Details for Patent: 11,026,951

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Which drugs does patent 11,026,951 protect, and when does it expire?

Patent 11,026,951 protects CAPLYTA and is included in one NDA.

This patent has fifty-three patent family members in sixteen countries.

Summary for Patent: 11,026,951

Title:	Methods of treating bipolar disorder
Abstract:	The disclosure provides the use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of residual symptoms of psychosis or schizophrenia. The disclosure also provides novel long acting injectable formulations of particular substituted heterocycle fused gamma-carboline compounds and use of such long acting injectable formulations for the treatment of residual symptoms of psychosis or schizophrenia.
Inventor(s):	Kimberly Vanover, Peng Li, Sharon Mates, Robert Davis, Lawrence P. Wennogle
Assignee:	Intra Cellular Therapies Inc
Application Number:	US16/507,956
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 11,026,951
Patent Claim Types: see list of patent claims	Use;

US Patent 11,026,951: Lumateperone Bipolar Disorder Patent Scope, Expiration and Generic Risk

US Patent No. 11,026,951 protects the use of lumateperone, including lumateperone tosylate, as a single antipsychotic treatment for bipolar I or bipolar II disorder. The strongest commercial coverage is directed to once-daily 60 mg lumateperone tosylate, equivalent to approximately 41.7 mg of lumateperone free base, for bipolar depression without combination use of another antipsychotic.

The patent is a method-of-use patent. It does not broadly protect the lumateperone molecule, its core composition of matter, or every lumateperone formulation. Its practical value depends on the approved label, Orange Book listing, ANDA certifications and whether a generic applicant can design around the bipolar indication or dosage limitations.

What drug does US Patent 11,026,951 protect?

US 11,026,951 covers lumateperone treatment for bipolar disorder. The compound identified by Formula I, where X is —N(CH3)— and Y is —C(O)—, is lumateperone.

The commercially relevant product is Caplyta, marketed by Intra-Cellular Therapies, Inc. The active pharmaceutical ingredient is lumateperone tosylate, also known as lumateperone toluenesulfonate.

Patent element	Scope under US 11,026,951
Active compound	Lumateperone
Salt form	Free base or pharmaceutically acceptable salt
Specifically claimed salt	Toluenesulfonic acid addition salt, or lumateperone tosylate
Disease	Bipolar I and bipolar II disorder
Disease manifestation	Bipolar depression and bipolar disorder with psychotic symptoms
Dose range	20 mg to 60 mg per day, measured as free-base equivalent
Preferred dose	40 mg to 60 mg per day
Specific salt dose	60 mg lumateperone tosylate once daily, equivalent to about 41.7 mg free base
Combination limitation	Claim 1 excludes use with another antipsychotic agent
Monotherapy limitation	Dependent claims require the compound to be the sole therapeutic agent
Safety limitations	Certain claims require no hyperprolactinemia, EPS/akathisia, weight gain or cardiovascular side effects

The patent claims a treatment method rather than a product standing alone. A party generally risks direct method infringement when it administers lumateperone to a patient for a claimed bipolar indication in a claimed dose and form.

What are the independent and dependent claims?

Claim 1: Core bipolar treatment method

Claim 1 is the principal broad claim. It requires:

1. A patient in need of treatment.
2. Bipolar I and/or bipolar II disorder.
3. Administration of an effective amount of lumateperone.
4. Lumateperone in free-base or pharmaceutically acceptable salt form.
5. No combination with another antipsychotic agent.

The claim does not require the patient to have bipolar depression, psychotic symptoms or a particular dose. Those features appear in dependent claims.

The “not used in combination with another antipsychotic agent” limitation materially narrows the claim. It leaves potential room for treatment involving lumateperone plus a non-antipsychotic medicine, such as a mood stabilizer or antidepressant, depending on the facts and the scope of the relevant dependent claims.

Claims 2 and 3: Salt-form protection

Claim 2 covers pharmaceutically acceptable salt forms. Claim 3 narrows the protection to the toluenesulfonic acid addition salt.

Claim 3 is commercially important because Caplyta is supplied as lumateperone tosylate capsules. A generic applicant seeking approval for the same salt and the bipolar indication would face a direct overlap with the claimed product-use combination.

Claims 4 and 5: Bipolar I and bipolar II

Claims 4 and 5 separately cover treatment of bipolar I and bipolar II disorder. This prevents a generic applicant from avoiding the entire patent simply by omitting one subtype from its proposed labeling.

The claims distinguish the two disorders but do not require a particular episode type in these claims. Claims 11 through 18 focus more specifically on bipolar depression.

Claims 6 through 9: Dose and administration

The dosing claims create a commercially relevant hierarchy:

Claim	Dose limitation
6	20 mg to 60 mg per day, free-base equivalent
7	40 mg to 60 mg per day, free-base equivalent
8	About 40 mg per day, free-base equivalent
9	60 mg tosylate once daily, equivalent to about 41.7 mg free base

Claim 9 is particularly tailored to Caplyta’s marketed 60 mg capsule. The free-base conversion matters because lumateperone tosylate weighs more than the corresponding lumateperone free base.

A generic applicant could attempt to avoid claims 6 through 9 by proposing a dose below 20 mg, above 60 mg, a different salt, or a different administration schedule. That approach would not necessarily avoid claim 1, which does not specify a dose, or other patents covering the active ingredient, formulation or broader bipolar use.

Claims 10 through 18: Clinical presentation and bipolar depression

These claims cover:

• Bipolar disorder with psychotic symptoms.
• Bipolar depression.
• Treatment of depressive symptoms.
• Bipolar I depression.
• Bipolar II depression.
• The 60 mg tosylate regimen for bipolar I or bipolar II depression.

These claims are closely aligned with the FDA-approved bipolar depression use of Caplyta. They strengthen enforcement against a generic product whose labeling expressly identifies bipolar depression.

Claims 19 and 21: Sole therapeutic agent

Claims 19 and 21 require lumateperone to be administered as the sole therapeutic agent for bipolar disorder.

These claims are narrower than claim 1. Claim 1 prohibits combination with another antipsychotic, but does not necessarily require lumateperone to be the only therapeutic medicine. Claims 19 and 21 impose the stronger monotherapy limitation.

Claims 20, 22, 23 and 24: Safety outcomes

These claims require that treatment does not result in specified adverse outcomes, including:

• Hyperprolactinemia.
• EPS or akathisia.
• Weight gain.
• Cardiovascular side effects.

Claims 20 and 22 contain the broadest adverse-event combination. Claims 23 and 24 focus on EPS/akathisia and weight gain.

These limitations may be difficult to enforce in practice because infringement can depend on clinical outcomes in individual patients. They also create potential validity issues concerning whether the patent adequately describes and enables the claimed absence of adverse events across the full scope of the method.

How strong is the patent estate for Caplyta and lumateperone?

US 11,026,951 is important but is only one layer of the Caplyta patent estate.

Protection category	Relevance to Caplyta
Composition of matter	Protects lumateperone or related chemical matter; generally stronger than a later method patent
Salt and solid-state protection	Can cover lumateperone tosylate, polymorphs or crystalline forms
Formulation protection	May cover capsule composition, excipients, release profile or manufacturing attributes
Method of use	US 11,026,951 covers bipolar disorder treatment
FDA exclusivity	Regulatory exclusivity is separate from patent protection
Manufacturing protection	May cover synthesis, purification or salt formation

The earliest composition patents for lumateperone reportedly trace to the 2008 priority period. Continuations and later method patents extend the commercial estate beyond the basic chemical patent term. US 11,026,951 has a nominal term running from its effective filing or priority framework into approximately December 2036, subject to the official patent-term calculation, patent-term adjustment and any applicable terminal disclaimer. The USPTO patent record and FDA Orange Book control the operative expiration date.[1][2]

The patent is strongest when all of the following align:

• The product is lumateperone tosylate.
• The patient has bipolar I or bipolar II disorder.
• The indication is bipolar depression.
• The dose is 60 mg once daily.
• The use is monotherapy or excludes another antipsychotic.
• The product labeling identifies the protected indication.

The patent is weaker against use outside the claimed disease, dose, salt or treatment conditions. That does not eliminate risk because other Caplyta patents may cover the same product independently.

What is the Orange Book status of US 11,026,951?

US 11,026,951 is associated with Caplyta’s bipolar disorder use and is relevant to the Orange Book patent landscape for lumateperone capsules. FDA Orange Book listings for method-of-use patents use patent-use codes to connect a patent with a labeled indication rather than to claim every use of the active ingredient.[2]

An Orange Book listing has three commercial consequences:

1. An ANDA applicant must address the listed patent.
2. The applicant may submit a Paragraph III certification, Paragraph IV certification or, where applicable, a statement that the patent does not claim the reference product or an approved use.
3. A timely Paragraph IV notice can trigger Hatch-Waxman litigation and a potential 30-month stay of approval under the statutory conditions.[3]

A method patent does not necessarily block an ANDA for every indication. A generic applicant may pursue a “skinny label” that omits a patented use, but the commercial and litigation outcome depends on labeling language, prescribing behavior, product distribution and induced-infringement theories.

When does Caplyta lose regulatory and patent exclusivity?

Caplyta received FDA approval for schizophrenia on December 20, 2019. FDA later approved lumateperone for bipolar depression, including bipolar depression associated with bipolar I or bipolar II disorder, in December 2021.[4]

Milestone	Date or period
Initial FDA approval for schizophrenia	December 20, 2019
FDA approval for bipolar depression	December 2021
Five-year new chemical entity exclusivity	Approximately through December 2024
US 11,026,951 grant date	June 8, 2021
Estimated nominal term for US 11,026,951	Approximately December 2036, subject to official PTA and terminal-disclaimer data
Generic entry	Potentially before patent expiry only through a successful challenge, settlement license or non-infringing label

The 2019 approval date controls the original five-year NCE exclusivity period. The 2021 bipolar approval did not create a new five-year NCE period because it was a supplemental approval for the same active ingredient.

A three-year exclusivity period may apply to qualifying clinical investigations supporting the bipolar indication, but that period is distinct from the NCE period and does not independently establish the patent term.[4]

Which companies are challenging Caplyta patents?

Publicly disclosed ANDA activity and litigation involving lumateperone should be assessed patent-by-patent and defendant-by-defendant. The relevant challenge would normally involve a Paragraph IV certification against one or more listed Caplyta patents.

The key litigation questions are:

• Whether the ANDA applicant challenges US 11,026,951.
• Whether it also challenges composition, salt, formulation or manufacturing patents.
• Whether the proposed label includes bipolar depression.
• Whether a court accepts a carve-out of the patented indication.
• Whether the case is resolved by settlement before trial.

A single patent loss would not necessarily authorize generic launch. The generic applicant would still need to address every blocking Orange Book patent and any non-Orange Book patent that could support separate infringement litigation.

No biosimilar pathway applies. Lumateperone is a synthetic small molecule, so competitive entry would occur through an ANDA under section 505(j), not through a biosimilar application under the Biologics Price Competition and Innovation Act.[3]

What Paragraph IV launch scenarios exist for lumateperone?

Scenario 1: Full-label generic challenge

The applicant seeks approval for schizophrenia and bipolar depression. It certifies Paragraph IV against listed patents, including the bipolar-use patent.

Risk to the branded product is highest under this scenario because the generic label directly overlaps with the claimed bipolar indication.

Scenario 2: Carved-out bipolar indication

The applicant omits bipolar depression from its label and seeks approval for an unpatented or less heavily patented indication, such as schizophrenia.

This approach can reduce formal label overlap. It does not eliminate risk if the generic is marketed, promoted or distributed for the carved-out use, or if the branded company proves induced infringement.

Scenario 3: Post-expiry launch

The applicant accepts the listed patents and files Paragraph III certifications. Launch occurs after the latest blocking patent expires or after a licensed date under settlement.

This is the lowest litigation-risk route but may delay entry until the later method, formulation or salt patents expire.

Scenario 4: Settlement with an authorized generic or license

A settlement may establish an agreed launch date before patent expiration, subject to antitrust scrutiny and the terms filed with the Federal Trade Commission and Department of Justice where required.

The existence of a settlement does not itself establish patent validity. The operative date and permitted label must be reviewed.

How does US 11,026,951 compare with competing bipolar drugs?

Drug	Active ingredient	Bipolar use	Patent profile
Caplyta	Lumateperone	Bipolar depression, bipolar I and II; schizophrenia	Composition, formulation and method-of-use estate
Vraylar	Cariprazine	Bipolar mania, mixed episodes and bipolar depression	Multiple method and formulation patents
Latuda	Lurasidone	Bipolar depression and schizophrenia	Earlier-generation patent estate; generic entry has materially changed competition
Seroquel XR	Quetiapine fumarate	Bipolar depression, mania and maintenance	Core patent protection largely mature
Rexulti	Brexpiprazole	Schizophrenia and adjunctive major depressive disorder	Different indication profile and patent estate

US 11,026,951 gives Caplyta targeted protection for bipolar disorder, especially bipolar depression and the 60 mg tosylate regimen. It does not provide the broad indication breadth of a composition-of-matter patent.

What manufacturing and geographic barriers remain?

The patent covers administration and treatment, not every manufacturing step. A competitor could still face separate barriers involving:

• Lumateperone synthesis.
• Chiral control and impurity limits.
• Formation of lumateperone tosylate.
• Crystalline or polymorphic forms.
• Capsule filling and stability.
• Analytical methods.
• FDA chemistry, manufacturing and controls requirements.

US 11,026,951 has territorial effect only in the United States. Separate patent families may apply in Europe, Canada, Japan, China and other markets. FDA approval does not create international patent rights, and foreign launch timing depends on national patent registers, regulatory exclusivity and local litigation.

Key Takeaways

• US 11,026,951 is a targeted method-of-use patent for lumateperone treatment of bipolar I and bipolar II disorder.
• The commercial center of gravity is lumateperone tosylate 60 mg once daily, equivalent to approximately 41.7 mg free base.
• The patent covers bipolar depression, depressive symptoms and bipolar disorder with psychotic symptoms.
• Claim 1 excludes combination with another antipsychotic; separate claims require monotherapy.
• The patent does not independently protect the lumateperone molecule or every Caplyta formulation.
• The nominal patent term extends to approximately December 2036, subject to the official USPTO term calculation.
• Generic entry depends on the full Caplyta patent estate, not this patent alone.
• A skinny-label strategy may reduce direct overlap but does not eliminate induced-infringement risk.
• Lumateperone is a small molecule. Generic competition uses the ANDA pathway, not a biosimilar pathway.
• The patent’s commercial strength is high for a labeled 60 mg bipolar depression use and lower for off-label, non-bipolar, non-tosylate or non-labeled dosing.

FAQs About US Patent 11,026,951 and Caplyta

Does US 11,026,951 cover Caplyta for schizophrenia?

No. The supplied claims are directed to bipolar I and bipolar II disorder. Separate patents and regulatory protections may cover lumateperone for schizophrenia.

Does the patent cover lumateperone used with lithium or valproate?

The claims exclude combination with another antipsychotic, not every combination with another medicine. The precise infringement analysis depends on the treatment regimen and the scope of other claims.

Can a generic launch Caplyta before 2036?

Yes, but only if it prevails in patent litigation, obtains a license or settlement right, uses a legally effective carved-out label, or otherwise avoids the relevant blocking patents.

Is lumateperone eligible for biosimilar competition?

No. Lumateperone is a synthetic small-molecule drug. Competition proceeds through an ANDA rather than a biosimilar application.

Does the 60 mg Caplyta capsule directly practice claim 9?

A 60 mg lumateperone tosylate capsule administered once daily for a claimed bipolar disorder use corresponds closely to the limitations recited in claim 9.

References

1. United States Patent and Trademark Office. (2021). U.S. Patent No. 11,026,951, Methods of treating bipolar disorder.
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. (n.d.). Abbreviated new drug application approvals and patent certifications under the Hatch-Waxman Act.
4. U.S. Food and Drug Administration. (2019, December 20). FDA approves new drug for schizophrenia: Caplyta (lumateperone); U.S. Food and Drug Administration. (2021, December). Caplyta prescribing information.

Drugs Protected by US Patent 11,026,951

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Intra-cellular	CAPLYTA	lumateperone tosylate	CAPSULE;ORAL	209500-002	Apr 22, 2022		RX	Yes	No						TREATMENT OF BIPOLAR DISORDER I, BIPOLAR DISORDER II, OR BIPOLAR DEPRESSION
Intra-cellular	CAPLYTA	lumateperone tosylate	CAPSULE;ORAL	209500-003	Apr 22, 2022		RX	Yes	No						TREATMENT OF BIPOLAR DISORDER I, BIPOLAR DISORDER II, OR BIPOLAR DEPRESSION
Intra-cellular	CAPLYTA	lumateperone tosylate	CAPSULE;ORAL	209500-001	Dec 20, 2019		RX	Yes	Yes						TREATMENT OF BIPOLAR I DISORDER, BIPOLAR II DISORDER, OR BIPOLAR DEPRESSION

International Family Members for US Patent 11,026,951

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2014360452
Australia	2019200301
Australia	2020202386