Understanding the Scope and Claims of United States Patent 10,519,146: KRAS G12C Inhibitors
Introduction to KRAS G12C Inhibitors
United States Patent 10,519,146, issued on December 31, 2019, is a significant development in the field of oncology, particularly in the treatment of cancers driven by the KRAS G12C mutation. This patent, assigned to Amgen Inc., covers KRAS G12C inhibitors, their compositions, and methods of using these inhibitors.
Patent Overview
Inventors and Assignee
The patent was invented by a team of researchers including Lanman Brian Alan, Chen Jian, Reed Anthony B., and several others, all affiliated with Amgen Inc.[2].
Patent Expiration
The patent is set to expire on May 21, 2038, which is approximately 20 years from the date of filing, a standard duration for most patents[2].
Scope of the Patent
KRAS G12C Mutation
The KRAS G12C mutation is a specific point mutation in the KRAS gene that leads to the substitution of cysteine for glycine at position 12. This mutation is prevalent in various types of cancer, including pancreatic, colorectal, and lung cancers. The patent focuses on inhibitors that target this specific mutation[2].
Inhibitors and Compositions
The patent describes a class of small molecule inhibitors designed to covalently bind to the cysteine residue at position 12 of the KRAS protein. These inhibitors are detailed in terms of their chemical structure, synthesis, and pharmaceutical compositions. The compositions include various forms such as anhydrous, hydrate, and solvate forms, which are crucial for the stability and efficacy of the drug[2].
Claims of the Patent
Independent Claims
The patent includes multiple independent claims that define the scope of the invention. These claims cover:
- The chemical structure of the KRAS G12C inhibitors.
- Methods of synthesizing these inhibitors.
- Pharmaceutical compositions containing these inhibitors.
- Methods of treating cancers mediated by the KRAS G12C mutation using these inhibitors[2].
Dependent Claims
Dependent claims further specify the independent claims by detailing specific aspects such as:
- Particular chemical moieties and their substitutions.
- Specific pharmaceutical formulations.
- Dosage regimens and administration methods[2].
Methods of Using the Inhibitors
Therapeutic Applications
The patent outlines the therapeutic applications of the KRAS G12C inhibitors, primarily focusing on the treatment of cancers such as pancreatic, colorectal, and lung cancers. It also mentions potential applications in other cancer types where the KRAS G12C mutation is present[2].
Administration Methods
The methods of administering these inhibitors are also described, including oral, intravenous, and other routes of administration. The patent emphasizes the importance of optimizing the dosage and administration schedule to maximize efficacy and minimize side effects[2].
Patent Landscape
Related Patents
There are several related patents that complement the scope of US 10,519,146. For example:
- Solid State Forms: Patent 11,236,091, issued on February 1, 2022, covers crystalline and amorphous forms of the KRAS G12C inhibitor compound, including various solid state forms and their pharmaceutical compositions[2].
- Methods of Administration: Patent 11,426,404, issued on August 30, 2022, provides methods of administering a KRAS G12C inhibitor to cancer patients, further expanding the therapeutic utility of these inhibitors[2].
Exclusivity and Generic Entry
The patent's expiration date and exclusivity periods are crucial for understanding when generic versions of the drug may enter the market. The patent is set to expire in 2038, but exclusivity periods granted by the FDA could extend the period during which the patent holder has sole marketing rights[2].
Impact on Cancer Treatment
Clinical Significance
The development of KRAS G12C inhibitors represents a significant advancement in targeted cancer therapy. These inhibitors offer a new treatment option for patients with cancers driven by the KRAS G12C mutation, which were previously difficult to treat.
Market and Research Implications
The patent landscape around KRAS G12C inhibitors is dynamic, with ongoing research and development aimed at improving the efficacy and safety of these drugs. This patent and related ones are pivotal in shaping the market for targeted cancer therapies.
"Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers."[2]
Key Metrics and Analysis
Patent Scope and Claims
The scope of the patent is defined by the independent and dependent claims. Metrics such as independent claim length and count can be used to analyze the breadth and clarity of the patent claims. Narrower claims are often associated with a higher probability of grant and a shorter examination process[3].
Forward Citations and Patent Maintenance
The number of forward citations and patent maintenance payments can also indicate the importance and impact of the patent. Patents with more forward citations and higher maintenance payments typically reflect greater innovation and market relevance[3].
Conclusion
United States Patent 10,519,146 is a cornerstone in the development of targeted therapies for cancers driven by the KRAS G12C mutation. The patent's scope, claims, and related patents collectively provide a comprehensive framework for the use of these inhibitors in clinical settings.
Key Takeaways
- KRAS G12C Mutation: The patent targets the KRAS G12C mutation prevalent in various cancers.
- Inhibitors and Compositions: The patent describes small molecule inhibitors and their pharmaceutical compositions.
- Therapeutic Applications: The inhibitors are useful for treating pancreatic, colorectal, and lung cancers.
- Patent Expiration: The patent expires on May 21, 2038.
- Related Patents: Other patents cover solid state forms and methods of administration.
- Clinical Significance: The inhibitors offer a new treatment option for previously difficult-to-treat cancers.
FAQs
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What is the KRAS G12C mutation?
- The KRAS G12C mutation is a point mutation in the KRAS gene where cysteine replaces glycine at position 12, leading to cancer.
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What are KRAS G12C inhibitors?
- KRAS G12C inhibitors are small molecule drugs designed to covalently bind to the cysteine residue at position 12 of the KRAS protein.
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What cancers are treated by KRAS G12C inhibitors?
- These inhibitors are primarily used to treat pancreatic, colorectal, and lung cancers driven by the KRAS G12C mutation.
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Who is the assignee of the patent?
- The patent is assigned to Amgen Inc.
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When does the patent expire?
- The patent expires on May 21, 2038.
Sources
- US10519146B2 - KRAS G12C inhibitors and methods of using the same - Google Patents
- Generic Lumakras Availability - Drugs.com
- Patent Claims and Patent Scope - SSRN
- Heterocyclic inhibitors of kras g12c mutant proteins and uses thereof - Google Patents
- Drugs covered by patent 10,519,146 - Drug Patent Watch
