US Patent 10,940,142: Roflumilast Formulation Claims, Exclusivity and Patent Landscape

US Patent 10,940,142 protects roflumilast compositions containing hexylene glycol, with narrower claims covering specific emulsifiers, concentration ranges and topical delivery systems. Its commercial significance is strongest for roflumilast cream products, including Arcutis Biotherapeutics' ZORYVE. The patent does not protect roflumilast as an active pharmaceutical ingredient generally. It protects formulation combinations and, in several claims, the use of hexylene glycol to control crystal growth or particle-size changes.

Public patent records identify the patent as a continuation-family patent with priority dating to September 11, 2008. The listed expiration date is September 11, 2028, subject to any applicable patent-term adjustment or regulatory exclusivity. The patent is listed in FDA's Orange Book for ZORYVE cream products. [1-4]

What does US Patent 10,940,142 protect?

The patent has three principal claim groups:

A specific roflumilast emulsion system containing cetearyl alcohol, dicetyl phosphate and ceteth-10 phosphate.
A broader roflumilast and hexylene glycol composition using a pharmaceutically acceptable solvent.
A broader roflumilast, hexylene glycol and emulsifier composition.

The claims are composition claims. They do not require a particular manufacturing process, clinical indication or dosage regimen unless those limitations appear in the dependent claims.

Claim structure and scope

Claim	Subject matter	Practical scope
1	Roflumilast, hexylene glycol, cetearyl alcohol, dicetyl phosphate and ceteth-10 phosphate	Core specific emulsion combination
2	Claim 1, with hexylene glycol sufficient to inhibit crystal growth or particle-size changes	Adds functional performance limitation
3	Claim 1, with hexylene glycol at 0.1%-20% w/w	Broad concentration limitation
4	Claim 1, with roflumilast at 0.005%-2% w/w	Broad roflumilast range
5	Claim 1, with roflumilast at 0.005%-0.5% w/w	Narrower range nested within claim 4
6	Claim 1, with carriers for topical, parenteral or pulmonary administration	Extends formulation formats
7	Claim 6, with carriers suitable for topical administration	Commercially important topical limitation
8	Roflumilast, hexylene glycol and a pharmaceutically acceptable solvent	Broad composition claim
9	Claim 8, where the solvent is water	Water-based compositions
10	Claim 8, where roflumilast is near saturation	Solubility-focused limitation
11	Claim 8, with a second active agent from a long enumerated list	Combination therapy compositions
12	Roflumilast, hexylene glycol and an emulsifier	Broad emulsion claim
13	Claim 12, with emulsifier at 10% w/w	Quantified emulsifier limitation
14	Claim 13, with cetearyl alcohol, dicetyl phosphate and ceteth-10 phosphate as the emulsifier blend	Narrow commercial formulation claim

Claims 8 and 12 are materially broader than claim 1 because they do not expressly require all three identified emulsifier components. A competing product can therefore avoid claim 1 while remaining exposed to claims 8 or 12.

How broad are the independent claims?

Claims 1, 8 and 12 are the principal enforcement claims.

Claim 1: defined emulsifier system

Claim 1 requires the presence of five components:

Roflumilast
Hexylene glycol
Cetearyl alcohol
Dicetyl phosphate
Ceteth-10 phosphate

The claim does not specify concentrations. A product containing all five ingredients could fall within claim 1 even if it uses concentrations outside the ranges recited in claims 3-5, provided the composition otherwise satisfies the claim.

The absence of concentration limits makes claim 1 potentially broad in formulation space. The likely limitation is whether the accused product contains each ingredient as a component of the pharmaceutical composition, rather than as an incidental impurity or unrelated manufacturing residue.

Claim 8: roflumilast, hexylene glycol and solvent

Claim 8 is broader in ingredient selection. It does not require cetearyl alcohol, dicetyl phosphate or ceteth-10 phosphate. A formulation containing roflumilast, hexylene glycol and water could implicate claim 9. A formulation using another pharmaceutically acceptable solvent could implicate claim 8.

The claim can reach non-emulsion formulations, depending on how the product is formulated and how "pharmaceutically acceptable solvent" is construed. The term may encompass water and certain organic solvents commonly used in topical products.

Claim 12: roflumilast, hexylene glycol and emulsifier

Claim 12 occupies an intermediate position. It requires an emulsifier but does not require the particular three-component emulsifier blend in claim 14.

This creates a design-around distinction:

Removing hexylene glycol may avoid claims 8 and 12, but could affect roflumilast solubility and physical stability.
Replacing the emulsifier may avoid claim 12 only if the replacement does not qualify as an emulsifier under the claim.
Keeping hexylene glycol while using a different solvent and emulsifier may still leave exposure under claim 8.

What formulation is most closely covered by the patent?

The formulation most closely aligned with the patent is a topical roflumilast cream containing approximately 0.3% roflumilast, hexylene glycol and an emulsifier system based on cetearyl alcohol, dicetyl phosphate and ceteth-10 phosphate.

The 0.3% roflumilast concentration falls within:

Claim 4's 0.005%-2% range
Claim 5's 0.005%-0.5% range

A 0.3% topical cream containing the claimed excipient system would therefore present a direct claim-mapping issue under claims 1, 3, 4, 5, 7 and 14, assuming the product contains the required ingredients in the claimed composition.

Why hexylene glycol matters

The specification and dependent claims associate hexylene glycol with control of roflumilast crystal growth and particle-size changes. This is important because roflumilast is a poorly water-soluble compound, and topical formulation performance depends on maintaining a stable active-particle distribution.

Claim 2 is narrower than claim 1 because it requires a functional result: hexylene glycol must be present in an amount sufficient to inhibit crystal growth or particle-size changes. A challenger could dispute whether the claimed amount produces that result in the accused product. The claim may also raise proof questions concerning test method, storage conditions, baseline particle size and the meaning of "inhibit."

What are the key claim-construction and validity issues?

The patent estate has meaningful commercial coverage, but several claim features create potential validity or enforcement disputes.

"Pharmaceutical composition"

The claims require a pharmaceutical composition rather than a mere mixture of chemicals. An accused product would likely be analyzed based on its final dosage form, excipient function and intended therapeutic use.

"Pharmaceutically acceptable solvent"

Claim 8 does not limit the solvent to water. Claim 9 narrows the scope to water, but claim 8 remains available for other pharmaceutically acceptable solvents.

Potential disputes could concern whether a particular glycol, alcohol or co-solvent is functioning as a solvent, cosolvent, humectant or another excipient. Ingredient identity alone may not resolve the issue.

"Near saturation"

Claim 10 requires roflumilast to be "near saturation." That phrase is a potential indefiniteness and infringement issue because the claim does not state a numerical saturation threshold. The relevant analysis would likely consider the specification, formulation temperature, solvent system, roflumilast solubility and whether the product contains undissolved or crystallized drug.

Functional crystal-growth limitation

Claim 2 requires an amount of hexylene glycol sufficient to inhibit crystal growth or changes in particle size. That limitation can strengthen the claim against formulations designed around stability performance, but it also creates an evidentiary burden. The patent owner would need to establish that the accused composition satisfies the functional requirement.

Combination-agent claim

Claim 11 covers a long list of additional active agents, including corticosteroids, vitamin D analogues, biologics, bronchodilators and antibiotics. The claim is potentially useful for combination products, but its commercial relevance depends on whether a marketed product actually includes roflumilast, hexylene glycol, a pharmaceutically acceptable solvent and one listed additional agent.

The claim does not automatically cover every combination involving roflumilast. The base requirements of claim 8 remain applicable.

When does US Patent 10,940,142 lose exclusivity?

The patent's listed expiration date is September 11, 2028. The underlying priority date is September 11, 2008. The patent is therefore expected to lose ordinary patent protection in 2028, assuming no enforceable patent-term adjustment changes the date. [1,2]

Milestone	Date
Earliest priority date	September 11, 2008
US patent issuance	March 9, 2021
Listed patent expiration	September 11, 2028
Approximate remaining term from 2024	Four years
Regulatory product associated with the estate	ZORYVE topical products

Patent expiration does not necessarily create immediate generic entry. A generic applicant must also address other listed patents, FDA exclusivity, product-specific requirements and potential litigation.

What is the Orange Book status of US Patent 10,940,142?

US Patent 10,940,142 is listed in FDA's Orange Book for ZORYVE topical products. The listing connects the patent to Arcutis' roflumilast cream product and identifies the patent as relevant to the approved drug product. [3,4]

Orange Book listing is commercially important because an abbreviated new drug application applicant may need to make a Paragraph IV certification if it seeks approval before patent expiration. The listing does not itself establish that every claim is valid or infringed. It creates a regulatory patent-certification pathway.

FDA regulatory milestones for ZORYVE

Product	FDA milestone	Commercial relevance
ZORYVE cream 0.3%	Approved July 2022 for plaque psoriasis	First US topical roflumilast product
ZORYVE foam 0.3%	Approved 2023 for plaque psoriasis and seborrheic dermatitis	Separate dosage form and patent exposure
ZORYVE cream 0.15%	Approved 2023 for atopic dermatitis	Lower-strength cream formulation
ZORYVE cream 0.3%	Label expanded for additional dermatologic use	Increased use of the cream formulation

The patent's claims are not limited to psoriasis. Claims 1-14 are composition claims and can apply regardless of whether the composition is marketed for psoriasis, atopic dermatitis or another dermatologic condition.

Which companies are challenging the patent with Paragraph IV filings?

Publicly available information through June 2024 did not establish a marketed generic roflumilast cream approved after a Paragraph IV challenge to US Patent 10,940,142. No confirmed court judgment invalidating or disclaiming the patent was identified in the principal public records reviewed for this analysis.

The commercial risk remains concentrated near the 2028 expiration date. A generic applicant could file an ANDA with a Paragraph IV certification before expiration, triggering a patent-holder suit under the Hatch-Waxman framework. A timely suit can impose a 30-month stay of FDA approval, subject to statutory exceptions. [5]

Likely generic launch scenarios

Scenario	Expected outcome
No Paragraph IV filing	Approval generally waits for patent expiry or resolution of other listed patents
Paragraph IV filing with litigation	FDA approval may be stayed for up to 30 months
Successful invalidity or noninfringement case	Earlier approval becomes possible
Settlement with licensed entry	Entry date depends on negotiated terms
Product design-around	Generic may avoid one or more claims but must still satisfy FDA equivalence requirements

A generic cream that omits hexylene glycol may avoid the principal claims in this patent, but it would need to demonstrate equivalent pharmaceutical performance. For a topical product, formulation differences can create regulatory complexity involving qualitative and quantitative sameness, inactive-ingredient justification and comparative product performance.

What other patents protect topical roflumilast?

The relevant patent landscape has several layers.

Active-ingredient patents

Roflumilast's original systemic active-ingredient protection is largely expired. The principal commercial barriers for topical products are formulation, dosage-form, method-of-use and regulatory patents rather than basic composition-of-matter protection for roflumilast.

Formulation patents

US 10,940,142 is directed to roflumilast formulations containing hexylene glycol and selected solvents or emulsifiers. Other patent-family members and related applications address topical dosage forms, including creams and foams.

The key formulation distinction is:

Formulation issue	Relevance
Hexylene glycol	Central to claims 1, 8 and 12
Specific emulsifier blend	Narrower claims 1 and 14
Water or other solvent	Claims 8 and 9
Roflumilast concentration	Claims 3-5
Topical carrier	Claim 7
Foam technology	Generally evaluated against separate foam-focused patents
Particle stability	Central technical rationale for claim 2

Method-of-use patents

Method-of-use patents may protect treatment of psoriasis, atopic dermatitis, seborrheic dermatitis or other inflammatory skin conditions with roflumilast. They create separate exposure from this patent because US 10,940,142 does not require a particular disease-treatment method.

A generic applicant can challenge formulation patents, method-of-use patents or both. Skinny-label strategies may reduce exposure to patented indications, but they do not necessarily avoid composition claims.

Biosimilar risk

Biosimilar risk is not material for roflumilast. Roflumilast is a small-molecule drug, so competing products would ordinarily proceed through the ANDA pathway rather than the biologics-license application and biosimilar pathways under the Biologics Price Competition and Innovation Act.

How strong is the patent estate for ZORYVE?

The estate is strongest where a competing product reproduces the commercial cream architecture:

0.3% roflumilast
Hexylene glycol
A topical aqueous or emulsion vehicle
Cetearyl alcohol
Dicetyl phosphate
Ceteth-10 phosphate

The estate is weaker against formulations that remove hexylene glycol or use a genuinely different physical-stability strategy. The broader claims 8 and 12 reduce the value of simple excipient substitution, because they do not require the specific emulsifier blend in claim 1.

Strength assessment

Factor	Assessment
Coverage of commercial cream	Strong
Coverage of roflumilast generally	Weak; patent is formulation-specific
Design-around difficulty	Moderate
Dependence on excipient identity	High
Dependence on performance testing	High for claim 2
Small-molecule generic vulnerability	Meaningful near expiry
Biosimilar vulnerability	Not applicable
Geographic scope	United States only for this patent

The principal technical barrier is not roflumilast synthesis. It is achieving a stable, manufacturable topical dosage form with acceptable drug distribution, solubility, skin delivery and shelf life without reproducing the claimed excipient architecture.

Are there licensing deals affecting this patent?

Arcutis obtained rights to topical roflumilast from AstraZeneca under a licensing arrangement covering development and commercialization of topical roflumilast products. AstraZeneca's rights originated from the prior development chain involving Nycomed and Takeda. [6,7]

The commercial license is separate from patent ownership. A licensee may commercialize a product under patent rights even when the patent family has changed ownership or includes multiple assignees across jurisdictions. The operative business question is whether the licensed rights cover the relevant US patent, product, indication and territory.

What litigation and settlement issues affect generic entry?

The core litigation questions for an ANDA challenger would be:

Whether the proposed product contains hexylene glycol.
Whether the proposed emulsifier qualifies as the claimed emulsifier.
Whether the product contains cetearyl alcohol, dicetyl phosphate and ceteth-10 phosphate.
Whether roflumilast is present within the claimed concentration ranges.
Whether the product is a topical carrier.
Whether the composition satisfies "near saturation" or crystal-growth limitations.
Whether a formulation that omits one ingredient remains covered under the doctrine of equivalents.

No confirmed public settlement involving a generic launch date for US Patent 10,940,142 was identified through June 2024. Any settlement could materially change the effective entry date even if the formal patent expiration remains September 2028.

What geographic protection does the patent provide?

US 10,940,142 provides protection in the United States only. Foreign protection must be assessed through corresponding national patents and applications in the relevant jurisdictions.

A commercial launch outside the United States is not directly blocked by this US patent, but corresponding family members may affect Europe, Canada, Japan, Australia and other markets. Foreign patent terms, prosecution outcomes, claim scope and opposition histories can differ substantially from the US record.

What revenue exposure is linked to this patent?

ZORYVE is the principal commercial product associated with the patent estate. Arcutis reported rapidly growing ZORYVE revenue following launch, making the 2028 patent expiry commercially significant. The exact revenue-at-risk calculation requires separating cream revenue from foam revenue and identifying which later patents protect each dosage form. [7]

The patent is more directly relevant to cream revenue than to foam revenue. A competitor could enter the topical roflumilast market through a non-infringing cream, foam or other dosage form before the expiration of all relevant patents, but formulation and regulatory requirements would remain substantial.

Key Takeaways

US Patent 10,940,142 is a formulation patent, not a basic roflumilast molecule patent.
Claims 1, 8 and 12 create three layers of protection around hexylene glycol-containing roflumilast compositions.
The commercial cream formulation is closely aligned with the patent's claimed roflumilast, hexylene glycol and emulsifier system.
Claims 3-5 cover roflumilast concentrations that include the 0.3% and 0.15% ZORYVE cream strengths.
The listed patent expiration date is September 11, 2028.
The patent is listed in the Orange Book for ZORYVE-related products.
Paragraph IV litigation could delay or accelerate generic entry, but no confirmed public generic settlement or final invalidity judgment was identified through June 2024.
Biosimilar competition is not relevant because roflumilast is a small molecule.
The principal design-around strategy is to remove hexylene glycol or adopt a different stability and emulsifier system.
Separate patents may protect ZORYVE foam products, treatment methods and later indications.

FAQs About US Patent 10,940,142

Does US Patent 10,940,142 cover roflumilast cream at 0.3%?

It can. A 0.3% roflumilast cream containing hexylene glycol and the claimed emulsifier ingredients falls within the concentration ranges in claims 4 and 5 and may satisfy claims 1, 3, 7 and 14.

Can a generic avoid this patent by changing the emulsifier?

Changing the emulsifier may avoid claims 1 and 14, but it may not avoid claim 12 if the replacement remains an emulsifier. Claim 8 can also remain relevant if the generic contains roflumilast, hexylene glycol and a pharmaceutically acceptable solvent.

Does the patent cover roflumilast foam?

The claims are broad enough to recite topical, parenteral or pulmonary carriers, but infringement depends on the foam's actual ingredients and formulation. Separate foam-specific patents may provide more direct coverage.

What is the likely first generic entry date for topical roflumilast?

Absent successful Paragraph IV litigation, settlement or a non-infringing product approved through another pathway, the principal patent barrier identified here runs to September 11, 2028. Other Orange Book patents and regulatory exclusivities could change the effective entry date.

Is roflumilast subject to biosimilar competition?

No. Roflumilast is a small-molecule active ingredient. Generic competition would ordinarily proceed through an ANDA, not a biosimilar application.

References

United States Patent and Trademark Office. (2021). US Patent No. 10,940,142, Pharmaceutical compositions comprising roflumilast. https://patents.google.com/patent/US10940142B2/en
Google Patents. (n.d.). US10940142B2 patent family and legal status. https://patents.google.com/patent/US10940142B2/en
U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations, Orange Book. https://www.accessdata.fda.gov/scripts/cder/ob/index.cfm
U.S. Food and Drug Administration. (2022). ZORYVE cream prescribing information. https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/215985s000lbl.pdf
U.S. Food and Drug Administration. (2017). ANDA submissions: Amendments and requests for final approval to tentatively approved ANDAs. https://www.fda.gov/regulatory-information
Arcutis Biotherapeutics, Inc. (2023). Annual report pursuant to Section 13 or 15(d) of the Securities Exchange Act of 1934. U.S. Securities and Exchange Commission. https://www.sec.gov/edgar/browse/?CIK=1769759
Arcutis Biotherapeutics, Inc. (2024). Annual report pursuant to Section 13 or 15(d) of the Securities Exchange Act of 1934. U.S. Securities and Exchange Commission. https://www.sec.gov/edgar/browse/?CIK=1769759

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Arcutis	ZORYVE	roflumilast	CREAM;TOPICAL	215985-002	Jul 9, 2024		RX	Yes	Yes	⤷ Start Trial	⤷ Start Trial	Y				⤷ Start Trial
Arcutis	ZORYVE	roflumilast	CREAM;TOPICAL	215985-001	Jul 29, 2022		RX	Yes	Yes	⤷ Start Trial	⤷ Start Trial	Y				⤷ Start Trial
Arcutis	ZORYVE	roflumilast	CREAM;TOPICAL	215985-003	Oct 4, 2025		RX	Yes	Yes	⤷ Start Trial	⤷ Start Trial	Y				⤷ 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	2018282098	⤷ Start Trial
Australia	2021214399	⤷ Start Trial
Brazil	112019025748	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Summary for Patent: 10,940,142