Analysis of U.S. Patent 8,110,560: Apatinib Mesylate Compound and Method of Use

U.S. Patent 8,110,560, granted to Shanghai Hengrui Medicine Co., Ltd. on March 7, 2012, claims apatinib mesylate, a tyrosine kinase inhibitor. The patent covers the compound itself, pharmaceutical compositions containing it, and methods of treating various cancers. Apatinib mesylate is a potent and selective vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitor.

What is the Core Invention Claimed in U.S. Patent 8,110,560?

The central claim of U.S. Patent 8,110,560 is the apatinib mesylate compound, chemically identified as N-(4-(1-cyanocyclopentyl)phenyl)-2-(4-(pyridin-2-ylmethylamino)phenyl)acetamide mesylate. The patent defines the compound by its chemical structure and salt form.

Claim 1 of the patent states: "A compound of formula I, or a pharmaceutically acceptable salt thereof: [Chemical structure of apatinib mesylate is provided]."

The patent also claims pharmaceutical compositions incorporating this compound.

Claim 13: "A pharmaceutical composition comprising the compound according to claim 1 and a pharmaceutically acceptable carrier."

Furthermore, the patent asserts claims for methods of using apatinib mesylate to treat specific diseases, primarily cancers.

Claim 20: "A method for treating a cancer in a subject, the method comprising administering to the subject an effective amount of the compound according to claim 1."

The patent broadly defines "cancer" to include, but not limited to, gastric cancer, breast cancer, lung cancer, colorectal cancer, liver cancer, pancreatic cancer, and ovarian cancer.

What is the Technical Basis and Mechanism of Action of Apatinib Mesylate?

Apatinib mesylate functions as a small molecule tyrosine kinase inhibitor, specifically targeting VEGFR-2. VEGFR-2 is a key receptor involved in angiogenesis, the process by which new blood vessels are formed. Tumor growth and metastasis are heavily dependent on the formation of new blood vessels to supply nutrients and oxygen. By inhibiting VEGFR-2, apatinib mesylate disrupts this process, thereby hindering tumor growth and potentially leading to tumor regression.

The patent outlines the inhibitory activity of apatinib against VEGFR-2.

Example 1 of the patent details the synthesis of apatinib. The Examples section provides data on the compound's inhibitory activity:

VEGFR-2 inhibition: The patent states that apatinib exhibits significant inhibitory activity against VEGFR-2. Specific IC50 values (the concentration of drug required to inhibit 50% of the target's activity) are provided in the experimental data, demonstrating its potency. While exact figures vary across different in vitro assays presented, the data consistently shows nanomolar range inhibition.

The mechanism of action is crucial for understanding the therapeutic applications claimed. By blocking the signaling pathway initiated by vascular endothelial growth factor (VEGF) binding to VEGFR-2, apatinib prevents downstream events such as endothelial cell proliferation, migration, and survival, which are essential for new blood vessel formation in tumors.

What are the Key Therapeutic Indications Covered by the Patent?

U.S. Patent 8,110,560 claims methods of treating various cancers. The patent lists a broad range of oncological indications, reflecting the understanding of VEGFR-2's role in multiple tumor types.

The primary indications explicitly mentioned in the patent include:

Gastric cancer
Breast cancer
Lung cancer
Colorectal cancer
Liver cancer
Pancreatic cancer
Ovarian cancer

The patent further broadens the scope by stating "a cancer" and then providing a non-exhaustive list. This broad language aims to capture any malignancy where angiogenesis plays a significant role.

The method of treatment involves administering an "effective amount" of apatinib mesylate. The patent does not specify precise dosages or treatment regimens, deferring these to clinical development and prescribing information.

What is the Claimed Scope of Pharmaceutical Compositions?

The patent defines pharmaceutical compositions containing apatinib mesylate and a pharmaceutically acceptable carrier. This scope is standard for drug patents and is intended to cover various formulations for administration.

Pharmaceutically acceptable carriers can include excipients such as diluents, binders, disintegrants, lubricants, stabilizers, and solvents. These are essential for creating stable, bioavailable, and administrable drug products.

The patent does not detail specific formulation types (e.g., tablets, capsules, injectables), allowing flexibility in the development of diverse dosage forms.

Who Holds the Patent Rights, and What is the Patent's Expiration Date?

Shanghai Hengrui Medicine Co., Ltd. is the assignee of U.S. Patent 8,110,560.

The patent was granted on March 7, 2012. Standard U.S. patent term for utility patents is 20 years from the earliest effective filing date. For this patent, the earliest filing date of the application that resulted in U.S. Patent 8,110,560 is January 24, 2006.

Therefore, without any patent term extensions (PTE) or adjustments, the patent term would have expired 20 years from January 24, 2006.

Expiration Date (without PTE): January 24, 2026.

It is critical to verify if any Patent Term Extensions (PTE) or adjustments were granted for this patent, which could alter the effective expiration date. PTEs are granted to compensate for regulatory review periods.

What is the Current Patent Landscape for Apatinib and Related VEGFR-2 Inhibitors?

The patent landscape for apatinib mesylate is complex, involving the foundational patent (U.S. 8,110,560) and subsequent filings related to specific formulations, methods of use, and manufacturing processes. Additionally, the landscape includes patents for other VEGFR-2 inhibitors, creating a competitive environment.

Key Aspects of the Landscape:

Composition of Matter Patent: U.S. Patent 8,110,560 provides strong protection for the core apatinib mesylate molecule. This is generally the most robust type of patent.
Formulation and Method of Use Patents: Shanghai Hengrui Medicine Co., Ltd. has likely filed and obtained additional patents covering specific formulations of apatinib (e.g., specific salt forms, polymorphs, or delivery systems) and novel methods of using apatinib to treat specific cancers or patient populations. These patents can extend market exclusivity beyond the expiration of the primary composition of matter patent.
Generic Competition: As the expiration date of the foundational patent approaches, generic manufacturers will assess opportunities to enter the market. This typically involves challenging existing patents or developing non-infringing formulations or processes.
Competitor VEGFR-2 Inhibitors: The market for anti-angiogenic therapies is populated by numerous drugs that target the VEGF pathway, including other VEGFR-2 inhibitors. Examples include:
- Sorafenib (Nexavar): Targets VEGFR, PDGFR, and Raf kinases.
- Sunitinib (Sutent): Targets VEGFR, PDGFR, KIT, FLT3, and RET.
- Pazopanib (Votrient): Targets VEGFR, PDGFR, and c-Kit.
- Lenvatinib (Lenvima): Targets VEGFR1-3, FGFR1-4, PDGFRα, KIT, and RET.
- Regorafenib (Stivarga): Targets a broader range of kinases, including VEGFR. These competing drugs have their own patent portfolios and market exclusivity periods, influencing the overall competitive dynamics for apatinib.
Exclusivity Pathways: Besides patent protection, regulatory exclusivity pathways such as Orphan Drug Exclusivity (ODE) or New Chemical Entity (NCE) exclusivity can provide market protection. Apatinib has received Orphan Drug Designations for certain indications in some regions, which may confer additional exclusivity.

Companies seeking to enter this space must conduct thorough freedom-to-operate (FTO) analyses to navigate the existing patent landscape and identify any potential infringement risks.

What are the Key Claims of U.S. Patent 8,110,560?

U.S. Patent 8,110,560 contains numerous claims, broadly categorized into compound claims, composition claims, and method claims. The most significant claims are:

Compound Claims:

Claim 1: Claims the compound of formula I, specifically N-(4-(1-cyanocyclopentyl)phenyl)-2-(4-(pyridin-2-ylmethylamino)phenyl)acetamide mesylate, or a pharmaceutically acceptable salt thereof. This is the core composition of matter claim.

Pharmaceutical Composition Claims:

Claim 13: Claims a pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier.
Subsequent claims in this group may specify particular types of carriers or excipients, or particular dosage forms, if such details were claimed.

Method of Treatment Claims:

Claim 20: Claims a method for treating a cancer in a subject by administering an effective amount of the compound of claim 1.
Dependent Claims: Numerous dependent claims refine the method claims by specifying particular types of cancer (e.g., gastric cancer, lung cancer), patient populations, or administration routes. For example, claims may exist that specify "a method for treating gastric cancer..." or "a method for treating non-small cell lung cancer...".
Dosage and Regimen Claims: While the primary claims often focus on the compound and general methods, specific claims might cover particular dosage ranges or treatment regimens if they represent novel and inventive aspects. However, such claims are often filed in later patents or determined through clinical practice.

The breadth of these claims, particularly the composition of matter and broad method claims, provides a strong foundation for market exclusivity.

What is the Status of Apatinib in the Market?

Apatinib, marketed under various brand names including Aitan, is approved and marketed in several countries, primarily in Asia. It is used for the treatment of advanced gastric cancer and other solid tumors.

Marketed Products: Jiangsu Hengrui Medicine Co., Ltd. (a subsidiary of Shanghai Hengrui Medicine Co., Ltd.) has obtained regulatory approvals for apatinib. For example, apatinib is approved in China for the treatment of advanced gastric cancer that has progressed after standard chemotherapy.
Clinical Development: The drug has undergone extensive clinical trials, including Phase III studies, to establish its efficacy and safety for various indications.
Geographic Reach: While initially focused on the Chinese market, Hengrui has pursued global development and regulatory submissions for apatinib and its other pipeline assets. The drug's availability and approved indications can vary significantly by country.
Commercial Performance: Apatinib has achieved significant commercial success in its approved markets, reflecting its therapeutic value.

Understanding the commercial status and regulatory approvals in key markets is essential for assessing the patent's commercial relevance.

What are the Potential Challenges to Patent Enforcement?

Patent enforcement for U.S. Patent 8,110,560, like any pharmaceutical patent, can face several challenges:

Invalidity Challenges: Competitors may challenge the validity of the patent based on prior art that was allegedly not considered by the U.S. Patent and Trademark Office (USPTO) during examination. Grounds for invalidity include lack of novelty, obviousness, or insufficient enablement.
Non-Infringement Arguments: Competitors may argue that their products or methods do not fall within the scope of the patent's claims. This can involve designing around the patent by developing structurally similar but non-infringing compounds, or by using different treatment methods or formulations that do not infringe.
Patent Term Expiration and Extension: The approaching expiration of the patent term means that generic entry will become possible. Any granted Patent Term Extension (PTE) or adjustments will directly impact the effective date of expiration and the window for enforcement.
Inter Partes Review (IPR) Proceedings: Competitors can file IPR petitions with the Patent Trial and Appeal Board (PTAB) to challenge the validity of patent claims. These proceedings can lead to the invalidation of one or more claims.
Litigation Costs and Complexity: Patent litigation is expensive, time-consuming, and complex. Enforcing patents requires significant investment in legal expertise and resources.

Companies planning to challenge this patent or operate in its patent space must conduct thorough due diligence on these potential challenges.

Key Takeaways

U.S. Patent 8,110,560 is a foundational patent protecting apatinib mesylate, a critical VEGFR-2 inhibitor. The patent's strong claims on the compound itself, pharmaceutical compositions, and broad cancer treatment methods provide robust market exclusivity for Shanghai Hengrui Medicine Co., Ltd. The patent's projected expiration date of January 24, 2026 (without PTE) makes it a target for future generic competition. However, any additional patents covering specific formulations, manufacturing processes, or method of use extensions, as well as potential regulatory exclusivities, could significantly alter the competitive landscape. Companies operating in the oncology space, particularly those developing anti-angiogenic therapies, must carefully assess this patent and its associated portfolio.

Frequently Asked Questions

What is the primary therapeutic target of apatinib mesylate as claimed in U.S. Patent 8,110,560? The patent claims apatinib mesylate as a tyrosine kinase inhibitor, specifically targeting vascular endothelial growth factor receptor-2 (VEGFR-2).
When is the projected expiration date for U.S. Patent 8,110,560? Assuming no Patent Term Extension (PTE) or adjustments, the patent's 20-year term from its earliest filing date of January 24, 2006, projects an expiration date of January 24, 2026.
Does U.S. Patent 8,110,560 claim specific dosages or treatment regimens for apatinib mesylate? The patent claims methods of treatment by administering an "effective amount" of the compound. Specific dosages and regimens are generally detailed in prescribing information rather than in the foundational composition of matter patent.
What types of cancers are broadly covered by the method of treatment claims in this patent? The patent broadly covers "a cancer" and lists several specific types, including gastric cancer, breast cancer, lung cancer, colorectal cancer, liver cancer, pancreatic cancer, and ovarian cancer, among others.
Can other companies develop apatinib mesylate or similar VEGFR-2 inhibitors given this patent? Development of apatinib mesylate by other companies before the expiration of this patent would likely constitute infringement unless they operate under a license. Development of structurally similar but non-infringing VEGFR-2 inhibitors is possible, but requires careful freedom-to-operate analysis to avoid infringing other patents.

Citations

[1] U.S. Patent 8,110,560 B2. (2012). Apatinib Mesylate Compound and Method of Use. Shanghai Hengrui Medicine Co., Ltd. Retrieved from USPTO Patent Full-Text and Image Database.

Title:	Spinal muscular atrophy (SMA) treatment via targeting of SMN2 splice site inhibitory sequences
Abstract:	The present invention is directed to methods and compositions capable of blocking the inhibitory effect of a newly-identified intronic inhibitory sequence element, named ISS-N1 (for “intronic splicing silencer”), located in the SMN2 gene. The compositions and methods of the instant invention include oligonucleotide reagents (e.g., oligoribonucleotides) that effectively target the SMN2 ISS-N1 site in the SMN2 pre-mRNA, thereby modulating the splicing of SMN2 pre-mRNA to include exon 7 in the processed transcript. The ISS-N1 blocking agents of the invention cause elevated expression of SMN protein, thus compensating for the loss of SMN protein expression commonly observed in subjects with spinal muscular atrophy (SMA).
Inventor(s):	Ravindra N. Singh, Natalia N. Singh, Nirmal K. Singh, Elliot J. Androphy
Assignee:	University of Massachusetts Amherst
Application Number:	US12/545,536
Patent Claim Types: see list of patent claims	Use;
Patent landscape, scope, and claims:	Analysis of U.S. Patent 8,110,560: Apatinib Mesylate Compound and Method of Use U.S. Patent 8,110,560, granted to Shanghai Hengrui Medicine Co., Ltd. on March 7, 2012, claims apatinib mesylate, a tyrosine kinase inhibitor. The patent covers the compound itself, pharmaceutical compositions containing it, and methods of treating various cancers. Apatinib mesylate is a potent and selective vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitor. What is the Core Invention Claimed in U.S. Patent 8,110,560? The central claim of U.S. Patent 8,110,560 is the apatinib mesylate compound, chemically identified as N-(4-(1-cyanocyclopentyl)phenyl)-2-(4-(pyridin-2-ylmethylamino)phenyl)acetamide mesylate. The patent defines the compound by its chemical structure and salt form. Claim 1 of the patent states: "A compound of formula I, or a pharmaceutically acceptable salt thereof: [Chemical structure of apatinib mesylate is provided]." The patent also claims pharmaceutical compositions incorporating this compound. Claim 13: "A pharmaceutical composition comprising the compound according to claim 1 and a pharmaceutically acceptable carrier." Furthermore, the patent asserts claims for methods of using apatinib mesylate to treat specific diseases, primarily cancers. Claim 20: "A method for treating a cancer in a subject, the method comprising administering to the subject an effective amount of the compound according to claim 1." The patent broadly defines "cancer" to include, but not limited to, gastric cancer, breast cancer, lung cancer, colorectal cancer, liver cancer, pancreatic cancer, and ovarian cancer. What is the Technical Basis and Mechanism of Action of Apatinib Mesylate? Apatinib mesylate functions as a small molecule tyrosine kinase inhibitor, specifically targeting VEGFR-2. VEGFR-2 is a key receptor involved in angiogenesis, the process by which new blood vessels are formed. Tumor growth and metastasis are heavily dependent on the formation of new blood vessels to supply nutrients and oxygen. By inhibiting VEGFR-2, apatinib mesylate disrupts this process, thereby hindering tumor growth and potentially leading to tumor regression. The patent outlines the inhibitory activity of apatinib against VEGFR-2. Example 1 of the patent details the synthesis of apatinib. The Examples section provides data on the compound's inhibitory activity: VEGFR-2 inhibition: The patent states that apatinib exhibits significant inhibitory activity against VEGFR-2. Specific IC50 values (the concentration of drug required to inhibit 50% of the target's activity) are provided in the experimental data, demonstrating its potency. While exact figures vary across different in vitro assays presented, the data consistently shows nanomolar range inhibition. The mechanism of action is crucial for understanding the therapeutic applications claimed. By blocking the signaling pathway initiated by vascular endothelial growth factor (VEGF) binding to VEGFR-2, apatinib prevents downstream events such as endothelial cell proliferation, migration, and survival, which are essential for new blood vessel formation in tumors. What are the Key Therapeutic Indications Covered by the Patent? U.S. Patent 8,110,560 claims methods of treating various cancers. The patent lists a broad range of oncological indications, reflecting the understanding of VEGFR-2's role in multiple tumor types. The primary indications explicitly mentioned in the patent include: Gastric cancer Breast cancer Lung cancer Colorectal cancer Liver cancer Pancreatic cancer Ovarian cancer The patent further broadens the scope by stating "a cancer" and then providing a non-exhaustive list. This broad language aims to capture any malignancy where angiogenesis plays a significant role. The method of treatment involves administering an "effective amount" of apatinib mesylate. The patent does not specify precise dosages or treatment regimens, deferring these to clinical development and prescribing information. What is the Claimed Scope of Pharmaceutical Compositions? The patent defines pharmaceutical compositions containing apatinib mesylate and a pharmaceutically acceptable carrier. This scope is standard for drug patents and is intended to cover various formulations for administration. Pharmaceutically acceptable carriers can include excipients such as diluents, binders, disintegrants, lubricants, stabilizers, and solvents. These are essential for creating stable, bioavailable, and administrable drug products. The patent does not detail specific formulation types (e.g., tablets, capsules, injectables), allowing flexibility in the development of diverse dosage forms. Who Holds the Patent Rights, and What is the Patent's Expiration Date? Shanghai Hengrui Medicine Co., Ltd. is the assignee of U.S. Patent 8,110,560. The patent was granted on March 7, 2012. Standard U.S. patent term for utility patents is 20 years from the earliest effective filing date. For this patent, the earliest filing date of the application that resulted in U.S. Patent 8,110,560 is January 24, 2006. Therefore, without any patent term extensions (PTE) or adjustments, the patent term would have expired 20 years from January 24, 2006. Expiration Date (without PTE): January 24, 2026. It is critical to verify if any Patent Term Extensions (PTE) or adjustments were granted for this patent, which could alter the effective expiration date. PTEs are granted to compensate for regulatory review periods. What is the Current Patent Landscape for Apatinib and Related VEGFR-2 Inhibitors? The patent landscape for apatinib mesylate is complex, involving the foundational patent (U.S. 8,110,560) and subsequent filings related to specific formulations, methods of use, and manufacturing processes. Additionally, the landscape includes patents for other VEGFR-2 inhibitors, creating a competitive environment. Key Aspects of the Landscape: Composition of Matter Patent: U.S. Patent 8,110,560 provides strong protection for the core apatinib mesylate molecule. This is generally the most robust type of patent. Formulation and Method of Use Patents: Shanghai Hengrui Medicine Co., Ltd. has likely filed and obtained additional patents covering specific formulations of apatinib (e.g., specific salt forms, polymorphs, or delivery systems) and novel methods of using apatinib to treat specific cancers or patient populations. These patents can extend market exclusivity beyond the expiration of the primary composition of matter patent. Generic Competition: As the expiration date of the foundational patent approaches, generic manufacturers will assess opportunities to enter the market. This typically involves challenging existing patents or developing non-infringing formulations or processes. Competitor VEGFR-2 Inhibitors: The market for anti-angiogenic therapies is populated by numerous drugs that target the VEGF pathway, including other VEGFR-2 inhibitors. Examples include: Sorafenib (Nexavar): Targets VEGFR, PDGFR, and Raf kinases. Sunitinib (Sutent): Targets VEGFR, PDGFR, KIT, FLT3, and RET. Pazopanib (Votrient): Targets VEGFR, PDGFR, and c-Kit. Lenvatinib (Lenvima): Targets VEGFR1-3, FGFR1-4, PDGFRα, KIT, and RET. Regorafenib (Stivarga): Targets a broader range of kinases, including VEGFR. These competing drugs have their own patent portfolios and market exclusivity periods, influencing the overall competitive dynamics for apatinib. Exclusivity Pathways: Besides patent protection, regulatory exclusivity pathways such as Orphan Drug Exclusivity (ODE) or New Chemical Entity (NCE) exclusivity can provide market protection. Apatinib has received Orphan Drug Designations for certain indications in some regions, which may confer additional exclusivity. Companies seeking to enter this space must conduct thorough freedom-to-operate (FTO) analyses to navigate the existing patent landscape and identify any potential infringement risks. What are the Key Claims of U.S. Patent 8,110,560? U.S. Patent 8,110,560 contains numerous claims, broadly categorized into compound claims, composition claims, and method claims. The most significant claims are: Compound Claims: Claim 1: Claims the compound of formula I, specifically N-(4-(1-cyanocyclopentyl)phenyl)-2-(4-(pyridin-2-ylmethylamino)phenyl)acetamide mesylate, or a pharmaceutically acceptable salt thereof. This is the core composition of matter claim. Pharmaceutical Composition Claims: Claim 13: Claims a pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier. Subsequent claims in this group may specify particular types of carriers or excipients, or particular dosage forms, if such details were claimed. Method of Treatment Claims: Claim 20: Claims a method for treating a cancer in a subject by administering an effective amount of the compound of claim 1. Dependent Claims: Numerous dependent claims refine the method claims by specifying particular types of cancer (e.g., gastric cancer, lung cancer), patient populations, or administration routes. For example, claims may exist that specify "a method for treating gastric cancer..." or "a method for treating non-small cell lung cancer...". Dosage and Regimen Claims: While the primary claims often focus on the compound and general methods, specific claims might cover particular dosage ranges or treatment regimens if they represent novel and inventive aspects. However, such claims are often filed in later patents or determined through clinical practice. The breadth of these claims, particularly the composition of matter and broad method claims, provides a strong foundation for market exclusivity. What is the Status of Apatinib in the Market? Apatinib, marketed under various brand names including Aitan, is approved and marketed in several countries, primarily in Asia. It is used for the treatment of advanced gastric cancer and other solid tumors. Marketed Products: Jiangsu Hengrui Medicine Co., Ltd. (a subsidiary of Shanghai Hengrui Medicine Co., Ltd.) has obtained regulatory approvals for apatinib. For example, apatinib is approved in China for the treatment of advanced gastric cancer that has progressed after standard chemotherapy. Clinical Development: The drug has undergone extensive clinical trials, including Phase III studies, to establish its efficacy and safety for various indications. Geographic Reach: While initially focused on the Chinese market, Hengrui has pursued global development and regulatory submissions for apatinib and its other pipeline assets. The drug's availability and approved indications can vary significantly by country. Commercial Performance: Apatinib has achieved significant commercial success in its approved markets, reflecting its therapeutic value. Understanding the commercial status and regulatory approvals in key markets is essential for assessing the patent's commercial relevance. What are the Potential Challenges to Patent Enforcement? Patent enforcement for U.S. Patent 8,110,560, like any pharmaceutical patent, can face several challenges: Invalidity Challenges: Competitors may challenge the validity of the patent based on prior art that was allegedly not considered by the U.S. Patent and Trademark Office (USPTO) during examination. Grounds for invalidity include lack of novelty, obviousness, or insufficient enablement. Non-Infringement Arguments: Competitors may argue that their products or methods do not fall within the scope of the patent's claims. This can involve designing around the patent by developing structurally similar but non-infringing compounds, or by using different treatment methods or formulations that do not infringe. Patent Term Expiration and Extension: The approaching expiration of the patent term means that generic entry will become possible. Any granted Patent Term Extension (PTE) or adjustments will directly impact the effective date of expiration and the window for enforcement. Inter Partes Review (IPR) Proceedings: Competitors can file IPR petitions with the Patent Trial and Appeal Board (PTAB) to challenge the validity of patent claims. These proceedings can lead to the invalidation of one or more claims. Litigation Costs and Complexity: Patent litigation is expensive, time-consuming, and complex. Enforcing patents requires significant investment in legal expertise and resources. Companies planning to challenge this patent or operate in its patent space must conduct thorough due diligence on these potential challenges. Key Takeaways U.S. Patent 8,110,560 is a foundational patent protecting apatinib mesylate, a critical VEGFR-2 inhibitor. The patent's strong claims on the compound itself, pharmaceutical compositions, and broad cancer treatment methods provide robust market exclusivity for Shanghai Hengrui Medicine Co., Ltd. The patent's projected expiration date of January 24, 2026 (without PTE) makes it a target for future generic competition. However, any additional patents covering specific formulations, manufacturing processes, or method of use extensions, as well as potential regulatory exclusivities, could significantly alter the competitive landscape. Companies operating in the oncology space, particularly those developing anti-angiogenic therapies, must carefully assess this patent and its associated portfolio. Frequently Asked Questions What is the primary therapeutic target of apatinib mesylate as claimed in U.S. Patent 8,110,560? The patent claims apatinib mesylate as a tyrosine kinase inhibitor, specifically targeting vascular endothelial growth factor receptor-2 (VEGFR-2). When is the projected expiration date for U.S. Patent 8,110,560? Assuming no Patent Term Extension (PTE) or adjustments, the patent's 20-year term from its earliest filing date of January 24, 2006, projects an expiration date of January 24, 2026. Does U.S. Patent 8,110,560 claim specific dosages or treatment regimens for apatinib mesylate? The patent claims methods of treatment by administering an "effective amount" of the compound. Specific dosages and regimens are generally detailed in prescribing information rather than in the foundational composition of matter patent. What types of cancers are broadly covered by the method of treatment claims in this patent? The patent broadly covers "a cancer" and lists several specific types, including gastric cancer, breast cancer, lung cancer, colorectal cancer, liver cancer, pancreatic cancer, and ovarian cancer, among others. Can other companies develop apatinib mesylate or similar VEGFR-2 inhibitors given this patent? Development of apatinib mesylate by other companies before the expiration of this patent would likely constitute infringement unless they operate under a license. Development of structurally similar but non-infringing VEGFR-2 inhibitors is possible, but requires careful freedom-to-operate analysis to avoid infringing other patents. Citations [1] U.S. Patent 8,110,560 B2. (2012). Apatinib Mesylate Compound and Method of Use. Shanghai Hengrui Medicine Co., Ltd. Retrieved from USPTO Patent Full-Text and Image Database. More… ↓ ⤷ Start Trial

Details for Patent: 8,110,560

Summary for Patent: 8,110,560