United States Patent 9,566,252: Ospemifene Dyspareunia Claims, Exclusivity and Patent Landscape

US Patent No. 9,566,252 protects the use of ospemifene, also known as (deaminohydroxy)toremifene, to alleviate dyspareunia associated with menopause. The strongest commercial claim is claim 12, which covers oral administration of 60 mg per day. That regimen corresponds to the approved Osphena dosing regimen.

The patent is a method-of-use patent rather than a composition-of-matter patent. Its practical value depends on whether a competing product is labeled, promoted, or used for menopausal dyspareunia. The nominal patent expiration date is February 26, 2031, subject to any applicable patent-term adjustment or regulatory extension recorded by the USPTO or FDA.

What drug and indication does US Patent 9,566,252 protect?

The patent covers ospemifene for menopausal dyspareunia. Ospemifene is a selective estrogen receptor modulator marketed in the United States as Osphena by Shionogi Inc.

The FDA approved Osphena on February 26, 2013, for the treatment of moderate-to-severe dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause. The approved dose is 60 mg orally once daily with food.[1]

Item	Patent and product detail
US patent	9,566,252
Patent type	Method of treatment
Active ingredient	Ospemifene, also called (deaminohydroxy)toremifene
Covered condition	Dyspareunia during or after menopause
Primary commercial product	Osphena
Sponsor/marketer	Shionogi Inc.
FDA approval date	February 26, 2013
Approved dosage	60 mg orally once daily with food
Nominal patent expiration	February 26, 2031
Therapeutic class	Selective estrogen receptor modulator
Dosage form	Oral tablet

The claims do not require a particular tablet formulation, excipient, food effect, brand, manufacturer, or manufacturing process. They focus on the therapeutic use of the active ingredient.

What are the independent and dependent claims in US 9,566,252?

Claim 1 is the broadest claim. It covers administering an effective amount of ospemifene, or a pharmaceutically acceptable salt, to a woman to alleviate dyspareunia during or after menopause.

The claim has five principal limitations:

A method of treatment.
A woman in need of treatment.
Dyspareunia as the condition being alleviated.
Menopause as the relevant physiological context.
Administration of an effective amount of ospemifene or an acceptable salt.

Claim 1 does not specify:

Oral administration.
A 60 mg dose.
A particular duration of treatment.
Postmenopausal status.
A tablet or capsule.
Administration with food.
A specific formulation.
A particular severity of dyspareunia.

That breadth makes claim 1 the principal infringement risk for any product labeled for menopausal dyspareunia.

Claim-by-claim scope

Claim	Limitation added	Scope
1	Ospemifene or salt for menopausal dyspareunia	Broadest method claim
2	Ospemifene must not be a salt	Free-base ospemifene
3	Oral administration	Oral salt or free-base treatment
4	Free base, 25-100 mg daily	Non-salt dose range
5	Free base, 60 mg daily	Specific non-salt dose
6	Claim 5 plus oral administration	Oral, non-salt, 60 mg
7	Postmenopausal woman	Postmenopausal patient
8	Claim 2 plus postmenopausal woman	Postmenopausal, non-salt treatment
9	Claim 6 plus postmenopausal woman	Oral, non-salt, 60 mg, postmenopausal
10	30-90 mg daily	Dose range, salt or free base
11	60 mg daily	Specific dose, salt or free base
12	Oral administration at 60 mg daily	Core commercial regimen

Claim 12 is particularly important because it recites the approved Osphena regimen while retaining the broad claim 1 reference to ospemifene rather than expressly requiring the free base. Claim 6 is narrower because it depends on claim 5 and therefore requires the non-salt form.

How broad is claim 1 of US 9,566,252?

Claim 1 is broad in route, dose, formulation, and salt status, but narrow in disease context and patient population.

A potential treatment generally falls within claim 1 if:

The active ingredient is ospemifene or a pharmaceutically acceptable salt.
The patient is a woman.
The patient is experiencing dyspareunia.
The dyspareunia occurs during or after menopause.
The product is administered in an effective amount.
The purpose or clinical effect is alleviation of dyspareunia.

The claim does not require the drug to be approved for the indication. A clinical-use theory could therefore apply to off-label treatment if the other claim elements are met.

The claim also does not require the patient to be fully postmenopausal. Claims 7 through 9 separately narrow the population to postmenopausal women, indicating that claim 1 is intended to cover a wider menopausal population.

What dose and route are protected by the patent?

The claims cover both broad dose ranges and the 60 mg daily dose.

Claims 4 and 10 recite overlapping ranges:

Claim 4: 25 to 100 mg per day, non-salt ospemifene.
Claim 10: 30 to 90 mg per day, salt or non-salt ospemifene.

Claims 5, 11, and 12 capture the 60 mg regimen:

Claim 5: 60 mg per day, non-salt form.
Claim 11: 60 mg per day, salt or non-salt form.
Claim 12: oral 60 mg per day.

The commercial importance of claim 12 is high because the FDA-approved Osphena label uses a 60 mg oral tablet taken once daily with food.[1]

Regimen	Relevant claims
Any effective dose, any route	Claim 1
Oral administration, any stated dose	Claim 3
25-100 mg daily, free base	Claim 4
60 mg daily, free base	Claim 5
Oral 60 mg daily, free base	Claim 6
30-90 mg daily, salt or free base	Claim 10
60 mg daily, salt or free base	Claim 11
Oral 60 mg daily, salt or free base	Claim 12

Is US Patent 9,566,252 a formulation patent?

No. The patent claims a therapeutic method, not a particular formulation.

It does not expressly require:

A specific tablet composition.
A particular crystalline form.
A particle-size distribution.
A dissolution profile.
A coating.
A release mechanism.
A defined excipient.
Administration with food.
A manufacturing process.

A generic manufacturer could therefore avoid formulation-specific infringement only if its product and labeling also avoid the patented therapeutic use. Developing a different tablet formulation would not, by itself, avoid claims 1, 11, or 12 if the product is administered for menopausal dyspareunia.

Separate formulation, salt, polymorph, process, or dosage-form patents could create additional barriers, but those rights would be distinct from the claims supplied for US 9,566,252.

What is the FDA and Orange Book status of US 9,566,252?

Osphena is an FDA-approved small-molecule product, not a biologic. Biosimilar provisions under the Biologics Price Competition and Innovation Act do not apply.

The relevant FDA pathway for a competing ospemifene product is an abbreviated new drug application, or ANDA. An ANDA applicant would typically address any listed patents through one of four certifications:

Paragraph I: no patent information is listed.
Paragraph II: the listed patent has expired.
Paragraph III: the applicant will wait until patent expiration.
Paragraph IV: the patent is invalid, unenforceable, or will not be infringed.

If US 9,566,252 is listed in the Orange Book for Osphena, an ANDA applicant seeking approval before the patent’s expiration would face a Paragraph IV issue or would need to use a permissible labeling carve-out.

The approved indication creates a substantial skinny-label problem. Osphena’s principal FDA indication is menopausal dyspareunia, which overlaps directly with the patent claims. A generic applicant could attempt to omit patented use information from its labeling, but a carve-out would be commercially difficult if the remaining label does not support a viable non-infringing indication.

When does US Patent 9,566,252 lose exclusivity?

The patent’s nominal 20-year term is calculated from the earliest effective nonprovisional priority date. The relevant priority date is February 26, 2010. On that basis, the nominal expiration date is February 26, 2031.[2]

Exclusivity category	Date or status
FDA approval	February 26, 2013
Five-year new chemical entity exclusivity	Ended February 26, 2018
Patent term based on February 26, 2010 priority	Nominally ends February 26, 2031
Patent-protected 60 mg oral method	Potentially protected through patent expiration
Biosimilar exclusivity	Not applicable

FDA regulatory exclusivity and patent exclusivity are separate. The five-year NCE period protects the approved active ingredient from certain ANDA submissions, but it does not extend the patent term. Conversely, expiration of NCE exclusivity did not eliminate the method-of-use patent.

The final enforceable date should be determined from the USPTO patent record, including any patent-term adjustment, terminal disclaimer, disclaimer filing, or applicable pediatric extension.

What earlier patents form the ospemifene patent landscape?

The ospemifene estate includes earlier patents directed to the compound and its use in menopausal disorders. US Patent No. 8,133,890 is an important earlier family member associated with ospemifene therapeutic use and vaginal symptoms.[3]

The distinction between the earlier estate and US 9,566,252 is commercially important:

Patent category	Typical protection	Commercial effect
Composition-of-matter patent	Ospemifene compound or chemical class	Broadest product barrier
Therapeutic-use patent	Ospemifene for vaginal atrophy or related symptoms	Indication-specific barrier
US 9,566,252	Ospemifene for menopausal dyspareunia	Direct protection for the Osphena indication
Formulation patent	Tablet, salt, polymorph, excipient, or release profile	Product-specific barrier
Manufacturing patent	Synthesis or purification process	Supply-chain barrier

US 9,566,252 is therefore best characterized as an indication patent that protects the principal clinical use of Osphena. Its value is greater than a narrow secondary-use patent because the claimed condition corresponds closely to the FDA-approved indication and commercial product positioning.

Which companies could challenge the ospemifene patent?

The likely challengers are generic-drug companies with the capacity to submit an ANDA for ospemifene tablets. A Paragraph IV challenge could target:

Invalidity for lack of novelty or obviousness.
Inadequate written description or enablement.
Non-infringement based on a proposed label.
Lack of enforceability.
Inapplicability of particular claims to the proposed salt or dosage form.

The strongest invalidity theories would likely focus on prior art describing:

Ospemifene treatment of menopausal vaginal symptoms.
Treatment of dyspareunia with selective estrogen receptor modulators.
The use of 60 mg ospemifene.
Clinical evidence linking vaginal atrophy improvement to reduced dyspareunia.

The strongest non-infringement theory would involve a label that omits menopausal dyspareunia and does not encourage the patented use. That strategy may be constrained by the product’s approved indication and the commercial purpose of the generic launch.

No biosimilar challenger is relevant because ospemifene is a synthetic small molecule.

What patent litigation and settlement risks affect generic entry?

A Paragraph IV notice would likely trigger litigation under Hatch-Waxman procedures if the patent holder sued within the statutory 45-day period. Litigation could delay FDA approval for up to 30 months, subject to court action and statutory exceptions.[4]

Possible litigation outcomes include:

Patent upheld and infringed: generic approval remains blocked until expiration or settlement.
Patent invalidated: early approval becomes possible, subject to other listed patents and exclusivities.
Patent not infringed: approval may proceed if no other barrier applies.
Settlement with an agreed launch date: entry occurs before patent expiry under negotiated terms.
Label carve-out: approval proceeds for non-patented uses, if FDA accepts the proposed omission.

A settlement would require review for its launch date, restrictions on marketing, authorized-generic provisions, supply commitments, and any payment or commercial arrangement. The supplied claims alone do not establish the existence or terms of a settlement agreement.

How strong is the patent estate for Osphena?

The estate is strongest against a generic seeking approval for the same clinical use and dose as Osphena. The risk profile is lower for a product that:

Uses ospemifene for a different condition.
Omits dyspareunia from its label.
Is not directed to menopausal patients.
Uses a non-overlapping clinical indication.
Does not encourage the patented treatment.

The patent is less powerful as a manufacturing barrier because it contains no process claims. It is also less powerful against non-therapeutic research, laboratory use, or a commercial product whose labeling and marketing avoid the claimed indication.

Risk area	Assessment
Generic for Osphena indication	High
Generic 60 mg oral tablet	High
Alternative ospemifene indication	Lower, depending on labeling
Different formulation	Does not independently avoid method claims
Ospemifene salt	Still potentially covered by claims 1, 3, 10, 11, and 12
Biosimilar competition	Not applicable
Manufacturing substitution	Not directly covered
Off-label physician use	Potential method-of-use exposure

What generic launch scenarios exist for ospemifene?

Three launch scenarios are commercially plausible.

Launch after patent expiration

This is the lowest litigation-risk path. A generic would wait until the patent term ends and address any remaining Orange Book patents or regulatory exclusivity.

Paragraph IV launch

A challenger could seek approval before February 2031 by arguing invalidity, unenforceability, or non-infringement. This path creates litigation exposure but can produce a substantially earlier launch if successful.

Skinny-label launch

A generic could omit the patented dyspareunia use if FDA labeling rules permit a commercially viable carve-out. Because menopausal dyspareunia is the central Osphena indication, the practical value of this strategy may be limited.

An authorized generic or license arrangement could provide an earlier market entry while preserving some originator control. No such arrangement is established by the claim text.

What is the geographic scope of US Patent 9,566,252?

The patent is enforceable only in the United States. It does not directly block:

Manufacture and sale outside the United States.
Foreign clinical use.
Importation into countries without corresponding enforceable rights.

The commercial landscape must therefore be reviewed country by country. Foreign counterparts may have different claim scope, prosecution histories, expiration dates, opposition outcomes, and validity positions. A US patent does not establish protection in Europe, Canada, Japan, or other markets.

Key Takeaways

US 9,566,252 is an indication patent covering ospemifene treatment of menopausal dyspareunia.
Claim 1 is broad on dose, route, and salt status.
Claim 12 is the commercially important species claim because it covers oral 60 mg daily administration.
The patent does not claim a specific formulation or manufacturing process.
The nominal expiration date is February 26, 2031.
Osphena was FDA-approved on February 26, 2013, and its approved regimen directly overlaps claim 12.
Ospemifene is a small molecule, so biosimilar competition is irrelevant.
An ANDA applicant would face a Paragraph IV, Paragraph III, or potential skinny-label strategy.
Generic risk is highest for a product labeled for menopausal dyspareunia at 60 mg orally once daily.
The patent’s geographic effect is limited to the United States.

FAQs

Does US 9,566,252 cover ospemifene salts?

Yes. Claims 1, 3, 10, 11, and 12 expressly or implicitly retain coverage for ospemifene or a pharmaceutically acceptable salt. Claims 2, 4, 5, 6, 8, and 9 narrow the subject matter to the non-salt form.

Does a different ospemifene tablet formulation avoid US 9,566,252?

No. A different formulation does not avoid a method claim if the product is administered for the claimed menopausal dyspareunia use. Formulation changes matter only if separate formulation claims are asserted or the proposed use avoids the method claims.

Is the 60 mg dose required for infringement?

No. Claim 1 does not require a specific dose. Claims 5, 11, and 12 specifically address 60 mg, but a different effective dose could still fall within claim 1 if the other limitations are met.

Can a generic market ospemifene for a non-dyspareunia indication?

Potentially, if the proposed labeling, marketing, and use do not fall within the patent claims. FDA approval, other listed patents, and induced-infringement risks would still require separate analysis.

Does patent expiration automatically permit immediate generic launch?

No. Launch timing also depends on FDA approval, any remaining Orange Book patents, pediatric exclusivity, litigation outcomes, regulatory stays, and settlement terms.

References

U.S. Food and Drug Administration. (2013). Osphena (ospemifene) prescribing information.
United States Patent and Trademark Office. (2017). U.S. Patent No. 9,566,252, methods of treating dyspareunia.
United States Patent and Trademark Office. (2012). U.S. Patent No. 8,133,890, ospemifene therapeutic uses.
U.S. Food and Drug Administration. (2023). Approved drug products with therapeutic equivalence evaluations: Orange Book.

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	300289	⤷ Start Trial
Australia	2001258449	⤷ Start Trial
Australia	5844901	⤷ Start Trial
Bulgaria	107472	⤷ Start Trial
Bulgaria	65943	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 9,566,252

Summary for Patent: 9,566,252