United States Patent 11,911,380: Varenicline Nasal-Spray Claims, Scope, and Patent Landscape

U.S. Patent 11,911,380 covers methods of administering low-dose intranasal varenicline to activate trigeminal or anterior ethmoidal nerves and the nasolacrimal reflex. The claims are method-of-treatment claims, not composition claims. They require a sprayed liquid solution, a defined varenicline concentration, and a defined intranasal dose.

The claim set is closely aligned with the approved Tyrvaya product, which contains varenicline solution and is administered as one spray in each nostril twice daily for the treatment of the signs and symptoms of dry eye disease. The principal enforcement value is therefore directed at competing intranasal varenicline products and potentially at manufacturers, distributors, and users of a substantially similar nasal-spray regimen.

What does U.S. Patent 11,911,380 protect?

The patent protects three overlapping therapeutic mechanisms:

Independent claim	Protected activity	Required administration
Claim 1	Activating a trigeminal nerve	Local spray of liquid varenicline formulation into a nasal cavity
Claim 11	Activating an anterior ethmoidal nerve	Local spray of liquid varenicline formulation into a nasal cavity
Claim 21	Activating a nasolacrimal reflex	Local spray of liquid varenicline formulation into a nasal cavity

Each independent claim requires the following core elements:

An individual in need thereof.
Administration of a therapeutically effective amount of varenicline.
Local administration into a nasal cavity.
Administration as a spray.
A liquid pharmaceutical formulation.
Varenicline or a pharmaceutically acceptable varenicline salt in solution.
One or more pharmaceutically acceptable inactive ingredients.
Varenicline concentration of approximately 0.1 mg/mL to 10 mg/mL.
Intranasal dose of approximately 5 micrograms to 1,000 micrograms.

A product or method that omits any one of those limitations may avoid literal infringement of the independent claims, subject to claim construction and the doctrine of equivalents.

How broad are the independent claims?

The claims are broad within the specific field of low-dose intranasal varenicline, but they do not cover every varenicline product or every nasal formulation.

Claim 1: trigeminal nerve activation

Claim 1 covers intranasal varenicline administration where the claimed therapeutic purpose is activation of a trigeminal nerve. The claim does not limit the specific trigeminal branch, disease indication, spray device, excipient, or varenicline salt.

The broadest quantitative boundaries are:

Concentration: approximately 0.1 to 10 mg/mL.
Dose: approximately 5 to 1,000 micrograms.

The dependent claims narrow those ranges or add performance and formulation limitations.

Claim 11: anterior ethmoidal nerve activation

Claim 11 is narrower in its stated biological target because it requires activation of the anterior ethmoidal nerve. It otherwise repeats the formulation, concentration, route, and dose limitations of claim 1.

This claim may be commercially significant because the anterior ethmoidal nerve is associated with nasal sensory pathways implicated in tear production and ocular-surface reflexes. A competing product could face infringement exposure even if its labeling uses a dry-eye indication rather than expressly describing anterior ethmoidal nerve activation, depending on the evidence concerning the intended use and the meaning of the claim language.

Claim 21: nasolacrimal reflex activation

Claim 21 covers activation of the nasolacrimal reflex rather than activation of a named nerve. It may be the most commercially relevant claim for dry-eye products because it is framed around a physiological response associated with tear production.

The claim does not expressly require treatment of dry eye disease. A method directed to another condition could fall within the claim if the remaining elements are satisfied and the purpose is activation of the nasolacrimal reflex.

What formulations are covered by Patent 11,911,380?

The patent claims a liquid solution, not a suspension, emulsion, powder, implant, tablet, or injectable formulation.

Required formulation characteristics

The claimed formulation must contain:

Varenicline or a pharmaceutically acceptable varenicline salt.
One or more pharmaceutically acceptable inactive ingredients.
Varenicline in solution.
A concentration of approximately 0.1 to 10 mg/mL.
Delivery into the nasal cavity by spray.

The claims do not require a particular preservative, tonicity agent, surfactant, viscosity modifier, or container-closure system.

Buffer-dependent claims

Claims 8, 18, and 28 require a phosphate buffer or phosphate-citrate buffer.

Claims 9, 19, and 29 require a buffer with a pH of approximately 5.0 to 7.4.

Claims 10, 20, and 30 identify pH values of approximately 5.0, 6.0, 7.0, or 7.4.

These dependent claims create narrower formulation positions. A product using a non-phosphate buffer may avoid the buffer-specific claims while remaining potentially exposed to claims 1, 11, or 21.

How do the dose claims affect infringement risk?

The dose limitations create several overlapping ranges:

Claims	Dose range
Claims 1, 11, 21	5 to 1,000 micrograms
Claims 3, 13, 23	5 to 100 micrograms
Claims 4, 14, 24	25 to 500 micrograms
Claims 5, 15, 25	5 to 500 micrograms

A 30-microgram dose falls within every listed dose range. The approved Tyrvaya regimen uses 0.03 mg, or 30 micrograms, of varenicline per spray. That dose therefore falls within the independent claims and all of the dose-range dependent claims.

The phrase “about” expands the practical uncertainty around the numerical boundaries. Courts generally assess “about” in light of the intrinsic evidence, prosecution history, technical context, and ordinary meaning. A dose marginally outside a stated endpoint could remain disputed.

Does Tyrvaya practice the claimed subject matter?

Tyrvaya is an intranasal varenicline product approved by the FDA for the signs and symptoms of dry eye disease. The FDA-approved labeling describes a liquid nasal spray containing varenicline and instructs patients to administer one spray in each nostril twice daily (FDA, 2021).

The labeled dose is 30 micrograms per spray. The commercial formulation has been publicly described as a low-dose varenicline nasal solution. A concentration in the claimed range, combined with the labeled intranasal dose, would satisfy the principal quantitative limitations of claims 1, 11, and 21.

Tyrvaya characteristic	Patent requirement
Varenicline active ingredient	Satisfied
Liquid nasal spray	Satisfied
Local nasal administration	Satisfied
Low-microgram dose	Satisfied by 30 micrograms per spray
Concentration range	Consistent with claimed 0.1 to 10 mg/mL range
Dry-eye therapeutic use	Consistent with nasolacrimal-reflex theory
Twice-daily dosing	Not required by the claims

The claims do not require the specific Tyrvaya trade name, a particular device, or twice-daily dosing.

What do the “side-effect” limitations add?

Claims 6, 16, and 26 require that the administered amount does not result in clinically significant undesired psychoactive side effects.

Claims 7, 17, and 27 require that the dose does not result in clinically significant vomiting.

These limitations may narrow the claims, but they also create proof questions. The patent does not define a universal numerical threshold for “clinically significant.” In litigation, the parties would likely dispute:

Whether the limitation is an objective claim limitation or an intended result.
What patient population controls.
What level of psychoactive effect is clinically significant.
Whether the assessment is based on labeling, clinical-trial data, pharmacokinetics, or individual patient experience.
Whether the accused product must actually produce the claimed absence of side effects.

The limitations may help distinguish low-dose local administration from oral varenicline therapy, which is associated with higher systemic exposure and different tolerability considerations. They may also create additional invalidity arguments based on indefiniteness or lack of written description, depending on the patent specification and prosecution history.

What is the likely patent strength?

The estate has meaningful commercial relevance because the independent claims track the essential attributes of a low-dose varenicline nasal spray.

Strengths

Three independent claims cover related biological mechanisms.
The claims cover both the active ingredient and a defined route of delivery.
The concentration and dose ranges encompass the commercial 30-microgram-per-spray regimen.
The claims are not limited to one disease label.
The claims cover varenicline salts as well as varenicline itself.
The mechanism claims may reach products labeled for dry eye even if the label does not use the exact phrase “nasolacrimal reflex.”

Vulnerabilities

The claims are method claims and require proof of administration or intended use.
They do not cover every nasal varenicline formulation.
The nerve-activation and reflex-activation limitations may raise claim-construction disputes.
“About,” “therapeutically effective,” “selectively binds,” and “clinically significant” are flexible terms.
Prior-art exposure may be substantial because varenicline, nicotinic acetylcholine receptors, nasal administration, and ocular reflex pathways were each known technical areas.
A generic or competitor could design around the concentration, dose, buffer, route, or formulation requirements.

The patent is strongest against a product that reproduces the approved product’s active ingredient, liquid spray format, concentration, and 30-microgram intranasal dose.

Can a competitor design around the claims?

Potential design-around paths include:

Using a non-spray nasal delivery system, such as a gel, powder, insert, or nebulized system, if it does not satisfy the ordinary meaning of “spray.”
Using a concentration below approximately 0.1 mg/mL or above approximately 10 mg/mL.
Using a delivered dose outside the claimed approximately 5-to-1,000-microgram range.
Developing a formulation in which varenicline is not in solution.
Using a different active compound or a non-varenicline nicotinic receptor ligand.
Avoiding the claimed therapeutic purpose, although labeling and actual use would be relevant.
Using a different buffer to avoid the dependent buffer claims.
Developing a systemic or oral product rather than a local nasal product.

The most difficult design-around is likely to preserve the commercial profile of Tyrvaya while moving outside the claims. A substantial dose reduction, concentration change, or alternative nasal delivery format could affect tolerability, device performance, deposition, efficacy, or regulatory comparability.

What is the Orange Book status of Patent 11,911,380?

The claims provided do not establish whether U.S. Patent 11,911,380 is listed in the FDA Orange Book. Orange Book listing is an administrative and regulatory fact separate from claim scope. It depends on the sponsor’s submission and FDA listing records under the drug product’s application number.

For a small-molecule product such as Tyrvaya, an authorized generic or ANDA applicant would generally address listed patents through Paragraph IV certification, a section viii statement for a method-of-use patent, or another certification permitted by the Hatch-Waxman framework (21 U.S.C. § 355).

Because the patent claims are method claims directed to administration and physiological activation, a section viii carve-out may be relevant only if the applicant can omit the patented use from labeling and the remaining approved use does not practice the claimed method. If the commercial use necessarily corresponds to the claimed dry-eye mechanism, a Paragraph IV strategy would present greater litigation risk.

When does Patent 11,911,380 lose exclusivity?

The patent’s enforceable term cannot be calculated from the claim text alone. The relevant date depends on the patent’s earliest effective nonprovisional priority date, any patent-term adjustment, terminal disclaimer, and any applicable patent-term extension.

The issue date is not the expiration date. For a U.S. utility patent, the base term generally runs 20 years from the earliest effective nonprovisional filing date, subject to statutory adjustments and disclaimers (35 U.S.C. §§ 154, 156).

A reliable expiration analysis must distinguish:

Patent term expiration.
Patent-term adjustment.
Patent-term extension.
Terminal disclaimer.
Regulatory exclusivity.
Any separate continuation or divisional patents covering Tyrvaya.

The patent’s expiration date should therefore be taken from the USPTO Patent Center record and reconciled against FDA Orange Book data before making a launch or valuation decision.

What generic-entry risks exist?

ANDA entry

A generic varenicline nasal spray would face the highest risk if it duplicates:

Varenicline as the active ingredient.
A liquid nasal solution.
Spray delivery.
A concentration within approximately 0.1 to 10 mg/mL.
A dose within approximately 5 to 1,000 micrograms.
A dry-eye or reflex-mediated indication consistent with the claimed use.

An ANDA applicant could challenge the patent through Paragraph IV certification, seek a negotiated launch date, or pursue a label carve-out if the patented method can be omitted.

Biosimilar risk

Biosimilar risk is not applicable. Varenicline is a chemically synthesized small molecule, not a biologic. Competitive entry would proceed through the ANDA pathway rather than the abbreviated pathway for biosimilars under the Public Health Service Act.

Authorized-generic risk

An authorized generic or licensed competitor could enter under a commercial arrangement without relying on an unlicensed copy of the patented method. The patent would still matter if the licensed product practices the claimed administration regimen, unless the relevant rights were licensed or otherwise exhausted.

Which companies are commercially relevant?

The principal commercial reference product is Tyrvaya. Oyster Point Pharma developed the product, and Viatris acquired Oyster Point’s commercial operations and product portfolio. The relevant competitive set includes:

The sponsor or current marketer of Tyrvaya.
Potential generic manufacturers developing varenicline nasal sprays.
Contract manufacturers supplying nasal-spray devices or sterile/controlled liquid formulations.
Companies developing alternative dry-eye therapies, including immunomodulators, secretagogues, lubricants, and device-based products.

Alternative dry-eye products may compete commercially without infringing this patent if they do not use intranasal varenicline. Their presence limits the patent’s ability to exclude the broader dry-eye market.

What litigation and settlement issues matter?

The claim set creates several likely dispute points:

Whether the accused product administers a “spray.”
Whether the formulation is a solution rather than a suspension or dispersion.
Whether the product is administered “locally.”
Whether the claimed nerve or reflex is actually activated.
Whether a label or promotional material establishes the claimed method.
Whether the claimed dose is within the “about” ranges.
Whether “clinically significant” side-effect limitations are satisfied.
Whether earlier publications disclose the same combination of varenicline, intranasal spray, dose, concentration, and therapeutic purpose.

No litigation outcome or settlement term can be inferred from the claim language. Any freedom-to-operate conclusion should treat the patent as one component of a broader family analysis, including continuations, related formulation patents, device patents, and Orange Book-listed patents.

Key Takeaways

U.S. Patent 11,911,380 covers low-dose intranasal varenicline delivered as a liquid spray.
Claims 1, 11, and 21 separately target trigeminal nerve activation, anterior ethmoidal nerve activation, and nasolacrimal-reflex activation.
The principal quantitative scope is approximately 0.1 to 10 mg/mL and 5 to 1,000 micrograms per intranasal dose.
Tyrvaya’s 30-microgram intranasal regimen falls within the stated dose ranges.
The patent does not claim every varenicline product, every nasal formulation, or the broad treatment of dry eye disease.
Claims directed to phosphate buffers and pH values of approximately 5.0 to 7.4 provide narrower formulation protection.
Biosimilar analysis is not relevant because varenicline is a small molecule.
Generic risk will depend on Orange Book listing, the patent’s verified term, claim construction, and the ANDA applicant’s certification strategy.
The strongest infringement case would involve a product that copies the active ingredient, liquid spray format, concentration, and low-microgram intranasal dose.

FAQs

Is Patent 11,911,380 a composition patent?

No. The supplied claims are method-of-treatment claims. They require administration of a varenicline formulation and do not independently claim the formulation as a composition of matter.

Does the patent cover oral varenicline tablets?

No. The claims require local administration of a spray into a nasal cavity. Oral tablets do not satisfy that route limitation.

Does changing the buffer avoid the entire patent?

No. Changing the buffer may avoid claims 8-10, 18-20, and 28-30, but it would not necessarily avoid independent claims 1, 11, or 21.

Is a 30-microgram varenicline nasal dose within the patent claims?

Yes. Thirty micrograms falls within the independent 5-to-1,000-microgram range and each narrower dependent dose range recited in claims 3-5, 13-15, and 23-25.

Can a generic avoid infringement by removing “nasolacrimal reflex” language from its label?

Not necessarily. Infringement analysis can consider the product’s approved labeling, instructions, promotional materials, intended use, and actual use. Removing one phrase from a label does not automatically eliminate liability if the accused method otherwise practices the claimed limitations.

References

U.S. Patent No. 11,911,380. (2024). United States Patent and Trademark Office.
U.S. Food and Drug Administration. (2021). Tyrvaya (varenicline solution) nasal spray prescribing information. FDA.
U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations. FDA.
United States Code. 35 U.S.C. §§ 154, 156.
United States Code. 21 U.S.C. § 355.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Oyster Point Pharma	TYRVAYA	varenicline tartrate	SPRAY;NASAL	213978-001	Oct 15, 2021		RX	Yes	Yes	11,911,380	⤷ Start Trial				TREATMENT OF THE SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)	⤷ Start Trial
>Applicant	>Tradename	>Generic Name	>Dosage	>NDA	>Approval Date	>TE	>Type	>RLD	>RS	>Patent No.	>Patent Expiration	>Product	>Substance	>Delist Req.	>Patented / Exclusive Use	>Submissiondate

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2015336216	⤷ Start Trial
Australia	2020213351	⤷ Start Trial
Brazil	112017008097	⤷ Start Trial
Brazil	122022025737	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 11,911,380

Which drugs does patent 11,911,380 protect, and when does it expire?

Summary for Patent: 11,911,380