Details for Patent: 10,441,630

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Which drugs does patent 10,441,630 protect, and when does it expire?

Patent 10,441,630 protects CEQUA and is included in one NDA.

This patent has eighteen patent family members in fifteen countries.

Summary for Patent: 10,441,630

Title:	Topical formulations and uses thereof
Abstract:	Provided herein include formulations for topical administration, such as ophthalmic formulations, and methods of using such formulations. In some aspects and embodiments the formulations may include a polyoxyl lipid or fatty acid, and or a polyalkoxylated alcohol and may include nanomicelles. Also include methods of treating or preventing diseases or conditions, such as ocular diseases or conditions.
Inventor(s):	Ashim K. Mitra, Sidney L. Weiss, Eugene J. McNally
Assignee:	Sun Pharmaceutical Industries Ltd
Application Number:	US15/153,640
Patent Claim Types: see list of patent claims	Formulation;

United States Patent 10,441,630: Claim Scope, Cequa Relevance and Ophthalmic Nanomicelle Patent Landscape

U.S. Patent No. 10,441,630 protects an aqueous, clear ophthalmic nanomicellar formulation using hydrogenated castor oil or polyoxyl 35 castor oil together with a low concentration of a polyalkoxylated alcohol. The issued claims are formulation claims, not claims limited to a particular active ingredient. The broadest independent claim covers any active agent meeting the claimed excipient, concentration, aqueous, clarity and nanomicelle requirements.

The patent is commercially relevant to cyclosporine ophthalmic products, particularly the nanomicellar formulation marketed as Cequa. Its practical strength depends on whether a competing product uses the claimed surfactant system and whether the product can avoid the claimed concentration ranges or nanomicellar structure.

What does U.S. Patent 10,441,630 protect?

The patent protects a pharmaceutical formulation with six required characteristics:

1. An aqueous ophthalmic formulation.
2. A clear appearance.
3. Nanomicelles.
4. An active agent.
5. A polymer at 0.5% to 4.5% by weight.
6. A polyalkoxylated alcohol at 0.02% to 0.08% by weight.

The polymer must be one or more of the following:

• HCO-40;
• HCO-60;
• HCO-80;
• HCO-100;
• Polyoxyl 35 castor oil; or
• A combination of those materials.

The claims supplied do not restrict the active agent to cyclosporine. A product containing another ophthalmic active agent could fall within claim 1 if it uses the same structural and compositional elements.

Claim	Scope	Key limitation
1	Broad independent formulation claim	Polymer at 0.5%-4.5%; polyalkoxylated alcohol at 0.02%-0.08%; aqueous, clear, nanomicellar ophthalmic formulation
2	Dependent formulation claim	Polymer limited to HCO-40, HCO-60, HCO-80 or HCO-100
3	Dependent formulation claim	Polyalkoxylated alcohol is Octoxynol-40
4	Dependent formulation claim	Polymer is HCO-40
5	Dependent formulation claim	Polymer is HCO-60
6	Dependent formulation claim	Polymer concentration is 1%-4%
7	Dependent formulation claim	Octoxynol-40 is 0.05% by weight

Claim 1 is the principal commercial claim. Claims 2 through 7 narrow the formulation but may be easier to prove against a marketed product because they identify specific excipients and concentrations.

How broad is claim 1?

Claim 1 has substantial breadth because it is not limited to:

• Cyclosporine;
• Dry-eye disease;
• A particular dosage strength;
• A specified pH;
• A particular osmolality;
• A defined micelle size;
• A specific manufacturing process;
• A particular container or delivery device; or
• A named commercial product.

The claim is open-ended as to the active agent. The phrase “comprising” generally permits additional ingredients, provided the accused formulation still contains every required claim element.

A product could therefore infringe claim 1 even if it contains preservatives, buffers, tonicity agents, viscosity modifiers, chelators or other excipients not listed in the claim.

The main limiting issue is the combined requirement that the formulation be both “clear” and “nanomicellar.” A conventional emulsion, suspension or visibly turbid dispersion should not satisfy those limitations merely because it contains castor-oil-derived surfactants.

What formulations are protected by claims 2 through 7?

Claims 2 through 7 create a layered claim structure.

HCO-40 and HCO-60 formulations

Claims 4 and 5 are directed specifically to HCO-40 and HCO-60. A formulation using HCO-40 at 1% to 4%, together with Octoxynol-40 at 0.05%, would fall within claim 7 if it also satisfies the aqueous, clear, nanomicellar and ophthalmic limitations.

The concentration ranges are meaningful:

• Claim 1: polymer at 0.5%-4.5%.
• Claim 6: polymer at 1%-4%.
• Claim 7: Octoxynol-40 at exactly 0.05% by weight.

A product with 0.5% HCO-40 could potentially fall within claim 1 but not claim 6. A product with 4.5% HCO-40 could fall within claim 1 but not claim 6. A formulation using 0.09% Octoxynol-40 would likely fall outside claim 3 and claim 7, although other polyalkoxylated alcohol concentrations could still implicate claim 1 if within 0.02%-0.08%.

Polyoxyl 35 castor oil formulations

Claim 1 expressly includes polyoxyl 35 castor oil. Claim 2 does not. Accordingly, a formulation using only polyoxyl 35 castor oil may fall within claim 1 but would not satisfy claim 2, which is limited to the HCO-40, HCO-60, HCO-80 and HCO-100 group.

This distinction creates a potential design-around path if a competitor uses polyoxyl 35 castor oil in a formulation that avoids other claimed limitations. It does not eliminate claim 1 risk.

Octoxynol-40 formulations

Claim 3 identifies Octoxynol-40 as the polyalkoxylated alcohol. Claim 7 narrows the amount to 0.05% by weight. Octoxynol-40 is therefore a high-risk excipient where the product also uses one of the claimed castor-oil-derived polymers at a concentration within the stated range.

The claims do not require Octoxynol-40 in every embodiment. A competitor using another polyalkoxylated alcohol could still face claim 1 risk if that material falls within the claim's functional and chemical scope.

Does the patent cover cyclosporine ophthalmic products?

The claims supplied are active-agent neutral, but the patent is relevant to cyclosporine ophthalmic products because Cequa uses an aqueous nanomicellar delivery approach for cyclosporine ophthalmic administration. The FDA approved Cequa, cyclosporine ophthalmic solution 0.09%, for increasing tear production in patients with keratoconjunctivitis sicca associated with ocular inflammation [2].

The patent's commercial significance is therefore broader than the active ingredient. It protects the delivery platform used to solubilize and administer a poorly water-soluble ophthalmic active agent.

A cyclosporine product would face a strong literal infringement case if its formulation has:

• Cyclosporine as the active agent;
• A clear aqueous ophthalmic solution;
• Nanomicelles;
• HCO-40, HCO-60, HCO-80, HCO-100 or polyoxyl 35 castor oil at 0.5%-4.5%; and
• Octoxynol-40 or another covered polyalkoxylated alcohol at 0.02%-0.08%.

The patent does not, based on the supplied claims alone, require the cyclosporine concentration to be 0.09%. A competing cyclosporine strength could remain within scope.

What is the Orange Book status of U.S. Patent 10,441,630?

U.S. Patent 10,441,630 is associated with the patent estate for Cequa, a prescription cyclosporine ophthalmic product. Orange Book relevance must be assessed at the product level because FDA patent listings identify patents submitted for a specific approved drug and approved use, not every patent that might theoretically cover a formulation [3].

The listed patent's commercial implications are:

• An abbreviated new drug application for a generic version of Cequa may need to address the patent through a Paragraph IV certification.
• A Paragraph IV notice could trigger patent litigation under the Hatch-Waxman framework.
• A filing of an infringement action within the statutory period can create a 30-month stay of approval, subject to statutory exceptions and court action.
• The patent's formulation claims may be more difficult to avoid than a narrow method-of-use claim because a generic must disclose its composition in the ANDA.

The supplied information does not establish the patent's current Orange Book listing status, any delisting, or the existence of an approved ANDA with a final Paragraph IV outcome.

When does U.S. Patent 10,441,630 lose exclusivity?

The patent issued on October 15, 2019. Its enforceable term is generally calculated from the earliest effective nonprovisional U.S. filing date in the priority chain, subject to patent-term adjustment, patent-term extension, terminal disclaimers and any relevant prosecution history [1].

The issue date alone does not establish the expiration date. A reliable expiration analysis requires the complete continuity data and USPTO term calculation. Patent-term extension under 35 U.S.C. § 156 is generally associated with regulatory review of the approved product, while patent-term adjustment under 35 U.S.C. § 154 may extend the ordinary 20-year term for USPTO delay.

The practical exclusivity date for Cequa also may differ from the patent expiration date because:

• FDA orphan-drug exclusivity is not the primary exclusivity mechanism for Cequa;
• New chemical entity exclusivity generally does not apply to cyclosporine, an established active ingredient;
• Paragraph IV litigation can delay approval before expiration; and
• Other patents in the product estate may expire later than U.S. Patent 10,441,630.

How strong is the patent estate?

The supplied claims provide moderate-to-strong formulation coverage for products using the specified excipient architecture. Strength is highest where the commercial formulation uses the claimed excipients at readily measurable concentrations.

Risk factor	Assessment
Active-agent breadth	Strong; claim 1 is not limited to cyclosporine
Excipient specificity	Moderate; the polymer list is defined but commercially relevant
Concentration limits	Moderate; concentrations create measurable design-around opportunities
Nanomicelle limitation	Potentially important; requires technical characterization
Clear-solution limitation	Strong factual limitation for conventional emulsions or suspensions
Manufacturing coverage	Limited on supplied claims; no process claim is provided
Method-of-use coverage	None apparent in supplied claims
Product-by-process coverage	None apparent
Biosimilar relevance	Low; cyclosporine is a small molecule, not a biologic
Generic relevance	High; an ANDA product must disclose formulation composition

The strongest enforcement position would involve a product label or regulatory filing that identifies HCO-40 or a related hydrogenated castor oil polymer and Octoxynol-40 at concentrations within the claimed ranges.

The main vulnerabilities are claim construction and proof. The patent owner would likely need evidence that the accused product forms nanomicelles and is clear under the relevant testing conditions. A competitor could contest whether its formulation contains nanomicelles rather than another type of colloidal structure.

What generic entry risks exist for Cequa?

Generic entry risk is driven by three technical pathways.

Literal infringement

A generic product may infringe if its disclosed formulation falls within the numerical ranges and uses a claimed excipient combination. ANDA composition disclosures can provide a direct basis for claim comparison.

Doctrine of equivalents

A formulation outside a claimed range may still present risk under the doctrine of equivalents, although numerical range claims face limits where the prosecution history shows that the range was added to distinguish prior art.

Design-around formulation

A generic developer could attempt to avoid the patent by:

• Using a different solubilizer;
• Replacing HCO-40, HCO-60, HCO-80, HCO-100 and polyoxyl 35 castor oil;
• Moving the polymer concentration below 0.5% or above 4.5%;
• Using a polyalkoxylated alcohol outside the 0.02%-0.08% range;
• Avoiding Octoxynol-40;
• Developing a non-nanomicellar solution;
• Using an emulsion or suspension rather than a clear nanomicellar formulation; or
• Using a different delivery technology.

Each route creates formulation, stability, tolerability and bioavailability constraints. Avoiding the patent may require a formulation that no longer matches the reference product's performance or FDA-approved product characteristics.

Are biosimilar challenges relevant?

Biosimilar risk is low for this patent because cyclosporine is a small-molecule active ingredient. The relevant competitive pathway is an ANDA under section 505(j) of the Federal Food, Drug, and Cosmetic Act, not a biosimilar application under section 351(k) of the Public Health Service Act [2,4].

The patent can still affect generic competition materially because the claims cover the formulation platform rather than only the active ingredient. A generic applicant may need to choose between:

• A Paragraph IV challenge;
• A noninfringing formulation;
• A later-filed application after patent expiry; or
• A settlement arrangement that controls launch timing.

What litigation or settlement issues affect the patent?

The principal litigation risk is a Hatch-Waxman action following a Paragraph IV certification against a generic cyclosporine ophthalmic solution. The key issues would likely include:

1. Whether the generic product is “clear.”
2. Whether the product contains nanomicelles.
3. Whether the excipient qualifies as one of the claimed polymers.
4. Whether the concentrations are calculated on the same weight basis.
5. Whether the accused product contains a polyalkoxylated alcohol.
6. Whether prosecution history limits the scope of the claim.
7. Whether the patent is valid over prior nanomicellar ophthalmic formulations.

The supplied claims do not identify a litigation outcome, settlement agreement, injunction or final validity determination. No litigation conclusion should be drawn solely from the patent claims.

How does this patent compare with active-ingredient and method-of-use patents?

U.S. Patent 10,441,630 is structurally different from a conventional active-ingredient patent.

Patent type	Typical protection	Relevance to 10,441,630
Active-ingredient patent	Chemical compound or salt	Not apparent from supplied claims
Formulation patent	Excipients, concentrations and dosage form	Primary category
Method-of-use patent	Treating a disease or patient population	Not present in supplied claims
Manufacturing patent	Preparation or sterilization process	Not present in supplied claims
Device patent	Dropper, container or delivery system	Not present in supplied claims

The patent can block a competing formulation even when the active ingredient is off-patent. That is the central commercial value of the claim set.

What geographic coverage does the patent provide?

U.S. Patent 10,441,630 provides rights only in the United States. Corresponding international or foreign applications may create related rights in Europe, Canada, Japan, China and other markets, but those rights must be assessed separately by national patent number, claim set, prosecution history and local expiry rules.

A U.S. formulation patent does not prevent manufacture or sale outside the United States unless a corresponding foreign patent is in force. Export activity can create additional issues under U.S. law, including infringement based on making, using, selling or importing a patented invention in the United States.

Key Takeaways

• U.S. Patent 10,441,630 is a formulation patent covering clear aqueous ophthalmic nanomicelles.
• Claim 1 is broad because it is not limited to cyclosporine or any particular active agent.
• The principal excipient requirements are 0.5%-4.5% of specified castor-oil-derived polymers and 0.02%-0.08% of a polyalkoxylated alcohol.
• HCO-40, HCO-60 and Octoxynol-40 are expressly captured by narrower claims.
• Claim 7 targets a commercially specific combination: HCO-40 or HCO-60 with 0.05% Octoxynol-40.
• The patent is relevant to Cequa and potential generic cyclosporine ophthalmic products.
• Generic developers face the highest risk where their ANDA formulation reproduces the excipient system and concentration ranges.
• Biosimilar litigation is not the relevant pathway because cyclosporine is a small molecule.
• The supplied claims do not cover a treatment method, manufacturing process or delivery device.
• Patent expiration and current Orange Book status require review of the complete USPTO continuity record and FDA listing data.

Frequently Asked Questions

Does U.S. Patent 10,441,630 claim cyclosporine specifically?

No. The supplied claims recite an “active agent” without limiting that agent to cyclosporine.

Can a formulation using polyoxyl 35 castor oil avoid the patent?

Not necessarily. Polyoxyl 35 castor oil is expressly included in claim 1 when the other claim limitations are met.

Is Octoxynol-40 required in every claim?

No. Claim 1 covers a polyalkoxylated alcohol generally. Octoxynol-40 is required only in claims 3 and 7.

Would a cloudy ophthalmic emulsion infringe these claims?

A conventional cloudy emulsion would have a potential defense to the “clear nanomicellar” limitations, although the final result would depend on claim construction and technical evidence.

Does this patent prevent all generic cyclosporine eye drops?

No. It targets a defined nanomicellar formulation architecture. A generic using a materially different formulation may avoid literal infringement, subject to other patents and the doctrine of equivalents.

References

1. United States Patent and Trademark Office. (2019). U.S. Patent No. 10,441,630.
2. U.S. Food and Drug Administration. (2018). Cequa (cyclosporine ophthalmic solution) 0.09% prescribing information.
3. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations, Orange Book.
4. U.S. Food and Drug Administration. (n.d.). Abbreviated new drug application process and patent certifications.

Drugs Protected by US Patent 10,441,630

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Sun Pharm	CEQUA	cyclosporine	SOLUTION;OPHTHALMIC	210913-001	Aug 14, 2018		RX	Yes	Yes			Y

International Family Members for US Patent 10,441,630

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2013305539
Canada	2914472
Canada	3050298
Denmark	2887923
European Patent Office	2887923
European Patent Office	4218729
Spain	2948387