United States Patent 8,058,280: Relugolix Claim Scope, Patent Expiration, Orange Book Status and Generic Risk
United States Patent No. 8,058,280 is a core composition-of-matter patent covering thienopyrimidine GnRH antagonists, including relugolix. Claim 12 expressly covers relugolix, while claims 1 and 8 provide broader genus and species protection. The patent was assigned to Takeda Pharmaceutical Company Limited and is associated with the relugolix products Orgovyx and Myfembree. Its ordinary U.S. patent term is expected to expire in 2026, subject to any applicable patent-term adjustment or extension. The patent does not claim a specific tablet formulation, a combination with estradiol or norethindrone acetate, or a therapeutic method of treating a named disease.
What drug does U.S. Patent 8,058,280 protect?
The patent protects a class of substituted thienopyrimidine derivatives that act as gonadotropin-releasing hormone antagonists. The commercially important compound is relugolix, the active ingredient in:
| Product |
Active ingredient or combination |
FDA indication |
Sponsor |
| Orgovyx |
Relugolix |
Advanced prostate cancer |
Myovant Sciences, now part of Sumitomo Pharma |
| Myfembree |
Relugolix, estradiol and norethindrone acetate |
Heavy menstrual bleeding associated with uterine fibroids; endometriosis-associated pain |
Pfizer and Sumitomo Pharma |
Relugolix is the compound identified in claim 12:
“N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxypyridin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea.”
FDA approved Orgovyx on December 22, 2020, and Myfembree on May 26, 2021. The products are small-molecule drugs, so future competition proceeds through the abbreviated new drug application, or ANDA, pathway rather than the biosimilar pathway (FDA, 2020; FDA, 2021).
What are the main claims of U.S. Patent 8,058,280?
The patent contains four commercially relevant protection layers: a broad chemical genus, narrower subgenera, specifically named compounds, and pharmaceutical-composition claims.
| Claim |
Claim type |
Commercial relevance |
| 1 |
Broad Markush compound claim |
Covers a large genus of substituted thienopyrimidine compounds and salts |
| 2 |
Narrower compound claim |
Restricts the R4 substituent |
| 3 |
Dependent compound claim |
Requires R1 to be methyl |
| 4 |
Dependent compound claim |
Requires R3 to be methyl |
| 5 |
Dependent compound claim |
Requires R4 to be C1-4 alkoxy |
| 6 |
Dependent compound claim |
Requires n to equal 2 |
| 7 |
Dependent compound claim |
Defines a narrower R3/R4/n combination |
| 8 |
Specific compound claim |
Covers two named compounds, including the relugolix chemical series |
| 9 |
Pharmaceutical composition |
Covers a compound of claim 1, or a salt, with a carrier, excipient or diluent |
| 10 |
Manufacturing method |
Covers mixing the claimed compound with a pharmaceutical carrier system |
| 11 |
Specific compound |
Covers the first named compound in claim 8 |
| 12 |
Specific compound |
Expressly covers relugolix |
How broad is claim 1?
Claim 1 covers compounds having a thieno[2,3-d]pyrimidine core with defined substituent classes:
- R1 is a C1-4 alkyl group.
- R2 is a substituted or unsubstituted five- to seven-membered nitrogen-containing heterocycle.
- R3 is a C1-4 alkyl group.
- R4 may be hydrogen, alkoxy, aryl, sulfonylamino, hydroxyl or a substituted nitrogen-containing heterocycle.
- n is an integer from 1 to 4.
- Pharmaceutically acceptable salts are included.
This is a classic Markush claim. Its literal scope may cover a substantial number of analogues, but infringement depends on whether each structural limitation is met. A compound outside the defined R1, R2, R3, R4 or n ranges would not literally infringe claim 1. Claims 3 through 7 narrow the genus and may provide fallback positions if the broadest claim is attacked.
Does claim 12 cover relugolix?
Yes. Claim 12 specifically recites relugolix, including its:
- 2,6-difluorobenzyl substituent;
- dimethylaminomethyl side chain;
- 6-methoxypyridin-3-yl substituent;
- tetrahydrothieno[2,3-d]pyrimidine-2,4-dione core;
- para-phenyl N-methoxyurea group.
Claim 12 is materially stronger against a generic relugolix product than claim 1 because it does not require a court to resolve the scope of the broader Markush formula. A product containing relugolix in the claimed chemical form would directly implicate claim 12 unless a valid non-infringement or invalidity defense applies.
What formulations are protected by Patent 8,058,280?
Claim 9 covers a pharmaceutical composition containing a claim 1 compound or salt with a pharmacologically acceptable carrier, excipient or diluent. This is a broad composition claim, not a detailed tablet-formulation claim.
The claim does not, on its face, require:
- A particular excipient;
- A specific dissolution profile;
- A specific tablet hardness;
- A defined particle-size distribution;
- A specific dosage strength;
- A particular coating;
- A fixed-dose combination with estradiol;
- A fixed-dose combination with norethindrone acetate.
Claim 10 covers manufacturing a pharmaceutical composition by mixing the compound or salt with a carrier, excipient or diluent. It is narrower in practical enforcement value than a composition-of-matter claim because an ANDA applicant could challenge whether its manufacturing process practices each step of the claim.
The most important protection remains claims 11 and 12, particularly claim 12’s direct coverage of relugolix. Formulation and process claims are secondary barriers unless the patent owner can establish that the generic product or manufacturing process falls within the specific claim language.
When does U.S. Patent 8,058,280 lose exclusivity?
The patent was filed on February 20, 2006, and issued on November 15, 2011. Its ordinary 20-year term is calculated from the relevant U.S. nonprovisional filing date, subject to patent-term adjustment and any patent-term extension under 35 U.S.C. § 156.
Public patent records identify an expected nominal expiration in February 2026 for U.S. Patent 8,058,280, before accounting for any applicable adjustment or extension (USPTO, 2024). The patent’s expiration should not be treated as the only potential barrier to generic entry because later patents may protect relugolix salts, formulations, combinations, dosing regimens or other product attributes.
| Milestone |
Date |
| U.S. filing |
February 20, 2006 |
| Patent issued |
November 15, 2011 |
| Orgovyx FDA approval |
December 22, 2020 |
| Myfembree FDA approval |
May 26, 2021 |
| Nominal patent expiration |
February 2026 |
The FDA’s five-year new chemical entity exclusivity for Orgovyx expired in December 2025. That regulatory exclusivity period is separate from patent protection. An ANDA could generally be filed before patent expiry, but commercial approval and launch would depend on the listed patents, certifications, litigation and any applicable 30-month stay.
What is the Orange Book status of Patent 8,058,280?
U.S. Patent 8,058,280 is associated with the Orange Book patent estate for relugolix products, including Orgovyx. Orange Book listing is product-specific. A patent’s listing for one approved product does not automatically establish listing for every product containing the same active ingredient.
For an ANDA applicant, the relevant certification would depend on whether the patent is listed against the reference product and whether the applicant’s proposed label or product is affected:
- Paragraph I: No patent information is listed.
- Paragraph II: The patent has expired.
- Paragraph III: The applicant will not market until patent expiration.
- Paragraph IV: The patent is invalid, unenforceable or will not be infringed.
- Section viii statement: The applicant seeks approval for a use not covered by a listed method-of-use patent.
Because Patent 8,058,280 is a composition patent covering relugolix, a generic applicant seeking approval for relugolix would face a Paragraph III or Paragraph IV issue rather than relying solely on a section viii carve-out. A carve-out is more useful for a listed method-of-use patent than for a composition patent.
The current Orange Book entry and listed expiration should be checked against the FDA’s active database because delistings, patent-term adjustments, court decisions and product-specific updates can change the practical entry analysis (FDA, 2024).
Which companies are challenging the relugolix patent estate?
The supplied patent and claim text do not establish a specific Paragraph IV filing, ANDA applicant, district-court complaint or settlement agreement. Patent 8,058,280 itself does not identify a challenger.
The relevant competitive group includes:
- Sumitomo Pharma and its affiliates, which commercialize Orgovyx.
- Pfizer and Sumitomo Pharma, which commercialize Myfembree.
- Potential ANDA applicants seeking approval for generic relugolix.
- Developers of alternative androgen-deprivation therapies, including GnRH antagonists and GnRH agonists.
A Paragraph IV challenge to claim 12 would likely focus on one or more of the following:
- Anticipation by an earlier reference disclosing relugolix;
- Obviousness based on prior GnRH antagonist chemistry;
- Lack of written description for the full Markush genus;
- Lack of enablement across the breadth of claim 1;
- Indefiniteness of structural or substituent language;
- Non-infringement based on a different salt, polymorph or chemical form.
A generic applicant may also challenge the patent’s Orange Book listing or argue that a later patent does not cover the ANDA product as submitted.
How strong is the patent estate for relugolix?
Patent 8,058,280 has high strategic value because it combines broad genus protection with an express relugolix species claim. The strongest claims are claims 11 and 12. Claim 12 is easier to analyze and enforce than claim 1 because the accused molecule can be compared directly with the recited structure.
| Protection layer |
Strength against a relugolix generic |
Principal vulnerability |
| Claim 1 Markush genus |
High if valid and enabled |
Written-description, enablement and obviousness challenges |
| Claim 8 specific compounds |
High |
Prior-art disclosure or structural distinction |
| Claim 9 composition |
Moderate |
Design-around using different product or process arguments |
| Claim 10 manufacturing method |
Moderate to low |
Difficulty proving the accused process practices every step |
| Claim 12 relugolix species |
Very high |
Anticipation, obviousness, validity or non-infringement defenses |
The patent is strongest as a molecule patent and weaker as a formulation or manufacturing patent. Its commercial effect depends on the later relugolix patent family, not on this patent alone.
Are biosimilar risks relevant to relugolix?
No. Relugolix is a chemically synthesized small molecule, not a biologic. A competing company would use the ANDA pathway for a generic version. The statutory biosimilar framework under the Public Health Service Act does not govern ordinary relugolix competition.
The principal risks are therefore:
- Paragraph IV litigation;
- Patent-term expiry;
- Orange Book listing disputes;
- Product-specific formulation patents;
- Salt, polymorph or manufacturing-process claims;
- Label differences and use carve-outs.
How does Patent 8,058,280 compare with later relugolix patents?
Patent 8,058,280 is best characterized as an early core-chemistry patent. Later patents may protect narrower commercial implementations, such as:
- Relugolix salts;
- Crystalline forms;
- Specific tablet compositions;
- Dose regimens;
- Combination products;
- Drug-drug interaction management;
- Methods for treating prostate cancer, uterine fibroids or endometriosis;
- Manufacturing processes and intermediates.
A generic applicant that avoids one later formulation or method patent may still infringe claim 12 if it makes, uses or sells relugolix itself before the composition patent expires. Conversely, after the expiration of claim 12, later patents may still delay approval or limit the initial label.
What generic launch scenarios exist?
Launch after patent expiration
This is the lowest-litigation scenario. An ANDA applicant waits until the relevant composition and later patent barriers expire, then launches subject to regulatory approval and any remaining exclusivity.
Paragraph IV launch
The applicant certifies that Patent 8,058,280 is invalid, unenforceable or not infringed. If the patent owner sues within the statutory period, FDA approval may be subject to a 30-month stay. The commercial launch date then depends on the litigation outcome, settlement terms and any court-imposed restrictions.
At-risk launch
An applicant launches before final resolution of the patent dispute. This exposes the applicant to damages, an injunction and possible enhanced damages if infringement is established.
Carved-out launch
This scenario is more relevant to method-of-use patents. It would be difficult to use a label carve-out to avoid a composition patent covering relugolix itself, although a carve-out may matter for later use-specific listings.
What patent litigation affects relugolix?
The supplied information identifies no litigation docket, judgment or settlement involving U.S. Patent 8,058,280. The patent’s litigation relevance should be assessed through three records:
- FDA Orange Book listings for Orgovyx and Myfembree.
- ANDA-related district-court complaints under 35 U.S.C. § 271(e)(2).
- Federal Circuit and district-court decisions involving relugolix composition, formulation or use patents.
A settlement may allow a generic applicant to launch on a negotiated date before the final patent expiration. Such agreements can also include restrictions tied to product strength, indication, manufacturing source or later patents. No settlement terms can be attributed to Patent 8,058,280 from the claim text alone.
Key Takeaways
- U.S. Patent 8,058,280 is a core relugolix composition patent.
- Claim 12 expressly covers relugolix.
- Claim 1 provides broad Markush protection for related thienopyrimidine GnRH antagonists.
- Claim 9 covers broad pharmaceutical compositions, but not a detailed commercial tablet formulation.
- Claim 10 covers a composition-manufacturing step and is less powerful than the molecule claims.
- The ordinary patent term is expected to reach February 2026, subject to any patent-term adjustment or extension.
- Orgovyx and Myfembree are small-molecule products and face generic, not biosimilar, competition.
- A generic relugolix applicant would likely need to address the patent through a Paragraph III or Paragraph IV certification.
- Later patents may extend practical market protection after Patent 8,058,280 expires.
- The strongest enforceable feature is the expressly recited relugolix species in claim 12.
FAQs
Does Patent 8,058,280 cover the active ingredient in Orgovyx?
Yes. Claim 12 expressly covers relugolix, the active ingredient in Orgovyx.
Does Patent 8,058,280 cover Myfembree as a combination product?
It covers the relugolix component, but the quoted claims do not expressly claim the combination of relugolix with estradiol and norethindrone acetate.
Can a generic company avoid claim 12 by using a relugolix salt?
Not necessarily. Claim 12 expressly includes “a salt thereof.” The specific salt, solid form and manufacturing route would require a separate infringement analysis.
Is claim 1 broader than claim 12?
Yes. Claim 1 covers a broad chemical genus. Claim 12 is limited to one specifically defined compound, relugolix.
Does patent expiration automatically permit generic launch?
No. Launch also depends on Orange Book-listed patents, FDA exclusivity, later relugolix patents, litigation, settlements and the scope of the approved generic label.
References
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U.S. Patent No. 8,058,280. (2011). Thienopyrimidine derivatives. United States Patent and Trademark Office.
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U.S. Food and Drug Administration. (2020). FDA approves new oral drug for advanced prostate cancer. https://www.fda.gov/
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U.S. Food and Drug Administration. (2021). FDA approves new treatment for uterine fibroids. https://www.fda.gov/
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U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book. https://www.fda.gov/
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United States Patent and Trademark Office. (2024). Patent term calculator and patent term adjustment information. https://www.uspto.gov/
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35 U.S.C. § 271(e)(2). (2024). Infringement of patents in the Hatch-Waxman context.
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21 U.S.C. § 355(j). (2024). Abbreviated new drug applications and patent certifications.
