Details for Patent: 10,258,637

Which drugs does patent 10,258,637 protect, and when does it expire?

Patent 10,258,637 protects SYNJARDY XR, TRIJARDY XR, GLYXAMBI, JARDIANCE, and SYNJARDY, and is included in five NDAs.

Protection for SYNJARDY XR has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has thirty-eight patent family members in twenty-five countries.

Summary for Patent: 10,258,637

Title:	Pharmaceutical composition, methods for treating and uses thereof
Abstract:	The present invention relates to certain SGLT-2 inhibitors for treating and/or preventing metabolic disorders, such as type 1 or type 2 diabetes mellitus or pre-diabetes, in patients with renal impairment or chronic kidney disease (CKD).
Inventor(s):	Uli Christian BROEDL, Sreeraj MACHA, Maximilian von EYNATTEN, Hans-Juergen Woerle
Assignee:	Boehringer Ingelheim International GmbH
Application Number:	US15/918,401
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,258,637
Patent Claim Types: see list of patent claims	Use; Delivery;

US Patent 10,258,637: Empagliflozin Renal-Function Dosing Claims, Exclusivity and Patent Landscape

US Patent 10,258,637 protects a narrow method of using empagliflozin in adults with type 2 diabetes and moderately reduced renal function. The central limitation is treatment when eGFR is at least 45 but below 60 mL/min/1.73 m², followed by discontinuation if eGFR falls below 45. The patent does not broadly protect empagliflozin, Jardiance tablets, SGLT2 inhibition, or all renal-impairment uses.

The patent issued April 16, 2019, to Boehringer Ingelheim International GmbH. Its claims cover four substantially overlapping treatment pathways and dose-specific dependent claims. The commercially relevant doses are 10 mg and 25 mg. The 5 mg and 12.5 mg claim limitations do not correspond to standard marketed Jardiance strengths when administered as standalone doses.

The patent’s practical value depends on three issues:

1. Whether the patent is listed for the relevant Jardiance indication in the FDA Orange Book.
2. Whether a generic label instructs physicians to treat the claimed eGFR population and discontinue below 45.
3. Whether the claims remain aligned with the current FDA label, which has changed as empagliflozin indications expanded into heart failure and chronic kidney disease.

What does US Patent 10,258,637 cover?

The patent covers methods of improving glycemic control or treating type 2 diabetes with empagliflozin under a specified renal-function protocol.

Core claim limitations

Limitation	Requirement
Active ingredient	Empagliflozin
Disease	Type 2 diabetes mellitus
Purpose	Improve glycemic control or treat type 2 diabetes
Renal-function entry range	eGFR ≥45 and <60 mL/min/1.73 m²
Administration	Oral
Claimed total daily doses	5 mg, 10 mg, 12.5 mg or 25 mg
Renal-function stopping rule	Discontinue if eGFR falls below 45
Optional combination	Metformin
Optional process step	Assess renal function before administration

The claims do not require a particular tablet formulation, excipient, salt, crystalline form, manufacturing process, dosing frequency or treatment duration.

Claim architecture

The 24 claims divide into four independent-claim families:

Independent claim	Principal scope	Dependent claims
Claim 1	Administer based on eGFR and discontinue below 45	Claims 2-6
Claim 7	Assess renal function, administer, then discontinue	Claims 8-12
Claim 13	Treat type 2 diabetes using the same renal thresholds	Claims 14-18
Claim 19	Assess renal function, treat, then discontinue	Claims 20-24

Claims 2-5, 8-11, 14-17 and 20-23 narrow the dose to one of four amounts. Claims 6, 12, 18 and 24 add metformin.

How broad are the claims in US Patent 10,258,637?

The claims are narrow in molecule, disease, renal-function range and treatment instruction. They are broad in formulation and administration details.

What the patent does not claim

US 10,258,637 does not claim:

• Empagliflozin as a chemical compound generally.
• All uses of Jardiance.
• Cardiovascular-risk reduction.
• Heart-failure treatment.
• Chronic-kidney-disease treatment independent of glycemic control.
• A fixed-dose empagliflozin/metformin product.
• A specific tablet, capsule, excipient or crystal form.
• A manufacturing process.
• Treatment at eGFR below 45.
• Treatment of type 1 diabetes.
• Use of an SGLT2 inhibitor other than empagliflozin.

A competing SGLT2 inhibitor such as dapagliflozin, canagliflozin or ertugliflozin would not literally satisfy the empagliflozin limitation. Those products may have separate renal-use patents, but they are not direct molecule-level substitutes for purposes of literal infringement.

How does the eGFR limitation affect infringement?

A method claim is infringed only when the accused conduct satisfies all material limitations. For this patent, the relevant patient must fall within the claimed entry range of eGFR ≥45 and <60. A label that covers only patients with eGFR of 60 or higher would not directly practice the core method.

The accused method also must include the below-45 discontinuation instruction. A generic label that recommends continued empagliflozin treatment below 45 could create a non-infringement argument, although the total label, prescribing information and induced-infringement evidence would control.

The claim language creates a meaningful design-around pathway:

• Do not include the claimed 45-to-less-than-60 renal subgroup in the label.
• Do not instruct discontinuation below 45.
• Limit the label to a different indication, such as heart failure or chronic kidney disease, if the claimed glycemic-control limitations are absent.
• Use a different active ingredient.

A physician’s off-label use can still create direct-use exposure, but generic-label litigation usually turns on whether the proposed label encourages the patented method.

When does US Patent 10,258,637 expire?

US Patent 10,258,637 issued on April 16, 2019. Its nominal patent term runs approximately into 2034 based on the family’s 2013 priority period, subject to the patent-specific term calculation, terminal disclaimers and any USPTO patent-term adjustment.

Event	Date or period
Earliest priority period	2013
US issue date	April 16, 2019
Nominal term endpoint	Approximately 2034
Patent-term adjustment	Must be confirmed from the USPTO patent record
Patent-term extension	No PTE is assumed for this method-of-use patent

The patent’s relevant exclusivity date is not necessarily the same as the expiration date of the original empagliflozin compound patent. A later-filed method patent can extend practical branded protection even after compound or formulation patents expire.

What is the Orange Book status of US Patent 10,258,637?

The Orange Book analysis is indication-specific. A method patent can be listed for an approved drug only when the patent claims an approved method of using that drug. The patent’s commercial relevance therefore depends on the approved Jardiance labeling and the FDA’s patent listing record.

The key regulatory question is whether the current Jardiance label continues to describe:

1. Glycemic-control treatment in the eGFR 45-to-less-than-60 population; and
2. Discontinuation below eGFR 45.

Empagliflozin’s labeling has evolved. Earlier labeling used more restrictive renal thresholds for glycemic-control treatment. Later labeling expanded empagliflozin’s indications and revised renal warnings and limitations as clinical evidence developed. A patent claim may remain enforceable even if the label changes, but Orange Book listing and ANDA certification consequences depend on the approved use that the patent claims.

Orange Book consequences

If listed for a relevant Jardiance indication:

• An ANDA applicant would need a Paragraph I, II, III or IV certification.
• A Paragraph IV certification could trigger patent litigation under 35 U.S.C. §271(e)(2).
• A timely infringement action could delay approval for up to 30 months under the Hatch-Waxman framework.
• A successful non-infringement or invalidity decision would remove the patent as a barrier to that ANDA.
• A section viii statement could carve out a patented method if the remaining label does not encourage the claimed use.

If the patent is not listed for the proposed use, it may still be asserted under ordinary infringement provisions, but it would not create the same automatic ANDA approval stay.

What is the relationship between the patent and Jardiance?

Jardiance is Boehringer Ingelheim and Eli Lilly’s empagliflozin product. The patent protects a renal-function dosing and discontinuation protocol rather than the product’s active ingredient.

Jardiance product relevance

Product characteristic	Relevance to US 10,258,637
Active ingredient	Empagliflozin
Standard standalone strengths	10 mg and 25 mg
Claimed doses	Includes 10 mg and 25 mg
Fixed-dose combination	Metformin-dependent claims may implicate Synjardy use
Renal subgroup	eGFR ≥45 and <60
Glycemic endpoint	Improved glycemic control
Product type	Small-molecule drug
Regulatory pathway for generics	ANDA, not biosimilar 351(k)

The 5 mg and 12.5 mg claims may be met by dose splitting or administration of multiple dosage units, depending on the product and prescribing instructions. They do not require a commercially marketed 5 mg or 12.5 mg tablet.

The metformin claims are narrower than the parent claims because they require combination treatment. They could be relevant to empagliflozin/metformin products, including fixed-dose combinations, if the labeling instructs treatment of the claimed renal subgroup and discontinuation below 45.

What patents form the broader empagliflozin patent landscape?

The empagliflozin estate can be divided into five categories.

Compound patents

The original compound patents protect empagliflozin and related chemical subject matter. These patents generally present the earliest generic-entry barrier but have earlier expiration dates than later clinical-use patents.

Formulation and solid-state patents

These patents may cover:

• Tablet compositions.
• Crystalline forms.
• Particle-size ranges.
• Stability characteristics.
• Manufacturing processes.
• Fixed-dose combinations with metformin or other antidiabetic agents.

A generic applicant can sometimes avoid a formulation claim by using a different excipient system or process. Solid-form claims can be harder to design around when the marketed product depends on a particular crystalline form, but infringement must be assessed claim by claim.

Combination-product patents

Empagliflozin/metformin products may have separate patents covering:

• The combination itself.
• Dose ratios.
• Bilayer or multilayer tablets.
• Sequential or simultaneous administration.
• Pharmacokinetic characteristics.

Claims 6, 12, 18 and 24 of US 10,258,637 are method claims and should be analyzed separately from formulation claims directed to Synjardy.

Cardiovascular and heart-failure method patents

Empagliflozin’s cardiovascular and heart-failure evidence created later method-of-use opportunities. A patent directed to reducing cardiovascular death or treating heart failure may have a different infringement profile from US 10,258,637 because it may not require the claimed glycemic-control endpoint or eGFR entry range.

Chronic-kidney-disease method patents

Later kidney-disease indications may be protected by separate patents. Those patents can remain relevant to generic labels even when a generic sponsor carves out the older glycemic-control use.

How strong is the patent estate for US 10,258,637?

The patent is strongest against a label that expressly reproduces the claimed clinical algorithm. It is weaker against a label that omits the renal subgroup, omits the stopping rule, or seeks approval only for a non-glycemic indication.

Strength factors

• The claims identify a specific active ingredient.
• The renal entry range is objective and measurable.
• The claims include a defined discontinuation threshold.
• The claims cover both direct treatment language and an explicit renal-assessment sequence.
• The 10 mg and 25 mg claims correspond to standard empagliflozin strengths.
• The metformin claims extend coverage into combination therapy.

Vulnerability factors

• Renal dosing and discontinuation may be challenged as obvious in view of pre-existing renal-impairment studies, prescribing information and clinical pharmacology.
• The eGFR thresholds may be characterized as routine clinical optimization.
• The “wherein glycemic control is improved” language may raise questions about whether it adds a meaningful structural limitation or merely states the intended result.
• The 5 mg and 12.5 mg claims may face enablement or written-description scrutiny if the specification emphasizes other doses.
• A generic may avoid induced infringement by omitting the claimed use from its label.
• Changes in FDA labeling may reduce the overlap between the patent and the approved indication.

The principal validity risk is obviousness under 35 U.S.C. §103. The principal enforcement risk is inducement and label-scope analysis under 35 U.S.C. §§271(b) and 271(e)(2).

Which companies are challenging empagliflozin patents?

Generic empagliflozin competition is expected to proceed through ANDA filings and Paragraph IV certifications rather than biosimilar applications. The relevant challengers are generic-drug companies pursuing empagliflozin or empagliflozin/metformin products.

A public challenge to the broader Jardiance estate does not necessarily establish a challenge to US 10,258,637. Each patent must be tied to:

• The ANDA product.
• The certification.
• The asserted patent list.
• The filed district-court complaint.
• Any settlement or consent judgment.

No specific Paragraph IV challenger, litigation docket or settlement should be attributed to US 10,258,637 without matching the patent number to the Orange Book record and the asserted-patent allegations.

What patent litigation affects US Patent 10,258,637?

The patent creates two distinct litigation settings.

Hatch-Waxman litigation

An ANDA applicant may challenge the patent by alleging:

• Non-infringement.
• Invalidity for anticipation.
• Invalidity for obviousness.
• Lack of written description.
• Lack of enablement.
• Improper listing or absence of a matching approved use.

The litigation trigger is usually the filing of a Paragraph IV certification and notice letter. A complaint under §271(e)(2) concerns the anticipated commercial manufacture, use or sale of the ANDA product before patent expiry.

Post-launch method litigation

If a generic enters with a label that omits the patented use but the product is later promoted for that use, the patent holder may pursue induced-infringement claims. Evidence can include promotional materials, sales-force messaging, reimbursement materials and physician communications.

Settlement agreements

A settlement could permit launch before the nominal 2034 endpoint. Possible structures include:

• A fixed early-entry date.
• A license limited to certain indications.
• A covenant not to sue.
• A label carve-out arrangement.
• A payment or other negotiated consideration.

A settlement date cannot be inferred from patent expiration or FDA approval alone.

What generic launch scenarios exist for empagliflozin?

Scenario	Effect on US 10,258,637
Generic label includes glycemic treatment at eGFR 45-to-less-than-60 and discontinuation below 45	High infringement exposure
Generic label omits the renal subgroup	Stronger non-infringement position
Generic label omits glycemic-control use and retains only another approved indication	Potential section viii strategy, subject to remaining patents
Generic launches after patent expiry	No ordinary patent-barrier risk from this patent
Generic launches under a settlement license	Entry depends on negotiated terms
Generic uses a different SGLT2 inhibitor	No literal empagliflozin infringement
Generic uses empagliflozin/metformin	Claims 6, 12, 18 and 24 require separate review

The patent may therefore delay only some forms of generic entry. It is less likely to block an ANDA whose label is carefully drafted around the claimed renal-management protocol.

How does US 10,258,637 compare with competing SGLT2 patent estates?

Drug	Active ingredient	Relevance to US 10,258,637
Jardiance	Empagliflozin	Directly within claim scope
Farxiga	Dapagliflozin	Different molecule; separate patent estate
Invokana	Canagliflozin	Different molecule; separate patent estate
Steglatro	Ertugliflozin	Different molecule; separate patent estate
Synjardy	Empagliflozin/metformin	Potential relevance to metformin-dependent claims
Glyxambi	Empagliflozin/linagliptin	Empagliflozin component warrants separate method and formulation analysis

The patent is not a platform patent for SGLT2 inhibitors. Its economic value is tied to empagliflozin products and labels.

What is the revenue exposure from this patent?

The patent’s revenue exposure is narrower than the total Jardiance franchise because it covers only:

• Type 2 diabetes treatment.
• The eGFR 45-to-less-than-60 subgroup.
• A specific discontinuation protocol.
• Certain empagliflozin doses.
• Optional metformin combination use.

The exposure can still be material because renal impairment is common among patients with type 2 diabetes, and the 10 mg and 25 mg doses are standard commercial strengths. The patent is most valuable if it is listed against a label that a generic cannot practically carve out without losing a commercially important indication.

Revenue analysis should separate:

1. Jardiance standalone sales.
2. Synjardy sales.
3. Glyxambi sales.
4. Glycemic-control sales.
5. Heart-failure and chronic-kidney-disease sales.
6. Patients within the claimed eGFR range.

Key Takeaways

• US Patent 10,258,637 is a renal-function-guided method-of-use patent for empagliflozin.
• Its core range is eGFR ≥45 and <60 mL/min/1.73 m², with discontinuation below 45.
• The patent contains 24 claims organized around four overlapping independent methods.
• The commercially important dose claims are 10 mg and 25 mg.
• Claims covering metformin may affect empagliflozin/metformin products separately from standalone Jardiance.
• The patent does not cover empagliflozin as a compound, all SGLT2 inhibitors, or all Jardiance indications.
• Generic infringement risk depends heavily on the proposed label and whether the label encourages the claimed renal protocol.
• The nominal term extends approximately into 2034, subject to patent-term adjustment and the official USPTO term calculation.
• Empagliflozin is a small molecule. Biosimilar analysis under the 351(k) pathway does not apply.
• Orange Book relevance must be assessed against the patent listing and the current FDA-approved Jardiance uses, not against the patent claims alone.

FAQs

Can a generic sell empagliflozin before US Patent 10,258,637 expires?

Yes, potentially. A generic may pursue a Paragraph IV challenge, a section viii label carve-out, a settlement license or a non-infringing label. The result depends on the patent listing, certification and label language.

Does US Patent 10,258,637 cover Jardiance 10 mg tablets?

It can cover the method of administering a 10 mg total daily dose when the patient has the claimed eGFR range and the treatment is discontinued below eGFR 45. It does not claim the 10 mg tablet as a product.

Does the patent cover Synjardy?

Potentially. Claims 6, 12, 18 and 24 require administering metformin in addition to empagliflozin. A Synjardy label or use must still satisfy the renal, dose and discontinuation limitations.

Is the patent relevant to Jardiance heart-failure treatment?

Not automatically. The asserted method must satisfy the type 2 diabetes, glycemic-control and eGFR limitations. A heart-failure use outside those limitations requires separate patent analysis.

Can a different SGLT2 inhibitor avoid this patent?

Yes, as a literal matter. Dapagliflozin, canagliflozin and ertugliflozin are different active ingredients. Their products may face separate patents and regulatory barriers.

References

1. United States Patent and Trademark Office. (2019). US Patent No. 10,258,637, use of empagliflozin in patients with renal impairment. https://patents.google.com/patent/US10258637B2/en

2. U.S. Food and Drug Administration. (n.d.). Orange Book: Approved drug products with therapeutic equivalence evaluations. https://www.accessdata.fda.gov/scripts/cder/ob/

3. U.S. Food and Drug Administration. (2023). Jardiance (empagliflozin) prescribing information. Boehringer Ingelheim Pharmaceuticals, Inc. https://www.accessdata.fda.gov/drugsatfda_docs/label/

4. United States Code. (2024). 35 U.S.C. §§ 103, 154, 271 and 282. https://uscode.house.gov/

5. United States Code. (2024). 21 U.S.C. § 355 and the Hatch-Waxman approval framework. https://uscode.house.gov/

Drugs Protected by US Patent 10,258,637

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Boehringer Ingelheim	SYNJARDY XR	empagliflozin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208658-001	Dec 9, 2016		RX	Yes	No					Y
Boehringer Ingelheim	SYNJARDY XR	empagliflozin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208658-002	Dec 9, 2016		RX	Yes	No					Y
Boehringer Ingelheim	SYNJARDY XR	empagliflozin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208658-003	Dec 9, 2016		RX	Yes	No					Y
Boehringer Ingelheim	SYNJARDY XR	empagliflozin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208658-004	Dec 9, 2016		RX	Yes	Yes					Y

International Family Members for US Patent 10,258,637

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2014247092
Canada	2812519
Canada	2908635
Canada	3121761