Details for Patent: 11,793,760

Which drugs does patent 11,793,760 protect, and when does it expire?

Patent 11,793,760 protects NEXTSTELLIS and is included in one NDA.

This patent has seventy-five patent family members in forty-two countries.

Summary for Patent: 11,793,760

Title:	Orodispersible dosage unit containing an estetrol component
Abstract:	The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit consisting of: 0.1-25 wt. % of estetrol particles containing at least 80 wt. % of an estetrol component selected from estetrol, estetrol esters and combinations thereof; and 75-99.9 wt. % of one or more pharmaceutically acceptable ingredients; the solid dosage unit comprising at least 100 μg of the estetrol component; and wherein the solid dosage unit can be obtained by a process comprising wet granulation of estetrol particles having a volume weighted average particle size of 2 μm to 50 μm. The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.
Inventor(s):	Séverine Francine Isabelle JASPART, Johannes Jan Platteeuw, Denny Johan Marijn Van Den Heuvel
Assignee:	Estetra SRL
Application Number:	US18/196,617
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound; Dosage form;

US Patent 11,793,760: Estetrol Tablet Claims, Patent Scope, Exclusivity and Generic Risk

US Patent 11,793,760 protects a solid oral dosage form containing estetrol in dry, particle-controlled granules combined with tableting excipients. The independent claim is formulation-focused rather than molecule-focused. It requires a defined dosage-unit weight, granule composition, estetrol particle-size range, excipient balance and estetrol purity threshold.

The patent is most relevant to oral estetrol products, including estetrol-drospirenone contraceptive tablets such as Nextstellis. It does not, based on the supplied claims, independently protect estetrol as an active pharmaceutical ingredient, every estetrol formulation, or every product containing estetrol and drospirenone.

What does US Patent 11,793,760 protect?

The patent protects a solid pharmaceutical dosage unit meeting all of the following requirements:

Claim element	Scope
Dosage-unit weight	30 to 1,000 mg
Dry estetrol-containing granules	60 to 99.7 wt.% of dosage unit
Granulation excipients	70 to 95 wt.% of dry granules
Estetrol particles	5 to 30 wt.% of dry granules
Estetrol-particle purity	At least 90 wt.% estetrol component
Estetrol-particle volume median diameter	2 to 50 micrometers
Tableting excipients	0.3 to 40 wt.% of dosage unit
Estetrol content	At least 1 wt.% under claim 3
Estetrol dose	1 to 20 mg under claim 4
Dosage form	Tablet under claim 20
Optional progestin	0.1 to 5 mg drospirenone under claim 19

The claim uses a layered composition structure. Estetrol is first incorporated into dry granules. Those granules are then combined with tableting excipients to form the final dosage unit. A product that merely contains estetrol and excipients, without satisfying the claimed granule architecture and particle-size limits, would not fall within claim 1.

How broad is independent claim 1?

Claim 1 is technically detailed but commercially meaningful. It covers a broad range of oral solid formulations while imposing several limitations that narrow infringement analysis.

Composition limitations

The claim requires 60 to 99.7 wt.% dry estetrol-containing granules and 0.3 to 40 wt.% tableting excipients. The two ranges do not independently define the entire dosage-unit composition unless the remaining formulation components are consistent with the claim structure. A formulation with 60 wt.% granules and 40 wt.% tableting excipients falls at the upper boundary of both expressly stated fractions.

The granules must contain:

• 70 to 95 wt.% granulation excipients; and
• 5 to 30 wt.% estetrol particles.

The granulation-excipient range and estetrol-particle range sum to 75 to 125 wt.%. In practice, the actual composition must satisfy the stated percentages on the applicable dry-granule basis. The claim therefore creates a formulation window rather than a single composition.

Particle-size limitation

The estetrol particles must have a volume median diameter, or Dv50, of 2 to 50 micrometers. Dependent claim 6 narrows that range to 3 to 35 micrometers.

This limitation is commercially important because particle size can affect:

• dissolution rate;
• content uniformity;
• granulation behavior;
• compressibility;
• powder flow; and
• bioavailability.

A generic manufacturer could attempt to design around the patent by using estetrol particles above 50 micrometers or below 2 micrometers. That approach would require technical validation because changing particle size may alter dissolution and manufacturing performance.

Purity limitation

The estetrol particles must contain at least 90 wt.% of an estetrol component. The claim defines that component to include:

• estetrol;
• estetrol esters;
• estetrol hydrates; and
• combinations of those materials.

Claim 5 specifically covers estetrol monohydrate. The purity requirement applies to the estetrol particles, not necessarily to the total dosage unit.

What do the dependent claims add?

The dependent claims reinforce the patent around common commercial formulation choices.

Claims	Additional limitation
2	Estetrol particles contain at least 90 wt.% estetrol component
3	Final dosage unit contains at least 1 wt.% estetrol component
4	Final dosage unit contains 1 to 20 mg estetrol component
5	Estetrol component is estetrol monohydrate
6	Particle Dv50 is 3 to 35 micrometers
7	Granulation excipients include listed carbohydrate, filler, binder, disintegrant, glidant or lubricant materials
8	Tableting excipients include lactose, mannitol, xylitol, microcrystalline cellulose, starch, croscarmellose sodium or polyvinylpyrrolidone
9-11	Disintegrants, including modified starches, crospovidone, croscarmellose and sodium carboxymethyl starch
12-14	Granulation excipients contain at least 30%, 40% or 50% water-soluble carbohydrate
15	Dry granules contain 0.2 to 20 wt.% binder
16	Disintegration time is less than five minutes
17	At least 70% estetrol release after five minutes under the specified pH 6.8 dissolution test
18	At least 80% estetrol release after five minutes under the specified dissolution test
19	Dosage unit also contains 0.1 to 5 mg drospirenone
20	Dosage unit is a tablet

Claims 16 to 18 introduce performance limitations. These claims may be valuable against a product that has a substantially similar composition but attempts to dispute infringement based on minor compositional differences. They also create potential enforcement issues because testing method, sampling, analytical method and batch variability can affect the result.

What formulations are protected by US 11,793,760?

The clearest commercial embodiment is an immediate-release estetrol tablet containing:

• estetrol or estetrol monohydrate;
• a carbohydrate-rich granulation system;
• one or more binders;
• a disintegrant;
• tableting excipients; and
• optionally, drospirenone.

A product containing 14.2 mg estetrol and 3 mg drospirenone could fall within claim 19 if the total tablet weight, granule composition, particle size, purity and excipient percentages also satisfy claim 1.

The patent does not require drospirenone in claim 1. Claims 1 through 18 can therefore cover an estetrol-only tablet. Claim 19 is narrower because it requires drospirenone in a 0.1 to 5 mg amount.

Formulations likely outside the literal claim scope

Potential design-around categories include:

1. A liquid, capsule, implant, transdermal system or injectable product rather than a solid dosage unit.
2. A solid product using estetrol particles with a Dv50 outside 2 to 50 micrometers.
3. A product in which estetrol is not incorporated into the claimed dry granules.
4. A dosage unit with less than 60 wt.% dry estetrol-containing granules.
5. A product with no tableting excipient, or more than 40 wt.% tableting excipient.
6. A product using an estetrol particle purity below 90 wt.%.
7. A product containing drospirenone outside the 0.1 to 5 mg range, although that would not avoid claims 1 through 18 if the remaining elements are present.

These are claim-screening categories, not guaranteed freedom-to-operate positions. The doctrine of equivalents and related patent-family claims could affect the analysis.

When does US Patent 11,793,760 lose exclusivity?

The patent issued on December 12, 2023, as US Patent 11,793,760 B2. The statutory term for a US utility patent is generally 20 years from the earliest effective nonprovisional US filing date, subject to patent-term adjustment, terminal disclaimers and any applicable patent-term extension under 35 U.S.C. §§ 154 and 156.

The issue date alone does not establish the expiration date. The relevant commercial date is the patent’s expiration date shown in USPTO term records and, if listed for an FDA-approved product, the Orange Book.

Event	Date or status
US patent grant	December 12, 2023
Patent type	Utility patent
Core technology	Estetrol dry granules and solid dosage units
Statutory term	Generally 20 years from earliest effective nonprovisional filing
Patent-term adjustment	Must be checked in the USPTO record
Orange Book patent-term extension	No extension is established by the supplied claims
Pediatric exclusivity	No pediatric extension is established by the supplied claims

A patent can remain enforceable after approval of a product, but FDA approval does not itself establish patent validity or infringement.

What is the Orange Book status of US 11,793,760?

The supplied claims do not establish whether US 11,793,760 is listed in the FDA Orange Book for Nextstellis or another estetrol product. Orange Book listing must be confirmed against the FDA’s current Approved Drug Products with Therapeutic Equivalence Evaluations database and the relevant product-specific patent submission.

The patent is eligible in subject matter for possible listing if it claims an approved drug, an approved formulation or an approved method of use. Its strongest potential listing theory would be a formulation claim covering an approved estetrol tablet. A claim directed only to a manufacturing intermediate or an unapproved formulation would face a different listing analysis.

For an ANDA applicant, an Orange Book-listed patent can trigger:

• Paragraph I certification if the patent information is not yet applicable;
• Paragraph II certification if the patent has expired;
• Paragraph III certification accepting delayed launch until expiration; or
• Paragraph IV certification alleging that the patent is invalid, unenforceable or not infringed.

What Paragraph IV challenges could affect this patent?

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

Likely validity issues

The most material prior-art questions concern:

• earlier estetrol tablets;
• earlier dry-granulation processes;
• particle-size control for poorly soluble estrogen compounds;
• use of water-soluble carbohydrates in hormone tablets;
• immediate-release estetrol dissolution;
• estetrol monohydrate;
• combined estetrol-drospirenone products; and
• whether the claimed ranges produce an unexpected technical effect.

A challenge to claim 1 could argue that prior art disclosed a solid estetrol dosage unit, granulation excipients, tableting excipients and particle-size ranges overlapping the claimed ranges. The patent owner would likely rely on the specific combination of ranges and the rapid disintegration or dissolution results.

Overlapping numerical ranges are not automatically invalidating. The analysis would depend on whether a skilled person had reason to select the claimed subrange and whether the patent demonstrates unexpected results across the full range.

Infringement issues for an ANDA product

An ANDA applicant would need to compare its proposed product against:

• granule percentage;
• dry-granule composition;
• estetrol particle Dv50;
• estetrol purity;
• dosage-unit weight;
• binder level;
• carbohydrate level;
• disintegration;
• dissolution; and
• drospirenone content.

The applicant’s confidential manufacturing process may become central because particle size and granule composition may not be fully disclosed on the product label. FDA-approved product specifications, batch records and discovery could establish the relevant facts in litigation.

What patent litigation affects estetrol products?

The supplied materials identify no litigation docket, settlement agreement or Paragraph IV notice involving US 11,793,760. The patent number and claims alone cannot establish whether a case has been filed or resolved.

For commercial diligence, the relevant litigation checks are:

Issue	Business significance
ANDA Paragraph IV notice	May trigger a 45-day period for filing an infringement action
30-month stay	May delay ANDA approval if statutory conditions are met
Declaratory-judgment action	Can create earlier litigation exposure
Patent-owner settlement	May establish an agreed generic launch date
Inter partes review	Can challenge patentability before the PTAB
Federal court claim construction	Can narrow or expand practical infringement risk
Terminal disclaimer	May link expiration to another patent in the family

No settlement date or authorized generic arrangement should be assumed without a public agreement, court filing or FDA record.

How does this patent compare with other estetrol patents?

US 11,793,760 is a formulation patent. It should be separated from other patent categories that may protect an estetrol product.

Patent category	Typical protected subject matter	Relevance to generic entry
Active-ingredient patent	Estetrol compound, ester, salt or hydrate	May block use of the active ingredient
Combination patent	Estetrol plus drospirenone	Directly relevant to Nextstellis-type products
Formulation patent	Granules, tablet composition, particle size and dissolution	Directly relevant to the supplied patent
Method-of-use patent	Contraception, menopausal symptoms or other indications	Can restrict labeled use
Manufacturing patent	Synthesis, purification or crystallization	May create supply-chain barriers
Device or packaging patent	Delivery system or product configuration	Usually narrower than the formulation estate

A generic entrant may avoid one formulation patent while remaining exposed to compound, combination, method-of-use or manufacturing patents.

What is the biosimilar risk for this patent?

Biosimilar risk is not the appropriate framework. Estetrol is a chemically synthesized small molecule, not a biologic. A competing product would generally use the generic-drug pathway, including an ANDA and, where applicable, Paragraph IV certification.

The relevant regulatory risks are therefore:

• pharmaceutical equivalence;
• bioequivalence;
• product sameness;
• patent certifications;
• manufacturing-process disclosure; and
• potential formulation differences.

A follow-on product could use a different granulation process or particle-size distribution, but it would still need to meet FDA requirements for quality, performance and bioequivalence.

What licensing deals and commercial exposure are relevant?

Estetrol development has been associated with Mithra Pharmaceuticals and related operating entities, while commercial rights for estetrol products may involve regional licensees or marketing partners. The supplied patent claims do not establish ownership, current assignment, exclusive licensing or royalty obligations.

The principal commercial exposure is the oral contraceptive market for estetrol-drospirenone products. A formulation patent can affect:

• launch timing for generic contraceptives;
• licensing value of an approved product;
• acquisition diligence;
• manufacturing transfer;
• technology access; and
• settlement economics.

Revenue exposure cannot be quantified from the patent claims. It depends on product sales, geographic rights, reimbursement, market share, generic timing and the enforceability of the broader patent estate.

How strong is the patent estate for US 11,793,760?

The patent has moderate formulation-level strength based on the supplied claims.

Strengths

• Claim 1 covers the final solid dosage unit, not only a manufacturing step.
• The claim combines composition, particle size and dosage-unit limitations.
• Dependent claims cover commercially common excipients.
• Claims 16 to 18 add measurable performance requirements.
• Claim 19 directly addresses an estetrol-drospirenone combination.

Weaknesses

• The claim contains many numerical limitations that may provide design-around routes.
• Common excipients such as lactose, mannitol, starch and microcrystalline cellulose may be vulnerable to obviousness arguments when used in conventional tablets.
• Particle-size ranges can be difficult to enforce if the accused product’s Dv50 varies by batch or is measured by a different method.
• Dissolution claims require careful test-method control.
• The patent does not, from the supplied claims, cover every estetrol product or every drospirenone combination.

What generic launch scenarios exist?

Scenario	Likely outcome
No Orange Book listing and no enforceable blocking patent	Generic may launch after regulatory approval, subject to other patents
Paragraph III certification	Approval may be delayed until patent expiry
Paragraph IV certification with no timely suit	FDA approval can proceed under applicable rules
Paragraph IV litigation and 30-month stay	Approval may be delayed while litigation proceeds
Settlement with agreed entry date	Entry occurs on the negotiated date
Successful design-around	Generic avoids literal infringement risk for this patent
Patent invalidated or claims narrowed	Earlier entry becomes possible
Patent upheld and infringed	Launch may be blocked until expiration or settlement

Key Takeaways

• US Patent 11,793,760 is directed to solid estetrol dosage units made with dry estetrol-containing granules.
• Claim 1 requires a specific combination of granule content, excipient percentages, estetrol particle size and particle purity.
• Claim 19 covers tablets combining the claimed formulation with 0.1 to 5 mg drospirenone.
• The patent is relevant to Nextstellis-type products but does not, on the supplied claims, cover estetrol as a molecule or every estetrol formulation.
• Generic risk depends on the broader patent family, Orange Book listing, any Paragraph IV certification, litigation and settlement terms.
• Biosimilar analysis is inapplicable because estetrol is a small-molecule active ingredient.
• The principal design-around opportunities involve granule architecture, particle size, excipient percentages, dosage form and dissolution profile.
• The exact expiration date requires review of the patent’s earliest effective filing date, patent-term adjustment, terminal disclaimers and any patent-term extension.

FAQs About US Patent 11,793,760

Does US Patent 11,793,760 cover Nextstellis?

It may cover a Nextstellis-type tablet if the approved product satisfies the claimed granule composition, estetrol particle-size range, purity threshold and dosage-unit limitations. The patent claims alone do not establish FDA listing or infringement.

Does the patent cover estetrol monohydrate?

Yes. Claim 5 expressly recites estetrol monohydrate, provided the other limitations of claim 1 are satisfied.

Can a generic avoid this patent by changing the excipients?

Possibly. Changing excipients alone may not avoid claim 1 because the independent claim does not require every excipient listed in the dependent claims. The generic would need to avoid the complete combination of claim limitations.

Does claim 19 require drospirenone?

Yes. Claim 19 requires 0.1 to 5 mg drospirenone in addition to the limitations inherited from claim 1. Claims 1 through 18 do not require drospirenone.

Is US 11,793,760 a method-of-use patent?

No. The supplied claims are product and formulation claims. They do not recite contraception, menopausal treatment or another therapeutic method of use.

References

1. United States Patent and Trademark Office. (2023). U.S. Patent No. 11,793,760, solid pharmaceutical dosage unit comprising estetrol-containing granules.
2. United States Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations.
3. United States Code. (2023). 35 U.S.C. §§ 154, 156.
4. United States Food and Drug Administration. (2021). Nextstellis prescribing information.

Drugs Protected by US Patent 11,793,760

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Mayne Pharma	NEXTSTELLIS	drospirenone; estetrol	TABLET;ORAL	214154-001	Apr 15, 2021		RX	Yes	Yes			Y

International Family Members for US Patent 11,793,760

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	3701944		PA2022508	Lithuania
European Patent Office	3701944		PA2022508,C3701944	Lithuania
European Patent Office	3701944		202240021	Slovenia