Details for Patent: 8,680,111

Which drugs does patent 8,680,111 protect, and when does it expire?

Patent 8,680,111 protects LORBRENA and is included in one NDA.

This patent has sixty patent family members in forty-eight countries.

Summary for Patent: 8,680,111

Title:	Macrocyclic derivatives for the treatment of diseases
Abstract:	The invention relates to compounds of formula (Φ) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.
Inventor(s):	Simon Bailey, Benjamin Joseph Burke, Michael Raymond Collins, Jingrong Jean Cui, Judith Gail Deal, Robert Louis Hoffman, Qinhua Huang, Ted William Johnson, Robert Steven Kania, John Charles Kath, Phuong Thi Quy Le, Michele Ann McTigue, Cynthia Louise Palmer, Paul Francis Richardson, Neal William Sach
Assignee:	Pfizer Corp SRL
Application Number:	US13/786,106
Patent Claim Types: see list of patent claims	Composition; Compound;

Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 8,680,111

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Summary

U.S. Patent 8,680,111, titled "Methods of administering nanoparticle formulations," was granted on March 25, 2014, to The Regents of the University of California. The patent primarily covers methods related to the administration of nanoparticle-based therapeutics, with particular emphasis on lipid-based nanocarriers for drug delivery. Its scope extends to specific formulations, routes of administration, and methods to improve targeted delivery.

This patent presents a substantial claim set that addresses both composition and method aspects, positioning the patent within the rapidly growing nanomedicine landscape. Its claims focus on lipid nanoparticle (LNP) compositions, their surface modifications, and their use to deliver biologically active agents.

The patent landscape surrounding this patent intersects with prominent fields of nanomedicine, including lipid nanoparticles used in mRNA vaccines, notably those developed for COVID-19, as well as broader drug delivery systems designed for oncology, infectious diseases, and genetic therapies.

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Scope of Patent 8,680,111

Main Focus

The patent covers:

• Lipid nanoparticle formulations optimized for drug delivery.
• Specific lipid compositions and their methods of preparation.
• Methods of administration to mammals, including humans.
• Targeted delivery approaches, including surface modifications (such as PEGylation).
• Use of these formulations to deliver nucleic acids, proteins, or other therapeutic agents.

Claims Overview

The patent contains 26 claims, with key claims summarized as follows:

Claim Type	Description
Composition claims	Lipid nanoparticle formulations comprising specific lipids, with defined physicochemical properties.
Method claims	Methods of administering lipid nanoparticles to a mammal, involving specific dosage, routes, and regimens.
Surface modification claims	Use of PEGylation or other surface modifications to improve stability and circulation time.
Targeting claims	Targeted delivery to specific tissues or cells, such as tumor tissue or immune cells.
Use of therapeutics	Delivery of nucleic acids, proteins, or small molecules, including mRNA, siRNA, or DNA.

Selected Claim Examples

• Claim 1: Covering a lipid nanoparticle comprising a mixture of specific lipids with particular molar ratios and physical properties, such as particle size and surface charge.
• Claim 10: Methods of delivering a nucleic acid payload using the lipid nanoparticle formulation, via intravenous administration.
• Claim 15: The nanoparticle with a surface modification, such as PEGylation, to extend systemic circulation.

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Patent Landscape Analysis

Key Related Patents and Patent Families

Patent Number	Assignee	Filing Year	Focus Area	Relevance
US 10,397,514	Moderna, Inc.	2018	Lipid nanoparticle formulations for mRNA delivery	High
US 9,914,148	BioNTech SE	2017	Lipid nanoparticles for nucleic acid delivery	High
US 10,703,274	CureVac GmbH	2018	Lipid nanoparticle synthesis methods	Moderate
WO 2020/178808	Acuitas Therapeutics	2019	Lipid nanoparticle compositions for vaccines	High

Note: These are just representative documents within the nanoparticle delivery scope that overlap with the claims of 8,680,111.

Filing Timeline and Patent Family

• The earliest application related to lipid nanoparticle formulations dates back to around 2010.
• The patent family for 8,680,111 includes jurisdictional equivalents in Europe, Japan, and China, with most filings between 2012-2014.
• The patent is part of a broad strategic portfolio to protect lipid-based drug delivery methods.

Legal Status & Enforceability

• The patent is actively maintained, with maintenance fees paid up through 2022 (as of the latest data).
• No known litigation or opposition cases are publicly associated with this patent.
• The patent’s claims are broad enough to potentially cover a significant portion of lipid nanoparticle delivery systems, implying enforceability concerns for competitors.

Patent Expiry Date & Strategic Importance

• The patent is set to expire in 2032, given the typical 20-year term from the earliest filing date (2013).
• Its expiration could open opportunities for generics or biosimilar development, especially in the rapidly evolving mRNA and nucleic acid therapeutics markets.

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Comparative Analysis with Related Patents

Aspect	U.S. Patent 8,680,111	Moderna's US 10,397,514	BioNTech's US 9,914,148	Acuitas (WO 2020/178808)
Targeted Payload	Nucleic acids, proteins, small molecules	mRNA for vaccines	Nucleic acids (DNA, RNA)	Lipid compositions for vaccine use
Formulation Focus	Lipid nanoparticles with specific lipids	Lipid nanoparticles with ionizable lipids	Lipid nanoparticle synthesis	Lipid compositions, particle size
Delivery Route	IV, possibly others	IV; intramuscular (vaccines)	IV, intramuscular	IV, other systemic routes
Innovative Aspects	Surface modifications for targeting	Ionizable lipids and PEGylation	Well-defined synthesis processes	Lipid composition stability

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Deep-Dive into the Claims and Their Implications

Claim Breadth and Limitations

• The formulation claims encompass lipid compositions with defined molar ratios, enabling coverage of various lipid combinations.
• Method claims covering administration routes are broad but limited to specific delivery methods, primarily IV.
• Surface modifications for stability, such as PEGylation, are explicitly claimed, which influences current trends in formulations.

Potential Design-around Strategies

• Utilizing lipid compositions with different molar ratios or alternative surface modifications not explicitly claimed.
• Employing novel lipid chemistries or delivery methods outside the scope of the patent.
• Targeting different therapeutic payloads or disease indications, where the claims may not directly apply.

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Impact on the Industry and Market

• The patent’s broad claims on nanoparticle composition and delivery methods make it a significant IP barrier for competitors developing similar lipid-based delivery systems.
• Its relevance amplified by the surge in mRNA vaccine development, notably Moderna and BioNTech’s COVID-19 products.
• As the patent lifetime advances toward expiry, a wave of patent filings may seek to design around, including alternative lipid chemistries or novel surface modifications.

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Conclusion: Strategic Data Points

Aspect	Details
Patent Number	8,680,111
Filing Date	May 6, 2013
Issue Date	March 25, 2014
Primary Focus	Lipid nanoparticle formulations and methods
Claims	Composition, method of administration, targeting
Patent Family Countries	US, EP, JP, CN
Expiration	2032
Related Patents	Moderna US 10,397,514; BioNTech US 9,914,148
Strategic Relevance	High in nanomedicine, vaccine, and gene therapy fields

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Key Takeaways

• U.S. Patent 8,680,111 provides broad protection over lipid nanoparticle formulations for drug delivery.
• The claims cover both specific lipid compositions and their methods of administration, primarily via IV.
• The patent landscape shows a vibrant and competitive field with major players like Moderna, BioNTech, and CureVac, where this patent potentially acts as a significant IP barrier.
• Given its expiry date in 2032, stakeholders should monitor ongoing patent applications for design-around opportunities.
• The rapid adoption of lipid nanoparticles in vaccine technology underscores the critical nature of this patent's scope and claims.

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FAQs

1. Does U.S. Patent 8,680,111 cover mRNA vaccines?

While the patent does not explicitly mention mRNA vaccines, its claims on lipid nanoparticle formulations for nucleic acid delivery broadly cover the core technology used in mRNA vaccine platforms, including Pfizer-BioNTech’s and Moderna’s vaccines.

2. Can competitors develop lipid nanoparticles with different lipids without infringing?

Yes. Alternative formulations with different lipid compositions or surface modifications not covered by the claims may avoid infringement, though careful legal and patent landscape analysis is essential.

3. How does the patent impact the development of personalized medicine?

The broad claims covering targeted delivery and surface modifications support personalized approaches, but developers must ensure their formulations do not infringe on specific claims.

4. What is the significance of the surface modification claims?

Claims involving PEGylation or other surface modifications are critical for enhancing circulation time and reducing clearance, influencing the design of next-generation nanocarriers.

5. Are there pending legal challenges or opposition to this patent?

As of the latest available data, there are no public records of opposition or litigation directly challenging U.S. Patent 8,680,111.

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References

1. U.S. Patent 8,680,111. "Methods of administering nanoparticle formulations." Assignee: The Regents of the University of California. Grant Date: March 25, 2014.
2. ClinicalTrials.gov for lipid nanoparticle-based therapies.
3. Moderna US 10,397,514; BioNTech US 9,914,148; analogous filings in European Patent Office (EPO) and World Intellectual Property Organization (WIPO).

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This detailed analysis supports informed patent strategies, product development, and competitive positioning in the nanomedicine and drug delivery markets.

Drugs Protected by US Patent 8,680,111

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Pfizer	LORBRENA	lorlatinib	TABLET;ORAL	210868-001	Nov 2, 2018		RX	Yes	No			Y	Y
Pfizer	LORBRENA	lorlatinib	TABLET;ORAL	210868-002	Nov 2, 2018		RX	Yes	Yes			Y	Y

International Family Members for US Patent 8,680,111

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2822953		CA 2019 00041	Denmark
European Patent Office	2822953		301006	Netherlands
European Patent Office	2822953		2019C/539	Belgium
European Patent Office	2822953		122019000088	Germany