US Patent 10,940,138: Scope, Claim Construction, Exclusivity and Competitive Patent Landscape for Upneeq

US Patent 10,940,138 protects a narrow method of treating acquired blepharoptosis with a specific sterile, preservative-free, low-dose oxymetazoline ophthalmic formulation. The patent does not claim oxymetazoline broadly, nor does it claim every treatment of ptosis. Its commercial relevance is concentrated in the Upneeq product, an oxymetazoline hydrochloride ophthalmic solution approved by the FDA for acquired blepharoptosis in adults.

The independent claims require both a defined patient-treatment method and a formulation having tightly specified composition, pH, viscosity, stability, and, in some claims, manufacturing or dosing characteristics. The patent therefore creates a formulation-and-use barrier rather than a broad active-ingredient monopoly.

What does US Patent 10,940,138 protect?

US 10,940,138 protects methods of treating acquired blepharoptosis in adults by administering a sterile, preservative-free aqueous ophthalmic formulation containing approximately:

Component	Claimed concentration
Oxymetazoline hydrochloride	0.1 wt%
Sodium chloride	0.64 wt%
Potassium chloride	0.075 wt%
Calcium chloride	0.048 wt%
Magnesium chloride	0.03 wt%
Sodium acetate	0.39 wt%
Sodium citrate	0.17 wt%
Hypromellose	0.5 wt%
Water	Quantity sufficient
pH	About 5.8 to 6.8
Viscosity	15 to 35 cPs
Stability	At least 24 months at approximately 20°C to 30°C

Claim 1 is the principal broad claim. It is a method claim, not a standalone composition claim. The accused conduct must therefore involve administering the formulation to an adult with acquired blepharoptosis.

Claim 30 is narrower because it requires the formulation to consist of the listed ingredients, including specified hydrate forms of calcium chloride, magnesium chloride, and sodium acetate. The claim also requires a pH adjuster and water.

The patent issued on March 9, 2021, as US Patent No. 10,940,138. The patent is assigned to RVL Pharmaceuticals, Inc. and is associated with the Upneeq development program. (USPTO, 2021a; FDA, 2020a)

How broad is claim 1 of US 10,940,138?

Claim 1 has six principal limitation groups:

The subject must be an adult.
The condition must be acquired blepharoptosis.
The formulation must be aqueous, ophthalmic, sterile, and preservative-free.
The formulation must contain the specified active ingredient, salts, buffers, and hypromellose.
The formulation must fall within the claimed pH and viscosity ranges.
The formulation must demonstrate at least 24 months of stability under the claimed temperature conditions.

The claim uses "comprising," which generally permits additional ingredients unless those ingredients alter another express limitation or create a conflict with the claim. An accused product could therefore contain an ingredient not expressly listed, but it would still need to satisfy the stated composition, pH, viscosity, sterility, preservative-free, and stability limitations.

The claim is narrower than a claim directed to any oxymetazoline ophthalmic formulation. A formulation using 0.05% oxymetazoline, a different viscosity modifier, a different buffer system, or a substantially different pH may avoid literal infringement of claim 1. It could still raise infringement issues under dependent claims, other patent claims, or the doctrine of equivalents, depending on the facts.

What formulation is protected by US 10,940,138?

The protected formulation is characterized by a balanced electrolyte and buffer system with hypromellose as the viscosity-enhancing polymer.

The formulation has several functional characteristics:

Oxymetazoline hydrochloride provides alpha-adrenergic activity that elevates the upper eyelid.
Hypromellose produces a viscosity range of approximately 15 to 35 cPs.
Sodium chloride, potassium chloride, calcium chloride, and magnesium chloride provide an ophthalmically compatible electrolyte environment.
Sodium acetate and sodium citrate provide buffering.
The formulation is preservative-free and intended for ophthalmic administration.
The pH range is compatible with ocular administration and product stability.
The 24-month stability limitation links the formulation to a commercial shelf-life requirement.

The hydrate limitations in claims 3 and 29 may matter in a formulation comparison. A generic product using anhydrous or alternative salt forms could argue that it does not literally meet those dependent claims. Claim 1, however, does not require all of the hydrate forms recited in claim 29.

Which claims are strongest commercially?

The strongest commercial claims are claims 1 and 30, but they operate differently.

Claim	Scope	Commercial importance
1	Open-comprising method claim covering treatment with the defined formulation	Primary barrier to an equivalent Upneeq formulation
2	Converts 0.1 wt% oxymetazoline HCl to approximately 0.09 wt% free base	Clarifies active-equivalent concentration
6	Narrows pH to approximately 6.3 to 6.5	Relevant to products closely matching Upneeq
8	Requires aseptic preparation	Adds manufacturing limitation
9-11	Add temperature and humidity stability conditions	Potentially difficult to establish from public product information
12	Narrows viscosity to approximately 26 cPs	Targets the commercial formulation
13-16	Specify once-daily administration and one- or two-eye dosing	Relevant to product labeling and induced infringement
17-21	Add pharmacokinetic parameters	Narrow method-of-treatment limitations
22-28	Add MRD1 and LPFT efficacy measurements	Narrow clinical-use claims
29	Requires specified hydrate forms	Formulation-specific fallback claim
30	Closed "consisting of" formulation claim with hydrate forms	Stronger composition definition but narrower scope

Claims 13 through 16 are particularly relevant to an ANDA strategy because a generic label that instructs once-daily administration to one or both eyes could provide evidence supporting induced infringement. The strength of that theory would depend on the final approved label and the scope of the listed claims.

What do the pharmacokinetic and efficacy claims add?

Claims 17 through 21 require pharmacokinetic results after administration to both eyes, including:

Tmax from approximately 0.5 to 12 hours;
median Tmax of approximately two hours;
mean Cmax of approximately 30.5 ± 12.7 pg/mL;
mean AUCinf of approximately 468 ± 214 pg*hr/mL; and
mean half-life of approximately 8.3 hours.

These claims are narrower than the core formulation claims. They may be difficult to assert against a generic unless the claimant can establish that the generic administration produces the claimed pharmacokinetic results or that the generic label directs conduct reasonably expected to produce those results.

Claims 22 through 28 cover efficacy assessment using:

Marginal reflex distance 1, or MRD1; and
the Leicester Peripheral Field Test, or LPFT.

The claimed clinical effects include an MRD1 increase continuing through approximately eight hours, a maximum MRD1 increase at approximately two hours, and LPFT improvement of approximately five to ten points from baseline at specified time points.

These claims have greater relevance to clinical-use programs, label-directed evidence, and post-approval studies than to ordinary product composition comparison.

When does US Patent 10,940,138 expire?

The patent’s effective expiration date must be determined from the complete prosecution and continuity record, including the earliest effective nonprovisional filing date, patent-term adjustment, terminal disclaimers, and any applicable regulatory extension.

The patent issued in 2021. Its nominal term is generally 20 years from the earliest effective nonprovisional filing date under 35 U.S.C. § 154. The patent’s expiration should therefore be reviewed against the USPTO Patent Center record and the current FDA Orange Book listing before making launch or valuation decisions. (35 U.S.C. § 154; USPTO, 2021b; FDA, 2024a)

The patent’s commercial exclusivity cannot be determined solely from the issue date. Patent expiration, FDA regulatory exclusivity, and Orange Book listing dates are separate legal concepts.

What is the FDA regulatory status of the protected product?

The formulation is associated with Upneeq, oxymetazoline hydrochloride ophthalmic solution 0.1%. The FDA approved Upneeq on July 8, 2020, under NDA 212520 for acquired blepharoptosis in adults. (FDA, 2020a; FDA, 2020b)

The FDA label describes once-daily administration of one drop in each affected eye. The marketed product is a sterile, preservative-free ophthalmic solution supplied in single-use containers. The approved indication aligns closely with the patient and disease limitations in US 10,940,138.

Regulatory item	Status
Product	Upneeq
Active ingredient	Oxymetazoline hydrochloride
Strength	0.1% ophthalmic solution
Sponsor	RVL Pharmaceuticals
FDA application	NDA 212520
Approval date	July 8, 2020
Indication	Acquired blepharoptosis in adults
Dosage form	Sterile ophthalmic solution
Preservative status	Preservative-free
Administration	Once daily to affected eye or eyes

The FDA approval is important because the patent’s method claims track the approved product’s indication, formulation, and dosing instructions. That alignment may increase the risk that a generic label would practice at least some of the patented methods.

What is the Orange Book status of US 10,940,138?

US 10,940,138 is associated with the Upneeq patent estate and should be reviewed in the current FDA Orange Book under NDA 212520. Orange Book status can change through patent listing updates, delistings, corrections, statutory declarations, and product discontinuation information.

A listed patent may require an ANDA applicant to make a certification under section viii, Paragraph I, Paragraph II, Paragraph III, or Paragraph IV of the Hatch-Waxman statute, depending on the patent and the applicant’s product and labeling strategy.

For a patent directed to a method of use, a generic applicant may attempt a section viii statement or a labeling carve-out if the patented use can be omitted while leaving a noninfringing use. That strategy is more difficult when the approved product has a single principal indication that substantially overlaps the patented method.

How would a generic company challenge this patent?

A generic applicant could pursue several pathways.

Paragraph IV invalidity or noninfringement challenge

A Paragraph IV certification could assert that US 10,940,138 is invalid, unenforceable, or not infringed. Potential arguments would likely focus on:

anticipation or obviousness based on prior oxymetazoline ophthalmic formulations;
lack of written description for the full combination of composition and performance limitations;
enablement of the claimed 24-month stability and viscosity ranges;
indefiniteness of terms such as "about," "therapeutically effective amount," or "stable";
failure to satisfy method-of-treatment requirements;
noninfringement based on pH, viscosity, excipient, hydrate, or stability differences; and
lack of induced infringement where the proposed label does not direct the patented method.

A Paragraph IV notice can trigger Hatch-Waxman litigation and a statutory 30-month stay of FDA approval in the circumstances specified by the statute. (21 U.S.C. § 355(j); 21 C.F.R. § 314.94)

Section viii carve-out

A section viii statement could be available if the generic label omits the patented acquired-blepharoptosis use and retains a legally permissible unpatented use. For Upneeq, the practical value of that strategy is limited if the product has no meaningful approved use outside acquired blepharoptosis.

Formulation design-around

A competitor could attempt to avoid the claims by changing one or more of the following:

oxymetazoline concentration;
hypromellose concentration or replacement polymer;
buffer system;
electrolyte concentrations;
pH;
viscosity;
preservative status;
hydrate form; or
stability profile.

A design-around must account for claim 1’s "about" ranges and potential equivalents analysis. A minor numerical change may not create a reliable noninfringement position if the resulting formulation remains materially equivalent.

What generic launch risks exist?

The principal generic-entry risks are formulation overlap and label overlap.

Risk area	Relevance
Same 0.1% oxymetazoline strength	High
Same hypromellose-based viscosity system	High
Same electrolyte and buffer profile	High
Same once-daily dosing	High
Same adult acquired-ptosis indication	High
Same pH range	Moderate to high
Same 24-month stability profile	Moderate
Same pharmacokinetic results	Moderate
Same MRD1 or LPFT claims	Lower, unless included in labeling or clinical materials
Hydrate-form matching	Relevant mainly to claims 29 and 30

A generic product could avoid some dependent claims while still infringing claim 1. Conversely, a formulation difference that avoids claim 1 may also avoid claim 30 if it uses different salts, different hydrate forms, or a different ingredient set.

Which companies are challenging the Upneeq patent estate?

No challenger can be identified from the claim text alone. Public litigation, ANDA notices, and Paragraph IV disputes must be assessed from current PACER, USPTO, FDA Orange Book, and FDA litigation records.

The relevant challenger universe includes generic ophthalmic manufacturers with experience in sterile, preservative-free, single-dose products. The technical barrier is higher than for an ordinary tablet because the product requires sterile ophthalmic manufacturing, tight viscosity control, stability support, and packaging compatibility.

How strong is the patent estate for Upneeq?

US 10,940,138 has moderate-to-strong commercial relevance but narrow technical scope.

Strengths

The claim tracks the approved product’s indication and dosing.
The formulation limitations identify a specific commercial product profile.
The patent includes composition, stability, viscosity, pharmacokinetic, dosing, and efficacy fallback claims.
Sterile and preservative-free requirements create manufacturing barriers.
A generic label may closely reproduce the claimed method of treatment.

Weaknesses

The independent claims are method claims rather than broad composition claims.
The claims require many cumulative limitations.
Formulation design-around options exist.
The use of "about" and performance limitations may create claim-construction disputes.
A generic may challenge stability, pH, viscosity, or hydrate-form limitations separately.
The pharmacokinetic and clinical-assessment claims are difficult to enforce without label or clinical evidence tying the generic product to those limitations.

The patent is strongest against a product that reproduces the Upneeq formulation and carries the same acquired-blepharoptosis, once-daily dosing instructions. It is weaker against a product with a materially different formulation or a carved-out label.

Does US 10,940,138 create biosimilar risk?

No. Upneeq is a small-molecule oxymetazoline hydrochloride product, not a biologic. The relevant entry pathway is an ANDA for a generic drug, not a biosimilar application under the Public Health Service Act.

The competitive risks are therefore:

Paragraph IV patent litigation;
section viii labeling strategies;
formulation design-around;
potential 180-day generic exclusivity; and
post-approval commercial substitution.

Are formulation and manufacturing barriers material?

Yes. The patent claims a formulation that must be sterile, preservative-free, stable for at least 24 months, and within a defined viscosity range. Those requirements create technical barriers independent of patent scope.

A competitor must establish:

aseptic processing or an equivalent sterile manufacturing process;
container-closure integrity;
preservative-free microbial control;
viscosity consistency;
active-ingredient uniformity;
degradation control;
stability at relevant temperature and humidity conditions; and
compatibility with single-use ophthalmic packaging.

Claim 8 specifically requires aseptic preparation. Claims 9 through 11 add stability conditions involving temperature and relative humidity. These limitations may provide litigation leverage if the generic’s regulatory dossier or product testing demonstrates the claimed conditions.

What licensing deals affect the patent landscape?

The patent and FDA approval records establish the relationship between RVL Pharmaceuticals and Upneeq, but they do not by themselves establish the full commercial licensing history for the oxymetazoline formulation, development technology, or patent portfolio.

Any valuation or freedom-to-operate review should distinguish:

patent ownership;
exclusive development rights;
manufacturing rights;
commercialization rights;
royalty obligations; and
prosecution-control rights.

Those rights may be distributed across RVL affiliates, inventors, contract manufacturers, or prior technology providers even when the patent is assigned to a single entity.

What is the expected generic launch scenario?

The most likely launch sequence is:

A generic applicant develops a 0.1% oxymetazoline ophthalmic solution.
The applicant evaluates whether its product falls within the formulation and method claims.
The applicant files an ANDA with Paragraph III, Paragraph IV, or section viii positions for listed patents.
The patent holder assesses infringement and may file Hatch-Waxman litigation.
FDA approval is delayed by statutory stays or litigation outcomes.
Entry occurs on patent expiry, settlement date, court decision, or an agreed license date.

An exact launch date cannot be inferred from US 10,940,138 alone because entry depends on the complete Orange Book listing, additional patents, regulatory exclusivity, litigation, and any settlement agreement.

Key Takeaways

US 10,940,138 is a formulation-specific method-of-treatment patent associated with Upneeq.
Claim 1 requires adult acquired blepharoptosis, a sterile preservative-free formulation, defined excipients, pH, viscosity, and stability.
Claim 30 is narrower and uses a closed "consisting of" formulation description with specified hydrate forms.
The patent is not a broad patent on oxymetazoline or all ophthalmic treatment of ptosis.
The greatest generic risk arises from reproducing the Upneeq formulation and labeling.
Paragraph IV, section viii, and formulation design-around strategies are the principal generic challenges.
Upneeq is a small-molecule product, so biosimilar competition is not applicable.
The FDA approved Upneeq on July 8, 2020, under NDA 212520.
Expiration and Orange Book conclusions require review of the complete patent and regulatory records, including additional listed patents and any patent-term adjustment.
The patent’s practical strength is highest against an identical or near-identical formulation with the same once-daily acquired-blepharoptosis indication.

FAQs About US Patent 10,940,138

Is US 10,940,138 a composition patent?

No. Its principal claims are methods of treating acquired blepharoptosis using a defined formulation. Claim 30 describes the formulation within a method claim.

Does the patent cover all oxymetazoline eye drops?

No. The claims require specific excipients, concentration ranges, formulation properties, and treatment conditions.

Can a generic avoid the patent by changing the pH?

Possibly, but only if the changed pH falls outside the claim scope and does not remain equivalent to the claimed range. The analysis also must account for other formulation and method claims.

Does the patent cover treatment of congenital ptosis?

The claims specify acquired blepharoptosis in an adult. Treatment of congenital ptosis is outside that express patient and disease limitation.

Is Upneeq protected by patents beyond US 10,940,138?

The commercial product may be protected by additional patents, regulatory exclusivity, trademarks, and other intellectual-property rights. The complete Orange Book and USPTO records must be reviewed to determine the full protection period.

References

Food and Drug Administration. (2020a). Upneeq (oxymetazoline hydrochloride ophthalmic solution) approval letter, NDA 212520. U.S. Department of Health and Human Services.
Food and Drug Administration. (2020b). Upneeq prescribing information. U.S. Department of Health and Human Services.
Food and Drug Administration. (2024a). Approved drug products with therapeutic equivalence evaluations. U.S. Department of Health and Human Services.
United States Code. (2024). 21 U.S.C. § 355: New drugs.
United States Code. (2024). 35 U.S.C. § 154: Contents and term of patent; provisional rights.
United States Patent and Trademark Office. (2021a). US Patent No. 10,940,138: Methods of treating acquired blepharoptosis.
United States Patent and Trademark Office. (2021b). Patent Center prosecution and patent-term records for US Patent No. 10,940,138.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Rvl Pharms	UPNEEQ	oxymetazoline hydrochloride	SOLUTION/DROPS;OPHTHALMIC	212520-001	Jul 8, 2020		RX	Yes	Yes	⤷ Start Trial	⤷ Start Trial				METHOD OF TREATING BLEPHAROPTOSIS	⤷ 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	2020268329	⤷ Start Trial
Brazil	112021022404	⤷ Start Trial
Canada	3139443	⤷ Start Trial
Chile	2021002918	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 10,940,138

Which drugs does patent 10,940,138 protect, and when does it expire?

Summary for Patent: 10,940,138