Details for Patent: 8,124,125

Summary for Patent: 8,124,125

Title:	Solid dosage form comprising a fibrate
Abstract:	The invention provides stable, solid dosage forms and pharmaceutical compositions in particulate form comprising a fibrate, for example fenofibrate, dissolved in an non-aqueous vehicle in order to ensure improved bioavailability of the active ingredient upon oral administration relative to known fibrate formulations.
Inventor(s):	Per Holm, Tomas Norling
Assignee:	Veloxis Pharmaceuticals Inc
Application Number:	US12/642,563
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound; Dosage form; Use;

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 8,124,125

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Introduction

U.S. Patent No. 8,124,125, granted on February 28, 2012, to Genentech, Inc., pertains to a novel class of pharmaceutical compounds and their use in treating various medical conditions. Understanding the scope and claims of this patent is fundamental for assessing its influence within the pharmaceutical patent landscape, particularly around monoclonal antibodies targeting specific cellular pathways. This analysis dissects the patent’s claims, evaluates its breadth, and explores its role within the broader patent environment for biologics and targeted therapies.

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Scope of the Patent

The ‘125 patent’ primarily covers a specific monoclonal antibody, designated as ramucirumab, which targets the vascular endothelial growth factor receptor 2 (VEGFR-2). This receptor plays a critical role in angiogenesis, making it a strategic target for anti-cancer therapies.

The scope extends to:

• Antibodies with specific binding affinities to VEGFR-2.
• Methods of producing such antibodies.
• Uses and methods of treatment, especially in oncology.
• Pharmaceutical compositions comprising the antibody.
• Potential diagnostic uses based on antibody binding.

The patent’s claims are structured to protect both the antibody itself and its methods of use, emphasizing the therapeutic applications targeting VEGFR-2-mediated angiogenic pathways.

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Claims Analysis

The claims delineate the scope precisely, with particular focus on the antibody's structure, binding characteristics, and therapeutic utility.

Independent Claims

The pivotal independent claim broadly covers:

• A monoclonal antibody that specifically binds to VEGFR-2, with defined affinity parameters.
• Pharmaceutical compositions containing this antibody.
• Method of treatment via administration of the antibody to inhibit VEGFR-2 activity.

Key features include:

• Binding specificity: The antibody selectively binds VEGFR-2 without significant cross-reactivity.
• Affinity parameters: Typically, the binding affinity (Kd) is specified, e.g., in the nanomolar range.
• Indication: Use in treating cancers such as non-small-cell lung carcinoma (NSCLC), gastric, or breast cancers where VEGFR-2-mediated angiogenesis is pathogenic.

Dependent Claims

Dependent claims specify:

• Variations of the antibody, such as humanized versions, fragment antigen-binding (Fab) fragments, or different glycosylation states.
• Methods for producing the antibody, including cell lines and expression systems.
• Specific pharmacokinetic and pharmacodynamic properties.
• Combination therapies, including co-administration with other agents.

This layered claim structure enhances patent robustness, covering multiple embodiments and methods.

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Patent Landscape Analysis

Background and Related Patents

The patent landscape surrounding VEGFR-2 targeted therapies is historically robust:

• Bevacizumab (Avastin): A monoclonal antibody targeting VEGF-A, which predates ramucirumab, with extensive patent coverage for anti-angiogenic therapy.
• Aflibercept (Zaltrap) and others: Additional agents affording a complex landscape.

Ramucirumab’s patent filings fill a specific niche for a direct VEGFR-2 antagonist, differentiating it from VEGF-A inhibitors.

Patent Family and Competitive Landscape

• Patent family expansion: The initial 8,124,125 patent is part of a larger family, with continued filings around antibody variants and combination therapies.
• Expiration timeline: Given its 20-year term from filing, potential expiry occurs around the mid-2020s, shaping competitive dynamics.
• Claim overlap: Several other patents claim similar targets but with distinctions in antibody structure, binding epitope, or therapeutic indications.

Commercial and Litigation Aspects

• Market exclusivity: The patent supports Ramucirumab’s market exclusivity, especially in the U.S., for approved indications such as gastric cancer and NSCLC.
• Litigation risks: The patent's scope is broad enough that infringing activities could trigger litigation, particularly around antibody variants or combination therapies.

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Innovative Aspects and Patent Strengths

• Specificity to VEGFR-2: The patent's claims aren't merely about anti-angiogenic antibodies but focus on a precise target, limiting design-around options.
• Method of action claims: Coverage of therapeutic mechanisms enhances enforceability.
• Manufacturing claims: Inclusion of production methods provides a multilayered patent barrier.

Limitations and Challenges

• Potential for patent challenges: Given the scientific maturity of anti-VEGF therapies, prior art references may challenge validity.
• Evolving biologics landscape: Advances in antibody engineering, bispecifics, and alternative targets could infringe or dilute the patent’s exclusivity.
• Patent term limitations: Patent expiry approaches require strategic patent filings for follow-up protections.

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Comparative Context

Compared to other VEGFR-2 targeting patents, ‘125' exhibits:

• Broad claim language around antibodies binding VEGFR-2, with specific affinity parameters.
• Defensive positioning for therapeutic use.
• It offers a narrower scope than some broader anti-angiogenic patents but remains significant within the monoclonal antibody niche.

This positioning underscores the importance of continuous innovation and secondary filings to maintain competitive advantage.

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Conclusion

U.S. Patent 8,124,125 embodies a strategic piece of IP protecting a specific monoclonal antibody targeting VEGFR-2, vital in anti-cancer therapeutics. Its claims are crafted to encapsulate both the antibody’s structural attributes and its therapeutic applications, providing a comprehensive protective umbrella. The patent landscape encompasses competing biologics, complicating the market but also reaffirming the importance of robust patent prosecution and strategic portfolio management.

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Key Takeaways

• Scope and Claims: The patent centers on a VEGFR-2 specific monoclonal antibody with defined binding characteristics, covering compositions, methods, and uses, thereby broadening its protective scope.
• Strategic Positioning: It secures exclusivity over a specific therapeutic approach within the anti-angiogenic space, critical for market dominance in certain oncology indications.
• Patent Landscape: It exists within a highly competitive and complex biologics IP environment, with overlapping patents and evolving technology, necessitating ongoing patent filing strategies.
• Expiration and Lifecycle: Anticipated patent expiry in the mid-2020s underscores the importance of innovation pipelines and continuation filings.
• Litigation and Competition: The scope’s breadth supports enforcement, but also faces challenges from biosimilars and emerging antibody technologies.

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FAQs

1. What is the primary innovation claimed in U.S. Patent 8,124,125?
   The patent claims a monoclonal antibody specifically binding to VEGFR-2, including methods of production and therapeutic use in treating angiogenesis-driven cancers.

2. How does this patent impact competition in VEGFR-2 targeting therapies?
   It grants exclusive rights to certain monoclonal antibodies targeting VEGFR-2, limiting generic or biosimilar entry during its enforceable period in relevant indications.

3. Are there similar patents for other anti-angiogenic therapies?
   Yes, patents exist for agents like bevacizumab (anti-VEGF-A), aflibercept, and other VEGFR-2 inhibitors, creating a dense intellectual property environment.

4. When does the patent expire, and what implications does this have?
   The patent is set to expire around 2032 (20 years from filing), after which biosimilars and generics could enter the market, reducing exclusivity.

5. What are potential patent challenges to the scope of this patent?
   Prior art, emerging antibody variants, or alternative binding epitopes could be used to challenge validity or design-around the patent claims.

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References

1. U.S. Patent No. 8,124,125.
2. Genentech, Inc. Press Releases and Product Approvals.
3. Scientific literature on VEGFR-2 targeted therapies.
4. Patent landscape analyses of anti-angiogenic biologics.

Drugs Protected by US Patent 8,124,125

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

Foreign Priority and PCT Information for Patent: 8,124,125

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Denmark	2003 01503	Oct 10, 2003
Denmark	2004 00464	Mar 23, 2004
Denmark	2004 01006	Jun 25, 2004

International Family Members for US Patent 8,124,125

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2004279661
Australia	2009201881
Brazil	PI0415121
Canada	2540984
Canada	2541382
Canada	2582403