United States Patent 10,786,501: Relugolix Dosing Claims, Scope, Expiration, and Patent Landscape
U.S. Patent No. 10,786,501 protects a specific oral relugolix regimen for prostate cancer and hormone suppression: a 360 mg once-daily loading dose followed by 120 mg once-daily maintenance dosing for at least 24 weeks. The claims also require a sustained follicle-stimulating hormone, or FSH, level of approximately 2.4 mIU/mL or less. The patent does not claim relugolix itself, a general prostate-cancer treatment, or every relugolix dose. Its commercial value is tied to the FDA-approved Orgovyx regimen and the difficulty of designing a substitutive prostate-cancer product without practicing the claimed method.
What drug and treatment regimen does U.S. Patent 10,786,501 cover?
The patent covers relugolix, the active ingredient in Orgovyx. The chemical name recited in the claims is:
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.
The core regimen requires:
| Claim element |
Required limitation |
| Route |
Oral administration |
| Loading dose |
360 mg once daily |
| Loading period |
At least one day |
| Maintenance dose |
120 mg once daily |
| Maintenance period |
At least 24 consecutive weeks |
| Disease indication |
Prostate cancer or hormone-dependent prostate cancer |
| Biomarker |
FSH of approximately 2.4 mIU/mL or less after 24 weeks |
| Pharmacokinetic limitation in claim 6 |
Mean plasma AUC(0-tau) increases at least 1.5-fold from the first treatment day to the last day of the second treatment period |
| Optional combination |
Enzalutamide |
| Optional pharmacodynamic result |
Profound castration |
| Optional timing result |
Profound castration within 24 to 48 hours |
| Optional comparative result |
Longer time to castration resistance than GnRH agonist therapy |
Relugolix is a nonpeptide gonadotropin-releasing hormone, or GnRH, receptor antagonist. It suppresses luteinizing hormone and testosterone without the initial testosterone flare associated with GnRH agonists. FDA approved Orgovyx for the treatment of adults with advanced prostate cancer on December 18, 2020 (FDA, 2020).
How do claims 1 through 10 divide the patent scope?
Claims 1 and 6 are the independent claims
Claim 1 is a prostate-cancer treatment method. It requires the 360 mg loading dose, the 120 mg maintenance dose, the 24-week minimum maintenance period, and the FSH result.
Claim 6 is broader in disease framing but more demanding in pharmacokinetic detail. It covers suppression of one or more sex hormones in a subject with hormone-dependent prostate cancer. It requires:
- The same 360 mg loading dose;
- The same 120 mg maintenance dose;
- At least 24 consecutive weeks of maintenance treatment;
- FSH of approximately 2.4 mIU/mL or less; and
- A mean AUC(0-tau) increase of at least 1.5-fold between the initial and final treatment measurements.
The practical distinction is important. A product may satisfy claim 1 without satisfying claim 6 if the required AUC increase is not demonstrated. Conversely, claim 6 is not limited to the broader phrase “treating prostate cancer”; it is framed around suppression of sex hormones.
Claims 2 and 7 require profound castration
Claims 2 and 7 depend on claims 1 and 6, respectively. They require that profound castration be achieved. The phrase narrows the claims to a specified depth of androgen suppression, although the quoted claim text does not define an independent testosterone threshold.
Claims 3 and 8 require rapid and sustained castration
Claims 3 and 8 require profound castration within 24 to 48 hours after administration begins and maintenance through the end of treatment.
These claims are narrower than claims 1 and 6. A generic or follow-on product could face a different infringement position if it produces the same biochemical endpoint but does not achieve the claimed timing, although infringement would depend on the approved labeling, actual use, clinical evidence, and the court’s construction of the claim terms.
Claims 4 and 9 contain a comparative clinical limitation
Claims 4 and 9 require that time to castration resistance be longer than in a subject receiving GnRH agonist therapy.
This limitation raises proof issues. A patent owner would generally need to establish the relevant comparator, patient population, treatment duration, and clinical endpoint. The claim is not limited to a numerical extension, but the comparative result must be supported by evidence linked to the accused regimen.
Claims 5 and 10 cover use with enzalutamide
Claims 5 and 10 add administration of enzalutamide. These claims are narrower combination-treatment claims. They may have value against a relugolix product labeled for use with androgen-receptor pathway inhibitors, but they do not independently cover enzalutamide or a relugolix-enzalutamide composition.
What is the legal scope of U.S. Patent 10,786,501?
The patent is a method-of-use patent, not a compound patent. A potential infringer must practice the required steps with the claimed drug and dose sequence. The principal scope is therefore tied to labeled or foreseeable clinical use.
A literal infringement analysis would focus on whether the accused product or treatment protocol includes:
- 360 mg of relugolix once daily for at least one day;
- 120 mg of relugolix once daily for at least 24 weeks;
- Prostate-cancer or hormone-dependent prostate-cancer treatment;
- The claimed FSH result; and, for claim 6,
- The claimed 1.5-fold AUC increase.
The phrase “or a corresponding amount of a pharmaceutically acceptable salt thereof” extends the claims beyond a particular salt form. It prevents a design-around based solely on converting relugolix into a pharmaceutically acceptable salt, assuming the administered amount corresponds to the claimed active moiety.
The claims do not expressly require a particular tablet excipient, tablet strength, brand, manufacturing process, packaging configuration, or release profile. They also do not claim every possible maintenance dose or every use of relugolix in prostate cancer.
What formulations are protected by Patent 10,786,501?
The patent protects dosage forms that deliver the specified relugolix amounts in the claimed sequence. It does not, based on the quoted claims, require a particular formulation technology.
The practical formulation limitations are:
| Formulation issue |
Scope under the quoted claims |
| Oral tablet |
Covered if it delivers the claimed amount and is used as required |
| Oral capsule |
Potentially covered if it delivers the claimed amount |
| Immediate-release formulation |
Not expressly required |
| Extended-release formulation |
Not expressly excluded |
| 360 mg loading dose |
Required |
| 120 mg maintenance dose |
Required |
| Specific excipients |
Not required |
| Specific salt |
Not required, provided the corresponding active amount is used |
| Injectable formulation |
Outside the express oral-administration requirement |
| Different loading dose |
Potentially outside claims 1 and 6, subject to equivalents analysis |
| Different maintenance dose |
Potentially outside claims 1 and 6, subject to equivalents analysis |
Orgovyx is supplied as 120 mg tablets, with a recommended 360 mg loading dose on day one followed by 120 mg once daily. The commercial product therefore tracks the central dosing limitations of the patent (FDA, 2020).
When does U.S. Patent 10,786,501 expire?
The patent has a priority date associated with the relugolix clinical-development and dosing disclosures and has a nominal patent-term endpoint in the mid-2030s. Public patent and Orange Book records should be used to confirm the operative expiration date, including any patent-term adjustment or terminal disclaimer.
The principal commercial estimate is November 9, 2036, based on the relevant priority and international filing chronology. The exact enforceable endpoint should be taken from the USPTO patent record and the FDA Orange Book listing rather than inferred solely from the grant date (USPTO, 2020; FDA, 2025).
The patent was granted in 2020. Its expected expiration is materially later than FDA’s five-year new chemical entity exclusivity for Orgovyx, which ran from the December 2020 approval date through December 2025. Patent protection, rather than NCE exclusivity, is the primary long-term barrier for this regimen.
What is the FDA and Orange Book status of Orgovyx?
FDA approved Orgovyx, containing relugolix, for adults with advanced prostate cancer. The approved label specifies a 360 mg oral loading dose on the first day followed by 120 mg orally once daily (FDA, 2020).
The relevant regulatory protections are distinct:
| Protection |
Approximate status |
| FDA approval |
December 18, 2020 |
| NCE exclusivity |
Five years, ending in December 2025 |
| Patent 10,786,501 |
Method-of-use protection directed to the loading and maintenance regimen |
| Orange Book role |
Listed patent can support a Paragraph IV infringement action |
| Regulatory pathway for generics |
ANDA, subject to listed-patent certifications |
| Regulatory pathway for biosimilars |
Not applicable; relugolix is a small molecule |
The FDA Orange Book lists patents that the NDA holder identifies as covering the drug, its formulation, or approved methods of use. A generic applicant must address listed patents through a Paragraph I, II, III, or IV certification, or a section viii statement for a method-of-use patent where permitted (FDA, 2025).
What Paragraph IV risks apply to relugolix generics?
A generic applicant seeking approval before expiration of a listed patent may file a Paragraph IV certification alleging that the patent is invalid, unenforceable, or will not be infringed. The NDA holder may then file a patent-infringement action within 45 days, triggering a statutory stay of ANDA approval of up to 30 months under the Hatch-Waxman Act.
For Patent 10,786,501, likely dispute issues include:
- Whether the generic label induces the claimed 360 mg-to-120 mg regimen;
- Whether the FSH limitation is satisfied or inherent in the labeled use;
- Whether “about 2.4 mIU/mL” is definite and clinically reproducible;
- Whether the 24-week treatment requirement is met by the proposed labeling;
- Whether the 1.5-fold AUC requirement in claim 6 is present;
- Whether the patent claims are enabled across the full patient population;
- Whether the claims are obvious over earlier relugolix dose-ranging and GnRH-antagonist disclosures; and
- Whether the patent is enforceable in view of disclosure and inventorship issues.
A section viii statement could be relevant if a generic applicant seeks approval for indications or dosing instructions that do not correspond to the patented method. Its viability depends on whether the label can omit the patented use without encouraging the patented regimen.
Which companies are connected to the relugolix patent estate?
Myovant Sciences developed relugolix and commercialized Orgovyx in collaboration with Pfizer. Sumitomo Pharma acquired Myovant and became the corporate parent of the relugolix business. Pfizer has commercial rights in the United States under the collaboration arrangement.
| Entity |
Role |
| Myovant Sciences |
Original developer and patent holder associated with the relugolix program |
| Pfizer |
U.S. commercial collaborator for Orgovyx |
| Sumitomo Pharma |
Parent company following acquisition of Myovant |
| Generic companies |
Potential ANDA applicants and Paragraph IV challengers |
| FDA |
NDA approval and Orange Book authority |
| USPTO |
Patent examination, grant, and term records |
Ownership, assignment, and licensing rights can differ by patent and jurisdiction. A transaction review should examine the USPTO assignment database and the operative collaboration agreements rather than relying only on the product label.
How strong is the patent estate for relugolix?
The estate has several layers:
Compound protection
The core chemical patents protect relugolix and related GnRH-antagonist compounds. These patents are more difficult to avoid through dose changes because they cover the active molecule or chemical class.
Method-of-use protection
Patent 10,786,501 protects the clinically important prostate-cancer dosing sequence. Its commercial strength comes from alignment with the FDA-approved regimen.
Formulation protection
Separate patents may cover relugolix pharmaceutical compositions, tablet formulations, stability, or dosage forms. Those patents require claim-by-claim review because a generic may avoid a particular excipient or manufacturing limitation while still practicing the dosing patent.
Combination protection
The quoted claims include relugolix with enzalutamide. Separate combination or androgen-deprivation patents may cover other prostate-cancer treatment combinations.
Manufacturing and process protection
Process patents can create additional barriers if they cover a commercially efficient route, crystalline form, impurity profile, or scalable production method. Process protection is usually less direct than an approved-use patent because an ANDA applicant may use a noninfringing manufacturing route.
Overall, Patent 10,786,501 is strong against a product whose label copies Orgovyx’s approved regimen. It is weaker against a product with a genuinely different loading strategy, maintenance dose, indication carve-out, or clinical protocol, although the doctrine of equivalents and induced-infringement theories remain relevant.
What generic launch scenarios exist for Orgovyx?
| Scenario |
Commercial effect |
| No successful challenge |
Generic entry delayed until relevant patent expiry |
| Paragraph III certification |
ANDA approval deferred until patent expiration |
| Paragraph IV challenge defeated |
Approval remains blocked or delayed, depending on patent term and litigation outcome |
| Paragraph IV settlement |
Entry date depends on settlement terms |
| Section viii carve-out |
Potential approval for noncovered uses, subject to label and inducement risk |
| Noninfringing dose regimen |
Possible earlier entry if clinically and regulatorily acceptable |
| Patent invalidation |
Earlier generic launch, subject to other listed patents and exclusivity |
| Authorized generic |
Potential market entry controlled by the NDA holder or licensee |
The most commercially important challenge would target the 360 mg loading dose followed by 120 mg daily maintenance dosing because that sequence is central to the approved product and to claims 1 and 6.
How does Patent 10,786,501 compare with GnRH agonist protection?
GnRH agonists such as leuprolide use a different pharmacologic mechanism and often require depot injection. Patent 10,786,501 protects an oral GnRH-antagonist regimen with rapid hormone suppression and no initial testosterone flare characteristic of GnRH agonist treatment.
| Issue |
Relugolix under Patent 10,786,501 |
Typical GnRH agonist |
| Administration |
Oral, once daily |
Often injectable depot |
| Loading dose |
360 mg |
Product-specific |
| Maintenance dose |
120 mg daily |
Product-specific depot schedule |
| Mechanism |
GnRH receptor antagonism |
GnRH receptor agonism |
| Testosterone flare |
Generally avoided |
Can occur initially |
| Patent relevance |
Dose sequence and hormone endpoint |
Product-specific compound, formulation, and depot claims |
| Biosimilar pathway |
Not applicable |
Not generally applicable to small-molecule agonists |
| Generic pathway |
ANDA |
ANDA or other small-molecule pathway |
What litigation and settlement issues should investors monitor?
The principal monitoring points are:
- Orange Book changes for Orgovyx;
- New ANDA Paragraph IV notices;
- District-court complaints filed within the 45-day statutory period;
- Federal Circuit decisions involving relugolix patents;
- Patent-term adjustments or disclaimers;
- Patent assignments following corporate transactions;
- Settlements granting a licensed entry date;
- New FDA-approved indications or combination labels;
- Additional formulation or process patents; and
- U.S. sales exposure before and after NCE exclusivity expiration.
Publicly available patent records establish the patent and its claims. They do not, by themselves, establish the existence or terms of a confidential generic settlement. Settlement economics must be verified through court filings, SEC disclosures, or a redacted agreement.
Key Takeaways
- U.S. Patent 10,786,501 is a regimen patent for oral relugolix treatment.
- The core sequence is 360 mg once daily for at least one day, followed by 120 mg once daily for at least 24 weeks.
- Claims 1 and 6 require FSH of approximately 2.4 mIU/mL or less after 24 weeks.
- Claim 6 adds a 1.5-fold or greater increase in mean plasma AUC(0-tau).
- Dependent claims cover profound castration, rapid castration within 24 to 48 hours, longer time to castration resistance than GnRH agonist therapy, and combination use with enzalutamide.
- The patent does not claim relugolix itself or every relugolix formulation.
- Orgovyx’s FDA-approved regimen closely corresponds to the principal claims.
- The expected patent-term endpoint is in the mid-2030s, commonly identified as November 9, 2036, subject to the official USPTO term record.
- Generic entry will depend on the full Orange Book estate, Paragraph IV challenges, litigation outcomes, settlements, and any viable section viii carve-out.
- Relugolix is a small molecule, so biosimilar litigation is not the relevant pathway. The principal regulatory route is ANDA approval.
FAQs
Does Patent 10,786,501 cover a 120 mg relugolix tablet by itself?
No. The quoted claims require the complete loading-and-maintenance sequence. A 120 mg tablet used outside the claimed regimen may not practice the claims, although other patents may apply.
Can a generic avoid the patent by using a 240 mg loading dose?
Potentially, but the regulatory and infringement analysis would depend on the approved label, clinical equivalence, doctrine of equivalents, and other relugolix patents. The literal claims recite 360 mg, not 240 mg.
Does the patent cover prostate-cancer treatment with relugolix for less than 24 weeks?
Claims 1 and 6 expressly require maintenance treatment for 24 consecutive weeks or greater. Other claims or patents could have different duration limitations.
Is an FSH measurement required for every treated patient to infringe?
The claims recite an FSH result after 24 weeks. Whether infringement requires actual testing, an inherent pharmacodynamic result, or label-induced use would depend on claim construction and the factual record.
Does adding enzalutamide create a separate patent barrier?
Claims 5 and 10 create narrower relugolix-plus-enzalutamide method claims. Other patents may separately cover the combination, sequencing, prostate-cancer indication, or androgen-receptor pathway treatment.
References
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U.S. Food and Drug Administration. (2020). Orgovyx (relugolix) prescribing information. https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/214621s000lbl.pdf
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U.S. Patent and Trademark Office. (2020). U.S. Patent No. 10,786,501. https://patents.google.com/patent/US10786501
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U.S. Food and Drug Administration. (2025). Approved drug products with therapeutic equivalence evaluations: Orange Book. https://www.fda.gov/drugs/drug-approvals-and-databases/orange-book-data-files
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Congress of the United States. (1984). Drug Price Competition and Patent Term Restoration Act of 1984, 21 U.S.C. § 355(j).
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Myovant Sciences Ltd. (2020). Orgovyx collaboration and commercialization disclosures. Company SEC filings. https://www.sec.gov/edgar/browse/?CIK=1679082
