Details for Patent: 11,197,853

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Which drugs does patent 11,197,853 protect, and when does it expire?

Patent 11,197,853 protects ROCKLATAN and is included in one NDA.

This patent has twenty-nine patent family members in thirteen countries.

Summary for Patent: 11,197,853

Title:	Combination therapy
Abstract:	Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog. Compounds described herein include those in which an isoquinoline compound is covalently linked to a prostaglandin or a prostaglandin analog, and those in which an isoquinoline compound and a prostaglandin free acid together form a salt.
Inventor(s):	Casey Kopczynski, Cheng-Wen Lin, Jill Marie Sturdivant, Mitchell A. deLong
Assignee:	Alcon Inc
Application Number:	US17/238,554
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 11,197,853
Patent Claim Types: see list of patent claims	Composition; Compound;

US Patent 11,197,853: Netarsudil-Latanoprost Composition Claims, Expiration, Orange Book Status, and Generic Risk

US Patent 11,197,853 protects ophthalmic compositions combining netarsudil dimesylate with latanoprost. The broadest independent claims cover the two active ingredients across wide concentration ranges. Narrower claims specify D-mannitol, boric acid, benzalkonium chloride, a pH of about 5.0, and a netarsudil dimesylate concentration of at least about 0.020% to less than about 0.05%.

The patent is directed to the Rocklatan formulation, not to netarsudil generally, latanoprost generally, or a method of treating glaucoma independent of the claimed composition. A competing product containing only netarsudil or only latanoprost would fall outside these claims. A generic or follow-on product combining both ingredients would face the greatest risk if it uses the claimed excipient system and concentration ranges.

What drug and formulation does US Patent 11,197,853 protect?

The chemical compound identified in the claims is netarsudil, administered as its dimesylate salt. Netarsudil is a Rho kinase inhibitor. Latanoprost is a prostaglandin F2-alpha analog used to reduce intraocular pressure.

The commercial combination is Rocklatan ophthalmic solution, approved by the FDA in 2019 for reduction of elevated intraocular pressure in patients with primary open-angle glaucoma or ocular hypertension. Rocklatan contains netarsudil 0.02% and latanoprost 0.005% in an ophthalmic solution.[2]

Element	Claimed or commercial specification
First active ingredient	Netarsudil dimesylate
Netarsudil concentration	About 0.01% to about 1.0% w/v in independent claims
Narrow netarsudil range	At least about 0.020% to less than about 0.05% w/v
Second active ingredient	Latanoprost
Latanoprost concentration	About 0.005% w/v
Tonicity agent	Mannitol, particularly D-mannitol
D-mannitol concentration	About 4.7% w/v
Buffer	Boric acid
Boric acid concentration	About 0.05% w/v
Preservative	Benzalkonium chloride
Benzalkonium chloride concentration	About 0.02% w/v
pH	About 5.0
Dosage form	Pharmaceutical ophthalmic composition

The patent’s chemical definition of netarsudil is important because the claims require the dimesylate salt of the specified stereochemical compound. A formulation containing a different salt, free base, different stereoisomer, or different active ingredient would require separate infringement analysis.

What are the independent claims in US Patent 11,197,853?

Claims 1, 19 and 21 are the principal independent composition claims.

Claim 1: broad two-active composition

Claim 1 requires:

1. About 0.01% to about 1.0% w/v netarsudil dimesylate;
2. About 0.005% w/v latanoprost; and
3. At least one excipient.

This is the broadest claim in the patent. It does not require a particular buffer, tonicity agent, preservative, pH, or manufacturing process. A formulation that satisfies the two active-ingredient limitations and contains any excipient could potentially fall within claim 1.

The claim is composition-based. It does not require a specific therapeutic indication, dosing schedule, container, drop size, or route beyond what may be implied by the pharmaceutical composition context.

Claim 19: excipient-defined composition

Claim 19 requires the same two active ingredients and adds:

• Boric acid;
• Mannitol; and
• Benzalkonium chloride.

Unlike claim 1, claim 19 does not expressly specify the concentrations of those excipients. A formulation can therefore fall within claim 19 without matching the exact 4.7% mannitol, 0.05% boric acid, or 0.02% benzalkonium chloride levels recited in dependent claims.

Claim 21: commercial-formulation claim

Claim 21 is the most commercially specific independent claim. It requires:

• About 0.01% to about 1.0% w/v netarsudil dimesylate;
• About 0.005% w/v latanoprost;
• About 0.05% w/v boric acid;
• About 4.7% w/v D-mannitol;
• About 0.02% w/v benzalkonium chloride; and
• A pH of about 5.0.

Claim 21 closely tracks the commercial Rocklatan formulation. Its infringement analysis will depend on how the accused product’s actual composition is measured, including the meaning of “about” and whether the product contains the claimed ingredients at concentrations within legally relevant tolerances.

How do the dependent claims narrow the patent scope?

The dependent claims create a layered formulation estate.

Claim	Added limitation	Commercial significance
2	Tonicity agent	Captures isotonic ophthalmic formulations using a tonicity-adjusting excipient
3	Mannitol	Narrows the tonicity agent to mannitol
4	D-mannitol	Narrows the stereochemical form of mannitol
5	About 4.7% w/v D-mannitol	Tracks the commercial tonicity level
6	Buffer	Requires a buffer in addition to the excipient structure of claim 2
7	Boric acid and pH about 5.0	Adds buffer identity and pH
8	About 0.05% w/v boric acid	Tracks the commercial buffer concentration
12	Preservative	Requires a preservative
13	Benzalkonium chloride	Specifies the preservative
14	About 0.02% w/v benzalkonium chloride	Tracks the commercial preservative concentration
18	Netarsudil dimesylate at least about 0.020% to less than about 0.05%	Captures the commercial 0.02% strength and nearby concentrations
20	Claim 19 plus the narrow netarsudil range	Combines excipients with commercial-strength netarsudil
22	Claim 21 plus the narrow netarsudil range	Most specific claim to the commercial composition

Claims 18, 20 and 22 are particularly important because they narrow the broad 0.01% to 1.0% range to the commercially relevant interval beginning at about 0.020% and ending below about 0.05%. Rocklatan’s labeled netarsudil concentration is 0.02%, placing the marketed formulation within the apparent target of these claims.[2]

What formulation is most directly covered by the patent?

The formulation most directly covered is an ophthalmic solution containing:

• Netarsudil dimesylate at approximately 0.02% w/v;
• Latanoprost at 0.005% w/v;
• D-mannitol at approximately 4.7% w/v;
• Boric acid at approximately 0.05% w/v;
• Benzalkonium chloride at approximately 0.02% w/v; and
• A pH of approximately 5.0.

That formulation falls within claim 1 if it contains an excipient, claim 18 based on the netarsudil concentration, claim 21 based on the full composition, and claim 22 based on the full composition plus the narrow netarsudil range.

The claims also create multiple infringement paths. A product could avoid claim 21 by changing the pH or one excipient concentration while still potentially falling within claim 1. Conversely, a product that uses the same actives but replaces mannitol, boric acid or benzalkonium chloride may avoid claims 19 through 22 while remaining exposed to claim 1.

When does US Patent 11,197,853 lose exclusivity?

US Patent 11,197,853 issued on December 7, 2021.[1] Its expiration date should be determined from the patent’s effective nonprovisional filing date, terminal disclaimer status, and any patent-term adjustment. The patent’s continuation-family history is material to the final term calculation.

The patent should not be analyzed in isolation from related Rocklatan patents. A product may avoid US 11,197,853 and still face other patents covering the active ingredients, formulation, method of use, or related ophthalmic compositions.

Exclusivity issue	Effect on commercial entry
US 11,197,853 patent term	Blocks or complicates products meeting the composition claims during the enforceable term
FDA drug exclusivity	Separate from patent term and depends on the NDA and approval pathway
Orange Book listing	Determines whether an ANDA applicant must address the listed patent
Paragraph IV certification	May trigger patent litigation and a 30-month stay under Hatch-Waxman
Related formulation patents	Can extend practical protection beyond one patent
Regulatory review period	May support patent-term extension if statutory requirements are met

The exact market-entry date for a generic cannot be determined from the claims alone. Patent expiration, Orange Book listing status, any terminal disclaimer, patent-term adjustment, FDA exclusivity and litigation settlements must be evaluated together.

What is the Orange Book status of US Patent 11,197,853?

The FDA Orange Book identifies patents submitted by NDA holders for approved drug products. Rocklatan is approved under NDA 211548.[2] Orange Book treatment must be assessed at the drug-product level rather than inferred solely from the patent claims.

If US 11,197,853 is listed for Rocklatan, an ANDA applicant seeking approval for a therapeutically equivalent netarsudil-latanoprost product would generally need to submit a patent certification under 21 U.S.C. § 355(j)(2)(A)(vii). A Paragraph IV certification would assert that the patent is invalid, unenforceable or not infringed. Notice to the patent owner and NDA holder could permit a patent-infringement action and trigger the statutory 30-month stay.[3]

The relevant Orange Book questions are:

1. Is US 11,197,853 listed against Rocklatan?
2. Which claims are identified in the listing?
3. Is the listing active, delisted or subject to a dispute?
4. Are related patents listed for the same NDA?
5. Has any ANDA applicant filed a Paragraph IV certification?
6. Has litigation triggered a 30-month stay?

Patent listing and patent validity are separate issues. An Orange Book listing does not establish that the listed claims are valid or infringed.

What Paragraph IV challenges and generic entry risks exist?

A Paragraph IV challenger would likely focus on claim construction, written description, enablement, obviousness, anticipation and noninfringement.

Likely invalidity issues

The principal validity arguments could include:

• Prior-art disclosure of netarsudil and latanoprost combination therapy;
• Prior-art ophthalmic solutions containing latanoprost, mannitol, boric acid and benzalkonium chloride;
• Obviousness of combining known actives in an ophthalmic formulation;
• Obviousness of selecting approximately 0.02% netarsudil and 0.005% latanoprost;
• Lack of unexpected results across the full 0.01% to 1.0% netarsudil range;
• Written-description or enablement challenges to the broad concentration range;
• Indefiniteness disputes concerning “about,” “at least about,” and “less than about.”

The patent holder would likely rely on formulation stability, compatibility, tolerability, preservative performance, pH control, and clinical or pharmaceutical advantages to defend the claims. The narrow claims may be more resilient if the specification provides comparative data showing that the claimed excipient combination or concentration window produces an unexpected result.

Likely noninfringement strategies

A generic applicant could attempt to design around the patent by:

• Using a different netarsudil salt or formulation form;
• Reducing netarsudil below the claimed range;
• Using a netarsudil concentration outside the narrow range;
• Replacing D-mannitol with another tonicity agent;
• Replacing boric acid with a different buffer;
• Omitting benzalkonium chloride or using another preservative;
• Adjusting pH outside the claimed “about 5.0” range;
• Formulating the products as separate co-packaged products rather than one composition.

Claim 1 creates the principal design-around difficulty because it requires only the two active ingredients, the broad netarsudil range and at least one excipient. Changing the supporting excipients may not avoid that claim.

Is biosimilar risk relevant to Rocklatan?

No. Rocklatan contains chemically defined small-molecule active ingredients, not a biologic. A follow-on product would generally proceed through the ANDA pathway as a generic drug, not through the biosimilar pathway under the Biologics Price Competition and Innovation Act.

The relevant competitive risks are:

• ANDA filings;
• Paragraph IV patent challenges;
• Formulation design-arounds;
• Authorized generic or licensed generic entry;
• Separate generic availability for latanoprost;
• Generic competition to netarsudil monotherapy.

Biosimilar concepts such as interchangeability, reference biologics and biosimilar exclusivity do not govern this product.

Which companies compete with Rocklatan?

Rocklatan competes in the glaucoma and ocular-hypertension market with products using prostaglandin analogs, Rho kinase inhibition, or other intraocular-pressure-lowering mechanisms.

Product	Active ingredient or combination	Competitive relationship
Rocklatan	Netarsudil plus latanoprost	Fixed-combination product protected by US 11,197,853 claims
Rhopressa	Netarsudil	Same Rho kinase inhibitor without latanoprost
Xalatan and authorized/generic latanoprost	Latanoprost	Established prostaglandin comparator
Vyzulta	Latanoprostene bunod	Prostaglandin-related nitric-oxide donor
Lumigan	Bimatoprost	Prostaglandin analog competitor
Travatan Z	Travoprost	Prostaglandin analog competitor
Cosopt and generic dorzolamide/timolol	Dorzolamide plus timolol	Non-prostaglandin fixed combination
Combigan and generic brimonidine/timolol	Brimonidine plus timolol	Non-prostaglandin fixed combination

The most direct patent and commercial comparison is between Rocklatan and Rhopressa. Rhopressa may implicate netarsudil patents but does not contain latanoprost and therefore would not satisfy the two-active composition requirement in the claims provided here.

How strong is the patent estate for US 11,197,853?

US 11,197,853 has moderate-to-strong product-specific value because the claims cover the commercial combination and include a broad independent claim. Its strength is reduced by several factors:

1. The claims are composition claims rather than claims to a new chemical entity.
2. The active ingredients were individually known.
3. The broad netarsudil concentration range may attract enablement and obviousness challenges.
4. The word “about” creates potential boundary disputes.
5. A formulation competitor may be able to alter excipients while preserving clinical performance.
6. Related patents may be necessary to create a complete market-exclusion position.

The strongest practical claims are likely claims 21 and 22 because they correspond closely to the marketed formulation. The broadest commercial blocking claim is claim 1 because it does not require the specific excipient combination.

What litigation and licensing events affect the patent?

The patent record identifies the issued claims and prosecution history but does not, by itself, establish the complete litigation status of the patent. Litigation analysis should distinguish among:

• An ANDA notice letter;
• A filed Hatch-Waxman infringement action;
• A declaratory judgment action;
• A post-grant review or inter partes review;
• A settlement agreement;
• A consent judgment;
• A final invalidity or noninfringement judgment.

Aerie Pharmaceuticals developed Rocklatan and Rhopressa. Alcon acquired Aerie in 2022, transferring the commercial business and associated intellectual-property assets to Alcon.[4] That transaction is an acquisition, not a disclosed third-party license for the patent.

No settlement terms should be inferred from the patent grant or from FDA approval. A generic settlement, if any, would require review of the relevant court docket, FDA correspondence and any public settlement filing.

What manufacturing and geographic barriers exist?

The claims do not require a particular manufacturing process, container, dropper, sterilization method or fill-finish facility. They therefore create less process-specific protection than a patent directed to aseptic manufacturing, particle-size control, polymorphism, packaging or preservative delivery.

The principal manufacturing barriers are formulation-related:

• Maintaining netarsudil and latanoprost stability in one solution;
• Controlling pH near 5.0;
• Preserving the product with benzalkonium chloride;
• Achieving ophthalmically acceptable tonicity;
• Preventing precipitation, degradation or adsorption;
• Producing a sterile and consistent multidose product.

US 11,197,853 has territorial effect only in the United States. Foreign protection requires corresponding national or regional patents. A US design-around does not automatically avoid foreign patent rights, and a foreign patent family member does not create enforceable US rights unless granted in the United States.

Key Takeaways

• US 11,197,853 covers pharmaceutical compositions containing netarsudil dimesylate and 0.005% w/v latanoprost.
• Claim 1 is the broadest claim and requires only the two active ingredients, the stated netarsudil range and at least one excipient.
• Claims 19 and 21 add boric acid, mannitol and benzalkonium chloride.
• Claim 21 closely tracks the commercial Rocklatan formulation.
• Claims 18, 20 and 22 target netarsudil concentrations of at least about 0.020% to less than about 0.05%.
• The patent does not cover netarsudil monotherapy, latanoprost monotherapy or biosimilar products.
• Generic entry would likely proceed through an ANDA, with Paragraph IV certification if the patent is listed in the Orange Book.
• The principal legal vulnerabilities are obviousness, written description, enablement, indefiniteness and formulation design-around arguments.
• Alcon is the current commercial owner following its acquisition of Aerie Pharmaceuticals.
• The patent must be evaluated with related Rocklatan patents, FDA exclusivity, Orange Book listings and any ANDA litigation or settlement.

FAQs About US Patent 11,197,853

Does US 11,197,853 cover generic latanoprost by itself?

No. The claims require both latanoprost and netarsudil dimesylate in the same pharmaceutical composition.

Does a product with 0.02% netarsudil and a different preservative avoid the patent?

It may avoid claims requiring benzalkonium chloride, including claims 13, 14, 16, 17, 19, 20, 21 and 22. It may still face claim 1, which requires only at least one excipient.

Is Rocklatan a biologic subject to biosimilar competition?

No. Rocklatan is a small-molecule drug combination. The relevant pathway is an ANDA for a generic product.

Can a generic applicant avoid the patent by selling separate netarsudil and latanoprost bottles?

Separate products may avoid a composition claim requiring both active ingredients in one pharmaceutical composition. The outcome would depend on the product design, labeling, packaging and any separate method-of-use or induced-infringement theories.

What is the most important claim for commercial enforcement?

Claim 1 is the most important broad claim because it covers a wide range of excipient systems. Claim 21 is the most important formulation-specific claim because it tracks the commercial Rocklatan composition.

References

1. United States Patent and Trademark Office. (2021). U.S. Patent No. 11,197,853, pharmaceutical compositions comprising netarsudil and latanoprost.
2. U.S. Food and Drug Administration. (2019). Rocklatan (netarsudil and latanoprost ophthalmic solution) prescribing information.
3. U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book.
4. Alcon Inc. (2022). Alcon completes acquisition of Aerie Pharmaceuticals.

Drugs Protected by US Patent 11,197,853

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			Y

International Family Members for US Patent 11,197,853

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	3461484		301101	Netherlands
European Patent Office	3461484		2021C/515	Belgium
European Patent Office	3461484		132021000000068	Italy
European Patent Office	3461484		122021000036	Germany
European Patent Office	3461484		C202130024	Spain
European Patent Office	3461484		21C1024	France