical patents concerning axitinib. The first patent (CN114685434B), a formulation designed to enhance solubility and permeability, with an application date of December 28, 2020, and a publication date on June 16, 2023. 
- The second patent (CN113943271B) is insensitive to light, which promises improved bioavailability and efficacy in drug applications. It was filed on July 15, 2020, and published on November 14, 2023. 
- Both patents underscore efforts to optimize the physical and chemical properties of axitinib for enhanced therapeutic performance.

4. AIVIVA BIOPHARMA, INC. 
- This North American biopharmaceutical company holds a patent for suspension compositions of multi-target inhibitors, which include axitinib among other agents. The patent (CA3088185C) published on January 2, 2024, illustrates the development of aqueous suspension formulations designed for local administration to targeted tissues. This strategy addresses the need for direct drug delivery to desired sites while minimizing systemic side effects.

5. Cloudbreak Therapeutics LLC / CLOUDBREAK THERAPEUTICS LLC 
- These entities have contributed to the development of emulsion formulations for multikinase inhibitors that incorporate axitinib. Two patents illustrate this innovation:
- One patent (EP3843704B1) was filed on August 28, 2019, with a publication date of December 20, 2023. 
- Another patent (IN465149B) describes similar formulations, filed on March 20, 2021, and published on November 10, 2023. 
- Their work focuses on employing nanoemulsions with specific carriers and solubilizers that improve drug solubility and penetration, thereby facilitating ocular and other targeted therapies.

6. China Agricultural University
- This institution holds a patent related to the use of vascular endothelial growth factor receptor inhibitors such as axitinib. The invention emphasizes delaying ovarian aging by modulating angiogenesis in adult ovaries, with the patent (CN113456630B) filed on July 7, 2021, and published on January 12, 2024. 
- This patent represents an innovative application that expands the potential use of axitinib into reproductive health and age-related conditions.

7. 주식회사 스카이테라퓨틱스 (Skyt Therapeutics Co., Ltd.) 
- This company has secured a patent covering an amorphous nano-molecular assembly of tyrosine kinase inhibitors, which includes axitinib. The disclosed invention, recognized under patent number KR1020240115650A, was filed on January 19, 2023, and published on July 26, 2024. It is aimed at improving the storage stability and delivery efficiency of the inhibitor by forming amorphous nano-molecular complexes.

8. OCULAR THERAPEUTIX, INC. 
- This company is focused on ocular drug delivery systems. It holds patents for ocular implants that incorporate axitinib, with two notable patents: 
- One patent (WO2024215649A1) is for an ocular implant comprising axitinib polymorph IV, with a filing date indicating a focus on sustained drug release to treat retinal diseases, filed on April 9, 2024, and published on October 17, 2024. 
- A second patent (EP4252725A2) describes another ocular implant formulation that similarly relies on a sustained-release mechanism, filed on March 24, 2021, and published on October 4, 2024. 
- These patents illustrate the trend of repurposing axitinib into specialized delivery systems that extend its utility beyond systemic cancer therapies.

9. XSpray Pharma AB (publ) 
- The company is involved in the development of novel pharmaceutical compositions. One of its innovations includes stable, amorphous hybrid nanoparticles that incorporate protein kinase inhibitors such as axitinib. This approach is aimed at enhancing the oral bioavailability and therapeutic window of poorly water-soluble drugs, as disclosed in their patent (EP4218740A1) filed on January 11, 2013, and published on August 2, 2023.

10. Other Patents and Applications 
- In addition to the patents mentioned above, there is also an application that discloses the use of axitinib in treating nasopharyngeal cancer. Although this application does not clearly specify an assignee, it adds to the overall complexity and breadth of the patent landscape associated with axitinib. 
- The distributed nature of these patents reflects how various organizations have focused on different aspects—warranty formulations, novel delivery mechanisms, and expanded therapeutic applications—which means that while the original compound’s chemical patent might have originated with Pfizer, the development and enhancement of axitinib’s clinical utility have resulted in a multi-owner patent landscape.

Legal and Commercial Implications

Importance of Patent Ownership 
Patent ownership is a cornerstone of pharmaceutical innovation. The protection afforded by patents ensures that companies and institutions can secure exclusive rights to their innovations, allowing them to recoup investments in research and development. For axitinib, this principle is doubly significant because it covers a range of innovations—from the chemical entity itself to advanced formulation strategies intended to improve patient outcomes. 
- Exclusivity and Market Advantage: Original patents, such as those held by Pfizer for the core compound, provided market exclusivity that enabled significant clinical trial investments and subsequent market success. 
- Incentivizing Further Research: Subsequent patents by institutions like Wuhan University Zhongnan Hospital, Fudan University, and others have driven further research into optimizing drug delivery and expanding axitinib’s therapeutic applications. Such layered IP protection not only extends the commercial life of the drug but also provides a competitive edge for the holders. 
- Collaboration and Licensing: A diversified patent portfolio opens the door to licensing opportunities, joint ventures, and cross-collaborations. This, in turn, stimulates innovation and broader application, as seen with the ocular implant formulations and emulsion-based delivery systems.

Impact on Market and Competition 
The multiplicity of patents related to axitinib means that numerous players have a stake in how the drug is used, formulated, and commercialized: 
- Enhanced Innovation Ecosystem: With several entities holding patents that cover various aspects of axitinib, the innovation ecosystem becomes robust. This supports the introduction of various improved formulations, such as cocrystals and nanoemulsions, which can create additional layers of market exclusivity even as the original compound patent nears expiration. 
- Barrier to Generic Entry: The existence of multiple patents may delay the entry of generic competitors into the market. While the original compound may eventually fall into the public domain, novel formulations and specialized delivery methods remain protected, allowing patent holders to maintain a market advantage even post-expiry of the core patent. This layered protection structure creates a robust barrier for competitors and preserves profit margins. 
- Market Competition and Pricing: Different formulations aimed at niche applications (e.g., ocular delivery versus systemic administration) can cater to segmented markets, optimizing price points and treatment outcomes. Furthermore, the strategic management of these patents is critical in negotiations, litigation, and cross-licensing deals, all of which influence the competitive landscape.

Future Developments

Patent Expiry and Generic Competition 
One of the critical aspects in the pharmaceutical industry is the eventual expiry of core compound patents, which in this case would be the patents originating from the initial development of axitinib by Pfizer. 
- Core Patent Expiry: As the original axitinib patent reaches its expiration, the chemical compound itself may become accessible for generic manufacturers. However, while the basic molecule becomes generic, the advanced formulations—as developed by the other patent holders—continue to hold their exclusivity. 
- Generics vs. New Formulations: Generic competition typically focuses on the raw chemical entity, but novel formulations such as cocrystals, stable crystal forms, nanoemulsions, and ocular implants remain protected. This creates a scenario where generics can enter the market for the basic molecule, but innovative products continue to promise better efficacy and patient compliance, maintaining premium pricing and market segmentation. 
- Legal Challenges: As more players focus on repositioning and reformulating axitinib, legal challenges and patent litigations may arise over overlapping intellectual property claims. The management of these disputes will be instrumental in shaping market dynamics and could influence future pricing strategies and licensing agreements.

Innovations and New Applications 
In the future, the patent landscape of axitinib appears poised to expand further with the continuous evolution of pharmaceutical technologies and therapeutic needs: 
- New Therapeutic Indications: The application of axitinib beyond cancer—for instance, the antiviral potential against EV-A71 and potential uses in reproductive health—opens new avenues for patent filings and market expansion. Continued research into these novel indications will help consolidate the position of axitinib within multiple therapeutic domains. 
- Advanced Drug Delivery Systems: Developments such as the sustained-release ocular implants and amorphous nano-molecular formulations indicate a clear trend towards personalized and site-specific drug delivery. These innovations are at the forefront of personalized medicine and represent a significant opportunity for patent holders to secure exclusive rights, ensuring prolonged product life-cycle and continuous revenue streams. 
- Combination Therapy and Multi-Target Strategies: Multi-targeted approaches involving axitinib, as reflected in current patents related to suspension compositions and emulsion formulations, suggest a shift toward combinatorial strategies. The ability to co-formulate axitinib with other agents improves therapeutic outcomes and reduces dosing frequency, a significant advantage in clinical settings. This trend is likely to continue, thereby broadening the scope of patent filings in the near future.

Detailed Conclusion 
In summary, the patent landscape for axitinib is multifaceted, reflecting the evolution of a single active pharmaceutical ingredient into a platform for numerous innovative therapies. Initially developed and patented by Pfizer for its anti-angiogenic properties and targeted cancer applications, axitinib’s core chemical patent set the stage for subsequent innovations. Over time, various research institutions and pharmaceutical companies have built upon this foundation by securing patents that cover specific formulations, novel delivery systems, and additional therapeutic applications. 

Multiple current patent holders are now involved in the axitinib ecosystem:
- Wuhan University Zhongnan Hospital and Fudan University have expanded the clinical applications of axitinib into new therapeutic areas. 
- Lunan Pharmaceutical Group has focused on optimizing the physical properties of axitinib through innovative crystal and cocrystal formulations. 
- AIVIVA BIOPHARMA, INC., Cloudbreak Therapeutics LLC / CLOUDBREAK THERAPEUTICS LLC, and OCULAR THERAPEUTIX, INC. have developed advanced drug delivery systems, each targeting specific clinical scenarios. 
- Additional players such as China Agricultural University, 주식회사 스카이테라퓨틱스, and XSpray Pharma AB (publ) further exemplify the diversity of the patent landscape. 

This distributed ownership model enhances innovation while also establishing strong barriers to generic entry. While the original axitinib compound patent may eventually expire—opening up opportunities for generic manufacturers—innovative formulations and delivery methods will continue to enjoy proprietary protection. This creates a layered defense strategy where generics may access the base molecule, but value-added, superior formulations remain shielded by newer patents. 

Legally, the robust patent portfolio helps secure market exclusivity, supports strategic licensing and collaboration agreements, and provides a competitive edge for the stakeholders involved. Commercially, it enables price differentiation by segmenting the market according to the quality and specificity of the formulations, thereby ensuring sustained revenue streams even as the original compound patent ages.

Future developments are expected to drive further evolution of axitinib’s IP portfolio. Researchers and companies are geared toward expanding its therapeutic indications, refining its formulations for improved bioavailability, and integrating combination therapy strategies. These ongoing efforts underscore the importance of continuous innovation and dynamic patent management in maintaining axitinib’s role as a critical agent in oncology and beyond.

In conclusion, while Pfizer is historically recognized for holding the original chemical patent for axitinib, the current patent landscape is characterized by a broad array of current patent holders. Each entity contributes to different facets of axitinib’s development and commercialization—from novel pharmaceutical preparations and crystal forms to innovative delivery systems and expanded therapeutic uses. These diverse patents, held by entities such as Wuhan University Zhongnan Hospital, Fudan University, Lunan Pharmaceutical Group, AIVIVA BIOPHARMA, INC., Cloudbreak and CLOUDBREAK THERAPEUTICS LLC, China Agricultural University, 주식회사 스카이테라퓨틱스, OCULAR THERAPEUTIX, INC., and XSpray Pharma AB (publ), collectively demonstrate that the patent for axitinib is not held by a single organization. Instead, it is a complex nexus of intellectual property rights that underscores the multi-dimensional evolution of this important therapeutic agent.

Discover Eureka LS: AI Agents Built for Biopharma Efficiency

Stop wasting time on biopharma busywork. Meet Eureka LS - your AI agent squad for drug discovery.

▶ See how 50+ research teams saved 300+ hours/month

From reducing screening time to simplifying Markush drafting, our AI Agents are ready to deliver immediate value. Explore Eureka LS today and unlock powerful capabilities that help you innovate with confidence.