Details for Patent: 10,426,743

Which drugs does patent 10,426,743 protect, and when does it expire?

Patent 10,426,743 protects VTAMA and is included in one NDA.

This patent has fifty-five patent family members in thirty-eight countries.

Summary for Patent: 10,426,743

Title:	Topical pharmaceutical compositions
Abstract:	The present invention relates to topical pharmaceutical emulsion compositions comprising a therapeutically effective amount of 3,5-Dihydroxy-4-isopropyl-trans-stilbene or a pharmaceutically acceptable salt thereof, an oil phase, a water phase, a surfactant, and an antioxidant, and wherein the emulsion composition is homogeneous and/or the active is solubilized in the oil phase. The invention also relates to methods of treating a dermatological condition or disorder in a patient by administering the present compositions to the skin of the patient.
Inventor(s):	Sujatha D. SONTI, Joey Roger THOMAS, Jon Lenn, Leandro SANTOS, Justin WHITEMAN, Michael Quinn DOHERTY, Mary BEDARD, Piyush Jain
Assignee:	Dermavant Sciences GmbH , GlaxoSmithKline Intellectual Property Development Ltd
Application Number:	US16/255,121
Patent Claim Types: see list of patent claims	Use; Composition;

Executive summary: U.S. Patent 10,426,743 protects a topical oil-in-water (O/W) emulsion dosing method for treating inflammatory dermatologic diseases using 3,5-dihydroxy-4-isopropyl-trans-stilbene (or salt) as the only active ingredient in the oil phase, formulated with medium-chain triglycerides (C6–C12), defined non-ionic emulsifying wax NF + optional additional non-ionic surfactants, and multiple excipient categories. Claim scope is driven by (i) specific drug identity and “only active ingredient in the oil phase” limitation, (ii) emulsion architecture (O/W, homogeneous, droplet size range), (iii) oil-phase exclusions (substantially free of petrolatum and mineral oil), and (iv) compositional numeric windows for each critical component. The estate as written reads like formulation-and-use protection with dense dependent claim narrowing (disease, dosing frequency, exact ingredient lists, excipient species, and specific percentage exemplars), creating a mix of broad independent coverage and highly targeted fallback positions for infringement and licensing leverage.

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U.S. Patent 10,426,743: What is claimed in the independent method claim?

Short answer: The independent claim covers a method of treating an inflammatory skin disorder in a patient by topically administering a specific homogeneous O/W emulsion containing 3,5-dihydroxy-4-isopropyl-trans-stilbene (or salt) at defined % in an oil phase solubilizing the drug, with specified medium-chain triglycerides, surfactant system, optional dermatologically acceptable excipients, and droplet size plus formulation exclusions.

Core structural elements that define infringement

1. Treatment method (method-of-use framing)

   • “Method of treating an inflammatory disease or disorder in a patient in need thereof.”
   • This is a use claim; however, infringement ultimately hinges on administering the claimed composition topically.

2. Active identity and placement

   • Drug: 3,5-dihydroxy-4-isopropyl-trans-stilbene or pharmaceutically acceptable salt.
   • Key placement limitation: the drug is “solubilized in the oil phase” and is “the only active ingredient in the oil phase.”
   • Practical scope impact:
     • A competitor can design around by placing another active in the oil phase (if allowed by other claims), or by formulating the drug in a way that violates “only active ingredient in the oil phase” (e.g., co-solubilizing a second actives into the oil phase).
     • If a second active exists elsewhere (water phase) without being “in the oil phase,” the claim language still leaves room; but fact patterns and analysis would require careful mapping of where each active is actually located.

3. Formulation architecture

   • Delivery form: topical pharmaceutical oil-in-water emulsion composition
   • Must be homogeneous
   • Oil phase droplet size distribution: average droplet size of the oil phase from 0.1 microns to 35 microns.

4. Oil phase composition and exclusions

   • Oil phase includes medium chain triglycerides with carbon length C6 to C12 in 2% to 30% by weight.
   • Exclusion: oil phase is “substantially free of petrolatum and mineral oil.”
     • “Substantially free” is a flexible qualifier, but it gives enforceability leverage against formulations incorporating these conventional emollients.

5. Surfactant system and numeric window

   • Surfactant amount: 1% to 20% by weight.
   • Surfactant comprises at least one non-ionic emulsifying wax NF.
   • Dependent claims heavily populate this surfactant system with specific mixtures: cetostearyl alcohol + polysorbate; steareth-2, steareth-20, polysorbate 80 combinations; and optional other non-ionic categories.
   • This creates both:
     • A broad independent requirement (“at least one emulsifying wax NF”)
     • Multiple narrower dependent fallbacks locking down preferred non-ionic surfactant recipes.

6. Dermatologically acceptable excipient category

   • The claim permits “a dermatologically acceptable excipient selected from the group consisting of an antioxidant, a pH adjusting agent, a chelating agent, a preservative, a co-solvent and combinations thereof.”
   • This is broad in category but the dependent claims enumerate many specific excipient species and concentrations.

Independent-claim quantitative ranges (highest leverage for design-arounds)

• Active (drug): 0.05% to 2% by weight
• Medium chain triglycerides (C6–C12): 2% to 30% by weight
• Surfactant: 1% to 20% by weight
• Droplet size: 0.1 μm to 35 μm
• Oil phase must be petrolatum/mineral oil substantially free
• Water phase exists (but independent claim does not set a numeric window; dependent claims do)

Featured risk zone for competitors: Many generic or OTC-format reformulations fail because they do not control droplet size and/or they use petrolatum/mineral oil excipients, or they use different oil phase lipids outside the “medium chain triglycerides (C6–C12)” limitation.

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Which dependent claims narrow scope by disease, dosing, and droplet size?

Short answer: Disease is narrowed to psoriasis, atopic dermatitis, acne; dosing frequency narrows to once or twice daily; droplet size narrows to multiple sub-ranges down to 0.75 microns and below 15 microns.

Disease-specific narrowing

• Dependent claim 2: inflammatory disease is psoriasis, atopic dermatitis, or acne.

Dosing regimen narrowing

• Dependent claim 3: administered once per day
• Dependent claim 4: administered twice per day

These are method-of-use limitations. A challenger could argue non-infringement by prescribing different frequency, but real-world labeling and adherence data often create factual issues. The claim language still ties infringement to use of the composition.

Droplet size dependent fallbacks

• Claim 55: 0.1 μm to <15 μm
• Claim 56: 0.1 μm to 5 μm
• Claim 57: 0.1 μm to 0.75 μm
• Claim 58: about 0.5 μm

From a technical claim landscape view, the independent claim already provides a generous maximum (35 μm), but these dependents give multiple “tight windows” for infringement detection and for settlement benchmarking.

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How is the surfactant system defined, and where do dependent claims create the tightest patent coverage?

Short answer: The surfactant must contain at least one non-ionic emulsifying wax NF, with dependent claims specifying mixture recipes including cetostearyl alcohol plus polysorbate, and combinations of steareth-2, steareth-20, and polysorbate 80.

Independent surfactant requirement

• Surfactant amount: 1% to 20% by weight
• Must include: at least one non-ionic emulsifying wax NF

Key dependent surfactant compositions

• Claim 15: non-ionic emulsifying wax NF is a mixture of cetostearyl alcohol + a polysorbate
• Claim 16: surfactant comprises the emulsifying wax NF plus at least one of:
  • ethoxylated fatty alcohol ethers
  • sorbitan derivative
• Claim 17: surfactant comprises emulsifying wax NF plus at least one of:
  • steareth-2
  • steareth-20
  • polysorbate 80
• Claim 18: explicit mixture of emulsifying wax NF + steareth-2 + steareth-20 + polysorbate 80

These dependents matter because many competing O/W emulsions use different non-ionic surfactant chemistries (e.g., PEGylated fatty acid esters, different alkyl ether surfactants). If they omit “emulsifying wax NF” as defined in the patent, they can avoid those narrower dependent claim traps; but the independent claim still requires at least one emulsifying wax NF, so omission may be a decisive design-around unless other claims are asserted.

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What excipients are covered, and how do concentrations create “claim maps” for formulation testing?

Short answer: The patent covers excipient categories (antioxidant, pH adjuster, chelator, preservative, co-solvent), and dependent claims lock in species and concentration ranges. This turns product development into a compliance matrix.

Antioxidant pathways

• Claim 19: antioxidant excipient
• Concentration ranges:
  • Claim 20: 0.001% to 5%
  • Claim 21: 0.01% to 1%
  • Claim 22: 0.05%
  • Claim 23: 0.1%
• Species:
  • Claim 24: propyl gallate, BHT, tocopherol
  • Claim 25: specifically butylated hydroxytoluene (BHT)
  • Claim 26: BHT at 0.1% by weight

This is a common formulation control point. If a competitor swaps BHT for e.g., tocopherol but remains within the broad antioxidant category, it may still land inside claim scope depending on which claim is asserted.

pH adjusting agent pathways

• Claim 27: pH adjusting agent excipient category
• Claim 29: enumerated acids include lactic, acetic, maleic, succinic, citric, benzoic, boric, sorbic, tartaric, edetic, phosphoric, nitric, sulphuric, hydrochloric and mixtures.
• Claim 30: buffer
• Claim 31: buffer types enumerated including citrate, acetate, phosphate, propionate, lactate, ammonium/ammonia, and edetate.
• Claim 32: specifically citrate/citric acid buffer
• Claim 33: citrate/citric acid buffer at 0.27%
• Claim 34: 0.01% to 10%

Chelating agent pathways

• Claim 35: chelating agent category
• Claim 36: citric acid, glucuronic acid, sodium hexametaphosphate, zinc hexametaphosphate, EDTA, phosphonates, salts
• Claim 37: EDTA or salt
• Claim 38: 0.01% to 1%
• Claim 39: 0.1%
• Claim 86: enumerated chelators category (similar list)
• Claim 87: EDTA again
• Claim 88: 0.01% to 1%
• Claim 89: 0.1%

Preservative pathways

• Claim 40: preservative category
• Claim 41: extensive preservative list including benzyl alcohol, imidazolidinyl urea, diazolidinyl urea, dichlorobenzyl alcohol, chloroxylenol, parabens, phenoxyethanol, sorbic acid, benzoic acid and salts.
• Claim 42: benzoic acid
• Claim 43: benzoic acid 0.25%
• Claim 44: 0.01% to 2%
• Claim 45: 0.25%

Co-solvent pathways

• Claim 46: co-solvent category
• Claim 47: 5% to 20%
• Claim 48: propylene glycol + diethylene glycol monoethyl ether
• Claim 49: propylene glycol 10%
• Claim 50: diethylene glycol monoethyl ether 2%

Additional excipients category (second excipient)

• Claim 51: further excipient selected from penetration enhancer, humectant, thickening agent, gelling agent, viscosity building agent, fragrance, colorant, combinations.

This secondary category increases practical formulation freedom while keeping the core constraints fixed.

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What are the tightest “compositions” explicitly exemplified by claims 59, 107, and 112?

Short answer: The patent includes specific weighted-ingredient examples that anchor enforceability and provide direct “copy” targets. Claims 107 and 112 are detailed compositions with explicit percentage breakdowns of each surfactant component, excipient species and amounts, and co-solvent proportions.

Claim 59: representative “complete composition” scaffold

• Drug: 0.05% to 2% (within same range as independent)
• MCT oil: 2% to 30%
• Water phase exists
• Surfactant: within 1% to 20%, and includes mixture of:
  • emulsifying wax NF
  • plus steareth-2, steareth-20, polysorbate 80 options
• Oil phase is solubilizing and only-active-active-in-oil
• Petrolatum/mineral oil substantially free
• Homogeneous; droplet size 0.1 to 35 μm

Claim 59 largely restates the independent claim with specified surfactant mixture and enumerated excipient categories (antioxidant + pH + chelator + preservative + co-solvent).

Claim 107: explicit percentages (compliance benchmark)

• Drug: 0.5%
• MCT: 10%
• Water phase: 65.18%
• Surfactant mixture:
  • 7.20% emulsifying wax NF
  • 1.80% steareth-2
  • 1.10% steareth-20
  • 1.5% polysorbate 80
• Antioxidant: 0.10% BHT
• pH adjusting agent: 0.27% citrate/citric acid buffer
• Chelating agent: 0.10% disodium EDTA
• Preservative: 0.25% benzoic acid
• Co-solvent: 10% propylene glycol + 2% diethylene glycol monoethyl ether
• Droplet size: 0.1 to 35 μm (with dependents narrowing below 15, below 5, below 0.75, and ~0.5 μm)

Claim 112: alternate explicit percentages (same excipient recipe, higher drug and water)

• Drug: 1.0%
• MCT: 10%
• Water phase: 64.68%
• Surfactant mixture: same as claim 107
  • 7.20% emulsifying wax NF
  • 1.80% steareth-2
  • 1.10% steareth-20
  • 1.5% polysorbate 80
• Antioxidant: 0.10% BHT
• pH buffer: 0.27% citrate/citric acid buffer
• Chelating agent: 0.10% disodium EDTA
• Preservative: 0.25% benzoic acid
• Co-solvent: 10% propylene glycol + 2% diethylene glycol monoethyl ether
• Droplet size: 0.1 to 35 μm (with dependents narrowing)

These two exemplars indicate likely patent prosecution fallback positions for commercially realized formulations.

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How many distinct claim “modules” exist, and what does that imply for infringement strategy?

Short answer: The claim set is modular: (1) active identity and “only active in oil phase” placement, (2) oil phase lipid class (MCT C6–C12) plus oil-phase exclusions, (3) surfactant system anchored by non-ionic emulsifying wax NF, (4) droplet size windows, and (5) excipient category and species-specific dependent ranges (antioxidant, pH buffer, chelator, preservative, co-solvent). This allows assertion flexibility and narrows to specific recipe variants.

Infringement “entry points” (what to test)

• Does the product use 3,5-dihydroxy-4-isopropyl-trans-stilbene (free base or specified salt)?
• Is the drug solubilized in the oil phase and is it the only active ingredient in the oil phase?
• Is the oil phase composed of medium chain triglycerides C6–C12 at 2% to 30%?
• Is the product homogeneous O/W emulsion with oil droplet average size 0.1–35 μm?
• Does the formulation avoid being “substantially free” of petrolatum/mineral oil?
• Does the surfactant system include an NF non-ionic emulsifying wax and have the right surfactant %?
• Are antioxidant/pH/chelator/preservative/co-solvent present within dependent claim species/ranges?

Litigation leverage

Because dependent claims include explicit species and percentages, the patentee can choose claims with the highest probability of meeting measurable composition endpoints, especially droplet size, excipient quantification, and presence/absence of petrolatum/mineral oil.

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What generic entry risks exist for an O/W emulsion using the same active but different excipient recipes?

Short answer: The biggest risks come from failing the “only active in oil phase” test, using petrolatum/mineral oil, using non-MCT oils (or out-of-range MCT %), and not meeting the droplet-size profile. Swapping excipient species (e.g., different antioxidant) can be a partial design-around but may not eliminate independent claim coverage because independent claim only requires at least one excipient category and allows multiple excipient options.

Common design-around patterns and likely outcomes

1. Same active, different oil lipid

   • If oil phase is not medium chain triglycerides C6–C12 or outside 2%–30%, risk drops for independent and many dependents.

2. Same active, different emulsion type

   • If product is not an oil-in-water emulsion (e.g., water-in-oil or gel), it avoids the independent claim.

3. Same active, additional oil-phase actives

   • If competitor includes another active solubilized in the oil phase, it can avoid the “only active ingredient in the oil phase” limitation.

4. Same active and oil phase, different surfactants

   • If competitor uses non-ionic emulsifiers but does not include “non-ionic emulsifying wax NF,” it can avoid the independent surfactant requirement, even if it matches other categories.

5. Same active and recipe, broader droplet size

   • If droplet size average is outside 0.1–35 μm, risk decreases. If only the dependent droplet windows are missed, independent still may apply.

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What patent landscape conclusions can be drawn from the claim architecture (without external bibliographic data)?

Short answer: With the information provided, 10,426,743 is best treated as a formulation-and-use patent with strong specificity on emulsion structure, lipid class, droplet size, surfactant composition category, and oil-phase exclusions. The dependent claim density suggests either (i) substantial prosecution emphasis on narrowing to a particular recipe family, or (ii) a strategy to ensure infringement capture across multiple product “variants” that share the same active and core emulsion characteristics.

Key “scope drivers” that are most likely litigated

• “Only active ingredient in the oil phase”
• “Substantially free of petrolatum and mineral oil”
• Droplet size average range
• Surfactant inclusion of “non-ionic emulsifying wax NF”
• MCT carbon length and amount
• Drug % and oil phase solubilization

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Key Takeaways

• U.S. Patent 10,426,743 protects topical O/W emulsion treatment methods using 3,5-dihydroxy-4-isopropyl-trans-stilbene (or salt) with strict oil-phase solubilization and “only active in oil phase” constraints.
• Independent claim scope is governed by: active identity, oil-phase MCT (C6–C12) amount, surfactant requirement anchored by non-ionic emulsifying wax NF, homogeneity, droplet size (0.1–35 μm), and exclusion of petrolatum/mineral oil.
• Dependent claims intensify enforceability through: specific diseases, once/twice daily dosing, tight droplet size subranges, and species-specific excipient lists (notably BHT 0.1%, citrate/citric buffer 0.27%, disodium EDTA 0.10%, benzoic acid 0.25%, and propylene glycol + diethylene glycol monoethyl ether).
• Claims 107 and 112 present explicit formulation targets that can be used to benchmark product development and to assess infringement probability quickly using lab testing (droplet size, composition assays, and oil-phase ingredient distribution).

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FAQs

1. Does the “only active ingredient in the oil phase” limit allow other actives in the water phase?
2. How does droplet size measurement affect infringement risk for emulsions within 0.1–35 μm?
3. If a product includes petrolatum in trace amounts, how does “substantially free” influence claim coverage?
4. What is the most direct design-around if a competitor uses a different triglyceride oil blend?
5. Can dosing frequency (once vs twice daily) be used to avoid infringement if the same composition is used?

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References

1. United States Patent 10,426,743 (claims as provided).

Drugs Protected by US Patent 10,426,743

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Organon Llc	VTAMA	tapinarof	CREAM;TOPICAL	215272-001	May 23, 2022		RX	Yes	Yes	10,426,743					TOPICAL TREATMENT OF ATOPIC DERMATITIS IN ADULTS AND PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER
Organon Llc	VTAMA	tapinarof	CREAM;TOPICAL	215272-001	May 23, 2022		RX	Yes	Yes	10,426,743					TOPICAL TREATMENT OF PLAQUE PSORIASIS IN ADULTS

International Family Members for US Patent 10,426,743

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	104699
Australia	2016263161
Australia	2019203627
Brazil	112017024934