Details for Patent: 10,940,141

Which drugs does patent 10,940,141 protect, and when does it expire?

Patent 10,940,141 protects INGREZZA and INGREZZA SPRINKLE and is included in two NDAs.

This patent has thirty patent family members in twenty-five countries.

Summary for Patent: 10,940,141

Title:	Methods for the administration of certain VMAT2 inhibitors
Abstract:	Provided is a method of administering a vesicular monoamine transporter 2 (VMAT2) inhibitor to a subject in need thereof, wherein the subject has severe renal impairment.
Inventor(s):	Gordon Raphael Loewen, Sha Rosa Luo
Assignee:	Neurocrine Biosciences Inc
Application Number:	US16/989,206
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,940,141
Patent Claim Types: see list of patent claims	Use; Dosage form;

US Patent 10,940,141: Valbenazine Renal-Impairment Claims, Patent Scope and Competitive Landscape

US Patent 10,940,141 protects methods of treating tardive dyskinesia with valbenazine in patients with severe renal impairment, generally defined as creatinine clearance below 30 mL/min. The patent’s principal commercial limitation is a same-dose requirement: treatment continues at the dose used for patients with normal renal function. The claims cover valbenazine free base and pharmaceutically acceptable salts, including valbenazine ditosylate and polymorphic Form I, administered orally as tablets or capsules.

The patent is a method-of-use patent rather than a broad compound patent. Its strongest coverage concerns treatment of tardive dyskinesia in severe renal impairment at 40 mg, 60 mg, or 80 mg once daily, and continuation of therapy after renal impairment is identified. The claims do not cover every use of valbenazine, every patient with renal impairment, or every VMAT2 inhibitor.

What drug and therapeutic use does US 10,940,141 cover?

The chemical entity described in the claims is valbenazine, the active pharmaceutical ingredient in Ingrezza. The claims use the full chemical name rather than the United States Adopted Name. Valbenazine is a VMAT2 inhibitor approved by the FDA for treatment of tardive dyskinesia and chorea associated with Huntington's disease.

The patent claims treatment of tardive dyskinesia, not the treatment of Huntington's disease chorea. A competing or follow-on product used solely for Huntington's disease chorea would not fall within the claims unless the use also satisfied the claimed tardive-dyskinesia limitations.

Claim element	Required limitation
Disease	Tardive dyskinesia
Active agent	Valbenazine or a pharmaceutically acceptable salt
Patient population	Severe renal impairment
Renal threshold	Creatinine clearance below 30 mL/min in dependent claims
Dose concept	Same therapeutically effective amount used in normal renal function
Specific doses	40 mg, 60 mg, or 80 mg valbenazine free-base equivalent once daily
Dosage form	Tablet or capsule in dependent claims
Exposure limitation	Substantially similar Cmax or AUC0-∞ compared with normal renal function
Administration route	Oral administration in claim 14 and its dependents

The patent therefore targets a specific prescribing scenario: a patient receiving valbenazine for tardive dyskinesia who has severe renal impairment, or who is subsequently found to have severe renal impairment.

How many independent claims does US 10,940,141 have?

The patent has three independent method claims: claims 1, 14, and 27. Each creates a different infringement theory.

Claim 1: treatment at the normal-renal-function dose

Claim 1 requires:

1. A patient with tardive dyskinesia.
2. Administration of valbenazine or a pharmaceutically acceptable salt.
3. Severe renal impairment.
4. Administration of the same therapeutically effective amount used for a patient with normal renal function.

Claims 2 through 13 narrow claim 1 by specifying dose, dosage form, salt, polymorph, renal threshold, exposure, and clearance characteristics.

The central legal issue is the meaning of “the same amount.” The phrase ties the renal-impaired patient’s dose to the dose used in a comparator patient with normal renal function. A product label that expressly recommends the same dose in severe renal impairment would create a direct regulatory and litigation concern. A label that recommends no treatment, dose reduction, or a different dosing regimen would present a stronger non-infringement position, although actual prescribing conduct could still create induced-infringement exposure.

Claim 14: continuation after renal impairment is identified

Claim 14 covers a sequence:

1. Oral administration of valbenazine for tardive dyskinesia.
2. Subsequent determination that the patient has severe renal impairment.
3. Continued administration of the same therapeutically effective amount.

This claim is directed to clinical management after diagnosis or test results reveal severe renal impairment. It does not require that renal impairment be known before the first dose.

Claims 15 through 26 narrow the claim to tablets or capsules, salts, Form I ditosylate, specified doses, creatinine clearance below 30 mL/min, similar exposure, and lack of primary renal clearance.

Claim 27: titration followed by continued treatment

Claim 27 covers a more specific treatment sequence:

1. An initial dose equivalent to 40 mg once daily for one week.
2. An increase to 80 mg once daily after one week.
3. A subsequent determination of severe renal impairment.
4. Continued administration of a therapeutically effective amount.

Claim 27 is narrower than claims 1 and 14 because it requires the specified titration sequence. Claims 28 through 30 narrow the salt and post-diagnosis dose.

What formulations and chemical forms are protected?

The claims do not independently protect a new chemical compound or a new solid form. Instead, the formulation and salt limitations appear as dependent claim restrictions.

Valbenazine free base equivalent

The 40 mg, 60 mg, and 80 mg amounts are expressed as free-base equivalents. This is important because a ditosylate salt tablet contains more total molecular weight than the corresponding amount of valbenazine free base. Infringement analysis would therefore require conversion of the marketed salt dose to the claimed free-base equivalent.

The claims cover:

• About 40 mg once daily.
• About 60 mg once daily.
• About 80 mg once daily.

The word “about” creates an ordinary claim-construction issue. A competing product with a nominally different strength could still be within scope if its dose falls within the accepted range for “about” the claimed amount and otherwise satisfies the claim.

Ditosylate salt

Claims 7, 8, 17, and 18 specifically identify the ditosylate salt and polymorphic Form I. The dependent claims strengthen product-specific coverage because the approved valbenazine product is administered as a ditosylate salt.

A generic manufacturer using the same salt and polymorphic form would face a narrower but more product-specific claim set. A different salt or solid form could avoid those dependent claims, but it would remain exposed to the broader independent claims if the method otherwise uses valbenazine or a pharmaceutically acceptable salt.

Tablet and capsule dosage forms

Claims 5 and 15 expressly cover tablets and capsules. The dosage-form limitation is absent from the independent claims. A tablet or capsule therefore falls within the broader claims without reliance on the dosage-form dependents, assuming the remaining elements are met.

What is the renal-impairment limitation?

The patent uses two related renal concepts:

• Severe renal impairment as a condition in the independent claims.
• Creatinine clearance below 30 mL/min in claims 9 and 22.

The independent claims do not expressly define severe renal impairment by creatinine clearance. A court could interpret the term using the specification, clinical practice, FDA labeling, and the patent’s prosecution history. The dependent claims provide a clear numerical embodiment but do not necessarily limit the independent claims to that threshold.

Claims 10 through 12 and 23 through 25 add pharmacokinetic limitations. The claimed exposure must be substantially similar between severe renal impairment and normal renal function, measured by:

• Cmax.
• AUC0-∞.
• Both the parent drug and active metabolite [+]-α-HTBZ.

These exposure claims could create proof issues. A patent owner would likely need patient-level or population-level pharmacokinetic evidence showing substantial similarity under the claimed regimen. “Substantially similar” is less precise than a fixed numerical ratio and may be contested under written-description, enablement, definiteness, or infringement theories.

When does US 10,940,141 lose exclusivity?

US 10,940,141 was issued on March 9, 2021, according to USPTO patent records. Its expected basic patent-term endpoint is in 2038, based on the patent’s underlying priority and filing history. The exact enforceable expiration date depends on the patent’s term calculation, including any patent-term adjustment and terminal disclaimer information recorded by the USPTO.

Event	Date or status
Patent	US 10,940,141
Issue date	March 9, 2021
Patent type	Method-of-use patent
Drug	Valbenazine
Core indication	Tardive dyskinesia
Core population	Severe renal impairment
Expected term period	Through approximately 2038, subject to official USPTO term data
Patent-term extension	Not established from the supplied claim information
Regulatory exclusivity	Separate from patent term and determined under FDA statutes

Patent expiration does not automatically establish generic launch permission. A generic applicant may challenge the patent earlier through an ANDA Paragraph IV certification, obtain an at-risk launch, or negotiate a settlement with the patent owner.

What is the Orange Book status of US 10,940,141?

Orange Book listing is a regulatory question separate from patent validity. A patent can be legally enforceable without being listed in the Orange Book, although an unlisted patent generally does not trigger the same FDA approval stay associated with an ANDA Paragraph IV certification.

For Ingrezza, the relevant listing analysis should distinguish:

1. Drug-substance patents covering valbenazine.
2. Salt or solid-form patents.
3. Formulation patents.
4. Method-of-use patents covering tardive dyskinesia.
5. Renal-impairment method patents such as US 10,940,141.

If US 10,940,141 is listed with an FDA use code covering treatment of tardive dyskinesia in severe renal impairment, an ANDA applicant could be required to address it through a Paragraph IV certification or a section viii statement, depending on the proposed label. A section viii carve-out would be difficult if the approved label instructs use of the same dose in severe renal impairment.

FDA’s Approved Drug Products with Therapeutic Equivalence Evaluations and the patent-and-exclusivity information submitted by the New Drug Application holder are the controlling sources for current Orange Book status.[1]

Which companies are challenging valbenazine exclusivity?

The relevant competitive set includes generic manufacturers seeking approval for valbenazine products and Neurocrine Biosciences, the commercial sponsor of Ingrezza. Publicly reported challenge status must be separated into three categories:

Challenge type	Business effect
Paragraph IV certification	Creates patent-litigation risk and can trigger a statutory approval stay
Paragraph III certification	Accepts patent validity and delays approval until patent expiration
Section viii statement	Attempts to omit a patented method from the generic label

The supplied patent information does not identify a specific ANDA applicant, Paragraph IV notice, district-court complaint, settlement, or license agreement. No particular challenger or settlement should be treated as established solely from the claims.

The most commercially relevant challenge would involve an ANDA for valbenazine ditosylate tablets that includes the tardive-dyskinesia indication and does not carve out severe renal impairment. Such an ANDA could implicate claims 1, 2, 3, 4, 5, 6, and 7, depending on the salt and dose. A label that expressly directs 40 mg, 60 mg, or 80 mg once-daily treatment in patients with creatinine clearance below 30 mL/min would present the highest risk.

What generic launch risks exist?

Full-label generic launch

A full-label generic would face the broadest exposure. The product would likely be indicated for tardive dyskinesia and administered in the same oral dosage forms and strengths as Ingrezza. Claims 1 and 14 could be asserted even if the generic label does not reproduce every dependent limitation.

Renal-impairment carve-out

A carve-out excluding severe renal impairment could reduce label-based induced infringement. The strategy would be less effective if:

• The FDA requires renal-impairment language for safe and effective use.
• Prescribers receive the renal-impairment information through other approved labeling.
• The generic’s marketing, medical information, or promotional materials encourage the patented use.
• The product is clinically useful for the patented population and the manufacturer expects that use.

At-risk launch

An at-risk launch before resolution of patent litigation could expose the generic manufacturer to damages, an injunction, and possible market disruption. The commercial attractiveness would depend on Ingrezza sales, the number of generic entrants, the probability of invalidity or non-infringement, and the remaining patent term.

How strong is the patent estate for valbenazine?

US 10,940,141 has moderate strength as a targeted method-of-use patent and weaker breadth than a compound or composition patent.

Strength factor	Assessment
Disease limitation	Narrow; limited to tardive dyskinesia
Patient limitation	Narrow; severe renal impairment required
Dose coverage	Useful commercial coverage at 40, 60, and 80 mg
Product coverage	Stronger for ditosylate Form I
Independent claims	Three distinct treatment-sequence theories
Pharmacokinetic claims	Potentially valuable but fact-intensive
Compound exclusivity	Not provided by this patent
Formulation exclusivity	Only through dependent method claims
Design-around potential	Possible through renal dosing, label, salt, or use restrictions
Litigation leverage	Highest if FDA labeling requires same-dose use

The most defensible commercial value lies in the combination of a labeled tardive-dyskinesia indication, severe renal impairment, and continued same-dose treatment. The claims are less useful against products that omit the patented population from the label or use a different clinical protocol.

How does valbenazine compare with competing VMAT2 drugs?

Product	Active ingredient	TD indication	Renal-impairment patent issue
Ingrezza	Valbenazine	Yes	US 10,940,141 targets same-dose use in severe renal impairment
Austedo	Deutetrabenazine	Yes	Separate compound, formulation, and method-of-use estate
Xenazine	Tetrabenazine	Yes	Older active ingredient and separate patent position

Valbenazine and deutetrabenazine compete directly in tardive dyskinesia. US 10,940,141 does not block deutetrabenazine because the claims require valbenazine. A competing VMAT2 inhibitor would face its own regulatory, formulation, dosing, and method-of-use patent landscape.

Biosimilar risk is not applicable in the ordinary statutory sense. Valbenazine is a chemically synthesized small molecule, not a biologic. Competitive entry would generally proceed through the ANDA pathway rather than the biosimilar pathway under section 351(k) of the Public Health Service Act.

What manufacturing and geographic barriers remain?

The claims do not independently block manufacture of valbenazine outside the claimed treatment context. They are method claims. Manufacturing risk would instead arise from separate patents covering:

• Valbenazine synthesis.
• Chiral resolution or stereochemical control.
• Ditosylate salt formation.
• Polymorphic Form I.
• Tablet composition.
• Manufacturing processes.
• Analytical controls and impurity profiles.

US 10,940,141 is enforceable only in the United States. It does not itself provide protection in Europe, Japan, China, Canada, or other jurisdictions. Foreign counterparts must be analyzed separately for national-phase status, granted claims, term, supplementary protection certificates, and local litigation.

What patent litigation and settlement issues matter?

The patent’s litigation value will turn on four issues:

1. Whether severe renal impairment is required to appear in the generic label.
2. Whether “same amount” is sufficiently definite and supported.
3. Whether the accused regimen produces substantially similar exposure.
4. Whether the patent is listed in the Orange Book and properly supports a Paragraph IV suit.

Potential validity challenges could target written description, enablement, indefiniteness, obviousness, and anticipation. The renal-dose discovery may be attacked as an obvious application of known valbenazine pharmacokinetics, while the patent owner would rely on the claimed clinical finding that severe renal impairment permits the same effective dose and produces comparable exposure.

No specific settlement agreement is established by the supplied material. If a settlement exists, its commercial terms would control the earliest licensed generic-entry date and could materially change the patent’s practical value.

Key Takeaways

• US 10,940,141 is a targeted valbenazine method-of-use patent.
• Its core population is patients with tardive dyskinesia and severe renal impairment.
• Claims 1 and 14 cover same-dose treatment and continuation after renal impairment is identified.
• Claim 27 covers a 40 mg-to-80 mg titration sequence followed by continued treatment.
• Dependent claims cover 40 mg, 60 mg, and 80 mg once-daily doses, tablets or capsules, ditosylate salt, and ditosylate Form I.
• The patent does not claim the valbenazine molecule generally.
• Generic exposure is greatest for a full-label ANDA that expressly permits same-dose valbenazine treatment at creatinine clearance below 30 mL/min.
• Biosimilar competition is not the relevant pathway because valbenazine is a small molecule.
• The expected patent term extends approximately through 2038, subject to the official USPTO term record.
• Orange Book listing, Paragraph IV activity, litigation, and settlement terms must be evaluated separately from the claim text.

Frequently Asked Questions

Does US 10,940,141 cover all Ingrezza prescriptions?

No. The claims require treatment of tardive dyskinesia and severe renal impairment, with additional limitations in the dependent claims. Routine use in patients without severe renal impairment is outside the stated scope.

Does the patent cover deutetrabenazine or tetrabenazine?

No. The claims specifically require valbenazine or its pharmaceutically acceptable salts. Deutetrabenazine and tetrabenazine are separate VMAT2 inhibitors.

Can a generic avoid the patent by using a different valbenazine salt?

Possibly for claims specifically limited to the ditosylate salt or Form I, but the broader independent claims cover valbenazine and pharmaceutically acceptable salts generally. Salt selection alone may not avoid all claims.

Is a generic allowed to omit the severe-renal-impairment use from its label?

A generic applicant may seek a section viii carve-out where permitted by FDA regulations. The effectiveness of that strategy depends on the approved reference-product labeling and whether the remaining label still induces the patented use.

Does patent expiration eliminate all valbenazine launch barriers?

No. Other patents, regulatory exclusivities, pediatric exclusivity, litigation outcomes, manufacturing patents, and FDA approval requirements can affect launch timing.

References

1. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations. FDA.
2. U.S. Food and Drug Administration. (2023). Ingrezza (valbenazine) prescribing information. Neurocrine Biosciences, Inc.
3. U.S. Patent and Trademark Office. (2021). U.S. Patent No. 10,940,141, methods of treating tardive dyskinesia. U.S. Department of Commerce.
4. U.S. Code, 21 U.S.C. § 355.
5. U.S. Code, 35 U.S.C. §§ 154, 271.

Drugs Protected by US Patent 10,940,141

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Neurocrine	INGREZZA	valbenazine tosylate	CAPSULE;ORAL	209241-001	Apr 11, 2017	AB	RX	Yes	No	10,940,141					TREATMENT OF TARDIVE DYSKINESIA
Neurocrine	INGREZZA	valbenazine tosylate	CAPSULE;ORAL	209241-003	Apr 23, 2021		RX	Yes	No	10,940,141					TREATMENT OF TARDIVE DYSKINESIA
Neurocrine	INGREZZA	valbenazine tosylate	CAPSULE;ORAL	209241-002	Oct 4, 2017	AB	RX	Yes	Yes	10,940,141					TREATMENT OF TARDIVE DYSKINESIA
Neurocrine	INGREZZA SPRINKLE	valbenazine tosylate	CAPSULE;ORAL	218390-001	Apr 30, 2024		RX	Yes	No	10,940,141					TREATMENT OF TARDIVE DYSKINESIA
Neurocrine	INGREZZA SPRINKLE	valbenazine tosylate	CAPSULE;ORAL	218390-002	Apr 30, 2024		RX	Yes	No	10,940,141					TREATMENT OF TARDIVE DYSKINESIA
Neurocrine	INGREZZA SPRINKLE	valbenazine tosylate	CAPSULE;ORAL	218390-003	Apr 30, 2024		RX	Yes	Yes	10,940,141					TREATMENT OF TARDIVE DYSKINESIA

International Family Members for US Patent 10,940,141

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2020336017
Australia	2025279628
Brazil	112022002834
Canada	3149033
China	114679906
Denmark	4017494
European Patent Office	4017494