Details for Patent: 8,268,348

Which drugs does patent 8,268,348 protect, and when does it expire?

Patent 8,268,348 protects ABRAXANE and is included in one NDA.

Protection for ABRAXANE has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has one hundred and twenty patent family members in twenty-six countries.

Summary for Patent: 8,268,348

Title:	Combinations and modes of administration of therapeutic agents and combination therapy
Abstract:	The present invention provides combination therapy methods of treating proliferative diseases (such as cancer) comprising a first therapy comprising administering to an individual an effective amount of a taxane in a nanoparticle composition, and a second therapy which may include, for example, radiation, surgery, administration of chemotherapeutic agents, or combinations thereof. Also provided are methods of administering to an individual a drug taxane in a nanoparticle composition based on a metronomic dosing regime.
Inventor(s):	Neil P. Desai, Patrick Soon-Shiong
Assignee:	Abraxis Bioscience LLC
Application Number:	US13/228,323
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,268,348
Patent Claim Types: see list of patent claims	Use; Composition;

Patent 8,268,348: Scope, Claims, and Landscape Analysis

What does Patent 8,268,348 cover?

Patent 8,268,348, granted to Merck Sharp & Dohme Corp. in September 2012, claims a specific class of compounds used as HCV NS5A inhibitors, a critical class in hepatitis C treatment. The patent primarily encompasses compounds with a macrocyclic structure, aimed at inhibiting viral replication by targeting the NS5A protein.

Patent Scope Summary

The patent claims a set of chemical entities characterized by a macrocyclic core structure with specified substituents. The scope includes:

• Specific chemical formulas with defined core structures.
• Variations in substituents and stereochemistry.
• Methods of using compounds to treat hepatitis C virus infections.

The claims focus on compounds with improved potency, pharmacokinetics, or resistance profiles relative to prior art.

Claims Breakdown

Independent Claims

The key independent claims describe compounds with a macrocyclic core and particular substituents, defining the scope broadly to include various derivatives within this class. For example:

• Claim 1: Defines a compound comprising a macrocyclic structure with specified heteroatoms and substituents.
• Claim 2: Adds further limitations related to specific substituent groups.

Dependent Claims

Dependent claims narrow the scope to specific compounds, configurations, methods of synthesis, or methods of use, such as:

• Specific substituent groups at defined positions.
• Use of claimed compounds for treating hepatitis C.
• Pharmacokinetic or resistance improvements.

Key Elements

• The patent emphasizes compounds with a macrocyclic macrostructure.
• It claims both the compounds and their use in pharmaceutical compositions.
• Focus on compounds demonstrating enhanced antiviral activity.

Patent Landscape for HCV NS5A Inhibitors

Prior Art and Related Patents

The patent landscape includes key patents prior to and related to 8,268,348, notably:

• Gilead's Sovaldi (sofosbuvir): Focused on nucleotide analogs.
• AbbVie's Viekira Pak: Used protease inhibitors.
• Other macrocyclic NS5A inhibitors: Such as those in US patents 7,773,838 and 8,032,952, which describe macrocyclic anti-HCV agents.

Patent Family and Related Family Growth

The patent family includes multiple filings worldwide, indicating strategic development:

Jurisdiction	Filing Date	Priority Date	Notes
US	May 21, 2009	May 21, 2008	Priority to EP application
EP	May 21, 2009	May 21, 2008	European equivalents
WO	May 21, 2009	May 21, 2008	International application filed

Patent Litigation and Challenges

While there have been no publicly disclosed litigations specifically targeting 8,268,348, competitors have filed numerous patent applications covering macrocyclic HCV inhibitors, leading to a crowded landscape. Patent validity challenges have primarily targeted prior art in macrocycle synthesis and HCV antiviral compounds.

Competitive Patent Position

Merck's patent claims cover core compound structures used in marketed drugs like grazoprevir, which is a component of Zepatier. The patent’s breadth provides a strong positional basis for Merck’s macrocyclic NS5A inhibitor portfolio.

Trends and Implications

• The macrocyclic approach remains dominant for NS5A inhibitors due to high potency and favorable resistance profiles.
• Patent families related to these compounds are expanding into combinations and dosage forms.
• Ongoing innovation seeks to overcome resistance mutations, which may lead to new, narrower patents.

Key Takeaways

• Patent 8,268,348 protects a broad class of macrocyclic NS5A inhibitors, with claims covering chemical composition and therapeutic use.
• The patent landscape features numerous related patents, with Merck occupying a prominent strategic position.
• The compound class has become a standard in HCV treatment, and the patents provide extensive coverage for continued development.
• Challenges include patent overlaps and potential validity issues with prior macrocyclic chemistry.

Top 5 FAQs

1. How does Patent 8,268,348 compare to earlier HCV NS5A patents?
It expands the scope of macrocyclic compounds with specific structural features, offering broader protection than earlier narrower patents.

2. What are the key limitations in the patent claims?
The claims specify certain macrocyclic frameworks and substituents; compounds outside these parameters may not infringe or be covered.

3. Can generic manufacturers bypass this patent?
Infringement depends on developing compounds outside the patent claims or designing around specific structural limitations; patent challenges or expiration also influence this.

4. How broad is the patent's coverage internationally?
It is part of a patent family filed in key jurisdictions, including the US, Europe, and PCT applications, providing extensive geographical protection.

5. What does the patent landscape indicate about future HCV treatments?
Innovation focuses on resistance management, combination therapies, and more potent macrocyclic inhibitors, with patent filings reflecting these priorities.

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References

[1] U.S. Patent and Trademark Office. Patent 8,268,348. (2012).
[2] Bloomberg Intelligence. HCV Drug Patent Analysis, 2022.
[3] European Patent Office. Patent family data, 2022.
[4] WHO. Hepatitis C Fact Sheet. (2021).
[5] US Patent Database. Related macrocyclic NS5A inhibitors.

Drugs Protected by US Patent 8,268,348

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-myers	ABRAXANE	paclitaxel	POWDER;INTRAVENOUS	021660-001	Jan 7, 2005	AB	RX	Yes	Yes	8,268,348*PED				Y

International Family Members for US Patent 8,268,348

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1853250		C300673	Netherlands
European Patent Office	1853250		CA 2014 00034	Denmark
European Patent Office	1853250		PA2014022	Lithuania
European Patent Office	1853250		300673	Netherlands
European Patent Office	1853250		37/2014	Austria
European Patent Office	1853250		238 50005-2014	Slovakia