Details for Patent: 10,010,612

Which drugs does patent 10,010,612 protect, and when does it expire?

Patent 10,010,612 protects PERSERIS KIT and is included in one NDA.

This patent has eighteen patent family members in eleven countries.

Summary for Patent: 10,010,612

Title:	Sustained delivery formulations of risperidone compounds
Abstract:	The present invention relates to a risperidone sustained release delivery system for treatment of medical conditions relating delusional psychosis, schizophrenia, bipolar disorder, psychotic depression, obsessive-compulsion disorder, Tourette syndrome, and autistic spectrum disorders. The sustained release delivery system includes a flowable composition containing risperidone, a metabolite, or a prodrug thereof and an implant containing risperidone, a metabolite, or a prodrug thereof. The flowable composition may be injected into tissue whereupon it coagulates to become the solid or gel, monolithic implant. The flowable composition includes a biodegradable, thermoplastic polymer, an organic liquid, and risperidone, a metabolite, or a prodrug thereof.
Inventor(s):	Eric Dadey, Qi Li, Christopher Lindemann
Assignee:	Indivior UK Ltd
Application Number:	US12/602,058
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Device;

United States Patent 10,010,612: Risperidone In-Situ Implant Claims, Patent Scope and Competitive Landscape

U.S. Patent No. 10,010,612 covers injectable, biodegradable risperidone compositions that form an implant after administration. Its core limitation is a solvent-polymer system containing risperidone base, 80/20 poly(DL-lactide-co-glycolide) with a carboxylic-acid end group, and N-methyl-2-pyrrolidone. The broadest independent composition claims cover defined weight ranges; narrower claims add dose, volume, pharmacokinetic, and sustained-release limitations. Claim 27 separately covers the in-situ implant formation method.

The patent is technically relevant to monthly subcutaneous risperidone products using Atrigel-type delivery technology, including Perseris. The most commercially important claim elements are the 80/20 acid-terminated PLGA, N-methyl-2-pyrrolidone solvent, risperidone base, and post-injection sustained-release profile.

What does U.S. Patent 10,010,612 protect?

The patent protects three principal subject-matter groups:

1. Injectable risperidone compositions.
2. Narrow formulations containing approximately 15 wt% risperidone, 45 wt% PLGA and 55 wt% N-methyl-2-pyrrolidone.
3. A method of forming a biodegradable implant in situ by injecting the composition and allowing the solvent to dissipate.

The claim set is composition-centric. It does not broadly claim every long-acting risperidone formulation, every PLGA risperidone microsphere, or every injectable risperidone product. A competing product would generally need to satisfy each limitation of at least one asserted claim.

Core composition limitations

Independent claim 1 requires:

Element	Claimed range
Risperidone base	10 wt% to 20 wt%
80/20 poly(DL-lactide-co-glycolide), carboxylic-acid end group	40 wt% to 50 wt%
N-methyl-2-pyrrolidone	50 wt% to 60 wt%

Independent claim 18 expands the formulation ranges:

Element	Claimed range
Risperidone base	1 wt% to 30 wt%
80/20 acid-terminated PLGA	20 wt% to 60 wt%
N-methyl-2-pyrrolidone	30 wt% to 70 wt%

Claim 28 is a point formulation claim covering approximately:

• 15 wt% risperidone base;
• 45 wt% 80/20 acid-terminated PLGA; and
• 55 wt% N-methyl-2-pyrrolidone.

Because these percentages total 115 wt%, the claim language must be interpreted in the context of the patent specification and its formulation-basis convention. The apparent total is a material drafting and claim-construction issue. It may reflect percentages calculated against a subset of formulation components, or it may create an ambiguity that affects enforcement and validity analysis.

How broad are the independent composition claims?

Claim 18 is the broadest composition claim on the supplied claim set because it extends the risperidone range to 1 wt% to 30 wt%, the polymer range to 20 wt% to 60 wt%, and the solvent range to 30 wt% to 70 wt%.

Its breadth is limited by four technical requirements:

1. Risperidone must be present as the base form.
2. The polymer must be an 80/20 poly(DL-lactide-co-glycolide).
3. The polymer must have a carboxylic-acid end group.
4. The solvent must be N-methyl-2-pyrrolidone.

A formulation using risperidone hydrochloride, a different lactide:glycolide ratio, an ester-terminated PLGA, or another solvent may avoid literal infringement of claim 18, subject to equivalents analysis.

Claim 1 is narrower in composition but more commercially targeted. Its 10 wt% to 20 wt% risperidone range and 40 wt% to 50 wt% polymer range center on the disclosed 15/45/55 formulation.

What formulations are protected by U.S. Patent 10,010,612?

The protected formulation space includes compositions with the following general architecture:

• crystalline or noncrystalline risperidone base dispersed or dissolved in the formulation;
• acid-terminated PLGA with an 80/20 lactide-to-glycolide ratio;
• N-methyl-2-pyrrolidone as the solvent or solvent component;
• a flowable pre-injection composition that becomes a depot after solvent exchange with bodily fluid.

Claims 2 through 4 and 20 cover compositions containing approximately 60 mg, 90 mg, or 120 mg of risperidone base. Claims 17 and 26 cover a formulation volume of approximately 0.75 ml to 1.0 ml.

The mass and volume limitations are important for product comparisons. A product can fall within the claimed composition ranges but avoid dependent claims directed to a particular dose or injection volume.

Formulation limitations with the strongest practical relevance

The most relevant limitations for an approved monthly injectable product are:

• 90 mg or 120 mg risperidone dose;
• 0.75 ml to 1.0 ml injection volume;
• rapid post-injection concentration;
• sustained exposure for at least 28 days;
• formation of a biodegradable implant after N-methyl-2-pyrrolidone dissipates.

The 60 mg claims may have development relevance but do not correspond to the standard Perseris dosing described in the FDA-approved labeling, which identifies 90 mg and 120 mg monthly doses. [2]

What do the pharmacokinetic claims cover?

Claims 5 through 8, 11 through 16, and 19 through 24 add pharmacokinetic and release-performance limitations.

The principal claimed parameters are:

Parameter	Claimed result
Cmax timing	Within about 2 hours after injection
Steady-state timing	About 3 days, or 3 to 42 days
Concentration	At least 15.8 ng/mL for about 28 days
Release profile	Linear sustained release for at least 28 days
Steady-state concentration	About 28.9 to 50.7 ng/mL
AUC Day 0-1	About 63.1 to 111.7 ng·day/mL
AUC Day 0-42	About 1,243.3 to 2,238.9 ng·day/mL
AUC Day 0-56	About 1,417.6 to 3,049.2 ng·day/mL
Dose-normalized AUC Day 0-42	About 15.9 to 20.9 ng·day/mL·mg

These claims create two enforcement questions.

First, the pharmacokinetic limitations may be difficult to assess from the product formulation alone. Infringement testing could require clinical or animal pharmacokinetic data, and results may vary according to dose, injection site, patient population, sampling schedule, assay, and whether risperidone, 9-hydroxyrisperidone, or both are measured.

Second, the claims use alternatives such as “risperidone and/or 9-hydroxyrisperidone.” That language potentially broadens the claimed analyte but may create claim-construction disputes concerning whether either compound independently satisfies the limitation.

What is the scope of the in-situ implant method claim?

Claim 27 requires:

1. injecting the flowable composition of claim 1 into a patient; and
2. allowing N-methyl-2-pyrrolidone to dissipate to produce an implant in the body.

This is a narrower method claim than the composition claims because it incorporates every limitation of claim 1. A method claim infringement case would likely focus on:

• the actual formulation administered;
• the polymer end group and lactide:glycolide ratio;
• the amount of each component;
• whether solvent dissipation produces an implant;
• whether the claimed result occurs in the patient.

The claim does not appear limited to a specific anatomical injection site, needle gauge, injection technique, or psychiatric diagnosis. It is directed to the delivery mechanism and implant-formation process.

Which claims are most vulnerable to invalidity challenges?

The strongest validity pressure points are likely to be written description, enablement, indefiniteness, anticipation, and obviousness.

Written description and enablement

The broad ranges in claim 18 cover a large formulation area. A challenger could argue that the specification does not adequately support the full combination of:

• 1 wt% to 30 wt% risperidone;
• 20 wt% to 60 wt% PLGA;
• 30 wt% to 70 wt% N-methyl-2-pyrrolidone;
• sustained linear release;
• rapid Cmax;
• concentration maintenance for at least 28 days.

The argument would be stronger if the examples concentrate on a much narrower formulation, such as 15/45/55, without demonstrating the full range.

Obviousness

The individual technical components were known in drug delivery:

• risperidone was an established antipsychotic;
• PLGA was widely used for biodegradable depots;
• N-methyl-2-pyrrolidone was known as a solvent in in-situ forming implants;
• long-acting risperidone formulations were previously developed using microspheres and other depot technologies.

The patentability case therefore depends heavily on the specific combination, polymer characteristics, concentration ranges, depot formation, and pharmacokinetic performance.

Indefiniteness and claim construction

The percentage language in claim 28 raises a significant drafting issue because the stated percentages total more than 100%. The same issue may affect other claims depending on how “wt%” is defined in the specification.

Other potential construction disputes include:

• the meaning of “flowable composition”;
• the required molecular-weight and end-group characteristics of the PLGA;
• the meaning of “linear sustained release”;
• the measurement method for Cmax and AUC;
• whether “about” permits material deviation from the stated values;
• whether “steady state” is a formulation limitation, a clinical result, or both.

How do claims 9 and 10 affect the patent estate?

Claims 9 and 10 are duplicates on the supplied claim text. Both state that the composition consists of risperidone base, 80/20 acid-terminated PLGA, and N-methyl-2-pyrrolidone.

A duplicate claim does not materially expand the technical scope. It may reflect an issued-claim transcription issue, a prosecution-history artifact, or an amendment carried into the final claim set. The operative analysis should rely on the official issued patent text and prosecution history rather than an informal claim reproduction.

The “consisting of” transition is significant. It excludes additional unrecited ingredients that materially alter the claimed composition, although ordinary impurities and incidental components may not be excluded. This limitation can provide a design-around path where a competing product requires an additional excipient, stabilizer, surfactant, or buffer.

When does U.S. Patent 10,010,612 lose exclusivity?

A patent expiration date cannot be established from the claims alone. The endpoint depends on the earliest effective nonprovisional or international filing date, terminal disclaimers, patent-term adjustment, patent-term extension, and any applicable disclaimer recorded in the USPTO file.

The patent issued in 2018. Its practical exclusivity analysis should separate:

Exclusivity category	Relevance
Patent term	Depends on the patent-family filing date and USPTO term calculation
FDA new-drug exclusivity	Separate from patent term
Orange Book listing	Determines notice and Paragraph IV framework
Regulatory exclusivity	May block approval even after certain patent claims expire
Litigation settlement	May establish an agreed generic entry date

The FDA Orange Book should be used to confirm whether U.S. Patent 10,010,612 is listed against a particular risperidone drug product, its listed expiration date, and any patent-use code. [3]

What is the FDA regulatory status of the covered product?

The claim set corresponds technically to an in-situ forming, long-acting risperidone depot. FDA approved Perseris, a monthly subcutaneous risperidone product, in 2018 for the treatment of schizophrenia in adults. The approved product uses a proprietary delivery system and is supplied at 90 mg and 120 mg doses. [2]

The FDA label identifies Perseris as a once-monthly subcutaneous injection. Its delivery system forms a depot after administration. The approved labeling is relevant to claim analysis but does not, by itself, establish that every issued claim is infringed. Infringement requires comparing the commercial formulation and administration method with the complete claim language.

The 28-day and 42-day release limitations are commercially aligned with monthly administration. The pharmacokinetic claims may also be directed to performance characteristics demonstrated during product development.

What is the Orange Book and Paragraph IV significance?

If the patent is listed in the Orange Book for an approved risperidone product, an abbreviated new drug application applicant could address it through:

• Paragraph I, if no patent information is listed;
• Paragraph II, if the patent has expired;
• Paragraph III, if the applicant accepts approval after expiration;
• Paragraph IV, if the applicant asserts that the patent is invalid, unenforceable, or not infringed.

A Paragraph IV certification could trigger patent litigation under the Hatch-Waxman framework if the NDA holder or patent owner files suit within the statutory period. [4]

The product-specific Orange Book entry, patent-use code, and any delisting or expiration-date correction are essential to determining the actual generic-entry barrier. Patent 10,010,612 cannot be treated as an automatic barrier to an ANDA without confirming its listing and the approved product to which it is tied.

Which companies are challenging the patent?

No defensible list of challengers, Paragraph IV notices, lawsuits, or settlements can be derived from the supplied claims. The relevant public records are:

• FDA Orange Book patent listings;
• Federal district court docket records;
• PACER filings;
• ANDA litigation decisions;
• USPTO post-grant proceedings;
• SEC filings by the NDA holder or licensee.

A search should distinguish between challenges to U.S. Patent 10,010,612 and disputes involving related patents covering the same delivery platform. Related patents may concern manufacturing, formulation ranges, injection devices, dosing regimens, or methods of treating schizophrenia.

What patent landscape surrounds long-acting risperidone?

The competitive patent landscape has several technology groups.

Risperidone microsphere depots

Risperdal Consta uses a microsphere-based long-acting delivery technology. Its patent estate is technically distinct from the solvent-exchange in-situ implant claimed in Patent 10,010,612. Microsphere manufacturing, particle characteristics, reconstitution, and injection requirements create different IP barriers.

In-situ forming PLGA depots

This is the closest technology category. It includes compositions in which a biodegradable polymer is dissolved in a biocompatible solvent and precipitates or solidifies after solvent exchange in tissue. The key differentiation points are:

• polymer composition;
• lactide:glycolide ratio;
• polymer end group;
• solvent identity;
• drug loading;
• depot morphology;
• release kinetics.

Other long-acting antipsychotics

Paliperidone palmitate products, including Invega Sustenna, Invega Trinza, and Invega Hafyera, compete clinically with monthly or less frequent risperidone therapy but use a different active ingredient and delivery platform. Their patent estates do not directly anticipate the specific risperidone/PLGA/N-methyl-2-pyrrolidone combination, although they affect commercial substitution and market-entry strategy.

Manufacturing and device rights

A complete freedom-to-operate review must examine:

• polymer synthesis and end-group control;
• drug-polymer mixing;
• sterile filling;
• syringe or dual-chamber packaging;
• needle and injection-device design;
• depot-forming process parameters;
• analytical release testing.

A composition patent may be only one layer of the product’s total IP protection.

How strong is the patent estate for the claimed formulation?

The claims have meaningful commercial value because they combine a defined drug, a defined biodegradable polymer, a defined solvent, and a clinically relevant monthly-release profile.

The estate is strongest where:

• the commercial product falls within the 15/45/55 formulation;
• the product uses 80/20 acid-terminated PLGA;
• the dose is 90 mg or 120 mg;
• the injection volume is within 0.75 ml to 1.0 ml;
• the product produces the claimed pharmacokinetic profile;
• related patents cover manufacturing or device implementation.

The estate is weaker against products that use:

• a different PLGA ratio;
• ester-terminated or other end-group chemistry;
• a solvent other than N-methyl-2-pyrrolidone;
• a microsphere or nanocarrier rather than an in-situ implant;
• a substantially different drug loading;
• a release period shorter than the claimed period;
• an additional ingredient that defeats “consisting of” claims.

What generic launch scenarios exist?

A generic or follow-on entrant would likely evaluate four strategies:

1. Formulate outside the claimed polymer-solvent combination.
2. Use a different risperidone delivery platform, such as microspheres.
3. Submit a Paragraph IV certification and challenge validity or infringement.
4. Pursue a settlement with a negotiated launch date.

A non-infringing formulation would need to avoid the complete combination, not merely change the dose. Changing 120 mg to 90 mg would not avoid claim 1 or claim 18 if the formulation remains within their composition ranges.

The most direct design-around options are changing the solvent, polymer end group, lactide:glycolide ratio, or delivery architecture. Each option may create new regulatory, manufacturing, stability, injection-volume, and pharmacokinetic issues.

Key Takeaways

• Patent 10,010,612 primarily protects injectable risperidone base in an in-situ forming PLGA depot.
• Claim 18 is the broadest supplied composition claim.
• The central structural combination is 80/20 acid-terminated PLGA plus N-methyl-2-pyrrolidone.
• Claims 5 through 8 and 11 through 24 add pharmacokinetic and sustained-release limitations.
• Claim 27 covers in-situ implant formation after injection and solvent dissipation.
• Claims 9 and 10 are duplicative in the supplied text and should be checked against the official patent.
• Claim 28 presents a potential percentage-basis issue because its stated component percentages total 115 wt%.
• Perseris is the principal regulatory product technically associated with this formulation approach, with FDA-approved 90 mg and 120 mg monthly doses.
• Actual Orange Book status, patent expiry, Paragraph IV activity, litigation, and settlement terms require review of current FDA and court records.
• The most credible design-around routes involve changing the solvent, PLGA chemistry, polymer ratio, or delivery platform.

FAQs

Does Patent 10,010,612 cover all monthly risperidone injections?

No. It covers compositions and methods meeting the specific drug, polymer, solvent, concentration, and performance limitations. Microsphere-based or differently formulated monthly risperidone products may fall outside the claims.

Does a 120 mg risperidone dose infringe the patent by itself?

No. Dose alone is insufficient. The product must also satisfy the applicable composition and, where relevant, volume or pharmacokinetic limitations.

Can a competitor avoid the patent by using risperidone hydrochloride?

Potentially. The claims recite risperidone base. A hydrochloride formulation may avoid literal infringement, although the full patent, prosecution history, and doctrine-of-equivalents issues would control.

Are the claimed pharmacokinetic ranges automatically satisfied by Perseris?

Not automatically. The approved product’s formulation and clinical data must be compared with each claimed parameter and its measurement method.

Does a related patent create a separate generic-entry barrier?

Yes. Patents covering manufacturing, devices, formulations, dosing, or methods of treatment may remain relevant even if Patent 10,010,612 is invalidated or expires.

References

1. United States Patent and Trademark Office. (2018). U.S. Patent No. 10,010,612: Risperidone formulations and methods of use thereof.
2. U.S. Food and Drug Administration. (2018). Perseris (risperidone) extended-release injectable suspension prescribing information.
3. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations: Orange Book.
4. Drug Price Competition and Patent Term Restoration Act of 1984, 21 U.S.C. § 355(j).

Drugs Protected by US Patent 10,010,612

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Indivior	PERSERIS KIT	risperidone	FOR SUSPENSION, EXTENDED RELEASE;SUBCUTANEOUS	210655-001	Jul 27, 2018		DISCN	Yes	No	10,010,612		Y
Indivior	PERSERIS KIT	risperidone	FOR SUSPENSION, EXTENDED RELEASE;SUBCUTANEOUS	210655-002	Jul 27, 2018		DISCN	Yes	No	10,010,612		Y

International Family Members for US Patent 10,010,612

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2008262545
Brazil	PI0811319
Canada	2687979
China	101801415
European Patent Office	2152315
European Patent Office	2907524
Spain	2562878