US Patent 9,198,925: Dapagliflozin Propylene Glycol Hydrate Claims, Scope, and Patent Landscape

US Patent 9,198,925 protects specified methods of using dapagliflozin propylene glycol hydrate in solid oral formulations. The independent claims cover treatment or prevention of diabetes and a broad set of metabolic complications, with or without specified combination therapies. The practical enforcement value is concentrated in the formulation requirement, the hydrate form, dosage and composition ranges, and combination use with metformin, saxagliptin, and other antidiabetic agents.

The patent issued on December 1, 2015, to Bristol-Myers Squibb Company. It is associated with the dapagliflozin/Farxiga patent estate and should be analyzed with formulation, crystalline-form, method-of-treatment, and combination-product patents rather than as a standalone compound patent. The patent is directed to a small-molecule drug, so biosimilar law is not relevant. Generic applicants face ordinary ANDA and Paragraph IV risks.

What does US Patent 9,198,925 protect?

The patent claims methods that require administration of a pharmaceutical formulation containing dapagliflozin propylene glycol hydrate. The claims do not cover every dapagliflozin product. They require a particular solid formulation and specified dosing parameters.

The core limitations are:

Claim limitation	Scope
Active ingredient	Dapagliflozin propylene glycol hydrate
Patient	Mammalian subject or patient in need of treatment
Formulation	Tablet, stock granulation, or capsule
Carrier	Pharmaceutically acceptable carrier
Daily dose	About 0.1 to about 750 mg per day
Administration frequency	One to four administrations per day
Drug loading	0.1% to 70% of the tablet, stock granulation, or capsule
Therapeutic use	Diabetes and numerous metabolic, vascular, renal, ocular, neurologic, lipid, obesity, and hypertension indications
Combination claims	Specified antidiabetic, lipid-lowering, antihypertensive, anti-obesity, and appetite-suppressant agents

A generic or competing product must satisfy every limitation of an asserted claim for literal infringement. A product that contains dapagliflozin but uses a different solid form, different formulation category, or a composition outside the stated concentration range may avoid literal infringement, subject to doctrine-of-equivalents analysis.

How broad are the independent claims?

Claims 1, 3, 5, and 7 are the principal independent claims.

Claim 1: broad monotherapy and metabolic-disease claim

Claim 1 covers treatment or delayed progression or onset of:

Type I and Type II diabetes
Impaired glucose tolerance
Insulin resistance
Nephropathy, retinopathy, neuropathy, and cataracts
Hyperglycemia and hyperinsulinemia
Hypercholesterolemia, dyslipidemia, hyperlipidemia, and hypertriglyceridemia
Elevated free fatty acids or glycerol
Obesity
Wound healing and tissue ischemia
Atherosclerosis and hypertension
Syndrome X, or metabolic syndrome

The claim is broad in disease coverage but narrow in formulation structure. It requires dapagliflozin propylene glycol hydrate in a tablet, stock granulation, or capsule, within the stated dose and drug-loading ranges.

The phrase "treating or delaying the progression or onset" expands the claim beyond treatment of established disease. A method directed to prevention or delay of Type II diabetes may fall within the claim if the other formulation and dosing limitations are met.

Claim 3: Type II diabetes limitation

Claim 3 narrows the disease indication to Type II diabetes while retaining the same formulation, dose, frequency, and drug-loading requirements.

This claim has potentially greater commercial relevance than claim 1 because dapagliflozin's principal market is Type II diabetes, including use as monotherapy or add-on therapy. Its narrower disease scope may make it easier to prove against a product marketed for Type II diabetes, but it may also be more vulnerable to validity arguments based on prior art directed specifically to Type II diabetes treatment.

Claims 5 and 7: combination-treatment claims

Claims 5 and 7 require dapagliflozin propylene glycol hydrate plus at least one additional agent from specified therapeutic categories.

The listed categories include:

Antidiabetic and antihyperglycemic agents
Hypolipidemic or lipid-lowering agents
Anti-obesity agents
Antihypertensive agents
Appetite suppressants

Claim 7 is directed specifically to Type II diabetes. These claims are commercially important for combination products and coadministration regimens, including dapagliflozin with metformin or saxagliptin.

What do claims 9 through 16 add?

Claims 9 through 16 narrow the combination claims.

Claim	Limitation
9	Combination agent is an antidiabetic agent
10	Antidiabetic agent is selected from specified classes
11	Antidiabetic agent is a biguanide, GLP-1 agonist, or DPP-4 inhibitor
12	Antidiabetic agent is metformin
13	Antidiabetic agent is saxagliptin
14	Combination includes metformin and saxagliptin
15	Combination agent is an anti-obesity agent
16	Anti-obesity agent is phentermine

Claim 12 is particularly relevant to dapagliflozin/metformin products, including Xigduo XR-type commercial strategies. Claim 13 addresses dapagliflozin/saxagliptin combinations associated with Qtern. Claim 14 covers a triple combination of dapagliflozin, metformin, and saxagliptin.

The use of Markush language in claims 10 and 11 creates broad category coverage. A product containing a listed class member may fall within the claim even if the specific agent is not separately named, unless another claim limitation is absent.

What is the legal significance of the incomplete dependent claims?

Claims 2, 4, 6, and 8, as reproduced, end with the phrase "wherein the dapagliflozin propylene glycol hydrate is" and do not state the remaining limitation.

Those claims are incomplete in the supplied text and cannot be reliably construed from that text alone. The issued patent document, including the complete claim set and any certificates of correction, controls. The incomplete language should not be treated as a valid statement of the final scope of those dependent claims.

The independent claims remain analyzable from the supplied wording. Dependent-claim analysis for claims 2, 4, 6, and 8 requires the complete issued text.

What formulation characteristics are protected?

The formulation limitations create the main technical boundary of the patent.

Dapagliflozin propylene glycol hydrate

The claims require the hydrate form rather than generic dapagliflozin free form or an unspecified dapagliflozin solid. This limitation links the patent to the solid-state form used in commercial dapagliflozin development.

A generic applicant may therefore need to address:

Whether its product contains the claimed propylene glycol hydrate.
Whether the hydrate is present in the final dosage form.
Whether the product falls within the 0.1% to 70% drug-loading range.
Whether the dosage form is a tablet, stock granulation, or capsule.
Whether the proposed use meets a claimed therapeutic indication.

Tablet, stock granulation, or capsule

The claims do not expressly cover every dosage form. An oral solution, suspension, transdermal system, injectable formulation, or other non-listed dosage form would raise a substantial non-infringement issue under the literal claim language.

For commercial dapagliflozin products, tablets are the principal risk category. Stock granulation language is relevant to manufacturing intermediates and formulation processes in which the active ingredient is incorporated into a granulated blend before tableting or encapsulation.

0.1% to 70% drug loading

The concentration range is unusually broad. It covers low-loading formulations with substantial excipient content and high-loading formulations with relatively little excipient content.

The range may create substantial overlap with ordinary immediate-release and extended-release tablet formulations. A generic developer cannot assume that a conventional tablet avoids this limitation. The exact denominator, whether total tablet, granulation, or capsule contents, may become a claim-construction issue.

0.1 mg to 750 mg daily

The dose range is broader than commercial dapagliflozin dosing. Farxiga is generally marketed at 5 mg and 10 mg strengths, while combination products use comparable dapagliflozin doses. Those commercial doses fall within the claimed range.

The broad upper limit helps cover development-stage and off-label dosing but does not by itself establish infringement. The formulation and indication limitations must also be met.

How does US Patent 9,198,925 compare with dapagliflozin compound patents?

US Patent 9,198,925 is not the foundational dapagliflozin compound patent. It is a later formulation and method-of-use patent.

Patent category	Typical subject matter	Commercial effect
Compound patents	Dapagliflozin chemical structure and analogues	Broadest molecule-level protection
Solid-state patents	Dapagliflozin hydrates, solvates, and crystalline forms	Protect the form used in manufacturing or products
Formulation patents	Tablets, granulations, capsules, excipients, and drug loading	Protect finished dosage forms
Method-of-use patents	Diabetes and metabolic indications	Affect label and use-based infringement
Combination patents	Dapagliflozin with metformin, saxagliptin, or other agents	Affect combination products and coadministration
Manufacturing patents	Preparation, crystallization, purification, and conversion processes	May block alternative manufacturing routes

Key US patents commonly associated with the Farxiga/dapagliflozin estate include:

US patent	General subject
6,414,126	Dapagliflozin-related chemical compounds
7,919,598	Dapagliflozin formulation and related protection
8,513,202	Dapagliflozin product or formulation protection
8,889,159	Dapagliflozin-related formulation or use protection
9,198,925	Methods using dapagliflozin propylene glycol hydrate
9,486,453	Additional dapagliflozin protection
10,092,541	Later-listed dapagliflozin protection

The precise enforceability of each patent depends on claim amendments, terminal disclaimers, patent-term adjustment, Orange Book listing status, and any post-issuance proceedings.

When does US Patent 9,198,925 lose exclusivity?

The patent issued in 2015 from a continuation-era dapagliflozin application. Its effective expiration should be determined from the USPTO patent-term record and any terminal disclaimer. Public drug-patent listings commonly associate the patent with the late-2020s Farxiga patent expiry window, including an October 2028 date for related listed protection.

The relevant commercial dates are:

Event	Date or period
Patent issue	December 1, 2015
Farxiga FDA approval	January 8, 2014
Five-year NCE exclusivity	Expired in January 2019
Core dapagliflozin compound exclusivity	Expired before or around the early 2020s, depending on applicable patent-term adjustments
Later formulation and method patents	Extend protection into the late 2020s
Patent 9,198,925 commercial significance	Primarily tied to the remaining listed formulation and method claims

Patent expiration and regulatory exclusivity are separate. FDA NCE exclusivity prevented submission of certain ANDAs during the five-year period, but later patent claims can continue to block approval or launch.

What is the Orange Book status of dapagliflozin products?

The FDA Orange Book has listed patents for Farxiga and related dapagliflozin products. Orange Book listings can include patents covering the active ingredient, formulation, method of use, or product-specific combinations.

For a generic applicant, the practical question is not whether dapagliflozin's compound patent has expired. It is whether any listed patent covers the proposed product or the use described in the ANDA.

The principal products affected include:

Farxiga, dapagliflozin tablets
Xigduo XR, dapagliflozin and metformin extended-release tablets
Qtern, dapagliflozin and saxagliptin tablets
Other dapagliflozin-containing products approved in the United States

A patent may remain relevant to a combination product even if it does not cover dapagliflozin monotherapy. Claims 12 through 14 of US 9,198,925 are directed to combination use and are therefore more relevant to Xigduo XR and Qtern-type products than to a standalone dapagliflozin tablet.

What Paragraph IV challenges and litigation risks exist?

An ANDA applicant seeking approval before Orange Book patent expiration typically must address listed patents through one of four certifications:

Paragraph I: no patent information is listed.
Paragraph II: the patent has expired.
Paragraph III: approval is sought after patent expiration.
Paragraph IV: the patent is invalid, unenforceable, or will not be infringed.

For US 9,198,925, a Paragraph IV strategy could challenge:

Patent eligibility and written-description support for the broad disease list.
Obviousness based on known dapagliflozin formulations, hydrates, dosage ranges, and diabetes uses.
Enablement across the broad 0.1 mg to 750 mg dose range and many disease indications.
Anticipation by prior dapagliflozin treatment and formulation disclosures.
The scope and support for combination claims involving metformin and saxagliptin.
Whether a proposed product contains the claimed propylene glycol hydrate.
Whether a proposed label induces use for a patented indication.

A generic applicant may also use a section viii skinny-label strategy where the FDA-approved label permits omission of patented methods of use. That strategy is less useful where the formulation itself is protected or where the generic product label necessarily promotes the patented method.

Patent litigation involving dapagliflozin has included challenges by generic manufacturers to AstraZeneca and Bristol-Myers Squibb patent rights. The outcome for any particular applicant depends on the asserted patent, the ANDA product, the proposed label, settlement terms, and the court's construction of the formulation and method limitations.

Are biosimilar risks relevant to dapagliflozin?

No. Dapagliflozin is a chemically synthesized small molecule, not a biologic. Competitors file ANDAs, not abbreviated biologics license applications. The relevant competitive tools are:

Paragraph IV certification
Paragraph III certification
Section viii statement
Declaratory judgment actions
Formulation design-around
Alternative solid form or manufacturing route
Authorized-generic or settlement arrangements

Biosimilar interchangeability, the Biologics Price Competition and Innovation Act, and reference-product biologic exclusivity do not apply.

Which companies compete in the dapagliflozin patent landscape?

AstraZeneca is the principal commercial sponsor of Farxiga and has been responsible for the US commercial franchise. Bristol-Myers Squibb participated in the original dapagliflozin development and is identified in historical patent records.

The competitive landscape includes:

Company or group	Product or role
AstraZeneca	Farxiga; key patent and regulatory sponsor
Bristol-Myers Squibb	Original development and historical patent holder
Generic manufacturers	ANDA applicants challenging listed patents
Combination-product competitors	Products containing dapagliflozin with metformin or saxagliptin
Other SGLT2 manufacturers	Jardiance, Invokana, and related competitive products

Dapagliflozin competes pharmacologically with empagliflozin, canagliflozin, and ertugliflozin. Those products have separate patent estates and do not generally create direct infringement risk under US 9,198,925 because the claims require dapagliflozin propylene glycol hydrate.

How strong is the patent estate for US 9,198,925?

The patent has moderate commercial strength but narrower technical scope than a compound patent.

Strengths

It covers the hydrate form used in solid oral products.
The dose range captures commercial dapagliflozin strengths.
The drug-loading range is broad.
The independent claims cover both monotherapy and combination therapy.
Claims 12 through 14 target commercially important metformin and saxagliptin combinations.
Tablet claims align with the dominant commercial dosage form.

Vulnerabilities

The claims rely on broad treatment language covering many diseases.
The formulation limitations may permit design-around strategies.
The dose and concentration ranges may face obviousness challenges.
The patent is later than the original dapagliflozin compound patents.
Claims 2, 4, 6, and 8 are incomplete in the supplied text.
A generic applicant may challenge whether its final product contains the claimed propylene glycol hydrate.
A narrow or skinny label may reduce method-of-use exposure.

The highest-risk products are tablets containing the claimed hydrate at ordinary dapagliflozin strengths and marketed for Type II diabetes, particularly products combined with metformin or saxagliptin.

What generic launch scenarios exist?

Early launch after Paragraph IV litigation

A generic applicant may launch before patent expiry if it obtains a favorable judgment, reaches a license, or enters a settlement permitting an agreed launch date. Commercial launch may also occur at risk, although that exposes the applicant to damages and injunctive relief.

Launch after patent expiration

This is the lowest-litigation-risk path. It may still be delayed by other listed patents, regulatory exclusivity, pediatric extensions, or product-specific patents.

Formulation design-around

A competitor may attempt to avoid the claims by using:

A different dapagliflozin solid form
A formulation outside the stated drug-loading range
A non-tablet dosage form
A product label that omits patented indications
A manufacturing process that does not produce the claimed hydrate

Each approach requires technical confirmation. A change in manufacturing process does not avoid infringement if the final dosage form still contains the claimed hydrate.

Key Takeaways

US Patent 9,198,925 is a method-of-treatment and formulation patent, not the foundational dapagliflozin compound patent.
The claims require dapagliflozin propylene glycol hydrate in a tablet, stock granulation, or capsule.
Commercial 5 mg and 10 mg dapagliflozin products fall within the claimed dose range.
Claims 12 through 14 create specific risk for dapagliflozin/metformin, dapagliflozin/saxagliptin, and triple-combination products.
The patent does not create biosimilar risk because dapagliflozin is a small molecule.
Generic challenges will likely focus on obviousness, claim construction, solid-form identity, formulation ranges, and label-based infringement.
The patent must be evaluated with the broader Farxiga Orange Book estate, including compound, formulation, solid-state, combination, and later method patents.
The supplied versions of claims 2, 4, 6, and 8 are incomplete and cannot support reliable dependent-claim analysis.

FAQs

Does US Patent 9,198,925 cover Farxiga 10 mg tablets?

Potentially, yes. A Farxiga tablet containing dapagliflozin propylene glycol hydrate at a concentration within 0.1% to 70% and used for a claimed indication would satisfy the principal formulation and dose limitations.

Does the patent cover dapagliflozin monotherapy?

Yes. Claims 1 and 3 cover treatment without requiring a second active pharmaceutical ingredient. Claims 5 and 7 require combination therapy.

Does metformin create additional patent risk for dapagliflozin generics?

Yes. Claim 12 specifically identifies metformin, while the broader combination claims cover antidiabetic agents and biguanides. A generic dapagliflozin/metformin product must assess both dapagliflozin and metformin combination patents.

Can a generic company avoid the patent by using dapagliflozin anhydrous?

Possibly, if the product does not contain dapagliflozin propylene glycol hydrate and no equivalent claim applies. The solid form must be established analytically in the finished product.

Is a skinny label sufficient to avoid US Patent 9,198,925?

Not necessarily. A skinny label may reduce method-of-use exposure, but it does not eliminate infringement risk if the patent covers the formulation itself or if the marketed label still encourages a patented use.

References

AstraZeneca Pharmaceuticals LP. (2014). Farxiga (dapagliflozin) prescribing information. U.S. Food and Drug Administration.
Bristol-Myers Squibb Company. (2015). Methods of treating diabetes with dapagliflozin propylene glycol hydrate, U.S. Patent No. 9,198,925. United States Patent and Trademark Office.
U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book. Center for Drug Evaluation and Research.
U.S. Food and Drug Administration. (2024). Drugs@FDA: FDA-approved drugs. Center for Drug Evaluation and Research.
U.S. Patent and Trademark Office. (2024). Patent term adjustment and patent term examination records. United States Department of Commerce.
U.S. Food and Drug Administration. (2014). FDA approves Farxiga to treat type 2 diabetes. Center for Drug Evaluation and Research.

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2139494	⤷ Start Trial	PA2020522	Lithuania	⤷ Start Trial
European Patent Office	2139494	⤷ Start Trial	CA 2020 00035	Denmark	⤷ Start Trial
European Patent Office	2139494	⤷ Start Trial	301054	Netherlands	⤷ Start Trial
European Patent Office	2139494	⤷ Start Trial	122020000043	Germany	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 9,198,925

Summary for Patent: 9,198,925