Details for Patent: 7,858,122

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Which drugs does patent 7,858,122 protect, and when does it expire?

Patent 7,858,122 protects KEPPRA XR and is included in one NDA.

This patent has eighteen patent family members in sixteen countries.

Summary for Patent: 7,858,122

Title:	Extended release formulation of levetiracetam
Abstract:	An extended release pharmaceutical composition of Levetiracetam with once a day dosage regime and the process of preparing it. The extended release tablet of Levetiracetam is with the core comprising of Levetiracetam and water dispersible rate controlling polymer, and the tablet core is optionally functional coated comprising a combination of water non-dispersible and/or water dispersible polymer. It provides extended therapeutically effective plasma levels over a twenty four hour period with diminished incidences of neuropsychiatric adverse events by eliminating the troughs and peaks of drug concentration in a patients blood plasma, which comprises administering orally to a patient in need thereof, an extended release tablet that provides a peak blood plasma level of Levetiracetam in from about eight to about Sixteen hours. The core is prepared by Wet granulation, Dry granulation or Direct compression and optionally the tablet core is coated either in an coating pan or in and Fluidized bed system.
Inventor(s):	Rajesh Kshirsagar, Mayank Joshi, Yogesh Raichandani
Assignee:	UCB SA
Application Number:	US11/215,947
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,858,122
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound; Dosage form;

United States Patent 7,858,122: Levetiracetam Extended-Release Tablet Claims, Patent Scope and Competitive Landscape

U.S. Patent No. 7,858,122 protects a hydrophilic matrix tablet containing levetiracetam and a relatively high concentration of a water-dispersible rate-controlling polymer. The central enforceable concept is not levetiracetam alone. It is the combination of composition ranges, polymer viscosity, manufacturing options, and a defined 12-hour dissolution profile.

The broadest claim requires:

• 30% to 85% levetiracetam by weight;
• 20% to 40% of a specified water-dispersible polymer;
• polymer viscosity above 15 centipoise in a 2% w/w solution;
• an extended-release dissolution profile;
• a tablet dosage form.

The most commercially important narrower claims focus on hydroxypropyl methylcellulose, or HPMC, with levetiracetam concentrations of 50% to 80% or 61% to 73%.

What does U.S. Patent 7,858,122 protect?

Patent 7,858,122 protects an extended-release levetiracetam tablet using a polymeric matrix to control drug release. The claims cover a broad formulation genus but narrow materially through the dissolution requirement.

Claim	Protected subject matter	Commercial significance
1	Levetiracetam tablet with 30%-85% drug, 20%-40% rate-controlling polymer, specified viscosity and dissolution profile	Broad composition and performance claim
2	Claim 1 tablet providing 24-hour therapeutic levels with an 8-16 hour plasma peak	Pharmacokinetic limitation
3	Claim 1 tablet with 50%-80% levetiracetam and 20%-40% HPMC, optionally 1%-5% PVP	Important HPMC matrix formulation claim
4	Claim 1 tablet with 61%-73% levetiracetam, 25%-35% HPMC and optionally 1.1%-1.5% PVP	Narrowest and potentially easiest claim to design around
5	Claim 1 tablet made by wet granulation, dry granulation or direct compression	Manufacturing-process limitation

The patent is directed to a matrix tablet rather than an osmotic pump, multiparticulate capsule, transdermal system or parenteral dosage form. A product that achieves once-daily exposure through a different release mechanism may avoid literal infringement if it does not satisfy the claimed composition and dissolution limitations.

How should claim 1 be construed?

Claim 1 is a combination claim. Every material limitation must be present for literal infringement.

Levetiracetam concentration

The claimed tablet must contain approximately 30% to 85% levetiracetam by weight. Claims 3 and 4 narrow the range to:

• 50% to 80% in claim 3;
• 61% to 73% in claim 4.

A formulation containing less than approximately 30% or more than approximately 85% levetiracetam may avoid claim 1, although the legal effect of “about” depends on the specification, prosecution history and technical evidence.

Rate-controlling polymer

The polymer must constitute approximately 20% to 40% of the tablet and must be water dispersible. The listed polymer group includes:

• hydroxyethyl cellulose;
• hydroxypropyl cellulose;
• sodium alginate;
• carbomer;
• sodium carboxymethyl cellulose;
• xanthan gum;
• guar gum;
• locust bean gum;
• polyvinyl acetate;
• polyvinyl alcohol;
• HPMC;
• mixtures of those polymers.

The polymer must also have viscosity greater than 15 cps in a 2% w/w solution. This viscosity limitation is important. A polymer from the listed chemical class may still fall outside the claim if it does not satisfy the specified viscosity test.

For claims 3 and 4, HPMC is the required rate-controlling polymer. A generic HPMC product would therefore face greater literal infringement risk than a formulation using a different matrix polymer, assuming all other claim limitations are met.

Dissolution profile

The tablet must release levetiracetam under the following conditions:

• USP Apparatus 1, basket;
• 100 rpm;
• purified water;
• 37°C.

The claim requires:

Time point	Required average levetiracetam release
2 hours	Less than 35%
4 hours	35%-75%
12 hours	More than 75%

This is a performance limitation, not merely a formulation target. A tablet may contain the claimed quantities of levetiracetam and HPMC but avoid literal infringement if its measured release profile falls outside the specified ranges.

Testing methodology will be material in any dispute. Batch variability, tablet sampling, assay method, basket condition, dissolution-medium preparation and treatment of borderline results could affect infringement conclusions.

What does “consisting of” mean in the patent claims?

The repeated use of “consisting of” creates a materially closed claim structure.

In general, a “consisting of” formulation excludes additional ingredients that materially alter the basic and novel characteristics of the claimed tablet. Claim 1 expressly permits certain optional components, including:

• binders from the listed group;
• lubricants;
• anti-adherents;
• glidants;
• a non-functional coating containing hydrophilic film-forming polymer, colorant and opacifying agent.

The claim language gives a generic manufacturer less freedom to add unlisted functional excipients than an “open” claim using “comprising.” The principal question would be whether an added ingredient is an excluded formulation component or an incidental material that does not change the claimed matrix system.

The optional binder language also creates overlap. HPMC can operate as both the rate-controlling polymer and, depending on the formulation, a binder. PVP is expressly relevant to claims 3 and 4.

What formulations are protected by claims 3 and 4?

Claims 3 and 4 provide the clearest commercial read-through for HPMC-based generic products.

Claim 3

Claim 3 covers a tablet containing:

• 50%-80% levetiracetam;
• 20%-40% HPMC;
• optionally 1%-5% PVP.

Because claim 3 depends on claim 1, the tablet must also satisfy the claim 1 dissolution profile and the other incorporated limitations.

Claim 4

Claim 4 is narrower:

• 61%-73% levetiracetam;
• 25%-35% HPMC;
• optionally 1.1%-1.5% PVP.

The narrower concentration windows may reduce the number of directly covered commercial products. They also provide a potentially stronger validity position if the specification contains detailed examples within those ranges. At the same time, a generic applicant can potentially design around claim 4 by adjusting drug loading, HPMC concentration, PVP content or the selected HPMC grade.

A design-around must still be tested against claim 1. Moving outside the claim 4 ranges does not necessarily avoid the broader independent claim.

What is the legal significance of claim 2’s pharmacokinetic limitation?

Claim 2 requires:

1. extended therapeutically effective plasma levels over 24 hours; and
2. a peak blood plasma level between approximately 8 and 16 hours.

This limitation is more difficult to assess than the dissolution limitations. “Therapeutically effective” is functional language that may require interpretation from the specification and clinical data. The peak-time requirement is more measurable, but it may vary with:

• food intake;
• patient population;
• dose;
• sampling schedule;
• formulation strength;
• bioavailability;
• study design.

A product could meet claim 1 but avoid claim 2 if its pharmacokinetic profile produces a peak outside the 8-to-16-hour window. Conversely, a product could satisfy the pharmacokinetic profile without infringing claim 1 if its composition or dissolution profile falls outside the claim.

How does claim 5 affect generic manufacturing strategies?

Claim 5 covers tablets prepared by:

• wet granulation;
• dry granulation; or
• direct compression.

The claim is dependent on claim 1. It does not independently cover every levetiracetam tablet made by one of those methods.

The three listed processes cover the principal conventional tablet-manufacturing routes. A generic applicant using one of them would need to assess both the formulation and the process. A different manufacturing route may avoid literal infringement of claim 5 but would not avoid claim 1 if the final tablet otherwise satisfies the composition and dissolution requirements.

The claim also raises product-by-process issues. For infringement, the significance of the manufacturing limitation depends on how the claim is construed and whether the resulting product is materially distinguishable from tablets made by other processes.

When does U.S. Patent 7,858,122 lose exclusivity?

The patent claims priority to a June 28, 2005 priority date. On a standard 20-year patent-term calculation, the nominal expiration date is June 28, 2025, subject to any patent-term adjustment, patent-term extension, terminal disclaimer or other adjustment recorded in the USPTO file.

Event	Date or period
Earliest reported priority	June 28, 2005
U.S. patent grant	November 30, 2010
Nominal 20-year expiration	June 28, 2025
Pediatric extension	Not established from the supplied claim text
Post-expiration status	Depends on USPTO term records and any applicable adjustment

The grant date does not control expiration. The relevant calculation generally begins with the earliest effective nonprovisional or international filing date, subject to the patent-term rules applicable to the family.

If no term extension or adjustment applies, the patent’s substantive exclusionary term has reached its nominal endpoint. Any Orange Book or litigation analysis must still account for related patents, separate formulation claims, and enforceability issues.

What is the Orange Book status of patent 7,858,122?

Patent 7,858,122 is associated with the extended-release levetiracetam product class marketed as Keppra XR, manufactured by UCB entities. The FDA Orange Book is the operative source for determining whether the patent was listed against the relevant NDA and what expiration information was reported.

Orange Book status should be analyzed separately from technical claim scope:

• A patent may cover a product without being Orange Book listed.
• A listed patent can trigger an ANDA Paragraph IV certification.
• A patent’s expiration date in the Orange Book does not resolve validity, enforceability or infringement.
• A generic applicant may make a Paragraph III certification if the listed patent has not expired or a Paragraph IV certification if it contends the patent is invalid, unenforceable or not infringed.

The supplied claims do not establish the current Orange Book listing record. The relevant NDA is Keppra XR, NDA 022285, and the FDA Orange Book should control the current listing and certification analysis. [2]

Which companies are challenging levetiracetam extended-release patents?

The competitive field includes:

• UCB, as the originator associated with Keppra XR;
• generic companies filing ANDAs for levetiracetam extended-release tablets;
• contract manufacturers and formulation developers using hydrophilic matrix technology;
• companies pursuing alternative extended-release delivery systems.

Publicly available records have associated levetiracetam extended-release patent disputes with UCB and ANDA applicants. The principal litigation questions in such cases are typically:

1. whether the accused product meets the claimed levetiracetam and polymer ranges;
2. whether the polymer satisfies the viscosity limitation;
3. whether the product meets the specified dissolution profile;
4. whether the asserted patent is anticipated or obvious;
5. whether the patent was properly listed and certified against;
6. whether a settlement restricts launch timing.

A complete current litigation position requires the latest PACER, USPTO Patent Center and FDA Orange Book records. The claim text alone does not establish whether any particular ANDA applicant has an active Paragraph IV dispute or settlement.

What prior-art and validity issues affect patent 7,858,122?

The likely validity pressure points are predictable for a controlled-release matrix patent.

Anticipation

An anticipation challenge would need a single prior-art reference disclosing all material elements, including:

• the levetiracetam percentage;
• the 20%-40% polymer range;
• a listed polymer with the required viscosity;
• the claimed dissolution profile;
• the tablet form.

A general disclosure of extended-release levetiracetam would not necessarily anticipate the specific dissolution limitations.

Obviousness

Obviousness is likely the more substantial challenge. Prior art concerning:

• immediate-release levetiracetam;
• HPMC matrix tablets;
• once-daily antiepileptic formulations;
• polymer concentration optimization;
• routine dissolution testing;
• wet granulation and direct compression;

could be combined in an obviousness argument.

The patent holder’s response would likely rely on the particular release profile, the 24-hour pharmacokinetic result, unexpected performance, formulation tradeoffs and the claimed concentration windows.

Written description and enablement

Claim 1 covers multiple polymer classes, mixtures and manufacturing processes. A challenger could argue that the specification does not adequately support the full breadth of that genus or enable all claimed combinations without undue experimentation.

The patent holder would rely on working examples and the predictable nature of hydrophilic matrix formulation. The result would depend heavily on the specification’s examples, formulation tables and experimental data.

Indefiniteness

Potentially contestable terms include:

• “about”;
• “therapeutically effective plasma levels”;
• “water dispersible”;
• “non-functional coating.”

The dissolution limits are more objective than the pharmacokinetic language, but borderline results could still create disputes.

How strong is the patent estate for levetiracetam extended-release products?

Patent 7,858,122 has a moderate formulation-claim profile rather than a broad product monopoly.

Estate characteristic	Assessment
Active ingredient protection	Weak by itself; levetiracetam is not the protected invention
Dosage-form protection	Stronger for matrix tablets
Polymer protection	Broad in claim 1, narrower in claims 3 and 4
Dissolution protection	Important and potentially difficult to design around without testing
Pharmacokinetic protection	Narrower, data-dependent and potentially less predictable
Manufacturing protection	Covers three conventional processes but depends on claim 1
Design-around potential	Meaningful through polymer, concentration and release-profile changes
Remaining term	Nominally expired June 28, 2025 absent term adjustment

The commercial value of the patent was highest before generic entry and before expiration. Its remaining value now depends primarily on related unexpired patents, litigation posture, historical damages exposure and any continuing regulatory exclusivity.

What generic launch risks exist?

A generic levetiracetam extended-release applicant faces four main risk categories.

Formulation overlap

An HPMC matrix containing 50%-80% levetiracetam and 20%-40% HPMC is the clearest claim 3 risk. A formulation within 61%-73% levetiracetam, 25%-35% HPMC and 1.1%-1.5% PVP creates the clearest claim 4 risk.

Dissolution overlap

Even if the formulation differs slightly, the product may still fall within claim 1 if it satisfies the stated dissolution profile. Dissolution testing should therefore be used as a design-control parameter, not only as a regulatory quality test.

Paragraph IV exposure

If the patent was listed for the reference product while unexpired, an ANDA applicant could have faced a Paragraph IV certification and associated Hatch-Waxman litigation. The principal defenses would include noninfringement, invalidity and unenforceability.

Regulatory exclusivity

Patent expiration does not automatically resolve all barriers. FDA exclusivity, approved labeling, drug-product sameness, bioequivalence and any later-listed patents must be reviewed independently.

How does patent 7,858,122 compare with alternative extended-release technologies?

Technology	Likely relationship to patent 7,858,122
HPMC hydrophilic matrix tablet	Highest direct claim risk
Other hydrophilic polymer matrix	May fall within claim 1 if listed polymer, concentration, viscosity and dissolution requirements are met
Osmotic tablet	More likely to avoid literal infringement if it lacks the claimed matrix composition
Multiparticulate bead or pellet system	May avoid tablet and composition limitations
Layered tablet	Depends on whether the final product satisfies the claimed tablet composition and dissolution profile
Extended-release capsule	May avoid the tablet limitation, subject to claim construction
Abuse-deterrent or modified-release platform	Requires separate analysis of dosage form and release mechanism

A non-HPMC polymer is not automatically outside the patent. Claim 1 expressly lists several alternative polymers, including sodium alginate, carbomer, xanthan gum, guar gum, polyvinyl acetate and hydroxyethyl cellulose.

Key Takeaways

• Patent 7,858,122 covers an extended-release levetiracetam matrix tablet, not levetiracetam generally.
• Claim 1 combines drug loading, polymer loading, polymer viscosity and dissolution limitations.
• HPMC formulations are the principal commercial risk because claims 3 and 4 specifically target HPMC.
• The dissolution profile is a central infringement limitation and a potential design-around lever.
• Claim 2 adds a 24-hour pharmacokinetic requirement and an 8-to-16-hour peak concentration window.
• Claim 5 covers wet granulation, dry granulation and direct compression only through the limitations of claim 1.
• The patent has a reported June 28, 2025 nominal expiration date based on its 2005 priority date, subject to official term adjustments.
• Orange Book listing, current litigation and related-patent exposure must be assessed separately from the text of patent 7,858,122.
• Generic products using HPMC, 20%-40% polymer and the claimed dissolution profile present the highest historical infringement risk.
• Alternative dosage forms and release mechanisms offer meaningful design-around opportunities.

Frequently Asked Questions

Is levetiracetam itself still patent protected by U.S. Patent 7,858,122?

No. The patent does not claim levetiracetam as a molecule. It claims specific extended-release tablet compositions and related performance characteristics.

Does using HPMC automatically infringe patent 7,858,122?

No. HPMC use alone is insufficient. The product must also satisfy the applicable drug-loading, polymer-loading, viscosity, tablet and dissolution limitations.

Can a generic avoid the patent by using a polymer not listed in claim 1?

Potentially. A polymer outside the listed group may avoid literal infringement of claim 1, provided the product also avoids infringement under the doctrine of equivalents and any related patents.

Does a dissolution profile outside the claimed range eliminate infringement risk?

It can eliminate literal infringement of the dissolution limitation, but testing must use the claimed USP Apparatus 1 conditions. Related patents or alternative infringement theories may remain relevant.

Are biosimilars relevant to levetiracetam extended-release patent disputes?

No. Levetiracetam is a small-molecule drug. The relevant competitors are ANDA-based generic manufacturers, not biosimilar applicants under the Biologics Price Competition and Innovation Act.

References

1. United States Patent and Trademark Office. (2010). U.S. Patent No. 7,858,122, extended release formulations of levetiracetam.
2. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations: Orange Book.
3. U.S. Food and Drug Administration. (2008). Keppra XR prescribing information, NDA 022285.
4. United States Code, 35 U.S.C. §§ 154, 156.
5. United States Code, 21 U.S.C. § 355(j).

Drugs Protected by US Patent 7,858,122

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Ucb Inc	KEPPRA XR	levetiracetam	TABLET, EXTENDED RELEASE;ORAL	022285-001	Sep 12, 2008	AB	RX	Yes	No			Y
Ucb Inc	KEPPRA XR	levetiracetam	TABLET, EXTENDED RELEASE;ORAL	022285-002	Feb 12, 2009	AB	RX	Yes	Yes			Y

Foreign Priority and PCT Information for Patent: 7,858,122

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
India	81/MUM/2005	Jan 27, 2005

International Family Members for US Patent 7,858,122

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2005325930
Brazil	PI0518506
Canada	2595988