Details for Patent: 10,689,377

Which drugs does patent 10,689,377 protect, and when does it expire?

Patent 10,689,377 protects KRAZATI and is included in one NDA.

This patent has forty-one patent family members in thirty-one countries.

Summary for Patent: 10,689,377

Title:	KRas G12C inhibitors
Abstract:	The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
Inventor(s):	Blake James F., Burgess Laurence E., Chicarelli Mark Joseph, Christensen James Gail, Cook Adam, Fell Jay Bradford, Fischer John P., Marx Matthew Arnold, Mejia Macedonio J., Savechenkov Pavel, Vigers Guy P. A., Smith Christopher Ronald, Rodriguez Martha E.
Assignee:
Application Number:	US16191190
Patent Claim Types: see list of patent claims

Understanding the Scope and Claims of United States Patent 10,689,377: KRas G12C Inhibitors

Introduction

The United States Patent 10,689,377, issued on June 23, 2020, is a significant development in the field of oncology, particularly in the treatment of cancers driven by the KRas G12C mutation. This patent, held by Bristol Myers Squibb Co., covers compounds that irreversibly inhibit the activity of KRas G12C, along with pharmaceutical compositions and methods of use.

Patent Overview

Inventors and Assignees

The patent was invented by a team of researchers including Blake James F., Burgess Laurence E., Chicarelli Mark Joseph, Christensen James Gail, Cook Adam, Fell Jay Bradford, Fischer John P., Marx Matthew Arnold, Mejia Macedonio J., Savechenkov Pavel, Vigers Guy P. A., Smith Christopher Ronald, and Rodriguez Martha E. The assignees are Bristol Myers Squibb Co.[5].

Scope of the Patent

KRas G12C Mutation

The KRas G12C mutation is a specific point mutation in the KRAS gene, which is one of the most commonly mutated oncogenes in human cancer. This mutation is particularly prevalent in non-small cell lung cancer (NSCLC), colorectal cancer, and pancreatic cancer. The patent focuses on compounds that target and irreversibly inhibit this mutation, offering a new therapeutic approach for these cancers[1][4].

Compounds and Pharmaceutical Compositions

The patent describes a series of compounds designed to bind specifically to the KRas G12C protein, inhibiting its activity. These compounds are detailed in the patent claims, which include various chemical structures and modifications that enhance their efficacy and specificity. The pharmaceutical compositions covered by the patent include formulations suitable for administration, such as oral, intravenous, or other routes[1][5].

Claims of the Patent

Independent Claims

The patent includes multiple independent claims that define the scope of the invention. These claims are crucial as they outline the specific compounds, their structures, and the methods of use. For instance, the claims describe the chemical moieties that are essential for the inhibitory activity against KRas G12C, as well as the pharmaceutical compositions that contain these compounds[1][5].

Dependent Claims

Dependent claims further specify the independent claims by adding additional limitations or features. These claims help to narrow down the scope and ensure that the patent covers specific embodiments of the invention, such as particular dosages, administration methods, or combinations with other therapeutic agents[1].

Patent Landscape

Exclusivity and Patent Term

The patent is set to expire on May 17, 2037, which is approximately 12 years from the current date. This exclusivity period ensures that Bristol Myers Squibb Co. has the sole right to manufacture and market these compounds until the patent expires. Any changes in the patent term due to legal activities, such as term extensions or amendments, could affect the generic launch date of these drugs[2][5].

Related Patents and Prior Art

The patent landscape for KRas G12C inhibitors is complex, with multiple patents and applications filed by different companies. The patent in question references several prior art documents and other related patents, indicating a highly competitive and innovative field. Other companies, such as Mirati Therapeutics and Array Biopharma, also have patents related to KRas G12C inhibitors, highlighting the ongoing research and development in this area[1][4].

Impact on Cancer Treatment

Therapeutic Significance

The compounds described in this patent represent a significant advancement in the treatment of cancers driven by the KRas G12C mutation. By irreversibly inhibiting this mutation, these compounds offer a targeted therapeutic approach that can potentially improve patient outcomes. Clinical trials and ongoing research are crucial to fully understanding the efficacy and safety of these compounds[1][4].

Market Implications

The exclusivity granted by this patent gives Bristol Myers Squibb Co. a competitive edge in the market for KRas G12C inhibitors. The lack of generic versions until the patent expires in 2037 means that the company will have a monopoly on these specific compounds, influencing market dynamics and pricing strategies[2][5].

Legal and Regulatory Aspects

Patent Scope and Quality

The scope of the patent claims is a critical aspect of patent quality. Research has shown that narrower claims at publication are associated with a higher probability of grant and a shorter examination process. The examination process often narrows the scope of patent claims, ensuring that the granted patents are clear and valid[3].

Recent Legal Activities

Recent legal activities on the patent, such as the payment of maintenance fees and petition decisions, indicate ongoing efforts to maintain and potentially extend the patent's term. These activities are crucial for tracking the latest developments in the patent process and understanding any potential changes to the patent's expiry date[2].

Conclusion

United States Patent 10,689,377 is a pivotal development in the fight against cancers driven by the KRas G12C mutation. The patent's scope and claims are meticulously defined, ensuring that the compounds and pharmaceutical compositions covered are both innovative and legally protected. The exclusivity period and the competitive landscape highlight the significance of this patent in the oncology market.

Key Takeaways

• KRas G12C Mutation: The patent targets a specific mutation in the KRAS gene prevalent in various cancers.
• Compounds and Compositions: The patent describes specific compounds and pharmaceutical compositions designed to inhibit KRas G12C.
• Patent Term: The patent is set to expire on May 17, 2037.
• Market Impact: The exclusivity granted by the patent gives Bristol Myers Squibb Co. a competitive edge in the market.
• Legal and Regulatory: Ongoing legal activities and the examination process ensure the patent's validity and scope.

FAQs

Q: What is the KRas G12C mutation and its significance in cancer?

The KRas G12C mutation is a point mutation in the KRAS gene, commonly found in non-small cell lung cancer, colorectal cancer, and pancreatic cancer. It is a significant target for cancer therapy due to its prevalence and role in cancer progression.

Q: Who are the inventors and assignees of the patent?

The inventors include Blake James F., Burgess Laurence E., and others, with the assignee being Bristol Myers Squibb Co.

Q: What is the scope of the patent claims?

The patent claims cover specific compounds that irreversibly inhibit KRas G12C, pharmaceutical compositions, and methods of use.

Q: When is the patent set to expire?

The patent is set to expire on May 17, 2037.

Q: Are there any generic versions of Krazati available?

No, there are currently no therapeutically equivalent generic versions of Krazati available in the United States[5].

Sources

1. US10689377B2 - KRas G12C inhibitors - Google Patents
2. Krazati patent expiration - Pharsight
3. Patent Claims and Patent Scope - Hoover Institution
4. United States Patent - googleapis.com
5. Generic Krazati Availability - Drugs.com

Recent additions to Drugs Protected by US Patent 10,689,377

These patents are from the daily update and have not yet been integrated into the regular database

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Type	RLD	Patent No.	Product	Substance	Delist Req.	Patent Expiration	Usecode	Patented / Exclusive Use
Bristol	KRAZATI	adagrasib	TABLET	216340	Dec 12, 2022	RX	Yes		Y	Y			U-3490	TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC), AS DETERMINED BY AN FDA APPROVED TEST, WHO HAVE RECEIVED AT LEAST ONE PRIOR SYSTEMIC THERAPY
Bristol	KRAZATI	adagrasib	TABLET	216340	Dec 12, 2022	RX	Yes		Y	Y			U-3953	TREATMENT, IN COMBINATION WITH CETUXIMAB, OF ADULT PATIENTS WITH KRAS G12C-MUTED LOCALLY ADVANCED OR METASTATIC COLORECTAL CANCER, PER FDA APPROVED TEST, WHERE PRIOR TREATMENT WITH FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY

Drugs Protected by US Patent 10,689,377

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Bristol	KRAZATI	adagrasib	TABLET;ORAL	216340-001	Dec 12, 2022		RX	Yes	Yes			Y	Y		TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC), AS DETERMINED BY AN FDA APPROVED TEST, WHO HAVE RECEIVED AT LEAST ONE PRIOR SYSTEMIC THERAPY
Bristol	KRAZATI	adagrasib	TABLET;ORAL	216340-001	Dec 12, 2022		RX	Yes	Yes			Y	Y		TREATMENT, IN COMBINATION WITH CETUXIMAB, OF ADULT PATIENTS WITH KRAS G12C-MUTED LOCALLY ADVANCED OR METASTATIC COLORECTAL CANCER, PER FDA APPROVED TEST, WHERE PRIOR TREATMENT WITH FLUOROPYRIMIDINE-, OXALIPLATIN-, AND IRINOTECAN-BASED CHEMOTHERAPY

International Family Members for US Patent 10,689,377

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	3710439		301279	Netherlands
European Patent Office	3710439		CA 2024 00024	Denmark
European Patent Office	3710439		PA2024517	Lithuania
European Patent Office	3710439		LUC00350	Luxembourg