US Patent 11,903,942: Varenicline Nasal Spray Claims, Exclusivity, Orange Book Status, and Patent Landscape

US Patent 11,903,942 protects low-dose varenicline formulations for local nasal administration, including buffered liquid nasal sprays, spray bottles, and dosage configurations delivering approximately 5 to 100 micrograms of varenicline per spray. The broadest independent claims cover the formulation, the nasal spray dosage form, and a container holding the formulation. The patent does not require a specific therapeutic indication, although its commercial relevance is closely tied to Tyrvaya, the varenicline nasal spray developed for dry-eye disease.

The core commercial embodiment is a 50-microliter nasal spray containing approximately 0.03 mg of varenicline per spray, with a phosphate or phosphate-citrate buffer at a pH of approximately 5.0 to 7.4. The patent has substantial overlap with the product architecture of Tyrvaya, but its enforceability depends on claim construction, the written description, prosecution history, prior art, and the scope of any listed claims in the FDA Orange Book.

What does US Patent 11,903,942 protect?

US Patent 11,903,942 protects pharmaceutical formulations containing varenicline or a pharmaceutically acceptable varenicline salt for local administration into the nasal cavity. The claims cover both broad formulation categories and specific liquid nasal spray embodiments.

Claim group	Claims	Principal subject matter
Broad nasal formulation	1-15	Varenicline formulation for nasal administration
Liquid nasal spray	16-22	Liquid solution administered as a nasal spray
Spray bottle	23-30	Nasal spray bottle containing the claimed liquid formulation
Dose range	1-5, 16-20, 24, 29-30	5 to 1,000 micrograms, with narrower ranges
Buffer system	10-13, 21-22, 26-28	Phosphate or phosphate-citrate buffer
pH	12-13, 22, 27-28	Approximately pH 5.0 to 7.4
Spray volume	25, 29-30	Approximately 50 microliters per spray
Concentration	1, 14-16, 23	Approximately 0.1 to 10 mg/mL; preferred concentration approximately 0.5 mg/mL

The independent claims are composition- and container-focused. They do not expressly require treatment of dry-eye disease, smoking cessation, ocular disease, or another named condition.

How broad are the independent claims in US 11,903,942?

Claims 1, 16, and 23 are the principal scope-defining claims.

Claim 1: pharmaceutical formulation

Claim 1 requires:

A pharmaceutical formulation;
Local administration into a nasal cavity;
Varenicline or a pharmaceutically acceptable varenicline salt;
One or more pharmaceutically acceptable inactive ingredients;
Between 5 and 1,000 micrograms of varenicline in the formulation; and
A varenicline concentration between approximately 0.1 and 10 mg/mL.

The claim is broad in dosage form because it does not initially require a liquid, solution, spray, buffer, or specific pH. Dependent claim 6 expressly includes liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, and balm.

The claim is narrower than a generic “varenicline nasal product” claim because the accused product must satisfy both the total-amount limitation and the concentration limitation. The meaning of “amount in the formulation” also matters. A product with a large multidose reservoir may raise a different construction issue from a claim directed to the amount delivered per dose.

Claim 16: liquid nasal spray

Claim 16 narrows the formulation to:

A nasal spray;
A liquid pharmaceutical formulation;
A solution of varenicline or a pharmaceutically acceptable salt;
One or more inactive ingredients;
5 to 1,000 micrograms of varenicline; and
A concentration of approximately 0.1 to 10 mg/mL.

This claim is commercially important because it maps directly onto a liquid spray product rather than merely a nasal formulation.

Claim 23: nasal spray bottle

Claim 23 covers a physical product configuration: a nasal spray bottle containing the claimed liquid formulation. It requires a solution, the same varenicline amount range, and the same concentration range.

This claim creates a potential apparatus-plus-composition enforcement route. A product seller may face infringement exposure based on the filled bottle even if the accused party characterizes its activity as packaging or distribution rather than manufacture of the formulation.

What dosage ranges are protected?

The patent uses overlapping ranges rather than a single narrow dose.

Claim limitation	Covered range
Broad amount range	5 to 1,000 micrograms
Narrow amount range	5 to 100 micrograms
Intermediate range	5 to 600 micrograms
Intermediate range	5 to 500 micrograms
Narrow per-dose range	5 to 75 micrograms
Preferred concentration	Approximately 0.5 mg/mL
Broad concentration range	Approximately 0.1 to 10 mg/mL
Spray volume	Approximately 50 microliters
Specific per-spray content	5 to 100 micrograms or 5 to 75 micrograms

The dependent claims are layered. A product delivering 50 micrograms per 50-microliter spray at 1 mg/mL could fall within the broad claims and several narrower claims. A formulation delivering approximately 25 to 75 micrograms per spray at 0.5 mg/mL would be positioned near the commercial center of the claim set.

Because the claims use “about,” “around,” and range language, literal infringement analysis would likely examine accepted pharmaceutical measurement tolerances, manufacturing specifications, assay results, fill volume, and the ordinary meaning of approximate concentration and dose terms.

What formulations are protected by US 11,903,942?

The patent protects more than a single liquid formulation. Claim 6 lists multiple dosage forms, including:

Liquids;
Suspensions;
Aerosols;
Gels;
Ointments;
Dry powders;
Creams;
Pastes;
Lotions; and
Balms.

Claims 7 through 9 then narrow the formulation to a solution, liquid, and nasal spray. The practical value of the broad formulation claims depends on whether the accused product is intended for local nasal administration and contains the specified quantity and concentration of varenicline.

Buffer and pH limitations

Claims 10 through 13, 21 through 22, and 26 through 28 cover phosphate and phosphate-citrate buffer systems. The pH range is approximately 5.0 to 7.4, with specific examples at approximately:

pH 5.0;
pH 6.0;
pH 7.0; and
pH 7.4.

A competing spray using a different buffer may avoid these narrower claims while remaining exposed under claims 1, 16, or 23 if all other limitations are met. A nonbuffered formulation could present a stronger design-around position against the buffer-dependent claims, but it would not automatically avoid the independent claims.

Varenicline salt

The claims cover varenicline and pharmaceutically acceptable varenicline salts. This prevents a straightforward design-around based solely on converting the active ingredient from the free form to a pharmaceutically acceptable salt. The relevant analysis would include the identity of the salt, its pharmaceutical acceptability, the concentration calculation, and whether the claim measures varenicline on a free-base or salt-mass basis.

Does the patent cover Tyrvaya?

Tyrvaya is a varenicline nasal spray approved by the FDA in October 2021 for the treatment of signs and symptoms of dry-eye disease. The labeled product delivers 0.03 mg, or 30 micrograms, of varenicline per spray through a 50-microliter nasal spray device.[2]

That commercial configuration falls within the principal numerical limitations recited in US 11,903,942:

Tyrvaya characteristic	Patent limitation
30 micrograms per spray	Within 5 to 1,000 micrograms
30 micrograms per spray	Within 5 to 100 and 5 to 75 micrograms
50-microliter spray	Within claim 25
Approximate concentration of 0.6 mg/mL if 30 micrograms are delivered in 50 microliters	Within 0.1 to 10 mg/mL and near the 0.5 mg/mL dependent limitation
Liquid nasal spray	Claims 9, 16, and related dependents
Buffered solution	Potentially within claims 10-13, 21-22, and 26-28, depending on the commercial formulation

The patent claims do not require the dry-eye indication. That distinction matters because a competitor may infringe the formulation claims even if it markets varenicline for another local nasal use. Conversely, an accused product could avoid infringement if its concentration, dose, formulation, or delivery configuration falls outside the claim limitations.

What is the Orange Book status of US 11,903,942?

Tyrvaya is approved under NDA 214826 and is associated with patent listings in the FDA’s Approved Drug Products with Therapeutic Equivalence Evaluations, commonly called the Orange Book.[1][2]

The relevant Orange Book analysis has three separate questions:

Whether US 11,903,942 is listed against Tyrvaya;
Which claims are identified as covering the approved product; and
Whether a future ANDA applicant must make a Paragraph IV certification against the patent.

An Orange Book listing does not establish validity or infringement. It creates a statutory certification and notice framework for an ANDA applicant. A generic applicant that seeks approval before patent expiration may certify that the patent is invalid, unenforceable, or will not be infringed. That certification can trigger patent litigation under the Hatch-Waxman Act.[3]

The regulatory relevance is strongest for an ANDA seeking a product that is pharmaceutically equivalent to Tyrvaya. A 505(b)(2) applicant proposing a different formulation, delivery system, indication, or clinical bridge may face a different patent-certification analysis.

When does US Patent 11,903,942 lose exclusivity?

The patent’s nominal expiration is expected in 2039 based on the patent family’s priority and US patent-term rules. The operative date must be taken from the official USPTO Patent Center record, including any patent-term adjustment and terminal-disclaimer data.[4]

The commercial exclusivity timeline is separate from the patent term:

Event	Date or status
Tyrvaya FDA approval	October 15, 2021
US Patent 11,903,942 grant	February 20, 2024
Expected patent protection	Approximately 2039, subject to official term data
Small-molecule NCE exclusivity	Not the principal remaining barrier by the time of the 2024 grant
Generic entry	Potentially before patent expiry only through a successful challenge, settlement, license, or noninfringing product

FDA regulatory exclusivity and patent exclusivity should not be treated as interchangeable. FDA exclusivity may block certain approvals for a defined period, while a listed patent can support litigation and delayed approval through the Hatch-Waxman framework.

Which companies are challenging the varenicline nasal spray patents?

Publicly available patent-risk analysis should distinguish between an actual Paragraph IV filing and a theoretical future challenge. The claims create a clear Paragraph IV target because they cover the central dose, concentration, liquid-spray, buffer, and bottle features of Tyrvaya.

No publicly established Paragraph IV judgment or final settlement should be inferred solely from the existence of the patent. An ANDA applicant could challenge the patent on:

Anticipation;
Obviousness;
Written-description grounds;
Enablement;
Indefiniteness;
Noninfringement; or
Lack of statutory Orange Book listing eligibility.

A generic company may also choose a formulation design that avoids the narrow buffer, pH, or 50-microliter limitations. Such a product could still face claims 1, 2, 3, or 4 if its dose and concentration remain within the broad ranges.

What patent litigation affects US 11,903,942?

The principal litigation risk is a Hatch-Waxman action involving an ANDA or a 505(b)(2) application for a varenicline nasal product. The likely dispute points are:

Issue	Relevance
Dose measurement	Whether the claim measures reservoir content, delivered dose, or labeled dose
Concentration	Whether concentration is calculated from nominal fill volume or actual delivered volume
“About” language	Permitted analytical and manufacturing variation
Local administration	Whether the accused product is intended for nasal-cavity administration
Salt form	Whether a particular varenicline salt is pharmaceutically acceptable
Buffer composition	Whether phosphate or phosphate-citrate components are present
Spray volume	Whether approximately 50 microliters includes the accused device
Claim construction	Scope of “formulation,” “nasal spray,” and “amount”
Prior art	Earlier varenicline formulations, nasal delivery systems, and dose-ranging disclosures

The patent’s independent claims are vulnerable to prior-art arguments because they use broad functional and numerical language. The patentee’s strongest position is likely against products that reproduce the complete commercial combination: low-dose varenicline, liquid solution, nasal spray, approximately 50-microliter delivery, and a phosphate-based buffer.

How strong is the patent estate for varenicline nasal spray?

US 11,903,942 is strongest as a formulation and product-configuration patent. It is not primarily a method-of-use patent. Its commercial value comes from its proximity to the approved product and from the overlapping dependent claims that capture practical manufacturing specifications.

Strengths

Covers a broad 5-to-1,000-microgram amount range.
Covers 0.1-to-10 mg/mL concentration.
Reaches liquid solutions and nasal sprays.
Covers a spray bottle containing the formulation.
Includes the commercially relevant 50-microliter delivery volume.
Covers phosphate and phosphate-citrate buffers.
Covers varenicline salts as well as varenicline.

Limitations

The claims require nasal local administration.
The numerical limitations create potential design-around routes.
Several dependent claims require specific buffers or pH values.
The patent does not independently claim every possible therapeutic use.
A competitor may develop a different concentration, dose, spray volume, buffer, or device.
Validity may depend heavily on prior art involving varenicline, nasal delivery, and low-dose local administration.

The claims appear more difficult to design around when combined, but easier to attack individually. A competitor could target one limitation at a time: use a nonphosphate buffer, deliver a dose above 100 micrograms, use a different spray volume, alter the concentration outside the claimed range, or use a non-solution dosage form.

Does the patent create biosimilar risk?

No conventional biosimilar pathway applies. Varenicline is a small-molecule active ingredient, and a competing product would ordinarily use the ANDA pathway under section 505(j) or, depending on its differences, a 505(b)(2) application.[1][3]

The relevant competitive threats are:

Generic varenicline nasal spray;
Authorized generic or licensed product;
505(b)(2) nasal formulation;
Alternative nasal cholinergic or nicotinic-receptor agonist;
Different-device varenicline product;
Non-nasal dry-eye therapy.

A generic version of Tyrvaya would confront pharmaceutical-equivalence requirements, device compatibility questions, patent certifications, and possible clinical or comparative requirements imposed by FDA.

Are there licensing deals affecting the patent landscape?

Oyster Point Pharma developed Tyrvaya and was acquired by Viatris in 2022. The transaction transferred the commercial program and associated assets to Viatris, including the regulatory and intellectual-property position surrounding Tyrvaya.[5]

Pfizer originally developed varenicline as Chantix for smoking cessation. That historical relationship does not mean Pfizer owns the nasal formulation claims in US 11,903,942. Ownership and enforcement should be evaluated from the current patent assignment record, not from the identity of the original varenicline developer.

What generic launch scenarios exist?

Scenario	Commercial result
No challenge	Generic waits for patent and regulatory barriers to clear
Paragraph IV challenge unsuccessful	Patent remains a barrier until expiration or settlement terms permit entry
Paragraph IV challenge successful	FDA approval may proceed subject to other listed patents and exclusivities
Noninfringing formulation	Launch may occur if FDA requirements are satisfied and no other patent blocks entry
Licensed generic	Entry occurs under an agreement with the patent holder or commercial owner
505(b)(2) product	Potentially launches with a different formulation, indication, or delivery profile
Authorized generic	May compete without relying on an independent generic patent challenge

The biggest launch risk is not limited to US 11,903,942. A complete entry analysis must include the full Tyrvaya patent family, continuation patents, device claims, method-of-use claims, formulation patents, and any later-issued patents listed against the NDA.

What geographic coverage does the patent provide?

US 11,903,942 provides rights in the United States only. It does not automatically protect the formulation in Canada, Europe, Japan, China, or other markets.

International risk depends on corresponding applications and granted patents in the relevant jurisdictions. Patent term, prosecution history, claim scope, supplementary protection rights, and regulatory exclusivity must be reviewed country by country. A US noninfringement position does not predict the outcome under European or other national claims.

Key Takeaways

US 11,903,942 is a formulation, nasal-spray, and spray-bottle patent for low-dose varenicline.
Its broadest claims cover 5 to 1,000 micrograms and approximately 0.1 to 10 mg/mL.
Dependent claims focus on 5-to-100-microgram doses, 5-to-75-microgram doses, phosphate buffers, pH 5.0 to 7.4, and 50-microliter sprays.
Tyrvaya’s 30-microgram, 50-microliter nasal spray falls within the central commercial profile of the claims.
The patent is relevant to generic and 505(b)(2) entry, but no biosimilar pathway applies.
The main design-around variables are dose, concentration, spray volume, buffer, pH, salt form, and dosage form.
The expected patent term extends to approximately 2039, subject to the official USPTO term record and any terminal disclaimer.
A complete launch assessment must review all Orange Book-listed Tyrvaya patents, not US 11,903,942 in isolation.

FAQs

Is US 11,903,942 a method-of-use patent?

No. The supplied claims are directed primarily to pharmaceutical formulations, nasal sprays, and spray bottles. They do not require treatment of a specific disease or patient population.

Does a varenicline nasal spray automatically infringe US 11,903,942?

No. Infringement requires satisfaction of every limitation of at least one asserted claim. Dose, concentration, formulation type, nasal administration, buffer, and device characteristics are central limitations.

Can a competitor avoid the patent by using varenicline tartrate or another salt?

Not necessarily. The claims expressly cover varenicline and pharmaceutically acceptable varenicline salts. A salt change alone may not avoid infringement.

Does a product with a different buffer avoid all claims?

No. A different buffer may avoid buffer-dependent claims, but the broad independent claims do not expressly require a phosphate or phosphate-citrate buffer.

Is Tyrvaya’s 30-microgram dose within the patent claims?

Yes. A 30-microgram spray falls within the recited 5-to-1,000-microgram, 5-to-100-microgram, and 5-to-75-microgram ranges, assuming the other claim limitations are satisfied.

Sources

U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations.
U.S. Food and Drug Administration. (2021). Tyrvaya (varenicline solution) nasal spray prescribing information.
U.S. Congress. (1984). Drug Price Competition and Patent Term Restoration Act, 21 U.S.C. § 355 and 35 U.S.C. §§ 156, 271, 282.
United States Patent and Trademark Office. (2024). U.S. Patent No. 11,903,942, Patent Center record.
Viatris Inc. (2022). Viatris completes acquisition of Oyster Point Pharma and Famy Care.

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	11,903,942	⤷ Start Trial	Y				⤷ 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
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 11,903,942

Which drugs does patent 11,903,942 protect, and when does it expire?

Summary for Patent: 11,903,942