United States Patent 11,020,385: Netarsudil Glaucoma Treatment Claims and Patent Landscape
U.S. Patent No. 11,020,385 protects a dosing regimen for netarsudil dimesylate, the active pharmaceutical ingredient in Rhopressa. The patent covers daily ocular instillation of an approximately 0.02% netarsudil solution for glaucoma or ocular hypertension, including once-daily dosing for periods extending up to one year. It is a method-of-treatment patent, not a broad composition-of-matter patent.
The patent’s commercial relevance depends on whether a generic applicant seeks approval for the same once-daily 0.02% ophthalmic regimen and whether the patent is listed in the FDA Orange Book for the relevant reference product. The claims are narrower than a basic netarsudil compound patent because they require the specific active ingredient, ocular administration, daily dosing, and the specified disease indication.
What does U.S. Patent 11,020,385 protect?
U.S. Patent 11,020,385 protects methods of treating glaucoma or ocular hypertension by administering netarsudil dimesylate through ocular instillation. The principal claim limitations are:
| Claim element |
Scope |
| Disease |
Glaucoma or ocular hypertension |
| Route |
Ocular instillation |
| Active ingredient |
(S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate dimesylate |
| Drug class |
Rho kinase inhibitor |
| Frequency |
Daily administration |
| Duration |
Up to one year in dependent claim 2 |
| Concentration and volume |
About one drop of an about 0.02% solution per eye |
| Frequency refinement |
Once daily in claims 5 through 8 |
The chemical name identifies netarsudil dimesylate. The approved product Rhopressa contains netarsudil dimesylate ophthalmic solution at 0.02% and is labeled for reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.[2]
Claim 1 is the broadest independent claim. It requires all of the following:
- A subject has glaucoma or ocular hypertension.
- The subject receives a composition containing a Rho kinase inhibitor and a pharmaceutically acceptable carrier.
- The Rho kinase inhibitor is the specified netarsudil dimesylate compound.
- Administration occurs by ocular instillation.
- Administration is daily.
The claim does not expressly require once-daily dosing, a one-year treatment period, or the exact one-drop 0.02% regimen. Those limitations appear in dependent claims.
How do claims 1 through 8 differ?
Claims 1 through 8 form a progressively narrower regimen structure.
| Claim |
Added limitation |
Practical effect |
| 1 |
Daily ocular administration of netarsudil dimesylate for glaucoma or ocular hypertension |
Broadest method claim |
| 2 |
Daily administration for up to one year |
Adds treatment duration |
| 3 |
About one drop of an about 0.02% solution per eye |
Adds dose and concentration |
| 4 |
Claim 3 regimen for up to one year |
Combines dose, concentration, and duration |
| 5 |
Daily administration is once daily |
Narrows frequency |
| 6 |
Once daily for up to one year |
Combines frequency and duration |
| 7 |
One drop of about 0.02% solution per eye, once daily |
Closely tracks the Rhopressa labeled regimen |
| 8 |
One drop of about 0.02% solution per eye, once daily for up to one year |
Narrowest express claim |
Claim 8 is the closest match to the commercial Rhopressa dosing instructions. The FDA label directs administration of one drop in the affected eye once daily in the evening.[2]
What is the scope of the netarsudil method-of-use claims?
The scope is centered on regimen use rather than chemical identity alone.
A product could contain netarsudil dimesylate without necessarily infringing every claim. Infringement would generally require use of the product in a manner satisfying the claimed treatment conditions. For example, a formulation containing netarsudil could fall outside claim 8 if it is not administered once daily, is not delivered by ocular instillation, or is not used to treat glaucoma or ocular hypertension.
Claim 1 is broader than claims 3, 5, and 7 because it does not state:
- a one-drop volume;
- a 0.02% concentration;
- once-daily dosing;
- a treatment duration of up to one year.
A generic product administered once daily as a 0.02% ophthalmic solution would present the clearest literal infringement risk under claims 1, 3, 5, and 7, assuming the generic label directs use for glaucoma or ocular hypertension.
The use of “about” in claims 3, 4, 7, and 8 creates numerical flexibility around the one-drop volume and 0.02% concentration. The precise boundaries would depend on claim construction, specification support, prosecution history, and the accused product’s formulation and labeling.
When does U.S. Patent 11,020,385 expire?
U.S. Patent 11,020,385 was issued on June 1, 2021. Its family is associated with a July 29, 2016 priority date and Aerie Pharmaceuticals, Inc. as the original patent owner.[1]
The patent has a nominal statutory term extending into 2037, subject to the effective patent-term calculation, terminal disclaimers, and any patent-term adjustment shown in USPTO records. The relevant commercial planning date is therefore the 2037 patent-term horizon rather than the 2021 issue date.
| Event |
Date |
| Earliest reported priority |
July 29, 2016 |
| Patent grant |
June 1, 2021 |
| Nominal term horizon |
2037 |
| Product associated with the regimen |
Rhopressa 0.02% ophthalmic solution |
| Active ingredient |
Netarsudil dimesylate |
Patent expiration should be assessed together with earlier netarsudil patents, later continuation patents, Orange Book listings, and any pediatric exclusivity or patent-term adjustment. Patent 11,020,385 is not the only potential barrier affecting generic entry.
What is the Orange Book status of netarsudil and Rhopressa?
Rhopressa is an FDA-approved small-molecule ophthalmic drug, not a biologic. Its regulatory pathway is an abbreviated new drug application, or ANDA, for a generic product, rather than the biosimilar pathway under section 351(k) of the Public Health Service Act.
Orange Book relevance depends on whether the NDA holder listed particular patents for the approved drug and whether the listed patents include a method-of-use code that corresponds to the approved indication.[3] Method-of-use patents can be listed when they claim an approved method of using the drug. A generic applicant must address listed patents through an appropriate certification.
The key regulatory questions are:
- whether U.S. Patent 11,020,385 is listed against the relevant Rhopressa NDA;
- which use code is associated with the listing;
- whether the ANDA applicant seeks the same glaucoma or ocular-hypertension indication;
- whether the applicant uses a section viii statement to omit a patented use;
- whether the applicant files a Paragraph IV certification challenging validity, enforceability, or infringement.
An ANDA applicant cannot use a section viii statement to carve out the core indication if the proposed labeling still instructs use for the patented glaucoma or ocular-hypertension regimen. A successful carve-out would require a legally and regulatorily acceptable label that omits the patented method.
What Paragraph IV risks exist for generic netarsudil?
A Paragraph IV certification would assert that a listed patent is invalid, unenforceable, or will not be infringed by the proposed generic product. For Patent 11,020,385, likely challenge theories would focus on claim scope and patentability rather than chemical identity.
Potential invalidity theories include:
Anticipation
A challenger could argue that earlier clinical, patent, or regulatory disclosures described daily topical netarsudil use for glaucoma or ocular hypertension. The critical issue would be whether one prior-art reference disclosed all elements of the challenged claim, including the specified netarsudil dimesylate compound and the required daily ocular regimen.
Obviousness
A challenger could argue that daily topical administration of a ROCK inhibitor for elevated intraocular pressure was obvious in view of earlier netarsudil disclosures, clinical studies, or related ROCK-inhibitor patents. The patent holder would likely rely on clinical efficacy, tolerability, dosing selection, or unexpected results.
Written description and enablement
Claims 1 and 2 cover a treatment regimen extending up to one year. A challenger could examine whether the specification adequately supports the full claimed duration and whether the disclosed data enable treatment across the full scope of glaucoma and ocular-hypertension patients.
Indefiniteness
The terms “about one drop” and “about 0.02%” appear in the narrower claims. A challenge could address the boundaries of those terms, although approximate pharmaceutical concentrations and drop volumes are common claim language.
Noninfringement
A generic applicant could design its labeling, concentration, dosing frequency, or indication to avoid one or more claim limitations. The risk is highest when the proposed label reproduces the Rhopressa regimen.
Which companies are challenging the netarsudil patent estate?
The principal commercial challengers would be ANDA applicants seeking approval for generic netarsudil ophthalmic solution. A public challenge must be evaluated through FDA Paragraph IV notice litigation, district-court complaints under the Hatch-Waxman framework, and Orange Book records.
The available patent record identifies Aerie Pharmaceuticals as the original developer and patent owner associated with the netarsudil program. Alcon acquired Aerie in 2019 and obtained the Rhopressa and Rocklatan businesses.[4] The relevant competitive set therefore includes:
| Company category |
Role |
| Alcon |
Current commercial owner of the Aerie ophthalmology portfolio |
| Aerie Pharmaceuticals |
Original developer and patent-originator entity |
| Generic ophthalmic manufacturers |
Potential ANDA applicants |
| Specialty ophthalmic companies |
Potential licensees, acquirers, or development partners |
A generic company’s Paragraph IV notice is not equivalent to a final court ruling. Market entry depends on litigation timing, the 30-month stay, claim construction, settlement terms, and any appeal.
What litigation and settlement issues affect Patent 11,020,385?
A Hatch-Waxman action involving the patent could trigger a statutory stay of FDA approval for up to 30 months after receipt of a Paragraph IV notice, unless the litigation is resolved earlier or the court orders otherwise.[5]
The principal litigation questions would be:
- Is the patent listed for the relevant Rhopressa indication?
- Does the ANDA label direct the patented once-daily regimen?
- Does the generic formulation contain netarsudil dimesylate at approximately 0.02%?
- Can the generic sponsor establish noninfringement through a label carve-out?
- Are the claims valid over earlier ROCK-inhibitor and netarsudil disclosures?
- Has the patent owner entered into a settlement allowing a future generic launch?
A settlement could provide for:
- a fixed licensed entry date;
- an earlier launch tied to another generic entrant;
- supply or licensing rights;
- a covenant not to sue for specified products;
- restrictions on formulation, indication, or manufacturing.
No settlement should be treated as a market-entry date unless its terms are publicly filed or disclosed by the parties.
How does Patent 11,020,385 compare with composition and formulation patents?
Patent 11,020,385 is narrower in subject matter than a compound patent and different from a formulation patent.
| Patent type |
Typical protection |
Relevance to netarsudil |
| Composition of matter |
Netarsudil molecule or salt |
Broadest chemical exclusivity |
| Ophthalmic formulation |
Vehicle, pH, excipients, concentration, stability |
Can block formulation substitution |
| Method of use |
Treatment of glaucoma or ocular hypertension |
Targets labeled clinical use |
| Dosing regimen |
Once-daily or specified administration period |
Targets commercial prescribing instructions |
| Manufacturing process |
Synthesis, purification, crystallization, or salt formation |
Can create supply-chain barriers |
| Device or container |
Bottle, dropper, preservative system |
Usually narrower commercial protection |
The ’385 patent does not, based on the asserted claims, broadly claim every netarsudil composition. It claims administration of a specified netarsudil dimesylate composition in a particular therapeutic context. A generic company may therefore face a layered estate consisting of compound, formulation, use, and manufacturing patents.
Are biosimilar risks relevant to netarsudil?
No. Netarsudil is a synthetic small molecule. Biosimilar approval under section 351(k) does not apply. The relevant competitive route is an ANDA demonstrating pharmaceutical equivalence and bioequivalence, together with patent certifications and any required labeling carve-outs.
The principal generic development barriers are likely to include:
- ophthalmic solution equivalence;
- drop-volume consistency;
- preservative and excipient selection;
- container-closure performance;
- sterility assurance;
- stability;
- local tolerability;
- patent certification strategy.
What manufacturing and formulation barriers exist?
Netarsudil ophthalmic products must meet FDA requirements for sterile ophthalmic manufacturing. A generic sponsor must demonstrate product quality and bioequivalence while managing the formulation and device attributes that affect delivered dose.
The ’385 claims do not expressly require a particular preservative, buffer, viscosity agent, bottle, or manufacturing process. Those attributes may be protected elsewhere in the patent family or in separate formulation and process patents.
Manufacturing risks include:
- control of netarsudil dimesylate purity;
- salt-form consistency;
- degradation control;
- sterile fill-finish;
- drop-size reproducibility;
- compatibility with the bottle and closure;
- preservative concentration;
- stability throughout the labeled shelf life.
These technical issues can create practical launch delays even when a generic sponsor defeats or avoids a method-of-use patent.
How strong is the patent estate for the Rhopressa regimen?
The ’385 patent has strong claim-to-product alignment because claims 7 and 8 track the commercial 0.02% once-daily regimen. That alignment supports an infringement case against a generic label that reproduces the Rhopressa instructions.
Its limitations also create potential attack points. The patent does not claim the active ingredient without qualification. It requires the specified indication and daily ocular administration. A generic sponsor may focus on:
- prior-art disclosures of netarsudil dosing;
- obviousness of once-daily administration;
- the evidentiary basis for treatment of up to one year;
- the meaning of “about” in the dose claims;
- label-based noninfringement;
- the distinction between composition ownership and method-of-use enforcement.
The practical strength of the patent depends on the full prosecution history, cited prior art, Orange Book listing, claim construction, and the generic’s proposed label. The narrowest claims may be the most commercially useful because they map directly to the approved Rhopressa regimen, even though they contain more limitations.
What generic launch scenarios exist?
Launch after patent expiry
The lowest-risk scenario is entry after the effective expiration of the relevant listed patents and exclusivities. A generic company could launch an ANDA-approved product with the full approved indication if no surviving patent blocks that label.
Paragraph IV launch after a favorable judgment
A generic may launch before patent expiry after prevailing in litigation or obtaining a ruling that the patent is invalid, unenforceable, or not infringed. The launch could remain subject to appeal risk and other patents in the estate.
Launch under a settlement license
A settlement may authorize entry before expiration on a negotiated date. The commercial value of that date depends on whether other generic entrants receive the same rights.
Label-carved-out launch
A generic may seek approval with a label excluding a patented method under section viii. This strategy is difficult if the patented method overlaps the core glaucoma or ocular-hypertension indication and the approved label cannot be meaningfully separated from the claimed regimen.
What geographic coverage does the patent provide?
U.S. Patent 11,020,385 provides rights only in the United States. Related applications may exist in other jurisdictions through the same international patent family, but foreign rights have separate claim scopes, prosecution histories, expiration dates, and enforceability rules.
For global launch planning, the relevant analysis must separate:
- United States patent rights;
- European Patent Convention validations;
- Japan;
- Canada;
- Australia;
- China;
- other markets where Rhopressa or netarsudil products are approved.
A U.S. patent does not block sale in foreign markets. Conversely, foreign formulation or method patents may affect launch even after the U.S. ’385 patent expires.
What is the revenue exposure associated with the patent?
The patent protects a commercially important regimen because Rhopressa’s approved use is once-daily reduction of elevated intraocular pressure. A successful generic entry could affect:
- Rhopressa prescription volume;
- netarsudil franchise pricing;
- combination-product positioning for Rocklatan;
- payer formulary status;
- ophthalmology sales force economics;
- Alcon’s U.S. glaucoma portfolio.
The ’385 patent alone does not determine the full revenue-at-risk period. Revenue exposure must be modeled against the entire listed patent estate, regulatory exclusivity, generic filing activity, settlement dates, and the possibility of at-risk launch.
Key Takeaways
- U.S. Patent 11,020,385 is a netarsudil dimesylate method-of-treatment patent.
- It covers daily ocular instillation for glaucoma or ocular hypertension.
- Claims 7 and 8 closely track the Rhopressa regimen of one drop of approximately 0.02% solution once daily.
- The patent does not broadly claim every netarsudil composition.
- The patent was granted June 1, 2021 and has a nominal term horizon extending into 2037.
- Generic risk will turn on Orange Book listing, Paragraph IV certifications, label design, and the strength of prior art.
- Biosimilar competition is not relevant because netarsudil is a synthetic small molecule.
- Formulation, compound, manufacturing, and related method patents may create additional barriers beyond the ’385 patent.
- A section viii carve-out may be difficult if the proposed generic label necessarily includes the patented glaucoma or ocular-hypertension regimen.
- Any commercial launch forecast must analyze the full Rhopressa patent estate rather than Patent 11,020,385 in isolation.
FAQs about U.S. Patent 11,020,385
Does Patent 11,020,385 cover Rocklatan?
The asserted claims cover netarsudil dimesylate treatment, not a fixed combination containing latanoprost. Rocklatan contains netarsudil and latanoprost, so separate composition, formulation, or method claims may be relevant.
Can a generic avoid the patent by using a concentration other than 0.02%?
A concentration change could avoid the narrower claims that expressly require an approximately 0.02% solution. It may not avoid claim 1, which does not expressly require 0.02%, if the other claim elements remain satisfied.
Does twice-daily dosing avoid the once-daily claims?
Twice-daily dosing may avoid claims 5 through 8, which expressly require once-daily administration. It may still raise issues under claim 1 if the claim’s “daily administration” limitation is construed to include a regimen administered every day, regardless of the number of daily doses.
Is the patent limited to open-angle glaucoma?
The claims state glaucoma or ocular hypertension and do not expressly limit treatment to open-angle glaucoma. The approved Rhopressa indication is reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.
Can a generic launch before 2037?
Potentially, but only through a route that removes or manages the relevant patent barriers. Possible paths include a successful Paragraph IV challenge, a noninfringing label, a negotiated license, a court decision finding no infringement, or expiration of all blocking patents and regulatory exclusivities.
References
- United States Patent and Trademark Office. (2021). U.S. Patent No. 11,020,385, Methods of treating glaucoma with netarsudil. https://patents.google.com/patent/US11020385B2/en
- U.S. Food and Drug Administration. (2017). Rhopressa (netarsudil ophthalmic solution) 0.02% prescribing information. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208254s000lbl.pdf
- U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book. https://www.accessdata.fda.gov/scripts/cder/ob/
- Alcon, Inc. (2019). Alcon completes acquisition of Aerie Pharmaceuticals. https://investor.alcon.com
- U.S. Food and Drug Administration. (2024). Hatch-Waxman amendments and abbreviated new drug applications. https://www.fda.gov/drugs/abbreviated-new-drug-application-anda/abbreviated-new-drug-application-anda
