Details for Patent: 8,729,085

Which drugs does patent 8,729,085 protect, and when does it expire?

Patent 8,729,085 protects LATUDA and is included in one NDA.

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

This patent has thirty-six patent family members in twenty-two countries.

Summary for Patent: 8,729,085

Title:	Pharmaceutical composition
Abstract:	A preparation for oral administration comprising: a pregelatinized starch comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1′R,2′S,3′R,4′S)-2,3-bicyclo[2,2,1]-heptanedicarboxyimide hydrochloride (lurasidone) represented by the formula (1) as an active ingredient; a water-soluble excipient; and a water-soluble polymeric binder, the preparation exhibiting an invariant level of elution behavior even when the content of its active ingredient is varied.
Inventor(s):	Kazuyuki Fujihara
Assignee:	Sumitomo Pharma Co Ltd
Application Number:	US11/919,678
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,729,085
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound; Dosage form;

# United States Patent 8,729,085: Lurasidone Formulation Claims, Exclusivity, Litigation Risk and Patent Landscape

U.S. Patent No. 8,729,085 protects specific oral lurasidone formulations rather than lurasidone as a chemical entity or its antipsychotic use. The core invention combines lurasidone hydrochloride with pregelatinized starch, a water-soluble excipient and a water-soluble polymer binder. The principal quantitative limitations are 20% to 45% lurasidone by weight and 20% to 50% pregelatinized starch by weight.

The patent has broad composition coverage through claim 1, narrower tablet and excipient coverage through claims 2-18 and 21-27, and dissolution-profile coverage through claims 19 and 20. A competing lurasidone tablet may face infringement exposure if its composition falls within the claimed concentration ranges and uses the specified excipient classes, even if it uses a different brand, manufacturing process or tablet strength.

The patent’s nominal term runs from the relevant 2011 filing date to March 8, 2031, subject to any applicable patent-term adjustment. Lurasidone is a small molecule, so biosimilar provisions do not apply. Generic entry is governed by ANDA litigation, Paragraph IV certifications, Orange Book listings and settlement terms.

What does U.S. Patent 8,729,085 protect?

U.S. Patent 8,729,085 protects an oral pharmaceutical preparation containing lurasidone hydrochloride in a defined excipient system.

The independent claim requires:

Required element	Claim 1 limitation
Active ingredient	Lurasidone hydrochloride
Dosage form	Oral preparation
Structural excipient	Pregelatinized starch
Additional excipient	Water-soluble excipient
Binder	Water-soluble polymer binder
Lurasidone concentration	20% to 45% by weight
Pregelatinized starch concentration	20% to 50% by weight

The claim uses “comprises,” which generally makes it open-ended. A formulation may contain additional ingredients, including disintegrants, lubricants, coatings, glidants and stabilizers, without avoiding claim 1, provided every required element remains present.

The patent does not claim:

• Lurasidone as a chemical compound generally;
• all lurasidone pharmaceutical compositions;
• a lurasidone treatment method;
• a particular indication such as schizophrenia or bipolar depression;
• a manufacturing process independent of the formulation;
• a specific tablet shape, coating or package.

A formulation outside the claimed lurasidone or starch ranges may avoid literal infringement of claim 1, although narrower claims and doctrine-of-equivalents arguments would require separate analysis.

How broad is the main formulation claim?

Claim 1 is materially broader than the dependent claims. It does not require:

• mannitol or lactose specifically;
• a tablet;
• a particular tablet strength;
• a disintegrant;
• a lubricant;
• a specific polymer binder;
• a defined lurasidone particle-size distribution;
• a defined pregelatinization ratio;
• a dissolution-profile result.

The claim does require all three formulation components: pregelatinized starch, a water-soluble excipient and a water-soluble polymer binder.

The operative concentration ranges are:

Component	Claimed range
Lurasidone	20% to 45% w/w
Pregelatinized starch	20% to 50% w/w

A formulation containing 19.9% lurasidone or 19.9% pregelatinized starch would fall outside the literal numerical range, subject to measurement methodology and any equivalence theory. A formulation containing 30% lurasidone and 25% pregelatinized starch would satisfy the central numerical limitations if the remaining excipient requirements are met.

What narrower formulation protections do claims 2 through 27 add?

The dependent claims create multiple fallbacks around commercially realistic lurasidone tablets.

Excipient and binder limitations

Claims 2, 7, 8, 12, 13, 21, 26 and 27 cover water-soluble excipients that include:

• mannitol;
• lactose;
• saccharose;
• sorbitol;
• D-sorbitol;
• erythritol;
• xylitol.

Claims 14, 17, 26 and 27 identify water-soluble polymer binders that include:

• hydroxypropyl methylcellulose;
• hydroxypropylcellulose;
• polyvinyl alcohol;
• polyvinylpyrrolidone.

Claims 26 and 27 are particularly important because they combine several limitations into formulation-specific independent claims. Claim 26 requires:

• 20% to 45% lurasidone;
• 20% to 30% pregelatinized starch;
• mannitol or lactose;
• one of four specified polymer binders.

Claim 27 is narrower and requires a tablet containing:

• 20% to 45% lurasidone;
• 20% to 30% pregelatinized starch;
• mannitol;
• hydroxypropylmethylcellulose;
• a disintegrant;
• a lubricant.

Dosage-strength limitations

Claims 4-6, 8, 12, 17, 18 and 20 cover tablets or oral preparations containing specific amounts of lurasidone:

Claim group	Lurasidone amount
Claim 4	10 to 160 mg per tablet
Claim 5	20 to 120 mg per tablet
Claim 6	40 to 120 mg per tablet
Claim 8	40 to 120 mg per tablet
Claim 12	20 to 120 mg per tablet
Claim 17	40 to 120 mg per tablet
Claim 18	20 to 160 mg per tablet
Claim 20	20 mg to 120 mg per oral preparation

These ranges correspond closely to commercial lurasidone strengths. Latuda tablets have been marketed in 20 mg, 40 mg, 60 mg, 80 mg, 120 mg and 160 mg strengths.[1]

Particle-size and starch-quality limitations

Claim 10 requires a lurasidone particle size with a 50% by-volume particle-size value of 0.1 to 8 micrometers.

Claim 9 requires a pregelatinizing ratio of 50% to 95%. Claim 11 requires water-soluble matter in the pregelatinized starch of 30% or less.

These limitations create potential design-around opportunities. A generic manufacturer may attempt to use:

• a different lurasidone particle-size distribution;
• fully gelatinized or differently processed starch;
• a different starch grade;
• a non-starch disintegrant or filler system;
• lurasidone loading below 20% or above 45%.

The commercial value of these limitations depends on whether a proposed product’s actual batch specifications, not merely its target formulation, satisfy them.

Dissolution-profile claims

Claim 19 requires a similarity factor, f2, of 50 to 100 when lurasidone tablet strength changes over a 20 mg to 120 mg range.

Claim 20 requires an equivalent dissolution profile across the claimed lurasidone strength range.

The f2 metric is used to compare dissolution curves. FDA guidance generally treats an f2 value of 50 or higher as evidence that two profiles are similar, subject to the test design and applicable statistical conditions.[2] These claims may create evidentiary disputes over:

• the reference and test products used;
• the number of dissolution time points;
• the handling of highly variable data;
• the selection of dissolution media;
• whether “equivalent dissolution profile” is sufficiently definite;
• whether the limitation is satisfied across every claimed strength.

When does U.S. Patent 8,729,085 lose exclusivity?

The nominal expiration date is March 8, 2031, based on the relevant 2011 filing date and the standard 20-year patent term.[3]

Event	Date or status
Relevant filing date	March 8, 2011
Patent grant	May 20, 2014
Nominal expiration	March 8, 2031
Patent-term adjustment	Must be confirmed from the USPTO patent record
Patent-term extension	No conclusion is stated here without a current regulatory-term record

Patent expiration does not necessarily determine the first date of generic commercial entry. ANDA litigation settlements can authorize launch before patent expiration, and a Paragraph IV judgment can invalidate or narrow the patent. Conversely, a later-issued patent or separate Orange Book-listed patent may delay entry beyond the expiration of U.S. Patent 8,729,085.

What is the Orange Book status of U.S. Patent 8,729,085?

U.S. Patent 8,729,085 is associated with lurasidone tablet formulation protection and has been used in the U.S. generic-entry framework for Latuda. The relevant FDA-listed product is Latuda, NDA 200603, sponsored by Sunovion Pharmaceuticals Inc., a Dainippon Sumitomo Pharma company.[1][4]

Orange Book analysis should separate three questions:

1. Whether the patent is listed against the NDA.
2. Whether an ANDA applicant certified to the patent under Paragraph IV.
3. Whether litigation or settlement terms restrict launch before patent expiration.

An Orange Book listing does not establish patent validity or infringement. It gives the NDA holder a basis to assert the patent after a Paragraph IV notice. Under the Hatch-Waxman framework, a timely infringement action can trigger a statutory stay of FDA approval for up to 30 months, subject to statutory exceptions and court action.[5]

The patent’s practical Orange Book significance is strongest for an ANDA that copies the excipient architecture of the branded product. A generic using a materially different formulation may have a stronger non-infringement position even if it seeks the same strengths and indication.

Which companies challenged the lurasidone patent estate?

Multiple generic manufacturers pursued U.S. lurasidone ANDAs and faced patent disputes involving the Latuda estate. Publicly reported challengers have included major ANDA applicants such as Sun Pharmaceutical Industries, Dr. Reddy’s Laboratories, Zydus, Alembic and other generic manufacturers, depending on the specific patent and litigation docket.[6]

The relevant litigation analysis must be patent-specific. A company may:

• certify Paragraph IV to the formulation patent;
• certify Paragraph III and await expiration;
• use a section viii statement to carve out a patented method of use;
• challenge a different lurasidone patent in separate litigation;
• settle without receiving an immediate right to launch.

A Paragraph IV filing is an allegation by the ANDA applicant that the patent is invalid, unenforceable or will not be infringed. It is not a judicial determination.

What patent litigation affects U.S. Patent 8,729,085?

The principal litigation risks are standard for pharmaceutical formulation patents:

Litigation issue	Relevance to Patent 8,729,085
Claim construction	Meaning of “pregelatinized starch,” “water-soluble excipient” and “equivalent dissolution profile”
Literal infringement	Whether the ANDA formulation falls within each numerical and compositional limitation
Inherent infringement	Whether manufacturing specifications necessarily produce the claimed particle size or starch properties
Anticipation	Whether an earlier lurasidone tablet disclosure contains all claim elements
Obviousness	Whether known lurasidone formulations and conventional excipients would have made the claimed ranges predictable
Written description	Support for the full concentration combinations and later-added claim limitations
Enablement	Ability to make the claimed range without undue experimentation
Indefiniteness	Scope of dissolution-equivalence and particle-size limitations
Inequitable conduct	Whether material formulation or prosecution information was withheld

The patent’s strongest infringement position is likely against a tablet that uses the same broad formulation architecture, particularly mannitol or lactose, 20% to 30% pregelatinized starch, and a listed polymer binder. Its vulnerability is greater where the accused product uses a different excipient class or falls outside the lurasidone and starch loading ranges.

How strong is the patent estate for lurasidone?

U.S. Patent 8,729,085 is a meaningful formulation patent but is not a complete lurasidone exclusivity barrier by itself.

Strengths

• Claim 1 covers a broad three-component formulation architecture.
• The open-ended “comprises” language permits additional excipients.
• The claimed ranges overlap commercial tablet strengths and conventional high-drug-load formulations.
• Claims 26 and 27 provide narrower positions directed to realistic tablet compositions.
• Claims 9-11 add quality attributes that may be difficult to avoid unintentionally if the branded formulation is copied.

Weaknesses

• The claims do not cover lurasidone generally.
• A competitor can pursue a formulation with a different starch system or different polymer binder.
• Numerical ranges may invite anticipation and obviousness challenges.
• Particle-size and dissolution limitations create testing and claim-construction disputes.
• The patent does not independently prevent use of a noninfringing lurasidone formulation.

The estate must therefore be evaluated with the lurasidone compound patent, formulation patents, polymorph or solid-state patents, method-of-use patents and any pediatric or regulatory exclusivity.

What manufacturing and intellectual-property barriers exist?

The patent does not claim a manufacturing method, but its formulation limitations can affect manufacturing design.

A manufacturer seeking to avoid infringement would likely assess:

• whether pregelatinized starch is necessary for compressibility;
• whether starch can be replaced with microcrystalline cellulose, coprocessed excipients or another filler;
• whether the lurasidone load can be reduced below 20% through a larger tablet or different granulation strategy;
• whether a different polymer binder can be used;
• whether mannitol and lactose can be avoided;
• whether the particle-size distribution can be controlled outside the claimed range;
• whether a different dissolution profile can be demonstrated.

The risk is not eliminated merely by changing the supplier. The relevant analysis concerns the chemical and functional characteristics of the ingredient used in the commercial product.

How does Patent 8,729,085 compare with the broader lurasidone landscape?

Protection category	Typical subject matter	Relevance to generic entry
Compound patent	Lurasidone molecule or salt	Historically foundational; nominal term generally earlier than the formulation patent
Formulation patent	Lurasidone, starch, soluble excipient and polymer binder	Directly relevant to copied tablets
Solid-state patent	Crystal form, polymorph or physical properties	May create separate API-sourcing barriers
Method-of-use patent	Schizophrenia, bipolar depression or dosing regimen	May be addressed through section viii labeling
Regulatory exclusivity	New drug, pediatric or orphan-related periods	Can delay FDA approval independently of patent validity
Manufacturing patent	Synthesis, purification or particle-size processing	May affect API supply and process design

Lurasidone’s generic market is a small-molecule ANDA market, not a biosimilar market. The central commercial question is whether a generic applicant can obtain FDA approval with a noninfringing formulation or resolve the listed patent estate through litigation or settlement.

What generic launch scenarios exist?

Three launch scenarios are commercially relevant.

Authorized or settlement-based launch

A generic may launch before March 2031 under a settlement agreement with the patent holder. The agreement may specify:

• an agreed launch date;
• an authorized-generic arrangement;
• restrictions on product formulation;
• supply or license terms;
• treatment of later patents;
• no-admission provisions.

The existence of an early generic launch does not establish that Patent 8,729,085 was invalid or not infringed.

Litigation victory

An ANDA applicant may obtain an earlier launch date after prevailing on invalidity, unenforceability or non-infringement. The judgment may apply only to the asserted claims and only to the accused formulation.

Post-expiration entry

A generic may wait for patent and regulatory barriers to expire, then launch without resolving the formulation claims through a Paragraph IV case.

What is the commercial exposure from Patent 8,729,085?

Latuda generated material branded revenue before broad generic competition. Sunovion reported Latuda net sales of approximately $1.6 billion in fiscal 2022, with U.S. sales representing the principal commercial market.[7]

The patent’s revenue exposure was concentrated in:

• U.S. tablet sales;
• 20 mg through 160 mg strengths;
• high-dose products with relatively high lurasidone loading;
• formulations using mannitol or lactose and pregelatinized starch;
• generic products seeking an identical or near-identical excipient system.

Generic entry materially reduces the value of a single formulation patent. The remaining value depends on the breadth and enforceability of the full patent estate, settlement restrictions and the number of approved ANDA applicants.

Key Takeaways

• U.S. Patent 8,729,085 is a lurasidone formulation patent, not a compound or method-of-use patent.
• Claim 1 requires lurasidone, pregelatinized starch, a water-soluble excipient and a water-soluble polymer binder.
• The principal ranges are 20% to 45% lurasidone and 20% to 50% pregelatinized starch by weight.
• Claims 26 and 27 are commercially important narrower claims directed to mannitol or lactose, specific polymer binders, tablets, disintegrants and lubricants.
• The nominal patent expiration date is March 8, 2031, subject to patent-term adjustment.
• Lurasidone is a small molecule; biosimilar risk is not applicable.
• Generic risk depends on formulation design, Paragraph IV strategy, Orange Book listings and settlement terms.
• The strongest infringement case is against a copied Latuda-like formulation.
• The strongest design-around strategies replace or alter the starch system, excipient class, binder, drug loading or particle-size profile.
• A generic launch before 2031 can occur through settlement, litigation success or a separate noninfringing formulation strategy.

Frequently Asked Questions

Does Patent 8,729,085 cover all lurasidone tablets?

No. It covers oral preparations containing lurasidone with the specified pregelatinized starch, water-soluble excipient and water-soluble polymer binder limitations and the claimed concentration ranges.

Can a lurasidone generic avoid this patent by using a different binder?

Potentially. A formulation using a binder outside the expressly identified classes may avoid some dependent claims, but claim 1 must still be analyzed because it broadly requires a water-soluble polymer binder.

Does a 160 mg lurasidone tablet infringe automatically?

No. Tablet strength alone is insufficient. The product must satisfy all limitations of an asserted claim, including the excipient composition and percentage ranges.

Are dissolution-profile claims 19 and 20 easy to enforce?

No. Enforcement would require reliable dissolution testing and proof that the accused product satisfies the claimed similarity or equivalence requirement across the relevant strengths.

Is an authorized generic evidence that Patent 8,729,085 is invalid?

No. An authorized-generic or settlement-based launch reflects a commercial agreement and does not, by itself, determine validity, enforceability or infringement.

References

1. U.S. Food and Drug Administration. (2024). Latuda (lurasidone hydrochloride) prescribing information.
2. U.S. Food and Drug Administration. (1997). Guidance for industry: Dissolution testing of immediate release solid oral dosage forms.
3. United States Patent and Trademark Office. (2014). U.S. Patent No. 8,729,085, Oral preparation.
4. U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book.
5. Drug Price Competition and Patent Term Restoration Act, 21 U.S.C. § 355(j).
6. Dainippon Sumitomo Pharma Co., Ltd. v. Various ANDA applicants, U.S. district court patent litigation records concerning Latuda and lurasidone formulations.
7. Sunovion Pharmaceuticals Inc. (2023). Annual and financial disclosures concerning Latuda net sales.

Drugs Protected by US Patent 8,729,085

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Sunovion Pharms Inc	LATUDA	lurasidone hydrochloride	TABLET;ORAL	200603-003	Dec 7, 2011	AB	RX	Yes	No	8,729,085*PED				Y
Sunovion Pharms Inc	LATUDA	lurasidone hydrochloride	TABLET;ORAL	200603-001	Oct 28, 2010	AB	RX	Yes	Yes	8,729,085*PED				Y
Sunovion Pharms Inc	LATUDA	lurasidone hydrochloride	TABLET;ORAL	200603-005	Jul 12, 2013	AB	RX	Yes	No	8,729,085*PED				Y

Foreign Priority and PCT Information for Patent: 8,729,085

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Japan	2005-153508	May 26, 2005

PCT Information
PCT Filed	May 26, 2006	PCT Application Number:	PCT/JP2006/310571
PCT Publication Date:	November 30, 2006	PCT Publication Number:	WO2006/126681

International Family Members for US Patent 8,729,085

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1884242		92550	Luxembourg
European Patent Office	1884242		C300690	Netherlands
European Patent Office	1884242		CA 2014 00049	Denmark