US Patent 11,224,598 (Drug): Scope, Claims, and U.S. Patent Landscape for Nasal Varenicline to Increase Lacrimal Proteins
US Patent 11,224,598 claims a use-and-method approach: nasally administering varenicline in defined dose (microgram range) and formulation concentration (mg/mL range) to increase one or more lacrimal proteins in an individual, including specific tear proteome proteins and use around LASIK. The claim set is structured to capture (i) dose bands, (ii) concentration ranges, (iii) dosing frequency, (iv) multiple nasal dosage forms and delivery devices, (v) dry eye disease and symptom/diagnostic predicates, and (vi) preservative-free formulations.
The landscape implications in the U.S. follow the claim architecture: broad method coverage anchored on nasal varenicline and a lacrimal-protein mechanism, with narrower dependent claims layering clinical context (dry eye signs, Schirmer cutoffs, LASIK timing) and product attributes (preservative-free; liquid/suspension/aerosol/gel/ointment/dry powder/cream/paste/lotion/balm/nasal spray).
What does the independent claim cover (claim 1)?
Claim 1 recites a method of increasing “one or more lacrimal proteins” produced in an individual in need thereof via nasal administration of varenicline under two quantitative constraints:
Core elements (claim 1)
- Action: “increasing the amount or concentration” of one or more lacrimal proteins in an individual.
- Route: nasally administering.
- Dose: between 5 micrograms and 1000 micrograms of varenicline.
- Formulation requirement: varenicline is in a pharmaceutical formulation formulated for nasal administration.
- Concentration range in the formulation: between about 0.1 mg/mL and about 10 mg/mL of varenicline.
Quantitative scope at a glance (claim 1)
- Dose range: 5 to 1000 micrograms varenicline
- Formulation strength range: 0.1 to 10 mg/mL
This independent claim is the central license boundary: it does not require a specific tear proteome member, specific dry eye diagnostic test, specific dosing frequency, or specific device.
Which dependent claims define the lacrimal-protein and clinical use scope?
Which tear proteins are explicitly claimed (claim 2)?
Claim 2 limits the “one or more lacrimal proteins” to a defined list:
- Epithelial growth factor (EGF)
- lactoferin
- lacritin
- prolactin
- adrenocorticotropic
- leucine enkephalin
- ALS2CL
- ARHGEF19
- KIAA1109
- PLXNA1
- POLG
- WIPI1
- ZMIZ2
- “or other proteins of the tear proteome”
Key point for scope: claim 2 does two things at once:
- provides a predefined set; and
- keeps coverage open with “other proteins of the tear proteome,” which helps preserve mechanism-based breadth even when a particular protein is not measured.
Is LASIK timing covered (claim 3)?
Claim 3: varenicline is administered prior to or after LASIK surgery.
This creates a dedicated peri-procedural indication path, relevant for exclusivity strategy and payer/labeling arguments because it defines timing rather than only disease state.
How do the dose-dependent claims tighten the microgram range (claims 4–6)?
Claims 4–6 split the claim 1 microgram window into narrower bands:
- Claim 4: 5–600 micrograms
- Claim 5: 5–100 micrograms
- Claim 6: 100–750 micrograms
Two scope effects follow:
- The dependent claims cover overlapping subranges, which increases infringement probability if a product lands in any common commercial dose interval.
- The dependent bands do not cleanly “partition” claim 1; they create multiple hooks that can match product development outcomes (especially if the final dose is iterated during formulation/device selection).
How does dosing frequency expand or constrain the method (claims 7–9)?
Claims introduce temporal frequency limitations:
- Claim 7: at least once daily
- Claim 8: at least twice daily
- Claim 9: at least once weekly
These are not mutually exclusive in claim logic; they provide multiple independent frequency predicates that can be used in enforcement depending on how an accused regimen is structured.
Which nasal dosage forms and devices are covered (claims 10–11)?
Dosage forms (claim 10)
Claim 10 lists multiple acceptable nasal administration types:
- liquid
- suspension
- aerosol
- gel
- ointment
- dry powder
- cream
- paste
- lotion
- balm
- nasal spray
This is unusually broad for a single method claim, and it supports coverage across common nasal product platforms.
Delivery devices (claim 11)
Claim 11 expands coverage to multiple delivery mechanisms:
- syringe
- dropper
- bottle nebulizer
- atomization pump
- inhaler
- powder spray device
- vaporizer
- patch
- medicated stick
- pipette
- jet of liquid
- nasal spray bottle
This list increases risk for developers using alternative delivery hardware, because infringement can be argued without being tied to a single device category.
How does the patent define dry eye disease and diagnostic criteria (claims 12–17)?
Disease signs/symptoms predicate (claims 12–13)
- Claim 12: individual has one or more signs and symptoms of dry eye disease.
- Claim 13: symptoms comprising itchiness, dryness, photophobia, blurriness, pain, sticky feeling, burning, stinging, foreign body sensation.
This breadth helps match real-world clinical coding (symptom clusters) and reduces the need to prove a specific dry eye subtype beyond sign/symptom presence.
Schirmer test cutoff (claims 16–17)
- Claim 16: Schirmer tear test ≤10 mm/5 minutes in at least one eye prior to administration.
- Claim 17: Schirmer test performed with topical anesthetic.
These introduce objective thresholds. From a landscape perspective, they can shape enforcement strategy by making it easier to show a defined patient population in clinical documentation.
How do formulation concentration dependent claims narrow the mg/mL range (claims 18–19)?
Claim 1 already covers 0.1–10 mg/mL. Dependent claims create additional landing zones:
- Claim 18: 0.2–3 mg/mL
- Claim 19: 0.5 mg/mL, 1 mg/mL, or 2 mg/mL
This is commercially actionable. If an accused product uses one of these discrete strengths, claim 19 becomes a direct matching hook, while claim 18 supports a broader intermediate range.
What is the practical claim scope for enforcement risk in the U.S.?
Infringement-relevant “design parameters” (from claims)
An accused product or regimen is most plausibly evaluated against:
- route: nasal
- active: varenicline
- per-administration dose: 5–1000 micrograms
- formulation strength: 0.1–10 mg/mL
- evidence of “increase” of lacrimal proteins (mechanism claim element)
- optionally, whether regimen matches dependent predicates:
- proteins in the tear proteome list
- peri-LASIK timing
- dose band (5–600, 5–100, or 100–750 micrograms)
- frequency (once daily, twice daily, once weekly)
- dosage form and device
- dry eye symptom/sign presence
- Schirmer score threshold (≤10 mm/5 minutes) and topical anesthetic use
- preservative-free formulation (claim 14–15)
Preservative-free coverage (claims 14–15)
- Claim 14: formulation is preservative-free
- Claim 15: varenicline is provided as a preservative-free nasal spray
This creates an attribute-specific pathway for enforcement against “clean” formulations.
How does this claim architecture position the patent in the U.S. landscape?
Without reproducing non-provided family data, the landscape conclusion that follows from claim breadth is straightforward:
- Active ingredient is not novel in itself (varenicline is known as a drug), but the patent is positioned around a new route + new intended mechanism + quantified regimen for lacrimal proteins in a dry-eye context.
- Coverage is broad on dosage forms and delivery devices, which reduces “design-around” options limited to platform changes.
- Enforcement can be anchored in either:
- the independent method (route, dose, concentration, mechanism), or
- the dependent clinical and product predicates (dry eye symptoms, LASIK timing, Schirmer ≤10, preservative-free, and specific dose/concentration subranges).
Key scope summary table (claims-to-variables)
| Variable |
Claim(s) |
Covered range / options |
| Route |
1 |
Nasal administration |
| Active |
1 |
Varenicline |
| Dose per administration |
1, 4–6 |
5–1000 micrograms (1); 5–600 (4); 5–100 (5); 100–750 (6) |
| Concentration in formulation |
1, 18–19 |
0.1–10 mg/mL (1); 0.2–3 mg/mL (18); 0.5 / 1 / 2 mg/mL (19) |
| Frequency |
1, 7–9 |
≥ once daily (7); ≥ twice daily (8); ≥ once weekly (9) |
| Dosage form |
10 |
liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, balm, nasal spray |
| Device |
11 |
syringe, dropper, bottle nebulizer, atomization pump, inhaler, powder spray device, vaporizer, patch, medicated stick, pipette, jet of liquid, nasal spray bottle |
| Dry eye predicate |
12–13 |
signs and symptoms; list includes itchiness, dryness, photophobia, blurriness, pain, sticky feeling, burning, stinging, foreign body sensation |
| Diagnostic cutoff |
16–17 |
Schirmer ≤10 mm/5 min; performed with topical anesthetic |
| Mechanism protein list |
2 |
EGF, lactoferin, lacritin, prolactin, ACTH, leucine enkephalin, ALS2CL, ARHGEF19, KIAA1109, PLXNA1, POLG, WIPI1, ZMIZ2, or other tear proteome proteins |
| Surgery timing |
3 |
prior to or after LASIK |
| Preservation attribute |
14–15 |
preservative-free; preservative-free nasal spray |
Key Takeaways
- US 11,224,598 is a nasal varenicline lacrimal-protein increase method patent with strong quantitative anchors: 5–1000 micrograms and 0.1–10 mg/mL (independent claim).
- The patent also creates enforcement hooks through overlapping dose bands, specific formulation strengths (0.5/1/2 mg/mL), and frequency predicates (once daily, twice daily, once weekly).
- Coverage is broad across nasal dosage forms and delivery devices, limiting common “platform” design-around strategies.
- The landscape positioning is built for dry eye and peri-procedural use: dry eye signs/symptoms, Schirmer ≤10 mm/5 minutes with topical anesthetic, and LASIK timing.
- Mechanism scope is supported by an explicit tear proteome list plus a “other tear proteome proteins” catch-all.
FAQs
1. What is the independent claim’s main structure?
A method of increasing lacrimal proteins by nasally administering varenicline in a 5–1000 microgram dose and 0.1–10 mg/mL formulation concentration.
2. Does the patent require a specific tear protein?
Dependent claim 2 lists specific tear proteins but also allows “other proteins of the tear proteome,” so it is not limited to only one protein.
3. Are there specific Schirmer test requirements?
Yes. Dependent claim 16 requires Schirmer ≤10 mm/5 minutes in at least one eye, and claim 17 specifies use of topical anesthetic during the test.
4. What nasal product forms are covered?
The claims list many formats, including liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, balm, and nasal spray.
5. How does the patent handle LASIK?
It covers administration prior to or after LASIK surgery under dependent claim 3.
References
[1] Claims provided by user for U.S. Patent 11,224,598 (text of claims 1–19).
