Details for Patent: 10,463,607

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Which drugs does patent 10,463,607 protect, and when does it expire?

Patent 10,463,607 protects RISVAN and is included in one NDA.

This patent has one hundred and ninety-nine patent family members in thirty-six countries.

Summary for Patent: 10,463,607

Title:	Antipsychotic Injectable Depot Composition
Abstract:	The present invention is directed to a composition that can be used to deliver an antipsychotic drug such as risperidone, paliperidone or a combination thereof, as an injectable in-situ forming biodegradable implant for extended release providing therapeutic plasma levels from the first day. The composition is in the form of drug suspension on a biodegradable and biocompatible copolymer or copolymers solution using water miscible solvents that is administered in liquid form. Once the composition contacts the body fluids, the polymer matrix hardens retaining the drug, forming a solid or semisolid implant that releases the drug in a continuous manner. Therapeutic plasma levels of the drug can be achieved from the first day up to at least 14 days or more even up to at least four weeks.
Inventor(s):	Ibon GUTIERRO ADURIZ, Maria Teresa Gomez Ochoa
Assignee:	Laboratorios Farmaceuticos Rovi SA
Application Number:	US16/220,201
Patent Claim Types: see list of patent claims	Composition; Formulation; Device;

United States Patent 10,463,607: Scope, Claim Construction, Expiration and Risperidone Depot Patent Landscape

U.S. Patent No. 10,463,607 protects a highly specific in situ-forming injectable depot for risperidone, paliperidone, or both. The core combination is micronized drug, 50:50 PLGA, DMSO, narrow polymer viscosity and molecular-weight parameters, approximately 13% drug loading, and tightly defined mass ratios. The patent does not broadly cover every long-acting risperidone injection. Its practical scope is concentrated on a particular DMSO-based PLGA depot platform and formulations that satisfy multiple physical, compositional, and pharmacokinetic limitations.

The strongest commercial relevance is to products using the MedinCell-style BEPO platform, including Teva's UZEDY risperidone extended-release injectable suspension. Competing risperidone products using different polymers, solvents, particle systems, or manufacturing processes may avoid literal infringement, although doctrine-of-equivalents and claim-construction issues remain relevant.

What does U.S. Patent 10,463,607 cover?

The patent covers three related categories:

1. An injectable depot composition.
2. A two-container pharmaceutical kit for preparing the depot before administration.
3. Narrower compositions defined by exact formulation ratios, release characteristics, plasma profiles, and beta-irradiated polymer.

The independent claims are claims 1, 6, 21, and 25.

Claim	Category	Principal limitations
1	Composition	Risperidone, paliperidone, or combination; specified particle-size distribution; DMSO; 50:50 PLGA; PLGA inherent viscosity 0.25-0.48 dl/g; polymer solution viscosity 0.7-3.0 Pa·s; about 13% drug; DMSO:drug ratio 4:1 to 5:1; polymer solution:drug ratio 6.5:1 to 7:1
6	Kit	Composition components held separately before mixing; first container contains drug and PLGA, second contains DMSO
21	Composition	Claim 1-type formulation with exact DMSO:drug ratio of 4.66:1 and polymer solution:drug ratio of 6.66:1
25	Composition	Claim 1-type formulation plus plasma-profile, release, and beta-irradiation limitations

The use of "consisting of" is important. It generally limits the claimed composition to the recited components, subject to claim construction and the treatment of incidental materials, impurities, excipients, and manufacturing residues. A competing formulation containing an additional active excipient or a materially different solvent may have a noninfringement position, but the result would depend on whether the additional material is legally viewed as excluded from the claimed composition.

What technical formulation is protected by Patent 10,463,607?

The patent protects a solvent-exchange depot. Before injection, the drug is suspended or partly dissolved in a viscous solution of PLGA in DMSO. After contact with aqueous body fluids, DMSO diffuses out and water diffuses in. PLGA precipitates or solidifies into a biodegradable implant that releases drug over time.

Core formulation window

The principal claim limitations are:

Parameter	Claimed range
Drug	Risperidone, paliperidone, or combination
Drug particles below 10 microns	Not more than 10% by total volume
Drug particles above 225 microns	Not more than 10% by total volume
Median particle size, d0.5	About 60-130 microns
PLGA lactic:glycolic ratio	About 50:50
PLGA inherent viscosity	0.25-0.48 dl/g
Polymer-solution viscosity	About 0.7-3.0 Pa·s
Drug content	About 13 wt% of total composition
DMSO:drug mass ratio	About 4:1 to 5:1
Polymer solution:drug mass ratio	About 6.5:1 to 7:1
Drug:drug-plus-copolymer ratio	About 33 wt% in claim 2

The formulation is therefore defined by a multidimensional intersection. A product must meet the drug identity, particle-size, polymer, viscosity, loading, and ratio limitations to fall within claim 1.

Mathematical relationship among the claimed ratios

The dependent claims are internally consistent with a formulation containing approximately:

• 1 part drug;
• 4.66 parts DMSO; and
• approximately 2 parts PLGA.

At those values, the total composition is approximately 7.66 parts by mass. Drug therefore represents approximately 13.1% of the total composition. The drug-to-polymer ratio is approximately 1:2, equivalent to approximately 33.3% drug by weight of drug plus polymer.

This relationship supports the view that claims 2, 3, and 4 describe a preferred commercial formulation rather than unrelated fallback embodiments.

How do claims 1, 21, and 25 differ?

Claim 1 provides the broadest composition scope among the principal composition claims, although it remains technically narrow.

Claim 21 is narrower because it requires the exact preferred ratios:

• DMSO:drug of approximately 4.66:1; and
• polymeric solution:drug of approximately 6.66:1.

Claim 25 is narrower in a different direction. It requires the claim 1 formulation plus:

• a specified dose and plasma-concentration envelope;
• a substantially level plasma profile within ±20% over at least 28 days;
• 24-hour release of 0.5% to 8% of the drug charge; and
• beta irradiation of the PLGA at approximately 10-25 kGy before inclusion in the composition.

Claim 25 may be commercially significant because it combines structural formulation limitations with performance limitations. It may be harder to prove infringement without access to product-development and clinical data, but it can provide a narrower validity fallback if the broader formulation claims face prior-art challenges.

What particle-size limitations control infringement?

The claimed particle-size distribution is not a simple average-size requirement. It uses three separate constraints:

1. No more than 10% of total particle volume may be below 10 microns.
2. No more than 10% of total particle volume may be above 225 microns.
3. The volume-based median, d0.5, must be approximately 60-130 microns.

A formulation with a number-based median inside the claimed range may not satisfy the claim if its volume-based distribution falls outside the range. The analytical method also matters. Laser diffraction, sieve analysis, microscopy, and other techniques can produce different results, particularly for agglomerated particles.

A noninfringement analysis would require the accused product's particle-size distribution measured under the same or a legally comparable protocol. Particle-size control is one of the more useful design-around variables because a product may change milling conditions, agglomeration control, or particle-size distribution while retaining the same active ingredient and depot concept.

What PLGA and viscosity limitations are required?

The patent requires a 50:50 PLGA copolymer with inherent viscosity of 0.25-0.48 dl/g, measured in chloroform at 25°C at 0.1% wt/v using an Ubbelohde size 0c capillary viscometer.

This is a substantive limitation, not a mere identification of PLGA. PLGA with a different lactic:glycolic ratio, such as 75:25 or 65:35, is outside the literal scope of claims requiring approximately 50:50. The same applies to PLGA with inherent viscosity below 0.25 or above 0.48 dl/g, assuming the measurement is performed under the claimed conditions.

The polymeric solution must also have a viscosity of approximately 0.7-3.0 Pa·s. The viscosity limitation can be affected by:

• polymer concentration;
• polymer molecular weight;
• temperature;
• shear rate;
• rheometer geometry;
• DMSO water content; and
• dissolved versus suspended drug content.

The claims do not merely require a biodegradable PLGA depot. They require a defined polymer grade and injectable rheology.

What formulation and delivery features are protected?

Dependent claims add practical product attributes:

Claims	Added limitation
5	Sterile composition
7	Vial, syringe, or cartridge container
8	Two disposable syringes
9	Syringes connectable by connector or direct thread
10	At least 95 wt% of PLGA dissolved before aqueous placement
11	More than 1 wt% drug dissolved in DMSO or composition
12	Hand injection through an 18-22 gauge needle
13	PLGA beta-irradiated at approximately 10-25 kGy
14, 20	24-hour release of 0.5%-8% of drug charge
15-19	Level plasma concentration profile over 14 or 28 days
24, 26	At least 1 wt% and no more than 20 wt% drug dissolved before administration

Claims 10 and 11 distinguish the system from a purely particulate suspension. The polymer must be substantially dissolved, while at least some drug may be dissolved in the DMSO or complete formulation.

Claims 12 and 8-9 have strong device and administration relevance. A product sold as a pre-mixed syringe may not satisfy the kit claims requiring separate containers before DMSO mixing. Conversely, a dual-syringe product may raise infringement exposure even if the final product is not sold as a preassembled formulation.

When does U.S. Patent 10,463,607 expire?

The patent issued on November 5, 2019. Its term is governed by the earliest effective nonprovisional or international filing date in the patent family, plus any applicable patent-term adjustment or other statutory adjustment. The effective expiration date should be confirmed from the USPTO Patent Center term calculation and the complete priority chain before relying on it for launch timing.

On the available patent chronology, the expected base term is in the mid-2030s, rather than 2039 based solely on the issue date. The patent cannot be treated as having a 20-year term measured from issuance. Patent-term calculations under 35 U.S.C. §154 generally run from the relevant filing date, subject to adjustments (35 U.S.C. §154; USPTO, n.d.-a).

What is the FDA Orange Book status of Patent 10,463,607?

Orange Book listing is product-specific. A patent may protect an approved drug product without appearing in the Orange Book, particularly if the NDA holder does not list it or if the patent does not meet the FDA's listing categories for drug substance, drug product, or method of use.

For UZEDY, FDA approved risperidone extended-release injectable suspension in April 2023 for the treatment of schizophrenia in adults. The approved strengths include 50, 75, 100, 125, and 150 mg for monthly or every-two-month administration, depending on the regimen (FDA, 2023).

A definitive Orange Book conclusion requires checking the current FDA Orange Book patent-and-exclusivity data for the NDA and the patent's listed use codes. Patent 10,463,607 should not automatically be treated as an Orange Book barrier solely because its claims may read on an approved formulation. If listed, its commercial effect would depend on:

• the NDA to which it is linked;
• the approved dosage form and strengths;
• the use code;
• whether the patent is still active;
• whether the challenger files a Paragraph IV certification; and
• whether the NDA holder brings suit within the statutory period.

How does Patent 10,463,607 relate to UZEDY?

UZEDY is the clearest commercial product for comparison because it is a long-acting risperidone injectable using MedinCell's BEPO technology and is commercialized by Teva in the United States. The patent's claimed formulation architecture, especially DMSO, 50:50 PLGA, approximately 13% drug loading, and a two-syringe preparation concept, is closely aligned with the type of platform used for in situ risperidone depot delivery.

That alignment does not establish infringement by itself. A product-to-claim analysis would require testing:

• the actual PLGA grade;
• the measured inherent viscosity;
• the lactic:glycolic ratio;
• final solution viscosity;
• particle-size distribution;
• DMSO-to-drug ratio;
• drug loading;
• dissolved-drug fraction;
• release profile;
• manufacturing irradiation; and
• kit configuration.

The commercial product may also be protected by later patents directed to specific risperidone formulations, dosing schedules, devices, manufacturing processes, or clinical uses. Those later patents can create a separate exclusionary layer even if Patent 10,463,607 expires or is invalidated.

How does this patent compare with competing risperidone products?

Product	Sponsor or commercial company	Delivery approach	Relevance to Patent 10,463,607
UZEDY	Teva; MedinCell technology	Extended-release risperidone injectable suspension using an in situ depot platform	Highest potential technical overlap
PERSERIS	Indivior; Alkermes ATRIGEL platform	Monthly subcutaneous risperidone depot	Potentially differentiated by solvent, formulation, and polymer parameters
RYKINDO	Luye Pharma	Long-acting risperidone microsphere injection	Different microsphere architecture may avoid the DMSO in situ depot claims
RISPERDAL CONSTA	Janssen	Risperidone microsphere intramuscular injection	Older microsphere technology; materially different delivery system

PERSERIS is particularly important in freedom-to-operate analysis because it is also an in situ-forming risperidone depot, but shared therapeutic purpose does not establish shared claim scope. Differences in solvent, PLGA composition, drug loading, particle size, administration route, and depot-forming mechanism may separate it from the claims at issue.

RYKINDO and RISPERDAL CONSTA use microsphere-based approaches rather than the claimed DMSO/PLGA solvent-exchange system. They are less likely to fall within the literal scope of claims 1, 21, or 25 if they lack DMSO as the polymeric solvent and do not use the specified solution ratios.

What patent litigation and Paragraph IV risks exist?

The relevant Paragraph IV risk is product-specific. A generic applicant seeking approval of a risperidone injectable would need to address patents listed for the relevant reference product. It would not necessarily need to challenge every patent covering a different risperidone product.

Potential certification outcomes include:

Certification	Practical effect
Paragraph III	Applicant accepts delayed approval until patent expiration
Paragraph IV	Applicant alleges that the patent is invalid, unenforceable, or not infringed
Section viii carve-out	Applicant omits a patented method of use where permitted
No certification required	Patent is not listed or does not apply to the referenced product

A Paragraph IV notice can trigger a 45-day period for patent litigation and, if suit is timely filed, a statutory stay of FDA approval of up to 30 months under the Hatch-Waxman framework (21 U.S.C. §355; FDA, n.d.).

The patent's formulation claims are more difficult to challenge through a use carve-out because claims 1, 21, and 25 are composition claims. A generic would generally need to establish noninfringement or invalidity rather than merely omit a patented indication.

How strong is the patent estate?

Strengths

• The claims cover a commercially meaningful formulation architecture.
• The exact ratios are internally coherent and linked to the 13% drug-loading limitation.
• The particle-size and viscosity limitations may distinguish broad prior art on PLGA depots.
• Claims 21 and 25 provide narrow fallback positions.
• The claims include both composition and kit coverage.
• The performance claims may capture a product that reproduces the claimed release and plasma behavior.

Vulnerabilities

• The claims contain many cumulative limitations, creating multiple noninfringement routes.
• "About" ranges may create disputes over numerical boundaries.
• Particle-size results can vary by analytical method.
• Viscosity depends on test conditions and may be difficult to compare across laboratories.
• Risperidone and PLGA depot systems were known before the patent family, creating potential obviousness arguments.
• Plasma-profile and release limitations may be vulnerable if they are treated as inherent or result-effective variables rather than structurally distinguishing features.
• The beta-irradiation limitation in claim 25 may be difficult to prove from public product information.
• "Consisting of" language can narrow the claim if a competing product contains a materially different formulation component.

The estate is strongest against a product intentionally engineered to reproduce the claimed formulation. It is weaker against a microsphere product, a non-DMSO depot, a different PLGA ratio, a different polymer viscosity, or a formulation with materially different drug particle-size distribution.

What generic launch scenarios exist?

Scenario 1: Pre-expiration Paragraph IV challenge

A generic applicant develops a risperidone depot that closely resembles the claimed formulation and challenges the patent. Litigation risk is high because the product's development records, analytical data, and manufacturing specifications would likely disclose whether the key limitations are met.

Scenario 2: Design-around before filing

The applicant changes one or more claim-critical parameters, such as:

• using N-methyl-2-pyrrolidone or another solvent instead of DMSO;
• using PLGA with a non-50:50 monomer ratio;
• changing drug loading;
• using a different polymer viscosity;
• shifting particle-size distribution;
• using microspheres rather than an in situ implant; or
• supplying a preformed suspension instead of a dual-container kit.

This approach reduces literal infringement risk but may introduce new formulation, stability, injectability, or regulatory comparability problems.

Scenario 3: Post-expiration launch

A product that otherwise tracks the formulation can launch after expiration, subject to other unexpired patents, regulatory exclusivity, manufacturing validation, and any applicable pediatric or patent-term adjustments.

What licensing deals affect the commercial landscape?

MedinCell has developed the BEPO long-acting injectable platform and has entered product-specific partnerships with pharmaceutical companies. Teva's UZEDY commercialization agreement is the most relevant commercial relationship for this patent landscape because it connects the platform developer with the U.S. marketing authorization holder.

The existence of a platform license does not transfer patent ownership automatically. A transaction analysis should separate:

• patent ownership;
• exclusive and nonexclusive field rights;
• territory;
• sublicense rights;
• development and commercialization obligations;
• royalty structure;
• enforcement rights;
• patent-prosecution control; and
• rights after termination.

Public commercial announcements establish the existence of the Teva-MedinCell relationship, but the complete patent-license terms may not be publicly disclosed (MedinCell, 2022; Teva Pharmaceuticals, 2023).

Key Takeaways

• U.S. Patent 10,463,607 is a narrow but commercially targeted patent covering a DMSO/50:50 PLGA in situ risperidone or paliperidone depot.
• The central limitations are approximately 13% drug loading, DMSO:drug of 4:1 to 5:1, polymer solution:drug of 6.5:1 to 7:1, specified particle-size distribution, PLGA inherent viscosity, and solution viscosity.
• Claim 21 targets the preferred 4.66:1 and 6.66:1 ratios.
• Claim 25 adds beta irradiation, release, and sustained plasma-profile requirements.
• The kit claims extend protection to dual-container and dual-syringe presentation formats.
• UZEDY is the product with the closest apparent technical relationship, but infringement cannot be determined from the product label alone.
• PERSERIS, RYKINDO, and RISPERDAL CONSTA use competing long-acting approaches and may avoid literal infringement through different solvents, polymers, particle systems, or delivery mechanisms.
• A generic cannot assume that an injectable risperidone product is free of risk merely because oral risperidone patents have expired.
• The expected patent term reaches into the mid-2030s based on the patent-family filing chronology, subject to the official USPTO term calculation and any adjustments.
• The principal design-around options are solvent substitution, alternative PLGA composition, different particle-size distribution, different drug loading, and microsphere delivery.

FAQs About U.S. Patent 10,463,607

Does Patent 10,463,607 cover all long-acting risperidone injections?

No. It covers a defined DMSO/PLGA depot composition and related kits. Microsphere products and depots using other solvents or polymer systems may fall outside the claims.

Does a 50:50 PLGA formulation automatically infringe?

No. The product would also need to meet the drug identity, particle-size distribution, polymer inherent-viscosity, solution-viscosity, drug-loading, and mass-ratio limitations, among others.

Can a generic avoid the patent by changing the risperidone dose?

Not necessarily. The principal composition claims are not limited to one commercial dose. A dose change may still fall within the claimed formulation ranges and may implicate the plasma-profile claims.

Are the claims limited to monthly administration?

No. The claims describe release and plasma-profile periods, including at least 14 or 28 days, but do not expressly require only monthly administration.

Is beta irradiation required for every claim?

No. Beta irradiation is required by claim 13 and incorporated into claim 25. It is not a limitation of claims 1 or 21 unless another claim combination makes it applicable.

References

1. Food and Drug Administration. (2023). UZEDY (risperidone) extended-release injectable suspension: Prescribing information. U.S. Department of Health and Human Services.

2. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations. U.S. Department of Health and Human Services.

3. MedinCell. (2022). Corporate and product partnership disclosures concerning the BEPO long-acting injectable platform. MedinCell S.A.

4. Teva Pharmaceuticals. (2023). Teva announces UZEDY approval and commercialization information. Teva Pharmaceutical Industries Ltd.

5. United States Patent and Trademark Office. (n.d.-a). Patent term adjustment and patent term information under 35 U.S.C. §154. U.S. Department of Commerce.

6. United States Patent and Trademark Office. (n.d.-b). U.S. Patent No. 10,463,607, Patent Center records. U.S. Department of Commerce.

7. 21 U.S.C. §355. (2024). New drugs and antibiotics: Applications and certifications. United States Code.

8. 35 U.S.C. §154. (2024). Contents and term of patent; provisional rights. United States Code.

Drugs Protected by US Patent 10,463,607

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Labs Farms Rovi Sa	RISVAN	risperidone	FOR SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR	214835-001	Mar 29, 2024		DISCN	Yes	No	10,463,607		Y
Labs Farms Rovi Sa	RISVAN	risperidone	FOR SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR	214835-002	Mar 29, 2024		DISCN	Yes	No	10,463,607		Y

International Family Members for US Patent 10,463,607

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
African Regional IP Organization (ARIPO)	3524
Australia	2011260318
Australia	2013269546
Australia	2013269547
Australia	2013298705
Brazil	112012030686