United States Drug Patent 9,993,470: Claim Scope, Netarsudil Combination Protection and Patent Landscape

U.S. Patent No. 9,993,470 protects compositions and treatment methods combining netarsudil dimesylate with a prostaglandin analog or related ocular hypotensive agent. The commercially important embodiment is the fixed combination of netarsudil dimesylate and latanoprost marketed as Rocklatan. The patent does not broadly protect netarsudil monotherapy, latanoprost monotherapy, or every glaucoma formulation containing either ingredient.

The patent’s core value is combination-product protection. A product must contain both the specified netarsudil salt form and at least one listed prostaglandin or prostaglandin-related agent to fall within independent claim 1. Claims 8 through 20 extend that combination coverage to methods of treating ocular disorders, particularly glaucoma, including topical administration.

What drug does U.S. Patent 9,993,470 protect?

The active compound identified in the claims is netarsudil, also known as AR-13324. The claims cover the dimesylate salt of three stereochemical forms:

Claimed form	Chemical status	Commercial relevance
(S)-netarsudil dimesylate	Active enantiomer used commercially	Primary form in Rhopressa and Rocklatan
(R)-netarsudil dimesylate	Opposite enantiomer	Covered expressly, subject to the combination requirement
Racemic netarsudil dimesylate	Mixture of the two enantiomers	Covered expressly, subject to the combination requirement

Netarsudil is a Rho-associated coiled-coil-containing protein kinase, or ROCK, inhibitor. Rhopressa contains netarsudil ophthalmic solution as a single active ingredient. Rocklatan combines netarsudil with latanoprost, a prostaglandin F2α analog. The patent’s claim structure is directed primarily to combinations rather than the standalone ROCK inhibitor.

What are the independent claims of U.S. Patent 9,993,470?

Claim 1: Combination composition

Claim 1 requires a composition comprising:

One of the three listed netarsudil dimesylate forms; and
At least one listed prostaglandin analog or related compound.

The second component may be:

Latanoprost
Bimatoprost
Travoprost
Tafluprost
AR-102
Cloprostenol
Latanoprostene bunod
Unoprostone
PGF2α
Fluprostenol
A pharmaceutically acceptable salt of one of those compounds

The use of “comprising” makes claim 1 open-ended. A formulation containing the required netarsudil salt and latanoprost may infringe even if it also contains additional active ingredients, provided the other claim limitations are met.

The claim does not specify:

A required concentration
A netarsudil-to-prostaglandin ratio
A particular dosage volume
A specific container or delivery device
A required pH
A required preservative system
A required order of administration
A requirement that both active ingredients be chemically combined in one solution

Those omissions expand literal claim coverage, although they do not eliminate other infringement and validity questions.

Claims 2 through 7: Composition subclaims

Claim 2 narrows claim 1 to latanoprost. Claims 3 through 5 identify the S, R and racemic netarsudil forms. Claim 6 combines the S form with latanoprost. Claim 7 adds conventional ophthalmic excipients.

A key drafting point is that claims 3, 4 and 5 remain dependent on claim 1. They do not protect netarsudil alone. Each inherits claim 1’s requirement for a listed prostaglandin or related agent.

Claim 7 covers compositions that also contain at least one of the following:

Buffer
Chelating agent
Tonicity agent
Preservative
Viscosity enhancer
Sugar
Sugar alcohol
Surfactant

The excipient language is broad and functional. It reaches common ophthalmic formulation systems, including buffered, preserved and viscosity-modified aqueous solutions.

How do claims 8 through 20 protect glaucoma treatment?

Claims 8 through 20 are method claims. They require administering a composition containing the same two active-component categories:

Netarsudil dimesylate in the S, R or racemic form; and
A listed prostaglandin analog or related agent.

The method claims cover treatment of an ocular disorder. Claim 15 specifically identifies glaucoma. Claims 16 and 17 narrow the treatment to glaucoma in combinations involving the S form of netarsudil, including the S-netarsudil/latanoprost combination.

Claims 18 through 20 address topical administration to an eye. These claims are commercially relevant because Rocklatan and the principal comparator products are topical ophthalmic products.

Method-claim infringement risks

A generic or follow-on company may face method-claim exposure if:

Its product label instructs use of netarsudil with latanoprost;
The product is indicated for lowering intraocular pressure through the claimed combination;
The label identifies glaucoma treatment;
The formulation contains one of the claimed netarsudil salt forms and a listed prostaglandin analog.

A product sold solely as netarsudil monotherapy generally does not meet the combination limitation. A prostaglandin monotherapy also does not meet the claim.

What formulations are protected by U.S. Patent 9,993,470?

The patent protects combination compositions containing the claimed active ingredients, not a particular formulation technology. The most direct commercial embodiment is a fixed-dose ophthalmic solution containing netarsudil dimesylate and latanoprost.

Formulation categories within the claim scope

Formulation category	Likely claim relevance
Fixed-dose netarsudil/latanoprost ophthalmic solution	Directly aligned with claims 1, 2 and 6
Separate containers used together under a treatment regimen	Potential method-claim issue; composition claims depend on whether the ingredients are in the same composition
Preserved aqueous solution	Covered if the active-ingredient limitations are met
Preservative-free solution	Covered if the active-ingredient limitations are met
Formulation containing buffer or tonicity agent	Expressly addressed by claim 7
Formulation containing viscosity enhancer or surfactant	Expressly addressed by claim 7
Netarsudil-only solution	Outside the express combination requirement
Latanoprost-only solution	Outside the express combination requirement

Claims 1 and 8 use the term “composition,” which creates an important distinction. A fixed combination in one bottle is the clearest composition claim target. A regimen involving separately packaged products may present a stronger method-claim question than composition-claim question.

When does U.S. Patent 9,993,470 lose exclusivity?

U.S. Patent No. 9,993,470 was issued June 12, 2018. Its nominal patent term is generally measured from the applicable nonprovisional or international filing date, subject to patent-term adjustment, terminal disclaimers and any patent-term extension.

The patent’s priority and prosecution history must be used to calculate the controlling expiration date. A nominal term in the March 2035 period is consistent with a 2015 nonprovisional filing, before any adjustment or extension. The issue date alone does not determine expiration.

Event	Date or status
U.S. patent grant	June 12, 2018
Patent number	9,993,470
Primary subject matter	Netarsudil dimesylate plus prostaglandin combinations
Commercial product most closely aligned	Rocklatan
Nominal term period	Approximately March 2035, before any adjustment or extension
PTE/PTE effect	Must be verified against the patent file and FDA regulatory history

FDA regulatory exclusivity and patent exclusivity are separate. A generic may be blocked by listed patents after regulatory exclusivity expires, while patent expiration does not itself guarantee immediate approval.

What is the Orange Book status of U.S. Patent 9,993,470?

The claims are structurally suited to an Orange Book listing for a fixed netarsudil/latanoprost product such as Rocklatan. They are not naturally suited to listing against netarsudil monotherapy because every independent claim requires a second active ingredient from the specified prostaglandin group.

The relevant regulatory products are:

Product	Active ingredient	FDA status
Rhopressa	Netarsudil ophthalmic solution	Approved by FDA in 2017
Rocklatan	Netarsudil and latanoprost ophthalmic solution	Approved by FDA in 2019
Xalatan and generic latanoprost	Latanoprost	Mature prostaglandin market
Lumigan	Bimatoprost	Approved prostaglandin comparator
Travatan Z	Travoprost	Approved prostaglandin comparator
Vyzulta	Latanoprostene bunod	Approved nitric oxide-donating prostaglandin analog
Zioptan	Tafluprost	Approved prostaglandin analog

An Orange Book listing must be assessed by product and patent-use-code entry. The claim language alone cannot establish the current listing status, delisting status or any applicable pediatric exclusivity.

Which products face the greatest generic-entry risk?

Rocklatan generic risk

Rocklatan is the product most directly exposed to the patent because it contains netarsudil dimesylate and latanoprost in a single ophthalmic product. An ANDA applicant seeking approval for a therapeutically equivalent fixed combination would need to address any Orange Book-listed Rocklatan patents through the applicable certification pathway.

A Paragraph IV certification could challenge the patent before expiration. The patent’s broad “comprising” language creates a meaningful infringement risk for fixed combinations containing the claimed ingredients, but the patent remains subject to standard validity and enforceability challenges, including written description, enablement, obviousness and claim-construction arguments.

Rhopressa generic risk

Rhopressa monotherapy is less exposed to this patent because the claims require both netarsudil and a listed prostaglandin or related compound. Generic netarsudil products would instead be evaluated against patents directed to:

Netarsudil compounds
Netarsudil salts
Ophthalmic formulations
Dosage forms
Methods of lowering intraocular pressure
Crystalline or solid-state forms
Manufacturing processes

Patent 9,993,470 is therefore a combination patent, not the principal standalone-netarsudil patent.

Prostaglandin generic risk

Generic latanoprost, bimatoprost, travoprost or tafluprost products do not inherently practice the claims. They would need to contain the claimed netarsudil salt or be used in a claimed combination regimen.

What Paragraph IV challenges are relevant?

A Paragraph IV challenge is relevant only to an ANDA applicant seeking approval for a product associated with a listed patent. For this patent, the most direct target would be an ANDA for a fixed-dose netarsudil/latanoprost product or another listed netarsudil/prostaglandin combination.

Potential challenge positions include:

The proposed product does not contain the claimed salt form.
The proposed product contains a different netarsudil form or formulation.
The claims are invalid for obviousness in view of known ROCK inhibitors and prostaglandin therapies.
The claims lack adequate written description or enablement across the full Markush group.
The patent is not infringed because the product does not contain a claimed prostaglandin agent.
The method claims are not infringed by the proposed label.
The relevant claims are unenforceable because of prosecution-history or patent-term issues.

The supplied claims do not identify any Paragraph IV notice, ANDA filer, district-court action or settlement agreement. Those matters require separate review of FDA, USPTO and court records.

How strong is the patent estate for netarsudil and Rocklatan?

Patent 9,993,470 has meaningful commercial scope because it covers the most important fixed combination associated with netarsudil: netarsudil plus latanoprost. Its strength is greatest against a one-bottle combination product that uses S-netarsudil dimesylate and carries a glaucoma indication.

Its limitations are equally important:

It does not claim netarsudil monotherapy.
It does not claim latanoprost monotherapy.
It does not require a particular concentration.
It does not, based on the supplied claims, claim a unique excipient system.
It reaches multiple prostaglandin agents, but broader Markush coverage may create validity pressure.
Its method claims depend on the composition containing the required combination.

The patent should be analyzed as one layer in a broader product estate. A commercial freedom-to-operate opinion for Rocklatan would also require review of compound, formulation, method-of-use, process and Orange Book patents.

Does the patent cover biologics or biosimilar products?

No. The claimed molecules are small-molecule chemical entities. Biosimilar analysis is not the relevant entry framework.

The applicable competitive pathways are:

ANDA approval for generic fixed combinations
505(b)(2) approval for reformulated or modified combination products
New drug applications for alternative prostaglandin/ROCK inhibitor combinations
State and federal patent litigation involving abbreviated applications

A biosimilar cannot substitute for a small-molecule netarsudil product under the Biologics Price Competition and Innovation Act.

What licensing and ownership issues affect the patent?

Netarsudil was developed by Aerie Pharmaceuticals. Alcon completed its acquisition of Aerie in 2022, bringing Aerie’s ophthalmic commercial products and related intellectual-property assets into Alcon’s portfolio. The supplied claim set does not identify a license, assignment, co-owner or royalty obligation for U.S. Patent 9,993,470.

Ownership should be confirmed through the USPTO assignment database. Commercial rights should be distinguished from patent ownership because development, commercialization and patent rights may be divided among different entities.

What patent litigation and settlement issues affect U.S. Patent 9,993,470?

The claim text does not establish litigation status. The relevant litigation triggers would include:

A Paragraph IV notice concerning Rocklatan
A Hatch-Waxman action filed within 45 days of notice
A declaratory judgment action
A patent-term or Orange Book dispute
A settlement establishing an authorized generic or agreed launch date
A covenant not to sue or license affecting a specific ANDA applicant

No litigation or settlement conclusion should be drawn solely from the issued claims. For transaction or launch analysis, the controlling records are the FDA Orange Book, USPTO Patent Center, PACER and district-court docket filings.

What geographic coverage does the patent provide?

U.S. Patent No. 9,993,470 provides territorial rights in the United States. It does not directly establish protection in Europe, Canada, Japan, China or other markets.

International protection would depend on corresponding national or regional applications from the same patent family. The commercial risk for a global Rocklatan launch must therefore be mapped separately by jurisdiction, including:

Patent-family members
National-phase status
Local claim scope
Patent-term adjustments
Supplementary protection certificates
Local Orange Book equivalents
National litigation and settlement records

Key Takeaways

U.S. Patent 9,993,470 is a netarsudil combination patent.
Its central commercial embodiment is netarsudil dimesylate plus latanoprost, corresponding to Rocklatan.
Independent claims require both a claimed netarsudil dimesylate form and a listed prostaglandin or related ocular hypotensive agent.
The patent does not broadly cover Rhopressa netarsudil monotherapy.
Claims 7 and 14 cover conventional ophthalmic excipients but do not require a unique formulation technology.
Claims 8 through 20 create method-of-treatment coverage for ocular disorders, glaucoma and topical eye administration.
A fixed-dose generic Rocklatan product presents the clearest infringement and Paragraph IV risk.
Generic netarsudil monotherapy would primarily confront other compound, formulation and method patents.
The nominal patent term appears to extend into approximately March 2035, subject to the controlling filing date, patent-term adjustment and any extension.
Biosimilar risk is not applicable because netarsudil and latanoprost are small molecules.
Litigation, Orange Book listing and settlement conclusions require review of the current regulatory and court records.

FAQs About U.S. Patent 9,993,470

Does U.S. Patent 9,993,470 cover Rocklatan?

Yes. Rocklatan contains netarsudil and latanoprost, the combination most directly aligned with claims 1, 2 and 6, assuming the commercial netarsudil component is the claimed dimesylate form.

Does the patent block a generic version of Rhopressa?

Not by itself. Rhopressa is netarsudil monotherapy, while the independent claims require netarsudil plus a listed prostaglandin or related compound.

Can a generic company avoid the patent by using a different prostaglandin?

Possibly, but not if the substitute is one of the expressly listed compounds, such as bimatoprost, travoprost, tafluprost or latanoprostene bunod. A nonlisted agent would require separate claim-construction and infringement analysis.

Is a separately packaged netarsudil and latanoprost regimen covered?

The composition claims are strongest against a single composition containing both actives. Separately packaged products may still raise method-claim issues if the labeling instructs their combined use for glaucoma.

Is U.S. Patent 9,993,470 the only patent relevant to Rocklatan?

No. Rocklatan’s full exclusivity position may include additional formulation, method-of-use, compound, process and regulatory patents. This patent should be treated as one component of the broader product estate.

Sources

U.S. Patent and Trademark Office. (2018). United States Patent No. 9,993,470, Compositions and methods for treating ocular disorders.
U.S. Food and Drug Administration. (2017). Rhopressa approval information and prescribing information.
U.S. Food and Drug Administration. (2019). Rocklatan approval information and prescribing information.
U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations.
Alcon Inc. (2022). Annual report and disclosures concerning the acquisition of Aerie Pharmaceuticals.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Alcon Labs Inc	ROCKLATAN	latanoprost; netarsudil dimesylate	SOLUTION/DROPS;OPHTHALMIC	208259-001	Mar 12, 2019		RX	Yes	Yes	9,993,470	⤷ Start Trial	Y	Y		REDUCTION OF ELEVATED INTRAOCULAR PRESSURE	⤷ 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
European Patent Office	3461484	⤷ Start Trial	301101	Netherlands	⤷ Start Trial
European Patent Office	3461484	⤷ Start Trial	2021C/515	Belgium	⤷ Start Trial
European Patent Office	3461484	⤷ Start Trial	132021000000068	Italy	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 9,993,470

Which drugs does patent 9,993,470 protect, and when does it expire?

Summary for Patent: 9,993,470