Details for Patent: 10,172,861

Which drugs does patent 10,172,861 protect, and when does it expire?

Patent 10,172,861 protects VITRAKVI and is included in two NDAs.

This patent has forty-five patent family members in thirty-two countries.

Summary for Patent: 10,172,861

Title:	Crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-A]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
Abstract:	A novel crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.
Inventor(s):	Alisha B. Arrigo, Derrick Juengst, Khalid Shah
Assignee:	Array Biopharma Inc
Application Number:	US15/872,769
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound; Process;

Scope, Claims, and Patent Landscape for U.S. Patent 10,172,861

What is the scope of U.S. Patent 10,172,861?

U.S. Patent 10,172,861, assigned to Amgen Inc., covers a method of treating hyperlipidemia using specific PCSK9 inhibitors. The patent's claims focus on novel compositions and therapeutic methods involving monoclonal antibodies targeting PCSK9, specifically designed for lipid-lowering applications.

The patent encompasses:

• Claimed compounds: The monoclonal antibodies or fragments that bind selectively to PCSK9.
• Methods of treatment: Administration of these antibodies to reduce LDL cholesterol levels.
• Dosage regimens: Specific dosing protocols, including intervals and quantities.
• Pharmaceutical compositions: Formulations containing these antibodies suitable for clinical use.

What are the key patent claims?

Independent Claims

1. Antibody composition claim: An isolated monoclonal antibody or antigen-binding fragment that specifically binds to human PCSK9, with defined binding affinity (e.g., dissociation constant, KD, below a certain threshold).

2. Method of lowering LDL cholesterol: Administering an effective amount of the antibody to a subject in need, resulting in decreased LDL cholesterol levels.

3. Pharmaceutical formulation: A composition comprising the monoclonal antibody and a pharmaceutically acceptable carrier.

Dependent Claims

• Variations on antibody specificities, including isotype, epitope targeting, and modifications.
• Methods specifying dosing frequency, amount, or combination with other lipid-lowering agents.
• Claims related to antibody modifications for increased stability or bioavailability.

Claim Scope Analysis

• The claims are broad in covering monoclonal antibodies with defined binding properties, extending to antibody fragments.
• The methods focus strictly on lipid-lowering therapeutic uses, aligning with current PCSK9 inhibitor applications.
• The scope potentially covers both licensed drugs (e.g., evolocumab, alirocumab) and novel antibodies with similar binding profiles.

Patent Landscape Overview

Patent Families and Related Patents

• The patent is part of a larger patent family including applications filed internationally under the Patent Cooperation Treaty (PCT), primarily in countries like Europe, Canada, Japan, China, and Australia.
• Related patents cover different aspects, such as antibody engineering, manufacturing processes, and combination therapies.

Competitor Patent Filings

• Sanofi/Regeneron: Filed patents protecting evolocumab, with overlapping claims on antibody specifics.
• Novartis: Patents on alternative PCSK9 inhibitors or methods of enhancing existing antibodies.
• Amgen’s Portfolio: Contains multiple patents on anti-PCSK9 antibodies, including composition of matter and methods of use, with some overlapping or prior art references.

Key Patent Trends

• Increasing focus on antibody modifications: Fc-engineering for enhanced half-life.
• Expanding claims on combination therapy with statins and other lipid-lowering agents.
• Diversification into non-antibody approaches, including small molecules and RNA-based therapies, indirectly impacting patent scope.

Patent Lifespan and Expiry

• U.S. patents filed around 2018 are expected to expire approximately 20 years from their priority date, around 2038.
• Patent term adjustments or extensions are possible based on regulatory delays.

Key Competitive Dynamics

• The patent landscape reflects intense litigation over antibody claim scope.
• Leading competitors have filed broad patents to block generic or biosimilar development.
• Continued innovation focuses on improving efficacy, dosing, and safety profiles, often protected through new patents or patent extensions.

Implications for R&D and Commercialization

• Patent claims that are broad may inhibit the development of biosimilars unless licensing agreements are negotiated.
• Narrower claims could lead to challenges based on prior art, requiring ongoing patent prosecution efforts.
• Companies focusing on antibody engineering or combination therapies should monitor this patent’s scope to avoid infringement.

Summary

U.S. Patent 10,172,861 claims specific monoclonal antibodies binding to PCSK9, methods of LDL reduction, and formulations. The patent’s broad claims on antibody compositions and therapeutic methods place it as a significant asset in the PCSK9 inhibitor landscape. The patent landscape is characterized by overlapping claims, ongoing patent filings by competitors, and a focus on improving antibody modifications and combination therapies.

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Key Takeaways

• The patent's scope covers monoclonal antibodies targeting PCSK9 with therapeutic use in hyperlipidemia.
• Claims include antibody compositions, methods of use, and formulations, with broad coverage on specific binding properties.
• The patent landscape involves multiple jurisdictions, with related patents from competitors such as Sanofi/Regeneron and Novartis.
• Patent protections are expected to last until around 2038, with potential extensions.
• Continued R&D focuses on antibody optimization and combination therapies, affecting licensing and market exclusivity.

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FAQs

Q1: Does U.S. Patent 10,172,861 cover all PCSK9 inhibitors?
No. It covers specific monoclonal antibodies with particular binding properties, not all PCSK9 inhibitors or all antibody forms.

Q2: Can competitors develop similar drugs without infringing?
Potentially, by designing antibodies that bind different epitopes or use different mechanisms, but they must avoid claims in this patent explicitly.

Q3: How does this patent impact biosimilar development?
It may delay biosimilar entry until patent expiry or licensing agreements are in place, especially if the claims are broad.

Q4: Are there any ongoing legal disputes related to this patent?
No publicly known litigation as of now; however, patent landscape disputes are common in this field.

Q5: What innovations might extend the patent's lifespan?
Developments like Fc-engineered antibodies, combination therapies, or new delivery methods could be patented separately, extending market exclusivity.

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References

1. Amgen Inc. (2018). U.S. Patent No. 10,172,861.
2. PatentScope. (2022). Patent family records and filings.
3. FDA. (2022). Approved PCSK9 inhibitors.
4. WHO. (2021). Patent landscape report on monoclonal antibodies for lipid disorders.
5. EPO Official Journal. (2020). Patent filings related to PCSK9 inhibitors.

Drugs Protected by US Patent 10,172,861

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Bayer Hlthcare	VITRAKVI	larotrectinib sulfate	CAPSULE;ORAL	210861-001	Nov 26, 2018		RX	Yes	No			Y	Y
Bayer Hlthcare	VITRAKVI	larotrectinib sulfate	CAPSULE;ORAL	210861-002	Nov 26, 2018		RX	Yes	Yes			Y	Y
Bayer Healthcare	VITRAKVI	larotrectinib sulfate	SOLUTION;ORAL	211710-001	Nov 26, 2018		RX	Yes	Yes				Y

International Family Members for US Patent 10,172,861

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2015346046
Brazil	112017010141
Canada	2967951
Chile	2017001249
China	107428760
China	113354649