Details for Patent: 10,071,066

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Which drugs does patent 10,071,066 protect, and when does it expire?

Patent 10,071,066 protects ORSERDU and is included in one NDA.

This patent has thirty-four patent family members in nineteen countries.

Summary for Patent: 10,071,066

Title:	Method of treating cancer using selective estrogen receptor modulators
Abstract:	Disclosed herein are methods of treating subjects suffering from estrogen receptor positive cancer of the brain by administering a selective estrogen receptor degrader (SERM). Also disclosed are methods of treating a cancer that is resistant to an estrogen receptor modulator by administering a SERM.
Inventor(s):	Suzanne E. Wardell, Erik R. Nelson, Donald P. McDonnell
Assignee:	Duke University
Application Number:	US15/214,187
Patent Claim Types: see list of patent claims	Use; Composition; Dosage form;

US Patent 10,071,066: Scope, Claims, Exclusivity and Patent Landscape for GDC-0927

US Patent 10,071,066 covers a method of treating estrogen receptor-positive breast cancer that is resistant to an estrogen receptor modulator by administering GDC-0927, also known as rintodestrant. The claims are method-of-treatment claims, not composition-of-matter claims. Their commercial value depends on whether GDC-0927 reaches approval and whether separate patents protect the compound, formulations, dosing regimens or combinations.

The patent does not cover every use of GDC-0927. The independent claim requires estrogen receptor-positive breast cancer, resistance to an estrogen receptor modulator and administration of the specified compound. The dependent claims narrow the population, prior therapy, dose, route and combination treatment.

What compound does US Patent 10,071,066 protect?

The claimed compound is:

(R)-6-{2-{ethyl[4-(2-ethylaminoethyl)benzyl]amino}-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol

This compound is associated with GDC-0927, an oral selective estrogen receptor degrader developed by Genentech and Roche for estrogen receptor-positive, HER2-negative breast cancer.

The patent does not claim the compound in isolation in the claims supplied. It claims administering a composition containing the compound to a defined cancer population.

What is the pharmacologic profile of GDC-0927?

GDC-0927 is a nonsteroidal estrogen receptor antagonist and degrader. Its intended mechanism is to bind estrogen receptors, inhibit estrogen signaling and promote estrogen receptor degradation. The development rationale was treatment of tumors that had become resistant to endocrine therapies such as tamoxifen, aromatase inhibitors or fulvestrant.

The compound is distinct from approved endocrine therapies including tamoxifen, fulvestrant, anastrozole, letrozole and exemestane. It is also distinct from newer oral SERDs such as elacestrant, which has a separate active ingredient and patent estate.

What does claim 1 of US Patent 10,071,066 cover?

Claim 1 requires all of the following elements:

Claim element	Scope
Disease	Estrogen receptor-positive breast cancer
Resistance status	Cancer is resistant to an estrogen receptor modulator
Treatment act	Administering a composition
Active compound	The specified R-enantiomeric tetrahydronaphthalene compound
Therapeutic context	Treatment of the resistant cancer

A potential infringement analysis would therefore ask whether a product or clinical protocol satisfies each element. A product containing the claimed compound would not fall within claim 1 merely because it treats breast cancer. The treated cancer must be estrogen receptor-positive and resistant to an estrogen receptor modulator.

The claim is narrower than a general claim to:

• treating any breast cancer;
• treating all estrogen receptor-positive cancer;
• using GDC-0927 as a first-line therapy;
• using any estrogen receptor degrader;
• using any compound with a related chemical structure; or
• treating endocrine-sensitive tumors without documented resistance.

The claim does not expressly require metastatic disease, HER2-negative status, postmenopausal status, a specific biomarker mutation or a particular line of therapy.

Does claim 1 require monotherapy?

No. Claim 1 requires administration of a composition comprising the claimed compound. It does not expressly exclude additional active ingredients. Claim 10 separately addresses combination treatment, but the existence of claim 10 does not necessarily mean that all combination use is outside claim 1.

Claim 10 narrows the treatment to administration of at least one additional agent selected from specified therapeutic classes. A combination therapy may therefore implicate both the broad method claim and the narrower combination claim.

How do claims 2 and 3 define endocrine resistance?

Claims 2 and 3 divide resistance into two categories:

• Claim 2 covers de novo resistance, meaning the cancer is resistant when treatment begins.
• Claim 3 covers acquired resistance, meaning resistance developed after prior exposure to an estrogen receptor modulator.

This distinction has practical importance. A clinical trial enrolling only patients whose tumors progressed during or after tamoxifen, fulvestrant or another endocrine therapy would more clearly implicate acquired-resistance claim 3. A trial enrolling patients whose tumors were resistant before exposure to the specified modulator would implicate claim 2.

The patent does not appear, from the supplied claims, to define a molecular test for resistance. The scope may therefore depend on clinical records, treatment history, tumor response and the construction of “resistant.”

Which estrogen receptor modulators are covered?

Claim 4 limits claim 1 to resistance against a selective estrogen receptor modulator. Claim 5 identifies four compounds:

Compound	Commercial or development context
Tamoxifen	Widely used SERM for breast cancer
Idoxifene	Investigational SERM
Raloxifene	SERM used primarily in osteoporosis and breast-cancer-risk reduction
ICI 182,780	Fulvestrant, generally classified as a selective estrogen receptor degrader

The inclusion of ICI 182,780 is legally notable. ICI 182,780 is the development code for fulvestrant, which is generally described as a selective estrogen receptor degrader rather than a conventional SERM. The claim language, however, expressly identifies it under the dependent claim. That express listing could support an argument that resistance to fulvestrant is within the intended scope of claim 5, subject to ordinary claim-construction principles.

The list is closed for claim 5. Resistance to an aromatase inhibitor such as anastrozole or letrozole is not expressly recited in that claim. Such resistance could still fall within claim 1 if an aromatase inhibitor is treated as an “estrogen receptor modulator” under the applicable construction, but that would present a more substantial interpretive issue than the expressly listed agents.

What dosing and administration methods are protected?

Claims 6 through 9 address treatment execution.

Claim	Limitation
6	Administration of an effective amount
7	Administration of a high dosage
8	High dosage of more than about 20 mg/kg
9	Oral, intravenous, intradermal, intramuscular or subcutaneous administration

Claim 8 is particularly narrow and potentially difficult to apply to human commercial dosing. A dose exceeding approximately 20 mg/kg is substantially higher than the milligram-per-kilogram dosing commonly used for many small-molecule oncology drugs. The claim may have been directed to preclinical dosing or a specific dose-ranging concept rather than the eventual clinical regimen.

The term “about” introduces an approximation issue. A court would likely assess the permitted variation based on the specification, technical context and prosecution history. The claim does not state whether the dose is calculated per administration, per day, per treatment cycle or by another dosing metric.

Claim 9 covers both systemic and parenteral administration. Oral administration is commercially important because GDC-0927 was developed as an oral endocrine therapy. Intravenous administration is also recited, even though the compound’s development profile centered on oral dosing.

What does claim 10 cover?

Claim 10 covers GDC-0927 administered with at least one additional agent from specified therapeutic classes:

• CDK4/6 inhibitors;
• antiestrogens;
• retinoic acid or retinoid X receptor ligands;
• antiprogestins;
• antiandrogens;
• vitamin D or a vitamin D metabolite;
• farnesyl transferase inhibitors;
• PPAR-alpha or PPAR-gamma agonists; or
• MAP kinase inhibitors.

The claim is technologically broad because it identifies pharmacologic classes rather than named products. Potential CDK4/6 inhibitor combinations could include palbociclib, ribociclib or abemaciclib, although the claim language supplied does not name them.

The claim also reaches combinations that were less commercially established in breast cancer, such as retinoid-receptor ligands, farnesyl transferase inhibitors and PPAR agonists. Those alternatives may have limited practical value unless supported by clinical development.

How strong is the patent estate for GDC-0927?

The supplied patent has moderate method-of-use value but does not, by itself, establish a strong core exclusivity position.

Strengths

1. The independent claim identifies a specific compound rather than a broad functional genus.
2. The claim targets endocrine-resistant estrogen receptor-positive breast cancer, a commercially relevant treatment population.
3. The dependent claims cover both de novo and acquired resistance.
4. The patent includes combination therapy with CDK4/6 inhibitors and other oncology agents.
5. The claim reaches multiple administration routes.

Weaknesses

1. The claims supplied do not claim the compound itself.
2. There is no express limitation to a biomarker-defined population.
3. “Resistant” may require factual proof and could create litigation over clinical interpretation.
4. The listed modulator category creates a classification issue for fulvestrant.
5. The high-dose claims may not track the eventual human regimen.
6. A competitor using a different active compound would not infringe these claims.
7. A competitor using GDC-0927 for endocrine-sensitive disease, absent the claimed resistance condition, may fall outside the literal scope.

The most important commercial question is whether separate composition-of-matter patents cover GDC-0927. A composition patent would generally provide broader protection against making, using, selling or importing the compound than this treatment patent. The supplied claims do not establish the priority date, expiration date or enforceability of any separate composition patent.

When does US Patent 10,071,066 lose exclusivity?

The patent issued on September 11, 2018. A reliable expiration date requires the patent’s earliest effective nonprovisional or international filing date, any patent-term adjustment, terminal disclaimer and possible patent-term extension.

The supplied claims alone do not establish those dates. The patent’s issuance date is not its expiration date. A patent that issued in 2018 may expire well after 2030 if its earliest effective filing date was in the early 2010s, but the exact date must be taken from the USPTO patent record and the relevant family prosecution history.

No FDA patent-term extension can be inferred from the patent claims. Any extension under 35 U.S.C. § 156 would require an approved product and a qualifying regulatory review period.

What is the FDA and Orange Book status?

GDC-0927 is not an FDA-approved drug based on the public development record. It therefore does not have an FDA-approved labeling record or a standard Orange Book listing.

The absence of approval has several consequences:

• no abbreviated new drug application can be filed against an approved GDC-0927 reference product;
• no conventional Orange Book Paragraph IV dispute currently operates against this patent;
• no FDA regulatory exclusivity period can be calculated from a new drug approval;
• no biosimilar pathway applies because GDC-0927 is a small molecule, not a biologic;
• commercial revenue from an approved GDC-0927 product is not established.

A future approval could create a new Orange Book listing strategy, but the listing would depend on whether the patent claims the active ingredient, formulation, approved method of use or another FDA-recognized patent category.

Are there Paragraph IV challenges or patent litigation?

No established Paragraph IV challenge can be inferred from the supplied claims. Paragraph IV litigation normally arises after an ANDA applicant challenges an Orange Book-listed patent for an approved reference drug. GDC-0927’s lack of an approved reference product means that a conventional ANDA-based Paragraph IV pathway is not presently the principal competitive risk.

The more relevant risks are:

• patent invalidity challenges if GDC-0927 is later commercialized;
• inter partes review or post-grant review of patentability;
• written-description or enablement attacks;
• claim-construction disputes over “resistant” and “estrogen receptor modulator”;
• freedom-to-operate disputes involving separate compound or formulation patents;
• licensing or development disputes involving Roche or Genentech rights.

No settlement agreement or active generic litigation is established by the supplied information.

How does GDC-0927 compare with competing oral SERDs?

Drug	Developer or commercial sponsor	Status	Distinctive patent risk
GDC-0927 / rintodestrant	Genentech/Roche	Clinical development program	Compound, method, formulation and combination families
Elacestrant	Radius Health, later Menarini	FDA approved in 2023	Approved-product Orange Book and method-of-use rights
Giredestrant	Roche/Genentech	Clinical development	Separate chemical and clinical-use patent estate
Camizestrant	AstraZeneca	Clinical development	Separate composition, formulation and regimen rights
Imlunestrant	Eli Lilly	Clinical development	Separate composition and method-of-use rights
Fulvestrant	AstraZeneca and authorized generic suppliers	FDA approved	Established injectable SERD market

GDC-0927’s patent position is narrower than a composition-of-matter monopoly if the supplied patent is considered in isolation. Its strongest strategic value would arise in combination with an unexpired compound patent and clinically relevant dosing or formulation patents.

What generic entry risks exist?

Generic entry risk is currently limited by the absence of an approved GDC-0927 reference product. If the drug is approved, generic risk would depend on:

1. the expiry of the compound patent;
2. any listed formulation or method-of-use patents;
3. the ability of an ANDA applicant to carve out patented indications;
4. patent-term adjustment or extension;
5. the commercial feasibility of demonstrating bioequivalence;
6. manufacturing complexity and impurity-control requirements.

A generic could potentially avoid a method-of-use claim by labeling treatment only for non-resistant disease, if the FDA-approved labeling and patent scope permitted an adequate carve-out. That strategy would be less effective against an unexpired composition patent.

What manufacturing and geographic barriers apply?

The claimed molecule is a single defined small molecule, so the patent does not create a biologics-style manufacturing barrier. Manufacturing risk would instead arise from:

• control of the R-enantiomer;
• stereochemical purity;
• process impurities;
• polymorph or salt selection;
• pharmaceutical formulation;
• analytical methods;
• protected synthetic intermediates or manufacturing processes.

The US patent provides territorial protection only in the United States. Related applications may have been filed in Europe, Japan, China and other jurisdictions, but geographic coverage cannot be assumed from US Patent 10,071,066. Foreign family members must be assessed separately for status, claim scope, opposition history and expiration.

Key Takeaways

• US Patent 10,071,066 is a method-of-treatment patent for GDC-0927 in estrogen receptor-positive breast cancer resistant to an estrogen receptor modulator.
• Claim 1 requires the specified compound, ER-positive disease and resistance to an estrogen receptor modulator.
• Claims 2 and 3 cover de novo and acquired resistance.
• Claim 5 expressly identifies tamoxifen, idoxifene, raloxifene and ICI 182,780.
• Claim 8 covers a high dose exceeding about 20 mg/kg.
• Claim 10 covers combinations with CDK4/6 inhibitors and several other drug classes.
• The patent does not, based on the supplied claims, establish composition-of-matter protection for GDC-0927.
• GDC-0927 has no established FDA approval or Orange Book listing.
• No conventional Paragraph IV or biosimilar pathway applies to the development-stage compound.
• The commercial strength of this patent depends on separate compound, formulation, process and regulatory-rights patents.
• The exact expiration date cannot be determined from the claims alone.

FAQs About US Patent 10,071,066 and GDC-0927

Is US Patent 10,071,066 a composition patent?

No. The supplied claims are method-of-treatment claims. They require administering a composition containing the specified GDC-0927 compound for resistant estrogen receptor-positive breast cancer.

Does the patent cover treatment with elacestrant?

No. Elacestrant is a different active ingredient. The claims identify a specific GDC-0927 structure and do not cover unrelated oral SERDs.

Does resistance to an aromatase inhibitor automatically satisfy the patent?

Not necessarily. The claims expressly focus on resistance to an estrogen receptor modulator and identify specific SERMs in dependent claim 5. Aromatase-inhibitor resistance would require analysis of the claim language, specification and prosecution history.

Can a CDK4/6 inhibitor combination infringe claim 10?

Yes, if the regimen uses the claimed GDC-0927 compound, treats the claimed resistant ER-positive breast cancer population and includes a qualifying CDK4/6 inhibitor.

Does the patent create a biosimilar barrier?

No. GDC-0927 is a small-molecule drug, so biosimilar approval under the Biologics Price Competition and Innovation Act is not the applicable pathway.

References

1. United States Patent No. 10,071,066. (2018). Methods of treating estrogen receptor positive breast cancer. United States Patent and Trademark Office.

2. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations. FDA Orange Book.

3. U.S. Food and Drug Administration. (n.d.). Purple Book: Database of licensed biological products. FDA.

4. ClinicalTrials.gov. (n.d.). Clinical studies evaluating GDC-0927 in estrogen receptor-positive breast cancer. U.S. National Library of Medicine.

5. Genentech, Inc. (n.d.). GDC-0927 clinical development information. Roche Group.

Drugs Protected by US Patent 10,071,066

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Stemline Therap	ORSERDU	elacestrant hydrochloride	TABLET;ORAL	217639-001	Jan 27, 2023		RX	Yes	No						TREATMENT OF AN ER-POSITIVE BREAST CANCER FOLLOWING AT LEAST ONE LINE OF ENDOCRINE THERAPY
Stemline Therap	ORSERDU	elacestrant hydrochloride	TABLET;ORAL	217639-002	Jan 27, 2023		RX	Yes	Yes						TREATMENT OF AN ER-POSITIVE BREAST CANCER FOLLOWING AT LEAST ONE LINE OF ENDOCRINE THERAPY

International Family Members for US Patent 10,071,066

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	3122426		CA 2024 00007	Denmark
European Patent Office	3122426		2024C/505	Belgium
European Patent Office	3122426		301263	Netherlands
European Patent Office	3122426		LUC00331	Luxembourg
European Patent Office	3122426		PA2024504	Lithuania
European Patent Office	3122426		122024000013	Germany
European Patent Office	3122426		3/2024	Austria