Details for Patent: 12,336,990

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Which drugs does patent 12,336,990 protect, and when does it expire?

Patent 12,336,990 protects ORGOVYX and is included in one NDA.

This patent has eighty-two patent family members in twenty-eight countries.

Summary for Patent: 12,336,990

Title:	Treatment of prostate cancer
Abstract:	Methods for treating prostate cancer, including advanced prostate cancer, in a subject in need thereof, include administering once-daily to the subject, at least 80 mg 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, or a corresponding amount of a pharmaceutically acceptable salt thereof. Another method includes: administering once-daily to the subject in need thereof, an oral load dose formulation having from 240 mg to 480 mg 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, or a corresponding amount of a pharmaceutically acceptable salt thereof, and thereafter administering once-daily to the subject, an oral maintenance dose formulation having 80 mg to 160 mg 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, or a corresponding amount of a pharmaceutically acceptable salt thereof.
Inventor(s):	Vijaykumar Reddy RAJASEKHAR, Brendan Mark JOHNSON, David B. MacLean, Lynn Seely, Paul N. MUDD, Jr., Hélène M. Faessel
Assignee:	Takeda Pharmaceutical Co Ltd , Sumitomo Pharma Co Ltd
Application Number:	US18/937,891
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 12,336,990
Patent Claim Types: see list of patent claims	Use;

US Patent 12,336,990: Relugolix Prostate-Cancer Treatment Claims, Scope, Expiration Risk, and Patent Landscape

US Patent 12,336,990 claims a specific oral relugolix treatment regimen for prostate cancer: a 360 mg loading dose followed approximately one day later by 120 mg once daily. The patent does not broadly claim relugolix, GnRH-antagonist therapy, or all prostate-cancer uses. Its principal protection is directed to the clinical dosing sequence and associated endocrine outcomes, including profound castration and suppression of FSH and LH.

The patent is strategically important because it covers the regimen used for ORGOVYX, the FDA-approved relugolix product marketed by Myovant Sciences and Sumitomo Pharma. The claims also address treatment interruption, testosterone recovery, treatment resumption, and reloading.

What drug and treatment regimen does US 12,336,990 protect?

The claimed active ingredient is relugolix, identified in the claims by its full chemical name:

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.

Relugolix is a nonpeptide, orally active gonadotropin-releasing hormone, or GnRH, receptor antagonist. ORGOVYX contains 120 mg relugolix tablets and is approved for the treatment of advanced prostate cancer.[1]

The core regimen requires:

Treatment step	Claimed requirement
Loading dose	360 mg orally
Timing of maintenance dose	Approximately one day after loading dose
Maintenance dose	120 mg orally
Frequency	Once daily
Disease	Prostate cancer
Patient	Subject in need of treatment

The claims therefore require more than administration of relugolix. A potentially infringing method must practice the specified 360 mg-to-120 mg sequence, or a dependent-claim variation of that sequence, in a prostate-cancer patient.

How broad are the independent claims in US 12,336,990?

The patent has four independent claim groups.

Claim 1: Dosing regimen and prostate-cancer treatment

Claim 1 is the principal regimen claim. It requires:

1. Oral administration of 360 mg relugolix.
2. Administration of 120 mg relugolix once daily.
3. The maintenance regimen beginning about one day after the loading dose.
4. Treatment of prostate cancer.

Claim 1 does not expressly require a particular testosterone concentration, FSH concentration, LH concentration, cancer stage, duration of therapy, or clinical response. Those requirements appear in dependent claims.

Its commercial relevance is high because the claimed sequence corresponds to the labeled ORGOVYX regimen. A generic applicant seeking approval for an identical relugolix product would face a method-of-use patent directed to the labeled dosing schedule, even if the generic applicant attempted to carve out certain treatment indications or endocrine endpoints.

Claim 15: FSH reduction

Claim 15 requires the same 360 mg loading dose and 120 mg daily regimen, but adds a result limitation:

• Serum FSH must be less than or equal to approximately 2.4 mIU/mL by approximately 24 consecutive weeks of treatment.

This claim is narrower than claim 1 because it requires a measurable hormonal outcome. It may be more difficult to establish in litigation if the accused product labeling does not expressly direct physicians to monitor or achieve the claimed FSH threshold. It may still be relevant if the claimed result is an inherent consequence of following the labeled regimen.

Claim 21: FSH and LH reduction

Claim 21 requires:

• FSH of no more than approximately 2.4 mIU/mL; and
• LH of no more than approximately 2.0 mIU/mL;

by approximately 24 consecutive weeks of treatment.

This claim adds a second biomarker limitation. It is narrower than claim 15 and requires proof of both laboratory outcomes.

Claim 25: Combined endocrine suppression and profound castration

Claim 25 requires the full regimen, the FSH and LH thresholds, and profound castration by approximately four consecutive weeks.

This is the narrowest independent claim. It combines dosing, treatment duration, two hormone thresholds, and a castration endpoint. The claim may have substantial evidentiary value in a clinical-use dispute, but its narrower scope creates more avenues for non-infringement and validity challenges.

What dependent claims cover treatment duration and endocrine outcomes?

The dependent claims create a layered protection strategy around the initial dose and subsequent maintenance period.

Claims	Protected subject matter
2	Profound castration
3	Profound castration within 24 to 48 hours after loading
4	Profound castration within approximately four weeks
5	Sustained profound castration through at least 24 weeks
6	Sustained profound castration through at least 36 weeks
7	Advanced prostate cancer
8-10	Suspension of 120 mg daily dosing, including suspensions of at least four or eight weeks
11	Testosterone return to baseline after suspension
12	Testosterone recovery to at least approximately 280 ng/dL
13	Resumption of 120 mg daily treatment after suspension
14	A new 360 mg loading dose approximately one day before resuming 120 mg daily treatment
16-19	FSH suppression by weeks 12, 4, 36, and 48
20	Advanced prostate cancer under the FSH claims
22-23	FSH suppression and duration under the FSH/LH claims
24	Advanced prostate cancer under the FSH/LH claims
26-30	Advanced disease, FSH duration, and sustained profound castration

Claims 8 through 14 are commercially distinctive. They attempt to cover an intermittent-treatment protocol rather than continuous daily use alone. The claims reach both the interruption period and the subsequent reinitiation protocol.

What is the strongest infringement theory under the patent?

The strongest literal infringement theory would involve a relugolix product prescribed according to the ORGOVYX regimen for prostate cancer:

• 360 mg on day one;
• 120 mg daily beginning about day two;
• treatment of advanced prostate cancer.

That fact pattern maps directly onto claim 1 and, where supported by clinical evidence, claims 2, 4, 5, 7, 15, 20, 21, 24, and 25.

Claims based on endocrine outcomes have a different litigation profile. A patentee would need to establish that the accused regimen produces, requires, or directs the claimed FSH, LH, testosterone, or castration results. A generic label that merely states the dose may create a stronger claim-1 theory than a claim-15, claim-21, or claim-25 theory.

Claims 8 through 14 require an actual treatment interruption or a label that directs interruption and resumption. A continuously administered generic product would not necessarily practice those claims.

Does the patent cover relugolix itself or the ORGOVYX formulation?

No. Based on the supplied claims, US 12,336,990 is a method-of-treatment patent.

It does not claim:

• The relugolix chemical structure as a composition of matter.
• A relugolix salt, polymorph, crystal form, or metabolite.
• A tablet formulation.
• Excipients or tablet manufacturing.
• Packaging or dosage-unit design.
• A manufacturing process for relugolix.
• All GnRH receptor antagonists.
• All prostate-cancer uses of relugolix.

Those subjects would normally be addressed in separate composition, formulation, process, or use patents.

The patent can still affect generic entry even though it does not claim the active ingredient. Under the Hatch-Waxman framework, an ANDA applicant may need to address listed method-of-use patents through a Paragraph IV certification or a section viii statement, depending on the patent listing and proposed label.[2]

What is the Orange Book status of US 12,336,990?

The FDA Orange Book is the controlling source for determining whether a patent is listed against the ORGOVYX NDA. Patent issuance alone does not establish Orange Book listing.

The relevant FDA regulatory facts are:

Item	Status
Product	ORGOVYX
Active ingredient	Relugolix
NDA	214621
Applicant	Myovant Sciences GmbH
FDA approval	December 18, 2020
Dosage form	Oral tablet
Approved indication	Advanced prostate cancer
Regulatory pathway	NDA under the Federal Food, Drug, and Cosmetic Act

A newly issued patent can be listed only if it satisfies FDA listing requirements and is submitted within the applicable statutory and regulatory time periods. If US 12,336,990 is listed, its practical impact will depend on the listed use code and whether an ANDA applicant’s proposed label overlaps the patented method.[3]

The patent should therefore be analyzed separately from:

1. FDA approval and exclusivity.
2. Orange Book patent listing.
3. Patent-term expiration.
4. Any litigation or settlement involving an ANDA applicant.

When does relugolix lose FDA exclusivity?

ORGOVYX received approval as a new chemical entity. New chemical entity exclusivity generally lasts five years from approval, subject to statutory exceptions for certain patent challenges.[2]

For ORGOVYX, the five-year NCE period runs from December 18, 2020, and would ordinarily reach December 18, 2025. NCE exclusivity does not prevent all forms of submission before that date, but it restricts FDA approval of an ANDA during the applicable exclusivity period.

Patent protection can extend beyond FDA exclusivity. The earliest composition-of-matter patent and later formulation or method patents may create separate barriers. A generic launch analysis must compare the proposed product and label against every relevant Orange Book-listed patent, not only US 12,336,990.

What patent landscape surrounds ORGOVYX and relugolix?

The relugolix estate is expected to include several patent categories:

Patent category	Commercial function	Relevance to US 12,336,990
Composition of matter	Protects relugolix itself	Separate and potentially earlier barrier
Pharmaceutical composition	Protects tablet composition or dosage form	Can block formulation substitution
Treatment method	Protects prostate-cancer dosing or endocrine effects	US 12,336,990 falls primarily here
Combination therapy	Covers relugolix with other anticancer agents	May affect expanded indications
Manufacturing process	Protects synthesis, intermediates, or purification	Can restrict alternative supply routes
Crystalline form or salt	Protects specific solid-state material	Relevant to API sourcing
Pediatric or supplemental use	Protects later-approved uses	Depends on FDA-approved labeling

The most important distinction is between an API patent and a regimen patent. A generic manufacturer may be able to make or source relugolix after composition patents expire, yet still face a method patent directed to the 360 mg loading dose and 120 mg maintenance dose.

Are there Paragraph IV challenges to US 12,336,990?

The supplied record does not establish a Paragraph IV certification, ANDA filing, district-court complaint, or settlement involving US 12,336,990.

A Paragraph IV challenge would typically assert that the patent is invalid, unenforceable, or not infringed. Likely challenge themes include:

• Obviousness of a 360 mg loading dose followed by 120 mg daily.
• Anticipation or obviousness based on earlier relugolix dosing studies.
• Written-description support for the specific FSH, LH, testosterone, and castration thresholds.
• Enablement of the claimed endocrine outcomes across the full patient population.
• Indefiniteness of terms such as “about one day,” “profound castration,” and “about four consecutive weeks.”
• Non-infringement based on a carved-out label or absence of claimed clinical instructions.
• Patent-term, listing, or Orange Book-use-code issues.

The dosing claims may be vulnerable to obviousness arguments if earlier clinical development materials disclosed the same loading and maintenance doses. The biomarker claims may present a stronger novelty position but can raise written-description and enablement questions, particularly where the claims define outcomes by threshold and treatment duration.

How strong is the patent estate for commercial purposes?

US 12,336,990 has meaningful commercial strength because claim 1 tracks the approved ORGOVYX dosing regimen. The patent’s value is highest if:

• It is Orange Book listed against NDA 214621.
• Its expiration date extends beyond NCE exclusivity.
• The FDA-approved generic label includes the same prostate-cancer indication and dosing sequence.
• No earlier patent blocks the same launch.
• The claims survive an obviousness challenge.

The estate is less secure for treatment-interruption claims because those claims depend on a physician actually suspending therapy and later resuming it. The endocrine-outcome claims are also narrower and may require clinical or pharmacodynamic evidence.

Relative claim strength

Claim group	Scope	Infringement practicality	Principal vulnerability
Claim 1	Core 360/120 regimen	High if label matches	Obviousness and label carve-out
Claims 2-7	Castration and advanced disease	Moderate to high	Proof of outcome and terminology
Claims 8-14	Treatment interruption and reload	Lower for routine continuous use	No direction to interrupt treatment
Claims 15-20	FSH suppression	Moderate	Biomarker proof and enablement
Claims 21-24	FSH and LH suppression	Moderate to low	Multiple laboratory limitations
Claims 25-30	Combined endocrine and castration outcomes	Narrow	Cumulative limitations and proof burden

What generic launch scenarios exist?

Scenario 1: Identical label with Paragraph IV challenge

An ANDA applicant seeking approval for the same relugolix indication and dosing regimen would likely need to address the listed method patents. If the applicant files a Paragraph IV certification and the patent holder sues within 45 days, a 30-month stay may delay approval under the Hatch-Waxman framework.[2]

Scenario 2: Section viii carve-out

A generic applicant may attempt to remove a patented method from its labeling. This strategy is more difficult for claim 1 if the patented regimen is the principal or only approved dosing schedule for the indication. It may be more feasible for claims directed to treatment interruption, FSH thresholds, LH thresholds, or testosterone recovery if those concepts are not necessary for the proposed label.

Scenario 3: Launch after patent expiry

The lowest-risk pathway is launch after all blocking Orange Book-listed patents expire or are invalidated. The relevant date is not necessarily the expiration date of US 12,336,990 alone. Composition, formulation, and other method patents must be assessed together.

Scenario 4: At-risk launch

A generic company could launch before final resolution of patent disputes. That would expose it to possible infringement litigation, damages, and an injunction. The commercial decision would depend on expected litigation duration, patent-term remaining, market size, and the strength of the Paragraph IV case.

What biosimilar risk applies to relugolix?

Biosimilar risk does not apply to ORGOVYX because relugolix is a chemically synthesized small molecule, not a biological product. Competitors would generally enter through the ANDA pathway rather than the abbreviated biosimilar pathway under the Public Health Service Act.

The relevant competitive threat is therefore generic relugolix, not a relugolix biosimilar.[4]

How does US 12,336,990 compare with competing prostate-cancer therapies?

Relugolix competes with injectable GnRH agonists and antagonists, including leuprolide and degarelix, as well as androgen-receptor pathway inhibitors used in advanced prostate cancer.

Product class	Administration	Hormonal mechanism	Relevance to this patent
Relugolix	Oral daily tablet	GnRH receptor antagonism	Directly covered by the claims
Leuprolide	Depot injection	GnRH agonism	Outside the chemical and dosing limitations
Degarelix	Injection	GnRH receptor antagonism	Outside the relugolix limitations
Androgen-receptor inhibitors	Oral	Blocks androgen signaling	Generally outside the claimed regimen

The patent does not prevent use of competing non-relugolix therapies. Its competitive effect is concentrated on generic substitution for ORGOVYX.

What are the key geographic and manufacturing barriers?

US 12,336,990 provides territorial protection only in the United States. Parallel patents may exist in Europe, Japan, China, Canada, and other markets, but this patent cannot be used directly to block conduct occurring solely outside the United States.

Manufacturing risk may arise from separate patents covering:

• Relugolix synthesis.
• Key intermediates.
• Purification.
• Solid-state forms.
• Tablet composition.
• Packaging or stability systems.

A non-infringing API route does not eliminate exposure under US 12,336,990 because the patent is directed to use of the drug in a specified regimen. Conversely, a method patent does not by itself block manufacture of relugolix for non-infringing uses.

What litigation and settlement issues should investors monitor?

The principal indicators are:

1. Orange Book listing against NDA 214621.
2. First ANDA filing and Paragraph IV certification.
3. A 45-day infringement complaint.
4. A potential 30-month stay.
5. Claim-construction rulings concerning “about one day” and “profound castration.”
6. Validity challenges based on prior clinical dosing disclosures.
7. Settlement terms governing the earliest generic launch date.
8. Any covenant restricting use of treatment-interruption or endocrine-outcome claims.
9. Patent-term adjustment or terminal-disclaimer issues.
10. FDA approval timing after exclusivity and patent disputes are resolved.

Settlement agreements can materially change launch timing even when a patent remains in force. The operative date may be earlier than patent expiration if the parties agree to a licensed entry date.

Key Takeaways

• US 12,336,990 is a relugolix method-of-treatment patent, not a broad composition-of-matter patent.
• Claim 1 covers the commercially important 360 mg oral loading dose followed about one day later by 120 mg once daily.
• Dependent claims cover profound castration, FSH and LH suppression, testosterone recovery, treatment interruption, treatment resumption, and reloading.
• The patent is most commercially significant if it is listed in the Orange Book for ORGOVYX and remains unexpired after NCE exclusivity ends.
• Generic relugolix, rather than biosimilar relugolix, is the relevant competitive threat.
• Claim 1 presents the strongest practical infringement risk for an identical generic label.
• Biomarker and treatment-interruption claims are narrower and carry greater proof and validity risks.
• A complete launch analysis must consider the entire ORGOVYX patent estate, FDA exclusivity, Orange Book listings, Paragraph IV filings, and any settlement terms.

FAQs

What is the active ingredient in US Patent 12,336,990?

The active ingredient is relugolix, the active pharmaceutical ingredient in ORGOVYX.

Does US 12,336,990 cover all relugolix treatments?

No. The supplied claims are limited to prostate-cancer treatment using a 360 mg loading dose followed approximately one day later by 120 mg once daily, together with specified dependent outcomes and treatment modifications.

Can a generic avoid US 12,336,990 by using 120 mg without a loading dose?

Potentially, but the answer depends on the approved label, other patents, clinical equivalence requirements, and whether the generic product can obtain approval without practicing the claimed loading-dose regimen.

Is “profound castration” the same as ordinary castration?

Not necessarily. The patent claims use the term as a clinical endpoint. Its precise meaning would depend on the specification, prosecution history, incorporated clinical definitions, and expert evidence.

Does this patent block relugolix manufacture outside the United States?

No. US 12,336,990 is territorial and is directed to treatment methods. Separate manufacturing, API, formulation, and foreign patents would determine other geographic risks.

References

1. U.S. Food and Drug Administration. (2020). ORGOVYX (relugolix) prescribing information. FDA.
2. Drug Price Competition and Patent Term Restoration Act, 21 U.S.C. § 355(j).
3. U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations. FDA.
4. Biologics Price Competition and Innovation Act, 42 U.S.C. § 262.

Drugs Protected by US Patent 12,336,990

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	ORGOVYX	relugolix	TABLET;ORAL	214621-001	Dec 18, 2020		RX	Yes	Yes						TREATMENT OF ADULT PATIENTS WITH ADVANCED PROSTATE CANCER

International Family Members for US Patent 12,336,990

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