Details for Patent: 11,957,684

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Which drugs does patent 11,957,684 protect, and when does it expire?

Patent 11,957,684 protects MYFEMBREE and is included in one NDA.

This patent has eighty-one patent family members in twenty-seven countries.

Summary for Patent: 11,957,684

Title:	Treatment of heavy menstrual bleeding associated with uterine fibroids
Abstract:	Methods for treating uterine fibroids, endometriosis, adenomyosis, or heavy menstrual bleeding in a subject, which include administering to the subject from 10 mg to 60 mg per day of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, and from 0.01 mg to 5 mg per day of a hormone replacement medicament. The present disclosure has methods for reducing menstrual bleeding in a subject, reducing bone mineral density loss in a subject caused by administering a GnRH antagonist to the subject, suppressing sex hormones in a subject, reducing vasomotor symptoms or hot flashes in a subject, and reducing symptoms of decreased libido in a subject having uterine fibroids, endometriosis, or adenomyosis. Further provided are methods of maintaining blood glucose profile, maintaining lipid profile, and/or maintaining bone mineral density in a pre-menopausal woman being treated for one or more conditions or symptoms of endometriosis, adenomyosis, uterine fibroids, or heavy menstrual bleeding; and methods of contraception and treating infertility.
Inventor(s):	Brendan Mark JOHNSON, Lynn Seely, Paul N. MUDD, Jr., Susan Wollowitz, Mark Hibberd, Masataka TANIMOTO, Vijaykumar Reddy RAJASEKHAR, Mayukh Vasant SUKHATME
Assignee:	Takeda Pharmaceutical Co Ltd , Sumitomo Pharma Co Ltd , Roivant Sciences Inc
Application Number:	US17/866,201
Patent Claim Types: see list of patent claims	Use; Dosage form;

US Patent 11,957,684: Claim Scope, Exclusivity, Litigation Risk, and Relugolix Patent Landscape

US Patent 11,957,684 protects a once-daily, fixed-dose oral regimen of relugolix 40 mg, estradiol 1 mg, and norethindrone acetate 0.5 mg for treating heavy menstrual bleeding associated with uterine fibroids in premenopausal women. The patent is directed primarily to the clinical use and treatment outcomes of the Myfembree regimen, rather than to the chemical composition of relugolix or the tablet’s manufacturing process.

The principal commercial risk is an FDA-approved generic or alternative product labeled for the same fibroid-related heavy menstrual bleeding indication. A product using the same three active ingredients at the claimed strengths and dosage frequency could face method-of-use infringement exposure, particularly if its labeling induces the patented treatment protocol.

What does US Patent 11,957,684 protect?

The independent claims cover two related treatment concepts:

Claim	Core subject matter
1	Daily oral administration of relugolix 40 mg, estradiol 1 mg, and norethindrone acetate 0.5 mg for fibroid-associated heavy menstrual bleeding, with menstrual blood loss below 80 mL or reduced by at least 50% from baseline
22	The same fixed-dose daily regimen, where the method treats heavy menstrual bleeding
2-21	Narrower treatment-outcome limitations, including amenorrhea, absence of vasomotor symptoms, preserved bone mineral density, ovulation prevention, reduced fibroid burden, reduced pelvic pain, reduced uterine volume, reduced FSH, and specified serum estradiol levels

The patent therefore combines:

1. A patient population: premenopausal women.
2. A disease: heavy menstrual bleeding associated with uterine fibroids.
3. A dosage form: a single oral dosage form.
4. A formulation: approximately 40 mg relugolix, 1.0 mg estradiol, and 0.5 mg norethindrone acetate.
5. A dosing schedule: once daily.
6. Clinical or pharmacodynamic results.

Claim 22 is commercially important because it does not recite the detailed blood-loss thresholds in claim 1. It requires the same dosing regimen and that the method treats heavy menstrual bleeding. Claim 1 is narrower in its express result limitation but may provide stronger linkage to the clinical trial endpoints supporting the patent.

How broad is the independent claim scope?

Claim 1 is a regimen claim, not a composition-of-matter claim. It does not cover every use of relugolix, every relugolix combination, or every treatment of uterine fibroids.

A potentially infringing product would generally need to satisfy all of the following elements:

Limitation	Scope assessment
Premenopausal woman	Excludes postmenopausal treatment and creates a patient-selection issue
Uterine fibroids	Requires the heavy menstrual bleeding to be associated with fibroids
Heavy menstrual bleeding	Requires treatment of the specified symptom, not merely fibroid suppression
Single dosage form	Favors a co-formulated tablet or other single oral unit
Relugolix	Approximately 40 mg, or an equivalent amount of a pharmaceutically acceptable salt
Estradiol	Approximately 1.0 mg
Norethindrone acetate	Approximately 0.5 mg
Once-daily oral administration	Excludes materially different administration schedules
Outcome limitation in claim 1	Requires less than 80 mL menstrual blood loss, at least 50% reduction, or both

The use of “about” creates numerical flexibility. The exact range would depend on claim construction, specification support, prosecution history, and the significance of formulation and measurement variability. A materially different strength could avoid literal infringement but could remain exposed under the doctrine of equivalents, subject to prosecution-history estoppel and other limitations.

The phrase “single dosage form” is also significant. A product requiring separate relugolix, estradiol, and norethindrone acetate tablets may present a stronger noninfringement position against claims requiring a single dosage form. That position would depend on the prescribing instructions, packaging, labeling, and whether the separate units are functionally directed to a combined regimen.

What outcomes are protected by dependent claims 2 through 21?

The dependent claims protect the treatment regimen when it produces specified clinical, hormonal, or structural results.

Clinical outcomes

Claims 2 and 11 protect treatment resulting in amenorrhea. Claims 7 and 16 cover reduced pelvic pain. Claims 6 and 15 cover reduction in the number or size of uterine fibroids. Claims 8 and 17 cover reduced uterine volume.

These claims may be difficult to enforce against a generic product based solely on the product’s composition. The relevant question would be whether the generic labeling directs use in a manner that causes or is intended to cause the claimed result.

Safety and tolerability outcomes

Claims 3, 12, 13, and 20 include:

• No vasomotor symptoms during treatment.
• Bone mineral density within plus or minus 3% of baseline.
• Combination results involving bone preservation, symptom control, amenorrhea, and fibroid reduction.

These limitations are narrower than the core regimen. They may be useful where clinical evidence establishes that the claimed treatment produces the result, but they also create proof issues. A patient-specific result may not occur in every treated patient. Enforcement would likely focus on whether the claim requires an inherent result of the regimen or an express treatment objective.

Hormonal and pharmacodynamic outcomes

Claims 5 and 14 require suppression of ovarian estrogen production demonstrated by prevention of ovulation. Claims 9 and 18 require a 2.1- to 4.1-fold reduction in median serum FSH concentration. Claims 10 and 18 require daily serum estradiol concentrations of 20 to 50 pg/mL between doses.

These claims are narrower and more technically demanding. They introduce testing methodology, baseline definitions, sampling timing, patient variability, and statistical interpretation. They may have value as fallback positions if broader regimen claims are invalidated or designed around.

How do claims 1 and 22 differ?

Claim 1 requires a treatment outcome based on menstrual blood loss:

• Less than 80 mL per cycle;
• At least a 50% reduction from baseline; or
• Both, under claim 21.

Claim 22 omits those express numerical endpoints and simply requires that the regimen treats heavy menstrual bleeding.

From an enforcement perspective, claim 22 may be the more important independent claim because it avoids the need to prove a particular blood-loss threshold. From a validity perspective, the absence of the numerical endpoint may also make claim 22 more vulnerable to prior-art arguments directed to the known use of the Myfembree regimen for fibroid-associated heavy menstrual bleeding.

What is the relationship between US Patent 11,957,684 and Myfembree?

Myfembree is the FDA-approved fixed-dose combination of relugolix, estradiol, and norethindrone acetate. The approved strengths correspond to the regimen recited in the patent claims: relugolix 40 mg, estradiol 1 mg, and norethindrone acetate 0.5 mg.

The FDA approved Myfembree in May 2021 for the management of heavy menstrual bleeding associated with uterine fibroids in premenopausal women. The FDA later approved an endometriosis indication in 2023. [2]

The patent claims align most closely with the fibroid indication. They do not, on their face, cover every use of Myfembree for endometriosis. A separate patent or regulatory exclusivity analysis is required for the endometriosis indication.

What is the patent type and likely exclusivity period?

US 11,957,684 is a utility patent with method-of-treatment claims. It is not a new chemical entity patent for relugolix and does not, based on the supplied claims, claim the active ingredients as a composition of matter.

Under the Patent Act, the ordinary patent term is generally 20 years from the earliest effective nonprovisional filing date, subject to patent-term adjustment, patent-term extension, terminal disclaimers, and other statutory modifications. [3] The grant date alone does not establish the expiration date.

The patent’s commercial exclusivity should therefore be analyzed through four separate dates:

Date category	Relevance
Earliest effective filing date	Determines the base 20-year term
Patent-term adjustment	Can extend the term for USPTO prosecution delays
Patent-term extension	May extend certain patents covering an approved product after regulatory review
Orange Book listing and use codes	Determines whether the patent can support a statutory notice-based challenge to an ANDA

A patent may be enforceable even if it is not listed in the Orange Book, but an unlisted patent generally does not generate the same Hatch-Waxman certification framework as a listed patent.

What is the Orange Book status of US 11,957,684?

The Orange Book question cannot be answered from the patent claims alone. FDA Orange Book listing is a separate regulatory record maintained by the FDA and generally identifies patents submitted by the NDA holder for an approved drug. Listed patents may include drug-substance, drug-product, and method-of-use patents. [4]

For a Myfembree generic applicant, the relevant issues would include:

• Whether US 11,957,684 is listed against Myfembree.
• Which FDA use code is associated with the patent.
• Whether the listed use code covers fibroid-associated heavy menstrual bleeding.
• Whether the patent is listed against the 2021 fibroid indication, the 2023 endometriosis indication, or both.
• Whether the patent is active on the proposed ANDA filing date.
• Whether any listed patent is subject to a statutory certification challenge.

A Paragraph IV certification would assert that a listed patent is invalid, unenforceable, or will not be infringed by the proposed generic product. A generic applicant could also use a section viii statement to carve out a patented method of use, if the remaining labeling does not encourage the patented use. [5]

What Paragraph IV challenges could arise?

A generic relugolix combination applicant could challenge the patent on several grounds.

Anticipation and obviousness

The core prior-art question is whether the claimed fixed-dose regimen and fibroid indication were disclosed or obvious before the relevant priority date. Relevant prior art could include:

• Earlier relugolix clinical studies.
• GnRH antagonist treatment of uterine fibroids.
• Relugolix monotherapy studies.
• Add-back therapy using estrogen and progestin.
• Clinical trial disclosures involving the 40/1/0.5 mg regimen.
• Earlier patent publications from the relugolix development program.

The strongest validity challenge would likely target claims 1 and 22 as predictable combinations of known components and a known indication. The patentee would rely on clinical performance, tolerability, bone-mineral-density preservation, bleeding control, and hormonal findings to establish unexpected results.

Written description and enablement

The claims cover treatment results across a population of premenopausal women with fibroids. A challenger could argue that the specification does not adequately support the full breadth of the claimed population or every result recited in the dependent claims.

Claims requiring serum estradiol, FSH, bone density, or ovulation outcomes may also raise questions about testing conditions and whether the specification teaches reliable achievement across the full claim scope.

Indefiniteness

Potential claim-construction disputes include:

• The meaning of “about” for each active ingredient.
• The scope of “single dosage form.”
• The meaning of “heavy menstrual bleeding.”
• The baseline and measurement methodology for menstrual blood loss.
• The meaning of “between daily doses.”
• The interpretation of “2.1- to 4.1-fold reduced.”
• Whether “treatment causes” requires intent, inherent result, or actual patient outcome.

These issues are particularly relevant to claims 9, 10, 18, and 19-20.

Which companies could challenge the patent?

The most likely challengers would be companies pursuing an ANDA for a generic relugolix, estradiol, and norethindrone acetate product. Potential participants in the broader generic women’s-health and hormonal-products market include Teva, Viatris, Sandoz, Lupin, Dr. Reddy’s Laboratories, Sun Pharmaceutical, and private-label or partnered ANDA applicants.

No company should be treated as an active challenger solely because it has a generic women’s-health business. Actual Paragraph IV activity must be confirmed through FDA patent certifications, litigation dockets, ANDA-related complaints, or settlement disclosures.

A biosimilar pathway is not relevant. Myfembree is a chemically synthesized small-molecule combination product, not a biologic. The competitive pathway is an ANDA, not a 351(k) biosimilar application.

What litigation and settlement risks apply?

A Paragraph IV notice concerning a listed patent can trigger patent litigation under 35 U.S.C. § 271(e)(2). If the NDA holder sues within the statutory period, FDA approval may be subject to a 30-month stay, subject to statutory exceptions and court rulings. [5]

Potential litigation theories would include:

Issue	Generic position	Patent-holder position
Single dosage form	Separate tablets or different packaging avoid the limitation	The regimen is functionally a single prescribed combination
“About” dosage	Proposed strength falls outside the claim	Commercial and therapeutic equivalence falls within “about”
Fibroid indication	Label carve-out avoids the use	Label, promotional materials, or prescribing instructions induce the use
Treatment outcome	No guarantee that every patient meets the endpoint	The result is inherent or expected from the regimen
Validity	Combination was obvious from prior art	Clinical benefits were unexpected and non-predictable
Patent listing	Patent is not properly listed or use code is overbroad	Listing accurately identifies an approved use

Settlement terms in pharmaceutical patent cases may include a delayed generic launch date, a license to enter before patent expiry, restrictions on labeling, or a supply arrangement. No settlement should be assumed without a publicly filed agreement, court order, Securities and Exchange Commission disclosure, or FTC-recorded document.

How strong is the patent estate for the relugolix combination?

US 11,957,684 is strategically meaningful but narrower than a composition-of-matter patent. Its strength depends on the surrounding patent family and the extent to which other patents cover:

• The relugolix active ingredient.
• The fixed-dose combination.
• Tablet formulation and release characteristics.
• Stabilization and manufacturing processes.
• Fibroid treatment.
• Endometriosis treatment.
• Long-term safety and bone-density preservation.
• Commercial packaging or delivery systems.

A layered estate is more difficult to design around than a single method patent. The principal weakness of the patent is that a generic applicant may attempt to avoid one or more claim limitations through a different dosage form, a different label, a different strength, or a carved-out indication.

What generic launch scenarios exist?

Scenario 1: Same fixed-dose tablet with Paragraph IV challenge

This is the highest litigation-risk scenario. The generic would likely challenge the listed patents and seek approval for the fibroid indication. Claims 1 and 22 would be central.

Scenario 2: Same active ingredients in separate dosage forms

This could avoid the “single dosage form” limitation, although the generic may face induced-infringement arguments if its labeling instructs simultaneous once-daily use of all three components.

Scenario 3: Section viii carve-out

A generic could attempt to omit the patented fibroid indication and retain only an unpatented indication. This approach is more viable if the remaining label does not encourage treatment of heavy menstrual bleeding associated with uterine fibroids.

Scenario 4: Alternative relugolix strength or add-back regimen

A different relugolix dose or different estrogen/progestin combination may avoid literal infringement, but the commercial product would no longer be therapeutically identical to Myfembree. The regulatory and market-access value of that design-around would be lower.

What manufacturing and geographic IP barriers exist?

The patent does not primarily protect a manufacturing process. It protects a therapeutic regimen. Manufacturing barriers would therefore arise from other patents, confidential know-how, supplier relationships, tablet formulation technology, analytical methods, and regulatory requirements.

US protection is territorially limited. A separate analysis is required for Europe, Japan, China, Canada, Australia, and other markets. Foreign family members may have different claim scope, prosecution histories, term dates, opposition outcomes, and regulatory-linkage rules.

A US patent does not block manufacture or sale in a foreign country unless corresponding rights exist there. Conversely, a foreign patent may create a market-specific barrier even after the US patent expires.

Key Takeaways

• US 11,957,684 is a method-of-treatment patent for the Myfembree-type regimen.
• The core regimen is relugolix 40 mg, estradiol 1 mg, and norethindrone acetate 0.5 mg in a single oral dosage form administered once daily.
• Claims 1 and 22 are the principal commercial claims.
• Claim 22 omits the specific menstrual-blood-loss thresholds and may be particularly important in enforcement.
• Dependent claims add amenorrhea, bone-density preservation, absence of vasomotor symptoms, ovulation suppression, fibroid reduction, pelvic-pain reduction, uterine-volume reduction, FSH reduction, and serum estradiol levels.
• The patent is not a relugolix composition-of-matter patent.
• Generic risk will depend heavily on Orange Book listing, FDA use codes, label design, dosage-form design, and the surrounding Myfembree patent family.
• Biosimilar competition is not applicable because Myfembree is a small-molecule combination product.
• The most credible generic strategies are Paragraph IV litigation, section viii labeling, separate dosage forms, or a materially different regimen.
• Exact patent expiry must be determined from the earliest effective filing date, patent-term adjustment, any terminal disclaimer, and any patent-term extension.

FAQs

Does US Patent 11,957,684 cover Myfembree itself?

It covers methods using the Myfembree active-ingredient combination for fibroid-associated heavy menstrual bleeding. It does not, based on the supplied claims, claim relugolix as a chemical compound or every composition containing relugolix.

Can a generic copy the 40 mg, 1 mg, and 0.5 mg strengths?

A generic may be able to copy the strengths only after resolving applicable patent and regulatory barriers. The combination of the strengths, single dosage form, once-daily schedule, and fibroid indication is central to the claimed method.

Does the patent cover relugolix treatment for endometriosis?

The supplied claims are directed to heavy menstrual bleeding associated with uterine fibroids. They do not expressly recite endometriosis treatment.

Can a generic avoid infringement by using separate tablets?

Separate tablets may avoid the “single dosage form” limitation, but infringement risk would depend on the actual prescribing instructions, labeling, packaging, and whether the combined regimen is encouraged.

Is a Paragraph IV challenge required if the patent is not in the Orange Book?

No. A Paragraph IV certification is tied to an Orange Book-listed patent. An unlisted patent may still be enforceable, but it generally does not create the same ANDA certification and 30-month-stay framework.

References

1. United States Patent and Trademark Office. (2024). U.S. Patent No. 11,957,684. https://patents.google.com/patent/US11957684B2/en
2. U.S. Food and Drug Administration. (2021). FDA approves Myfembree for treatment of heavy menstrual bleeding associated with uterine fibroids in premenopausal women. https://www.fda.gov/
3. 35 U.S.C. §§ 154, 156. Patent term and patent-term extension provisions. https://uscode.house.gov/
4. U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations, Orange Book. https://www.fda.gov/drugs/drug-approvals-and-databases/orange-book-data-files
5. 21 U.S.C. § 355 and 35 U.S.C. § 271(e). Abbreviated new drug applications and patent litigation provisions. https://uscode.house.gov/

Drugs Protected by US Patent 11,957,684

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Sumitomo Pharma Am	MYFEMBREE	estradiol; norethindrone acetate; relugolix	TABLET;ORAL	214846-001	May 26, 2021		RX	Yes	Yes	11,957,684					MANAGEMENT OF HEAVY MENSTRUAL BLEEDING ASSOCIATED WITH UTERINE LEIOMYOMAS (FIBROIDS) IN PREMENOPAUSAL WOMEN

International Family Members for US Patent 11,957,684

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	109759
Argentina	109762
Argentina	110636
Australia	2017334035
Australia	2017336338
Australia	2017336363
Australia	2022241582