Details for Patent: 8,772,315

Which drugs does patent 8,772,315 protect, and when does it expire?

Patent 8,772,315 protects MYRBETRIQ and is included in one NDA.

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

This patent has twelve patent family members in eleven countries.

Summary for Patent: 8,772,315

Title:	Pharmaceutical composition for treating overactive bladder
Abstract:	A pharmaceutical composition comprising (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or a pharmaceutically acceptable salt thereof and (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate or a pharmaceutically acceptable salt thereof, as active ingredients, in particular for improving various symptoms accompanying overactive bladder, such as urinary urgency, pollakiuria and/or urinary incontinence.
Inventor(s):	Masanori Suzuki, Masashi Ukai, Akiyoshi Ohtake
Assignee:	Astellas Pharma Inc
Application Number:	US13/748,956
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,772,315
Patent Claim Types: see list of patent claims	Use; Composition; Delivery;

US Patent 8,772,315: Mirabegron-Solifenacin Combination Claims, Patent Scope and Market Risk

US Patent 8,772,315 protects specified combinations of mirabegron and solifenacin for overactive bladder. The patent is directed to a dose-defined combination rather than to either active ingredient individually. Its strongest commercial coverage is the use of mirabegron at 25 or 50 mg with solifenacin at 5 mg, administered orally either together or at separate times.

The patent does not claim a broad class of beta-3 adrenergic agonist and antimuscarinic combinations. It identifies two specific molecules:

• Mirabegron, the R-enantiomer named in the claims.
• Solifenacin, specifically the succinate salt in the narrower claims.

The patent is commercially relevant to the FDA-approved add-on use of Myrbetriq, or mirabegron, with solifenacin in adults with overactive bladder.

What drugs and therapeutic combination does US 8,772,315 cover?

The first claimed compound is mirabegron:

(R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide.

The second claimed compound is solifenacin:

(3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate.

The patent claims the combination for treating urinary urgency, increased urinary frequency, and urinary incontinence associated with overactive bladder.

Claimed component	Commercial identity	Claimed amount
Mirabegron free base or pharmaceutically acceptable salt	Myrbetriq	25-50 mg
Solifenacin free base or pharmaceutically acceptable salt	Vesicare; solifenacin succinate	5 mg
Indication	Overactive bladder	Urgency, pollakiuria and/or incontinence

The claims use the active-ingredient-equivalent amount. For solifenacin, the patent specifies 5 mg calculated as solifenacin succinate. This distinction matters when evaluating a commercial tablet labeled by salt weight rather than active-moiety weight.

How many independent claims does US 8,772,315 have?

The patent has two principal independent claims:

1. Claim 1, a pharmaceutical composition claim.
2. Claim 5, a method-of-treatment claim.

The remaining claims narrow those two categories.

Claim group	Claim numbers	Legal subject matter
Composition	1-4	Mirabegron plus solifenacin in a defined dose combination
Treatment method	5-16	Treating overactive bladder with both compounds
Administration route	6, 8, 10, 12, 14, 16	Both products administered orally
Administration timing	7, 8, 13, 14	Simultaneous administration
Administration timing	9, 10, 15, 16	Administration at a time interval
Specific chemical forms	2-4, 11-16	Mirabegron free base and solifenacin succinate

What does claim 1 protect?

Claim 1 covers a pharmaceutical composition comprising:

• Mirabegron or a pharmaceutically acceptable salt at 25 to 50 mg; and
• Solifenacin or a pharmaceutically acceptable salt at 5 mg, expressed as solifenacin succinate.

The claim does not require:

• A particular excipient;
• A particular tablet, capsule, or other dosage form;
• A fixed-dose single tablet;
• A specified release profile;
• A specified dissolution profile;
• A specified particle size;
• A specified pharmacokinetic profile; or
• A particular manufacturing process.

The word "comprising" makes the composition claim open-ended. A product containing the two claimed actives at the specified quantities could remain within the claim even if it contains additional active or inactive ingredients.

The principal limitation is the combination and dose window. A composition containing mirabegron below 25 mg, above 50 mg, or solifenacin at a dose other than 5 mg would not literally satisfy the express dosage limitations of claim 1, although other infringement theories could become relevant depending on the facts.

Does claim 1 require a single co-formulated tablet?

Not expressly. Claim 1 recites a pharmaceutical composition comprising both active ingredients, but it does not state that the compounds must be physically present in the same tablet or capsule.

A single fixed-dose combination tablet is the clearest infringement scenario. A kit, blister package, or multi-unit package may require a more detailed analysis of claim construction, packaging, and whether the overall product is a claimed pharmaceutical composition.

The method claims are broader in practical administration terms because they expressly permit simultaneous dosing or dosing at a time interval.

What do claims 5 through 16 protect?

Claim 5 protects a method of treating overactive bladder by administering:

• Mirabegron at 25 to 50 mg; and
• Solifenacin at 5 mg, measured as solifenacin succinate.

The claim does not require simultaneous administration. Claims 7 and 8 address simultaneous administration, while claims 9 and 10 address administration at a time interval.

Claims 11 through 16 narrow the active ingredients to:

• Mirabegron free base; and
• Solifenacin succinate.

The method claims therefore cover the commercially relevant regimen in which a patient receives Myrbetriq 25 or 50 mg together with solifenacin 5 mg, whether the products are administered at the same time or at different times.

Limitation	Broad method coverage	Narrow dependent coverage
Mirabegron	Compound or acceptable salt	Mirabegron free base
Solifenacin	Compound or acceptable salt	Solifenacin succinate
Mirabegron dose	25-50 mg	25-50 mg
Solifenacin dose	5 mg equivalent	5 mg solifenacin succinate
Route	Not expressly limited in claim 5	Oral administration in selected dependent claims
Timing	Simultaneous or separated	Defined by claims 7-10 and 13-16
Disease	Overactive bladder symptoms	Same

How strong is the patent estate for mirabegron and solifenacin?

US 8,772,315 is a focused combination patent, not a foundational compound patent. Its strength depends on whether a competing product, label, or treatment protocol uses both active ingredients at the claimed doses.

Strengths

The patent has several commercially useful characteristics:

1. It covers the clinically important 25 mg and 50 mg mirabegron doses.
2. It covers the 5 mg solifenacin dose used in combination therapy.
3. It includes both composition and method claims.
4. It reaches simultaneous and separated administration.
5. It is directed to a recognized therapeutic use.
6. Its dependent claims identify the marketed free-base and succinate forms.

Limitations

The patent has important boundaries:

• It does not claim mirabegron alone.
• It does not claim solifenacin alone.
• It does not claim every mirabegron-solifenacin dose ratio.
• It does not claim a new chemical entity.
• It does not expressly claim a particular fixed-dose formulation.
• It does not cover a generic mirabegron product used only for monotherapy.
• It does not automatically cover a solifenacin product labeled only for antimuscarinic monotherapy.

The patent is therefore strongest against a product that reproduces the combination indication and doses, rather than against a generic single-agent launch.

What is the FDA regulatory status of the combination?

The FDA approved Myrbetriq for overactive bladder and later approved its use in combination with solifenacin for adults with overactive bladder symptoms. The combination regimen uses:

• Mirabegron extended-release tablets at 25 or 50 mg; and
• Solifenacin, generally at 5 mg, with dose adjustment governed by labeling and patient factors.

The FDA-approved combination is not the same as a single fixed-dose combination tablet. In clinical use, patients may receive separate Myrbetriq and solifenacin products.

The FDA labeling for Myrbetriq identifies combination use with solifenacin, while Vesicare labeling identifies solifenacin indications and dosing. Regulatory approval does not itself determine patent infringement, but an approved combination indication can create a direct relationship between the label and the method claims of US 8,772,315. [2, 3]

What is the Orange Book status of US 8,772,315?

US 8,772,315 is relevant to the Orange Book analysis for mirabegron products because the patent claims a method involving mirabegron at approved doses. Orange Book treatment depends on the patent listing submitted by the New Drug Application holder, the listed product, and the FDA-approved use code.

A patent listed against Myrbetriq can create a Paragraph IV issue for an abbreviated new drug application seeking approval before patent expiration. The practical effect depends on:

• Whether the patent is listed against the relevant Myrbetriq product;
• The use code assigned by the NDA holder;
• Whether an ANDA applicant seeks the combination indication;
• Whether the applicant uses a section viii statement to carve out the patented use; and
• Whether the NDA holder brings an infringement action within the statutory period.

The Orange Book is the controlling source for current listing status, patent-use codes, and any listed pediatric-exclusivity effect. [1]

When does US 8,772,315 lose exclusivity?

The patent’s enforceable term is determined under 35 U.S.C. §§ 154 and 156, including the patent’s earliest effective nonprovisional or PCT filing date, any patent-term adjustment, and any patent-term extension. The issue date, July 8, 2014, does not determine the expiration date. [4]

The patent should be analyzed against:

• The term shown in USPTO Patent Center;
• Any terminal disclaimer;
• Any patent-term adjustment;
• Any patent-term extension;
• Any reissue or certificate of correction; and
• Any later continuation or divisional patent claiming related subject matter.

The claims supplied in the question do not establish an exact expiration date. A legally operative expiration date cannot be calculated from the claim text alone.

Which Paragraph IV challenges could affect this patent?

An ANDA applicant challenging a listed patent would typically submit one of the following certifications:

Certification	Effect
Paragraph II	Patent has already expired
Paragraph III	ANDA approval is deferred until patent expiration
Paragraph IV	Patent is invalid, unenforceable, or not infringed
Section viii statement	Applicant omits the patented method from the label

For US 8,772,315, the most commercially relevant challenge would target the method claims. A generic mirabegron applicant could attempt to omit the combination-use language while retaining monotherapy indications. That approach could reduce exposure to claims 5-16, but it would not eliminate risk if the commercial label, promotional activity, or product instructions encourage use with solifenacin.

A generic solifenacin applicant would face a different problem. The patent is not directed to solifenacin monotherapy. A label limited to solifenacin-alone treatment would ordinarily present less direct exposure, while an indication for use with mirabegron would create greater risk.

What generic launch scenarios exist?

Scenario 1: Mirabegron monotherapy launch

A generic mirabegron product labeled only for overactive bladder monotherapy would not practice the combination limitations on its face. The principal risks would arise from:

• An included combination indication;
• Promotional instructions encouraging coadministration;
• Substitution practices;
• Induced infringement allegations; or
• Other patents covering mirabegron itself.

US 8,772,315 alone would not block a clean monotherapy launch after approval.

Scenario 2: Mirabegron with a section viii carve-out

A generic applicant could seek approval for unpatented mirabegron uses while omitting the patented combination method. The commercial value of this approach depends on whether the carved-out indication is material and whether the labeling can be drafted without encouraging the patented regimen.

Scenario 3: Fixed-dose mirabegron-solifenacin product

A fixed-dose product containing mirabegron 25 or 50 mg and solifenacin 5 mg would face the highest literal infringement exposure under claim 1, particularly if it is marketed as a pharmaceutical composition containing both actives.

Scenario 4: Alternative solifenacin dose

A combination using solifenacin 10 mg rather than 5 mg may avoid the literal dosage limitation, but it could remain exposed to other patents, regulatory restrictions, and potential equivalents arguments. Dose changes also require clinical and labeling support.

Scenario 5: Separate products administered at different times

This scenario remains within the express language of claims 9, 10, 15, and 16 if the doses, compounds, and indication match the claims.

Are biosimilar risks relevant?

No. Mirabegron and solifenacin are chemically synthesized small-molecule drugs, not biologics. Competitors would use the ANDA pathway rather than the biosimilar pathway under the Public Health Service Act.

The relevant competitive tools are:

• ANDA approval;
• Paragraph IV certification;
• Section viii labeling carve-outs;
• Paragraph III certification; and
• Post-expiration generic substitution.

The absence of biosimilar litigation does not reduce the significance of small-molecule formulation, method-of-use, and Orange Book-listed patent disputes.

What other patent barriers matter?

US 8,772,315 is only one part of the commercial patent landscape. A complete freedom-to-operate review should separate the following categories:

Patent category	Primary risk
Mirabegron compound patents	Generic mirabegron launch timing
Mirabegron salt and polymorph patents	Solid form and API sourcing
Extended-release formulation patents	Tablet design and release profile
Solifenacin compound and salt patents	Solifenacin product entry
Combination patents	Coadministration and fixed-dose products
Method-of-use patents	Labeling and promotional conduct
Manufacturing patents	API production and process sourcing
Regulatory exclusivity	Approval timing independent of patent term

The combination claims in US 8,772,315 do not eliminate separate risks associated with mirabegron API manufacture, extended-release delivery, solifenacin salt production, or other formulation designs.

Does US 8,772,315 cover a fixed-dose combination product?

Yes, potentially, if the product contains both claimed actives in the specified amounts. The patent does not require a fixed-dose tablet, but a fixed-dose tablet is a straightforward product that could satisfy claim 1.

The claim does not specify whether the two actives must be:

• Homogeneously blended;
• Present in a bilayer tablet;
• Present in separate compartments;
• Encapsulated together; or
• Supplied as a co-packaged kit.

Those design choices may affect infringement and claim construction, but they do not automatically avoid the claim.

What is the licensing and litigation position?

The patent is associated with the Astellas mirabegron product platform. The disclosed claims do not identify a third-party license, royalty arrangement, or settlement agreement.

No conclusion about a current Paragraph IV settlement, covenant not to sue, or litigation disposition follows from the patent claims alone. Such matters are transaction- and docket-specific and must be evaluated from USPTO, FDA, PACER, and district-court records.

For commercial diligence, the critical litigation questions are:

• Whether US 8,772,315 is currently listed in the Orange Book;
• Whether an ANDA applicant has filed a Paragraph IV notice;
• Whether Astellas filed an infringement action within 45 days;
• Whether the case was dismissed, settled, or adjudicated;
• Whether the settlement includes a licensed entry date; and
• Whether the agreement contains acceleration, supply, or authorized-generic provisions.

Key Takeaways

• US 8,772,315 covers mirabegron plus solifenacin for overactive bladder.
• The key dose combination is mirabegron 25-50 mg with solifenacin 5 mg.
• Claim 1 covers a composition; claim 5 covers treatment.
• The method claims reach simultaneous administration and administration at a time interval.
• Dependent claims specifically cover mirabegron free base and solifenacin succinate.
• The patent does not claim mirabegron or solifenacin individually.
• A monotherapy mirabegron launch is less exposed than a combination-label launch.
• A fixed-dose combination containing both actives at the claimed doses presents the highest direct infringement risk.
• Biosimilar law is not relevant because both products are small molecules.
• The exact expiration date cannot be established from the claim text alone.
• Orange Book listing, use-code scope, Paragraph IV activity, and patent-term records determine the practical launch risk.

FAQs

Does US 8,772,315 cover Myrbetriq alone?

No. The asserted combination claims require both mirabegron and solifenacin. Mirabegron-alone products may face separate patents, but this patent does not claim mirabegron monotherapy.

Does the patent cover Myrbetriq 25 mg with solifenacin 5 mg?

Yes. That dose combination falls directly within the express dosage limitations of the composition and method claims.

Does the patent cover taking Myrbetriq in the morning and solifenacin later?

Potentially yes. Claims 9, 10, 15, and 16 expressly address administration at a time interval rather than requiring simultaneous dosing.

Can a generic omit the combination indication from its label?

A generic applicant may pursue a section viii carve-out for a patented method if FDA labeling and promotional conduct can be structured consistently with the carve-out. The patent and regulatory consequences depend on the final label and Orange Book use code.

Is a separate Myrbetriq tablet and solifenacin tablet covered?

The method claims can cover separate products administered together or at different times if the claimed compounds, doses, and overactive-bladder treatment are present. The composition claim requires a separate analysis of what constitutes the claimed pharmaceutical composition.

References

1. U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book.
2. U.S. Food and Drug Administration. (2024). Myrbetriq (mirabegron) prescribing information. Astellas Pharma US, Inc.
3. U.S. Food and Drug Administration. (2024). Vesicare (solifenacin succinate) prescribing information.
4. United States Code. (2024). 35 U.S.C. §§ 154, 156, 271, and 282.
5. U.S. Patent and Trademark Office. (2014). U.S. Patent No. 8,772,315, Pharmaceutical composition. Applicant/assignee: Astellas Pharma Inc.

Drugs Protected by US Patent 8,772,315

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Apgdi	MYRBETRIQ	mirabegron	TABLET, EXTENDED RELEASE;ORAL	202611-001	Jun 28, 2012	AB	RX	Yes	Yes	8,772,315*PED				Y
Apgdi	MYRBETRIQ	mirabegron	TABLET, EXTENDED RELEASE;ORAL	202611-002	Jun 28, 2012	AB	RX	Yes	Yes	8,772,315*PED				Y

Foreign Priority and PCT Information for Patent: 8,772,315

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Japan	P2007-285802	Nov 2, 2007

International Family Members for US Patent 8,772,315

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Canada	2704298
Cyprus	1113670
Denmark	2216021
European Patent Office	2216021
Spain	2393525