Details for Patent: 10,406,161

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Which drugs does patent 10,406,161 protect, and when does it expire?

Patent 10,406,161 protects RYKINDO and is included in one NDA.

This patent has thirty-six patent family members in fourteen countries.

Summary for Patent: 10,406,161

Title:	Risperidone sustained release microsphere composition
Abstract:	A risperidone sustained release microsphere formulation is provided. The microsphere formulation comprise risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release microsphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.
Inventor(s):	Kaoxiang Sun, Rongcai Liang, Qilin Wang, Wenyan Wang, Wanhui Liu, Youxin Li
Assignee:	Luye Innomind Pharma Shijiazhuang Co Ltd
Application Number:	US16/144,614
Patent Claim Types: see list of patent claims	Use; Composition; Formulation;

US Patent 10,406,161: Risperidone Microsphere Claims, Expiration, Litigation and Competitive Patent Landscape

US Patent No. 10,406,161 protects a specific long-acting injectable microsphere platform for risperidone or 9-hydroxyrisperidone. The central limitation is a blend of two uncapped PLGA polymers with different lactide:glycolide ratios, molecular-weight or intrinsic-viscosity ranges, and blend proportions. The patent does not broadly cover every risperidone depot formulation.

The strongest commercial claim is claim 15, which narrows the invention to a microsphere containing 45% risperidone and 55% polymer, with an 80:20 blend of 75:25 and 50:50 uncapped PLGA. Claims 17-20 extend coverage to injectable dosage forms and treatment of psychosis for release lasting up to 28 days.

The patent is associated with the long-acting risperidone product Rykindo, an FDA-approved monthly injectable formulation developed by Luye Pharma. Public patent records identify US 10,406,161 as issued on September 10, 2019, with a reported patent-term expiration in 2035, subject to any terminal disclaimer, patent-term adjustment, or regulatory extension reflected in official records.[1]

What does US Patent 10,406,161 protect?

The patent protects pharmaceutical compositions in microsphere form that combine:

1. Risperidone, a salt of risperidone, 9-hydroxyrisperidone, or a salt of 9-hydroxyrisperidone.
2. A blend of two uncapped poly(lactide-co-glycolide), or PLGA, polymers.
3. Distinct lactide:glycolide composition ranges for the two PLGA components.
4. No capped PLGA in the claimed polymer blend.
5. A microsphere dosage form.

Independent claim 1 establishes the core composition. Claim 17 covers a sustained-release injectable formulation containing the microspheres and a pharmaceutically acceptable excipient. Claim 19 covers use for treating psychosis, and claim 20 limits the release period to up to 28 days.

The patent is therefore a formulation and method-of-treatment patent. It is not a broad compound patent covering risperidone itself.

What is the central technical limitation?

The central limitation is the use of two uncapped PLGA polymers with different degradation characteristics:

Feature	First uncapped PLGA	Second uncapped PLGA
Lactide:glycolide ratio	65:35 to 90:10	50:50 to 75:25
Preferred ratio	75:25	50:50
Intrinsic viscosity	0.4-0.9 dL/g	0.1-0.35 dL/g
Narrower viscosity range	0.45-0.8 dL/g	0.1-0.3 dL/g
Narrowest viscosity range	0.45-0.55 dL/g	0.2-0.3 dL/g
Weight-average molecular weight	50,000-145,000	4,000-45,000
Narrower molecular-weight range	55,000-110,000	4,000-35,000
Narrowest molecular-weight range	55,000-85,000	15,000-35,000
Blend proportion	50-95 wt%	5-50 wt%
Preferred blend proportion	70-90 wt%	10-30 wt%
Narrowest blend proportion	80 wt%	20 wt%

The claim language excludes a polymer blend containing a capped PLGA. That limitation may be important in both infringement analysis and validity analysis because many biodegradable drug-delivery systems use end-capped or ester-capped PLGA to alter hydrolysis and drug release.

How do claims 1 through 20 differ?

Claims 1-16: Composition claims

Claim 1 is the broadest composition claim. It requires the active ingredient, the two uncapped PLGA components, the specified ratio ranges, and microspheres.

Claims 2-5 narrow the composition through lactide:glycolide and intrinsic-viscosity limitations. Claims 6-8 use molecular-weight ranges instead. Claims 9-11 define the relative quantity of the two polymers.

Claims 12-14 establish active-drug and polymer loading ranges. Claim 15 combines most of the commercially important parameters into a single narrow formulation:

• 45% risperidone;
• 55% total polymer;
• 80:20 first-to-second PLGA ratio;
• first PLGA at 55,000-85,000 molecular weight;
• second PLGA at 15,000-35,000 molecular weight;
• first PLGA intrinsic viscosity of 0.45-0.55 dL/g;
• second PLGA intrinsic viscosity of 0.2-0.3 dL/g;
• first PLGA at 75:25 lactide:glycolide;
• second PLGA at 50:50 lactide:glycolide.

Claim 16 expands the eligible active ingredient to specified inorganic and organic acid salts.

Claims 17-18: Injectable formulation claims

Claim 17 covers a sustained-release injectable formulation containing the microspheres and an excipient.

Claim 18 lists excipients and excipient classes, including:

• sodium carboxymethyl cellulose;
• polyvinyl alcohol;
• polyvinylpyrrolidone;
• sodium alginate;
• glycerol;
• sodium chloride;
• glucose;
• mannitol;
• glucitol;
• polysorbates; and
• poloxamers.

A formulation that uses a different excipient may still infringe claim 17 if it satisfies claim 1. Claim 18 is narrower because it requires the listed excipient categories and selections.

Claims 19-20: Method-of-treatment claims

Claim 19 covers treating psychosis by administering the claimed sustained-release injectable formulation. The listed conditions include acute and chronic schizophrenia, positive and negative symptoms, other psychotic states, and affective symptoms related to schizophrenia.

Claim 20 adds a release period of up to 28 days. The wording is significant. It does not require exactly 28 days, so a formulation releasing the active ingredient over 14, 21, or 28 days may fall within the literal scope if the remaining limitations are met.

What is the likely patent expiration date?

US Patent 10,406,161 issued on September 10, 2019.[1] Public patent databases report a patent-term expiration date in 2035, commonly shown as March 3, 2035 for this patent family. The enforceable expiration date must be confirmed against the USPTO patent record because the calculation can be affected by:

• the earliest effective nonprovisional priority date;
• patent-term adjustment;
• terminal disclaimers;
• patent-term extension under 35 U.S.C. § 156; and
• any correction or reexamination certificate.

The reported 2035 expiration is materially more important than the 2019 issue date because the patent may block a formulation-specific generic or alternative long-acting risperidone product well after approval of the reference product.

Does FDA regulatory exclusivity extend beyond the patent?

Rykindo received FDA approval in 2023. FDA regulatory exclusivity and patent protection operate separately. New-drug exclusivity may expire before the reported 2035 patent date, leaving the formulation patent as the principal barrier to a competing product that must rely on an ANDA or 505(b)(2) pathway.[2]

Risperidone itself is an established active ingredient. The commercial protection for a monthly injectable product therefore depends more heavily on formulation, delivery technology, manufacturing process, and listed patent rights than on new-molecular-entity exclusivity.

What is the Orange Book status of US 10,406,161?

US Patent 10,406,161 has been associated with the Rykindo reference product and is relevant to FDA Orange Book patent-listing analysis.[2] An Orange Book listing can require an ANDA applicant to make a patent certification under section 505(j)(2)(A)(vii), including:

• Paragraph I, if the patent information has not been submitted;
• Paragraph II, if the patent has expired;
• Paragraph III, if the applicant will wait until expiration; or
• Paragraph IV, if the applicant asserts that the patent is invalid, unenforceable, or not infringed.

The commercial significance of the listing depends on the patent’s current FDA status, the listed use or formulation, and whether the patent is eligible for a 30-month stay after a Paragraph IV notice. FDA’s Orange Book should be treated as the operative source for current listing status, approved use codes, and any delisting.[2]

Which companies are challenging the patent?

No publicly established, high-profile Paragraph IV litigation against US 10,406,161 is identified in the information provided. A definitive challenger analysis requires matching FDA Paragraph IV notices, district-court complaints, and ANDA filing records against the patent number.

The absence of a publicly reported challenge does not mean that the patent is uncontested. An ANDA applicant could pursue:

• a Paragraph IV certification;
• a declaratory-judgment action;
• a section viii carve-out for method-of-use claims;
• a 505(b)(2) application using a different formulation or delivery profile; or
• a product outside the claim limitations.

The most likely litigation targets would be claims 1, 15, and 17. Claim 15 is commercially narrow but potentially strong if the accused product uses the same formulation profile. Claim 17 may be more important than claim 18 because it does not require the detailed excipient list in claim 18.

What are the principal infringement risks for a generic or competing product?

A competing product would face literal infringement risk if testing or product documentation establishes all material limitations.

Active ingredient

The claims cover risperidone and 9-hydroxyrisperidone. A product using paliperidone, which is 9-hydroxyrisperidone, may fall within the active-ingredient language if the remaining limitations are met. A product using a different antipsychotic would not satisfy this limitation.

Polymer architecture

The product must use two uncapped PLGAs in the claimed ranges. A competitor could reduce risk by using:

• a single PLGA;
• two PLGAs outside the claimed lactide:glycolide ranges;
• an end-capped PLGA;
• a different biodegradable polymer;
• a polymer blend with a different molecular-weight distribution; or
• a non-microsphere depot system.

The phrase "does not have a capped poly(lactide-co-glycolide)" creates a potentially meaningful design-around. The scientific and legal question would be whether the polymer is genuinely uncapped or has an end group that a court treats as a cap.

Microsphere structure

A formulation using in situ gel formation, a solid implant, nanoparticles, liposomes, or a different particulate system may avoid the microsphere requirement. Perseris, for example, uses a different delivery approach based on the ATRIGEL system rather than the same PLGA microsphere architecture.[3]

Release duration

Claim 20 covers release for up to 28 days. A product designed for substantially longer release may avoid claim 20, but it could remain within claims 1 or 17 if the microsphere and polymer limitations are satisfied.

Doctrine of equivalents

A design-around that changes only an immaterial parameter could face a doctrine-of-equivalents argument. The "uncapped" limitation, the two-polymer requirement, and the microsphere limitation are likely to receive substantial attention because they define the claimed invention’s architecture rather than a minor manufacturing variable.

How strong is the patent estate?

The patent appears strongest against products that copy the Rykindo formulation architecture. Its main strengths are:

• multiple nested composition claims;
• coverage of both risperidone and 9-hydroxyrisperidone;
• separate viscosity and molecular-weight claim branches;
• a specific 80:20 polymer blend claim;
• injectable formulation claims; and
• method-of-treatment claims tied to sustained release.

Its main weaknesses are claim specificity and potential prior-art exposure. PLGA microspheres, risperidone depots, uncapped PLGA, and sustained-release injectable antipsychotics were known technology areas before the patent’s priority date. A validity challenge could focus on whether prior art disclosed or rendered obvious the claimed combination of:

• 75:25 and 50:50 PLGA;
• the specified molecular-weight or intrinsic-viscosity ranges;
• an 80:20 blend;
• approximately 45% drug loading; and
• monthly release.

A challenger would also examine written-description and enablement issues for the broad ranges in claim 1, particularly whether the specification supports the full combination of polymer ratios, molecular weights, viscosities, drug loadings, salts, and release profiles.

How does this patent compare with competing risperidone products?

Product	Sponsor	Delivery system	Approximate dosing interval	Relationship to US 10,406,161
Rykindo	Luye Pharma	Risperidone microspheres	Monthly	Directly relevant commercial product
Risperdal Consta	Janssen	Risperidone PLGA microspheres	Every two weeks	Earlier PLGA microsphere platform; separate patent estate
Perseris	Indivior	In situ depot using ATRIGEL technology	Monthly	Different delivery platform; lower direct structural overlap
Uzedy	Teva	Extended-release subcutaneous injectable suspension	Monthly or every two months	Different product platform and separate patent estate

Risperdal Consta is the closest technological comparator because it also uses risperidone-loaded PLGA microspheres. The existence of that product creates prior-art and freedom-to-operate relevance, but it does not establish infringement or invalidity. The decisive issue is whether the earlier formulation discloses the specific two-uncapped-PLGA blend and parameter combinations claimed in US 10,406,161.[4]

What patent litigation and settlement issues matter?

A Paragraph IV dispute would likely involve three separate questions:

1. Whether the accused product uses two uncapped PLGAs within the claimed ranges.
2. Whether the product’s polymer and drug-loading data satisfy the narrower claims, including claim 15.
3. Whether claims 1, 15, and 17 are valid over earlier risperidone and PLGA microsphere disclosures.

A settlement could include:

• a date-certain generic launch;
• a license to the patent;
• a formulation redesign;
• a covenant not to sue;
• restrictions on manufacturing or supply;
• or an authorized-generic arrangement.

No public settlement involving this patent is established by the supplied record. A patent-number-specific settlement conclusion would require verified court and FDA records.

What manufacturing and geographic barriers does the patent create?

The patent has potential geographic value in the United States because the claims cover both the composition and injectable use. Manufacturing outside the United States may still create U.S. exposure if the patented product is imported, sold, or used in the United States. Section 271(g) may also be relevant if a patented process is involved, although the claims supplied here are primarily composition and use claims rather than process claims.

The technical barrier is not merely selecting PLGA. A competitor must control:

• end-group chemistry;
• lactide:glycolide ratio;
• molecular-weight distribution;
• intrinsic viscosity;
• polymer blend ratio;
• drug loading;
• particle-size distribution;
• residual solvent;
• injectability; and
• release kinetics.

These parameters are interdependent. A design-around that changes one variable can affect syringeability, burst release, depot integrity, and monthly exposure. That creates a practical manufacturing barrier even when a legally noninfringing composition is available.

What revenue exposure does the patent create?

The principal exposure is the U.S. monthly injectable risperidone market. The risk is highest for a generic that seeks to substitute for Rykindo using a materially similar microsphere formulation. A competing product based on a distinct delivery system faces less direct risk under these claims but may encounter separate patents covering its own polymer, excipient, manufacturing process, or dosing regimen.

Rykindo competes against established long-acting antipsychotics, including Risperdal Consta, Perseris, and Uzedy. Patent protection does not guarantee market exclusivity because physician adoption, dosing interval, administration route, payer coverage, supply reliability, and clinical differentiation also affect entry economics.

Key Takeaways

• US Patent 10,406,161 is a formulation patent for risperidone or 9-hydroxyrisperidone microspheres.
• The core invention requires two uncapped PLGA polymers with different lactide:glycolide ratios and defined physical-property ranges.
• Claim 15 is the most commercially specific claim and tracks a 45% risperidone, 55% polymer, 80:20 PLGA formulation.
• Claims 17-20 extend coverage to injectable formulations, psychosis treatment, and release lasting up to 28 days.
• Public records report patent protection extending to approximately March 3, 2035, subject to the official patent-term record.
• A generic using a single polymer, capped PLGA, a different delivery system, or materially different polymer parameters may have a credible design-around.
• Risperdal Consta is the closest prior commercial comparator, while Perseris and Uzedy use different delivery technologies.
• No verified Paragraph IV challenger or settlement is established from the supplied record.
• Validity risk will likely focus on obviousness and anticipation based on earlier risperidone PLGA microsphere disclosures.

FAQs

Does US Patent 10,406,161 cover paliperidone?

Potentially. The claims expressly cover 9-hydroxyrisperidone, which is paliperidone, but a paliperidone product must also satisfy the PLGA blend, microsphere, formulation, and other applicable limitations.

Can a generic avoid the patent by using capped PLGA?

A product using capped PLGA may avoid the literal "uncapped" limitation, but the chemical characterization of the polymer and any doctrine-of-equivalents theory would require product-specific analysis.

Does the patent cover Risperdal Consta?

The patent does not automatically cover Risperdal Consta. Both products involve risperidone PLGA microspheres, but infringement depends on whether Risperdal Consta meets the specific two-uncapped-PLGA and parameter limitations.

Does claim 20 require a full 28-day release profile?

No. Claim 20 recites release for a period of up to 28 days. A shorter sustained-release period may fall within the claim if all other limitations are met.

Is FDA approval enough to establish freedom to operate?

No. FDA approval addresses regulatory marketing authorization. It does not resolve patent infringement, validity, Orange Book certification, manufacturing-process rights, or third-party license requirements.

References

1. United States Patent and Trademark Office. (2019). US Patent No. 10,406,161, pharmaceutical composition comprising risperidone or 9-hydroxy risperidone and uncapped PLGA polymer blend.
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. (2023). Rykindo (risperidone) extended-release injectable suspension prescribing information.
4. U.S. Food and Drug Administration. (n.d.). Risperdal Consta (risperidone) long-acting injection prescribing information.
5. United States Code, 35 U.S.C. §§ 154, 156, 271.

Drugs Protected by US Patent 10,406,161

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Shandong Luye	RYKINDO	risperidone	FOR SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR	212849-001	Jan 13, 2023		DISCN	Yes	No			Y			TREATMENT OF SCHIZOPHRENIA IN ADULTS
Shandong Luye	RYKINDO	risperidone	FOR SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR	212849-002	Jan 13, 2023		RX	Yes	Yes			Y			TREATMENT OF SCHIZOPHRENIA IN ADULTS
Shandong Luye	RYKINDO	risperidone	FOR SUSPENSION, EXTENDED RELEASE;INTRAMUSCULAR	212849-003	Jan 13, 2023		DISCN	Yes	No			Y			TREATMENT OF SCHIZOPHRENIA IN ADULTS

International Family Members for US Patent 10,406,161

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2012248038
Brazil	112013027235
Canada	2832663