Details for Patent: 10,449,191

Which drugs does patent 10,449,191 protect, and when does it expire?

Patent 10,449,191 protects ORGOVYX and is included in one NDA.

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

Summary for Patent: 10,449,191

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.
Assignee:	Takeda Pharmaceutical Co Ltd , Sumitomo Pharma Co Ltd
Application Number:	US16/369,729
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,449,191
Patent Claim Types: see list of patent claims	Use; Formulation;

United States Patent 10,449,191: Relugolix Prostate-Cancer Regimen, Claim Scope, Exclusivity and Patent Landscape

US Patent 10,449,191 protects specific relugolix dosing regimens for prostate cancer, including a 360 mg oral loading dose followed by 120 mg once-daily maintenance treatment. Its principal commercial relevance is the Orgovyx regimen marketed by Myovant Sciences and Pfizer. The patent does not broadly claim relugolix, all androgen-deprivation therapy, or every use of Orgovyx. Its strongest protection is directed to the dose sequence, prolonged maintenance period, hormone suppression, pharmacokinetic exposure, and treatment interruption intended to permit testosterone recovery.

The patent’s independent claims are claims 1, 16, and 17. Claim 1 is the broadest practical method claim because it covers treatment followed by suspension to permit testosterone recovery. Claims 16 and 17 focus on FSH control and a defined increase in relugolix exposure over time. The patent is therefore most relevant to generic products that copy the labeled 360 mg/120 mg regimen and to clinical protocols using treatment interruptions.

What drug and product does US Patent 10,449,191 cover?

The compound named in the claims is relugolix, a nonpeptide gonadotropin-releasing hormone receptor antagonist. Relugolix is marketed in the United States as Orgovyx for the treatment of advanced prostate cancer. The FDA-approved label specifies a 360 mg loading dose on the first day followed by 120 mg once daily thereafter.[1]

Item	Patent and product relevance
Active ingredient	Relugolix
Brand	Orgovyx
Drug class	Oral GnRH receptor antagonist
Indication	Advanced prostate cancer
Claimed loading dose	360 mg once daily
Claimed maintenance dose	120 mg once daily
Claimed treatment duration	At least 24 consecutive weeks for claims 1, 16 and 17
Claimed combination	Enzalutamide in claims 15 and 23
Patent	US 10,449,191
Primary protection	Regimen, hormone-response and PK method claims

The claims use the full chemical name of relugolix rather than the United States Adopted Name. The phrase “or a corresponding amount of a pharmaceutically acceptable salt thereof” expands the claims beyond a specific free-base presentation, subject to the claim’s other limitations.

What are the independent claims in US Patent 10,449,191?

Claims 1, 16, and 17 define three separate infringement pathways.

Claim 1: intermittent relugolix treatment and testosterone recovery

Claim 1 requires all of the following:

1. A subject with prostate cancer.
2. Once-daily administration of 360 mg relugolix for at least one day.
3. Once-daily administration of 120 mg relugolix for at least 24 consecutive weeks.
4. Suspension of the oral formulation.
5. The suspension must allow an increase in serum testosterone.

The claim does not require a particular testosterone threshold. Those thresholds appear in dependent claims 2 through 4. The claim also does not expressly require that treatment be restarted after the suspension period.

This distinction matters. A regimen that uses the 360 mg loading dose and 120 mg maintenance dose for 24 weeks but does not include a treatment suspension may fall outside claim 1, while potentially implicating claims 16 or 17 if the FSH or PK limitations are met.

Claim 16: prolonged treatment with controlled FSH

Claim 16 requires the 360 mg loading dose, the 120 mg maintenance dose for at least 24 weeks, and FSH of approximately 0.6 to 1.6 mIU/mL over 48 weeks of treatment.

The FSH limitation is a performance-based limitation. In a litigation setting, infringement would likely depend on clinical, pharmacodynamic, or patient-specific evidence showing that the claimed FSH range is achieved over the required period. A generic manufacturer could face difficulty avoiding the claim merely by changing labeling if ordinary use of the product produces the claimed FSH profile.

Claim 17: prolonged treatment and a defined exposure increase

Claim 17 requires:

• the 360 mg loading dose;
• the 120 mg maintenance dose for at least 24 consecutive weeks; and
• a pharmacokinetic profile in which mean plasma AUC(0-tau) increases at least 1.5-fold from the first day of treatment to the last day of the second treatment period.

Claims 18 and 19 narrow claim 17 to FSH suppression and the 0.6 to 1.6 mIU/mL FSH range. Claims 20 and 21 add profound castration and the timing of castration. Claim 22 adds a comparative clinical outcome against GnRH agonist therapy. Claim 23 adds enzalutamide.

How broad are the dependent claims?

The dependent claims divide into four technical groups.

Claims	Subject matter	Practical effect
2-4	Testosterone recovery thresholds and timing	Protect measured recovery after treatment suspension
5-7	Suspension after 24, 36 or 52 weeks	Protect defined treatment durations before interruption
8-13	Clinical reasons for interruption	Cover illness, procedures, radiation, injury, recovery and quality of life
14	Medical castration through week 48	Protects sustained testosterone suppression
15, 23	Enzalutamide combination	Covers relugolix treatment with androgen-receptor inhibition
18-19	FSH suppression	Narrows claims 17 and 18 to a defined hormonal range
20-22	Profound castration and comparative resistance outcome	Adds pharmacodynamic and clinical-performance requirements

Claims 8 through 13 are commercially unusual because they tie treatment suspension to patient circumstances. The claims cover suspension before, during, or after a surgical or invasive procedure, radiation therapy, injury, or intercurrent illness. Claim 13 also covers a need for improved quality of life and energy levels.

These claims may be harder to enforce against a product label that recommends continuous treatment. They could remain relevant, however, to physician-directed use, clinical protocols, or evidence showing that a manufacturer promoted treatment interruption for testosterone recovery.

What formulations are protected by US Patent 10,449,191?

The patent claims oral load-dose and oral maintenance-dose formulations containing specified amounts of relugolix. The claims do not appear, based on the supplied text, to require a particular tablet excipient system, tablet coating, dissolution profile, crystal form, particle-size distribution, or manufacturing process.

The formulation limitations are therefore functional and dosage-based rather than formulation-technology claims. The relevant requirements are:

• oral administration;
• a 360 mg load dose;
• a 120 mg maintenance dose;
• once-daily administration;
• use of relugolix or a pharmaceutically acceptable salt.

A product containing 360 mg on day one and 120 mg daily thereafter would satisfy the dose limitations if the remaining claim elements are present. A different tablet strength could still infringe if the administered amount is equivalent to the claimed dose.

The patent does not, from the supplied claims, independently protect:

• a specific tablet composition;
• a particular excipient;
• a specific solid-state form;
• a manufacturing process;
• a long-acting injectable formulation;
• a transdermal or implantable delivery system.

Those subjects would ordinarily be evaluated under separate composition, formulation, solid-state, process, or device patents.

When does US Patent 10,449,191 expire?

The relevant patent term is generally calculated from the earliest effective US nonprovisional or international filing date, subject to patent-term adjustment, terminal disclaimers, and other statutory limitations. A reliable expiration-date determination requires the patent’s bibliographic record, priority chain, PTA calculation, and any terminal-disclaimer information.

The claims supplied by the user do not include those data. Accordingly, the patent’s legally operative expiration date cannot be determined from the claims alone.

The principal commercial exclusivity periods are separate from patent expiration:

Exclusivity category	Relevance
New chemical entity exclusivity	Orgovyx received FDA approval in December 2020; the NCE period generally runs five years from approval, subject to statutory rules
Orphan-drug exclusivity	Orgovyx was approved for advanced prostate cancer, but the applicable orphan designation and exclusivity scope must be assessed separately
Patent exclusivity	Depends on the US patent family, PTA, listed patents and enforceability
Regulatory exclusivity	Does not automatically prevent all abbreviated applications once statutory conditions are met
Formulation or method patents	May extend commercial protection beyond a basic compound patent

What is the Orange Book status of US Patent 10,449,191?

US Patent 10,449,191 is associated with the Orgovyx patent estate and is relevant to FDA-listed patent protection for relugolix tablets. Orange Book listing is significant because an ANDA applicant must address listed patents through a Paragraph I, II, III or IV certification, depending on patent status and the applicant’s proposed launch timing.[2]

For this patent, the central regulatory issue is whether the approved Orgovyx labeling and the proposed generic labeling would create a direct overlap with the patented 360 mg/120 mg regimen. A Paragraph IV certification would assert that the patent is invalid, unenforceable, or not infringed. If the patent holder files a timely infringement action, the FDA may apply the statutory 30-month stay to approval, subject to litigation outcomes and statutory exceptions.

A generic applicant could attempt a narrower certification position if its proposed labeling omits the patented method, but the analysis would depend on:

• whether the 360 mg loading dose remains in the label;
• whether 120 mg daily maintenance is included;
• whether treatment interruption or testosterone recovery is promoted;
• whether FSH or PK outcomes are claimed or described;
• whether the product is submitted under a full prescribing-information label or a permitted section viii carve-out.

A label that retains the standard Orgovyx regimen would present greater exposure than a label that omits treatment-interruption instructions, although omission of a use does not eliminate risk where the remaining labeled use practices necessarily practice the claims.

Which companies are challenging the relugolix patent estate?

The supplied material identifies no specific ANDA filer, Paragraph IV notice letter, district-court complaint, settlement, or final judgment. No particular challenger or settlement can be stated reliably from the claims alone.

The likely challenger class is an ANDA applicant seeking approval for generic relugolix tablets. Potential litigation would center on:

1. claim construction of “suspending administration”;
2. whether the approved regimen necessarily produces the claimed FSH or PK profile;
3. whether a generic label induces the claimed intermittent-use method;
4. written description and enablement for testosterone recovery and long-duration hormonal outcomes;
5. obviousness over prior relugolix dosing studies and GnRH-antagonist treatment;
6. anticipation by clinical protocols using a 360 mg loading dose and 120 mg maintenance dose.

Biosimilar litigation is not the relevant pathway. Relugolix is a small-molecule drug, so competitors would generally use the ANDA pathway rather than the biosimilar pathway under the Public Health Service Act.

How strong is the patent estate for relugolix?

US Patent 10,449,191 is strongest against a competitor that copies the complete labeled regimen and promotes treatment interruption or testosterone recovery. It is weaker against a competitor that avoids the patented clinical-use limitations through labeling or treatment design.

Risk factor	Assessment
Dose overlap	High if the competitor uses 360 mg followed by 120 mg
Oral route overlap	High for oral tablets
Duration overlap	High where treatment continues at least 24 weeks
Interruption overlap	Lower unless interruption is labeled or promoted
FSH limitation	Fact-intensive and potentially difficult to prove prospectively
PK limitation	Requires comparative exposure data
Enzalutamide combination	Relevant only when the combination is practiced
Compound coverage	Not supplied by these claims
Manufacturing coverage	Not supplied by these claims
Biosimilar risk	Not applicable
Design-around potential	Moderate for labeling and regimen design, lower for the standard commercial regimen

The patent’s claim breadth is narrower than a basic relugolix composition patent. Its commercial value comes from alignment with the approved Orgovyx dosing regimen and from additional claims directed to long-term pharmacodynamic outcomes.

What patent litigation issues are most likely?

Infringement

The most direct infringement theory would allege that a generic label instructs administration of 360 mg on the first day and 120 mg daily thereafter for at least 24 weeks. Claims 16 and 17 could be asserted even if the generic label does not expressly mention treatment suspension, provided the required FSH or PK limitations are shown.

Induced infringement would require evidence that the generic applicant knowingly encouraged or directed the claimed use. FDA-required labeling, promotional materials, medical-information responses, and post-approval communications could become relevant.

Validity

The main validity challenges would likely involve obviousness. The challenger could combine prior art disclosing:

• relugolix as a GnRH antagonist;
• a 360 mg loading dose;
• a 120 mg maintenance dose;
• sustained testosterone suppression;
• reversible testosterone recovery after discontinuation;
• use in prostate cancer.

The patent holder would likely rely on the claimed combination of dose, duration, FSH behavior, exposure increase, profound castration, and testosterone recovery.

Written description and enablement

Claims requiring recovery to specified testosterone thresholds within 30, 45, or 84 days may face scrutiny over whether the specification supports the full claimed patient population and treatment circumstances. Claims 8 through 13 also raise scope questions because they cover several clinical reasons for interruption.

What generic launch scenarios exist?

A generic relugolix applicant could face several launch scenarios.

Scenario 1: standard-label launch

The applicant retains the 360 mg loading dose and 120 mg maintenance dose. This creates the highest risk of a patent challenge because the label closely follows the commercial regimen.

Scenario 2: carved-out labeling

The applicant removes instructions concerning treatment interruption, testosterone recovery, quality of life, or specific clinical circumstances. This could reduce exposure to claim 1 and claims 2 through 13, but it may not avoid claims 16 and 17 if the remaining labeled regimen produces the claimed FSH and PK characteristics.

Scenario 3: delayed launch after patent expiration

The applicant accepts listed patent protection and seeks approval with a Paragraph III certification. This avoids Paragraph IV litigation but delays market entry until the relevant patent term ends.

Scenario 4: at-risk launch

The applicant launches after a favorable court ruling, settlement, or failure to obtain a preliminary injunction. Commercial exposure would depend on damages, injunctive relief, the number of asserted patents, and the scope of any settlement.

How does relugolix compare with GnRH agonist therapy?

The claims expressly compare relugolix with GnRH agonist therapy in claim 22, which requires a longer time to castration resistance in the relugolix-treated subject. The clinically important distinction is mechanism and testosterone kinetics.

Attribute	Relugolix	GnRH agonist therapy
Administration	Oral, once daily	Often injectable depot
Initial testosterone flare	Generally avoided by receptor antagonism	Common pharmacologic concern
Testosterone recovery	Relevant after treatment suspension	Depends on product and treatment duration
Reversibility	Central to claims 1-13	Product-specific
Adherence risk	Daily oral adherence required	Depot administration reduces daily adherence burden
Patent risk under this patent	High for 360/120 regimen	Generally outside direct product scope

The patent does not claim all clinical advantages of relugolix. It claims specific dosing and measured treatment outcomes.

What licensing and commercial issues affect the patent?

The commercial rights surrounding Orgovyx involve the relugolix product, regulatory approvals, patent rights and commercialization arrangements. The supplied claims do not identify a license agreement, assignment chain, co-development agreement, royalty obligation or settlement.

A business assessment should distinguish:

• ownership of US 10,449,191;
• exclusive commercialization rights;
• patent prosecution control;
• rights to sue generic applicants;
• royalty or milestone obligations;
• global rights outside the United States;
• rights to relugolix in other indications.

Patent ownership and marketing rights are not necessarily held by the same entity. The patent record and applicable SEC filings are the controlling sources for those questions.

Key Takeaways

• US 10,449,191 is a regimen patent directed to relugolix treatment for prostate cancer.
• The core regimen is 360 mg once daily as a loading dose followed by 120 mg once daily for at least 24 weeks.
• Claim 1 adds suspension of treatment to permit testosterone recovery.
• Claims 16 and 17 protect defined FSH and pharmacokinetic outcomes.
• Claims 15 and 23 cover use with enzalutamide.
• The patent does not, based on the supplied claims, broadly cover relugolix composition, tablet excipients, solid-state forms or manufacturing processes.
• The principal generic risk is a product using the standard Orgovyx regimen with labeling or conduct that supports the claimed clinical uses.
• Biosimilar competition is not the relevant pathway because relugolix is a small molecule.
• The legally operative expiration date, active Orange Book listing, Paragraph IV challenges, litigation status and settlements require the patent and FDA regulatory records, not the claim text alone.

Frequently Asked Questions

Does US Patent 10,449,191 cover all Orgovyx prescriptions?

No. It covers prescriptions that satisfy the specific claimed dose, duration, suspension, FSH or PK limitations. A continuous 360 mg/120 mg regimen without a treatment suspension may avoid claim 1 but could still implicate claims 16 or 17.

Can a generic avoid the patent by changing tablet strength?

Not necessarily. The claims focus on the administered amount of relugolix. Multiple tablets or a different tablet strength could still meet the 360 mg loading-dose and 120 mg maintenance-dose limitations.

Does the patent cover relugolix for indications other than prostate cancer?

The independent claims supplied here are directed to prostate cancer or hormone-dependent prostate cancer. They do not broadly claim every relugolix indication.

Is enzalutamide required for infringement?

No. Enzalutamide appears only in dependent claims 15 and 23. Claims 1, 16 and 17 do not require enzalutamide.

Does this patent protect the manufacturing process for Orgovyx?

No manufacturing limitation appears in the supplied claims. Process protection would require separate claims directed to synthesis, purification, crystallization, formulation manufacture or tablet production.

References

1. U.S. Food and Drug Administration. (2020). Orgovyx (relugolix) tablets: Prescribing information.
2. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations: Orange Book.
3. United States Patent and Trademark Office. (2019). U.S. Patent No. 10,449,191, treatment of prostate cancer with relugolix.
4. U.S. Food and Drug Administration. (2022). Abbreviated new drug application regulations and patent certifications.

Drugs Protected by US Patent 10,449,191

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	10,449,191					TREATMENT OF ADULT PATIENTS WITH ADVANCED PROSTATE CANCER

International Family Members for US Patent 10,449,191

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