United States Patent 9,125,868: Scope, Claims, Expiration, and Contrave Patent Landscape

U.S. Patent No. 9,125,868 protects a weekly dose-escalation regimen for extended-release bupropion and naltrexone, the active ingredients in Contrave. Its core regimen starts at 90 mg bupropion plus either 4 mg or 8 mg naltrexone daily and increases over four weeks to approximately 360 mg bupropion plus 16 mg or 32 mg naltrexone daily. The patent is directed primarily to method-of-use protection, not to the active ingredients themselves.

The commercially relevant embodiment is Contrave’s four-week titration schedule using 8 mg naltrexone and 90 mg bupropion per extended-release tablet. The patent’s principal commercial risk is therefore an ANDA applicant seeking approval for naltrexone/bupropion extended-release tablets with a label that reproduces or materially encourages the patented titration protocol.

What does U.S. Patent 9,125,868 protect?

The patent protects administering progressively larger daily amounts of a bupropion/naltrexone pharmaceutical formulation over four consecutive weeks.

Treatment week	Bupropion amount	Naltrexone amount	Equivalent 90 mg/8 mg tablet count
Week 1	About 90 mg	About 4 mg or 8 mg	1 tablet
Week 2	About 180 mg	About 8 mg or 16 mg	2 tablets
Week 3	About 270 mg	About 12 mg or 24 mg	3 tablets
Week 4	About 360 mg	About 16 mg or 32 mg	4 tablets

The claims cover both:

A method in which the formulation is administered to an individual; and
A method directed specifically to an obese individual for treatment of obesity.

The patent does not require a particular brand name. A competing product could implicate the claims if it contains the claimed active ingredients, dosage amounts, release characteristics, dosage forms and titration instructions.

What is the claim structure of Patent 9,125,868?

Independent claim 1

Claim 1 is the broadest principal claim. It requires:

Daily administration during a first week;
About 90 mg of bupropion;
About 4 mg or about 8 mg of naltrexone;
Approximately doubled amounts during week two;
Approximately tripled amounts during week three; and
Approximately quadrupled amounts during week four.

Claim 1 does not expressly require:

Obesity;
An oral dosage form;
A tablet, capsule or pill;
Sustained release;
A single product containing both drugs;
A multilayer tablet; or
A specific morning or evening dosing schedule.

The phrase “pharmaceutical formulation” is broad enough to cover a formulation containing both active ingredients, subject to claim construction and the specification. The claim also uses “comprises,” which is generally open-ended under U.S. patent law. A formulation containing additional excipients, additional active ingredients or other components would not automatically avoid the claim.

Claims 2 and 3

Claims 2 and 3 divide the two naltrexone alternatives:

Claim 2 requires about 8 mg naltrexone in the first-week amount.
Claim 3 requires about 4 mg naltrexone in the first-week amount.

For Contrave-style products, claim 2 is the commercially more important dependent claim because the approved tablet contains 8 mg naltrexone and 90 mg bupropion.

Claims 4 through 8

These claims narrow the regimen to a single oral dosage form and then to escalating numbers of that dosage form.

Claim	Added limitation
4	First-week amount is in a single oral dosage form
5	Dosage form is a tablet, pill or capsule
6	Week-two amount uses two dosage forms
7	Week-three amount uses three dosage forms
8	Week-four amount uses four dosage forms

These claims closely track a commercial titration pack in which the patient takes one tablet daily during week one, two tablets daily during week two, three tablets daily during week three and four tablets daily thereafter.

Claims 9 and 10

Claim 9 requires sustained-release bupropion and sustained-release naltrexone. Claim 10 combines that requirement with the one-, two-, three- and four-dosage-form escalation.

These claims create a narrower but commercially important infringement theory against extended-release tablets. An immediate-release product would have a stronger noninfringement position against claims 9 and 10, although it could remain exposed under claim 1 or other claims if the remaining limitations are met.

Claim 11

Claim 11 protects a multilayer tablet containing:

A first pharmaceutical layer with sustained-release bupropion;
A second pharmaceutical layer with sustained-release naltrexone; and
An intermediate layer configured to dissolve rapidly in vivo.

This is a formulation and delivery-system claim. It does not cover every extended-release combination tablet. The accused product would need to satisfy the multilayer architecture and the rapidly dissolving intermediate layer limitation.

A conventional monolithic matrix tablet, bilayer tablet without the claimed intermediate layer, or two separate tablets would have a potential noninfringement position against claim 11.

Claims 12 and 13

Claims 12 and 13 address separate dosage forms for bupropion and naltrexone.

Claim 12 requires:

One sustained-release bupropion dosage form and one sustained-release naltrexone dosage form during week one;
Two of each during week two;
Three of each during week three; and
Four of each during week four.

Claim 13 describes a more specific reuse pattern involving first, second, third and fourth dosage forms. These claims are less closely aligned with the commercial Contrave configuration, which uses a combination tablet, but they could be relevant to a two-product or co-packaged generic strategy.

Claims 14 through 17

Claims 14 through 16 add obesity treatment to earlier claim combinations. Claim 17 is an independent obesity-treatment claim that requires:

Identifying the individual as obese;
Providing the first-week amount;
Providing the second-, third- and fourth-week amounts;
Sustained-release bupropion and naltrexone; and
A single oral dosage form for the first-week amount.

Claim 17 is particularly relevant to a generic label that identifies obesity treatment and instructs the same four-week dose escalation.

How does the patent map to Contrave?

The FDA-approved Contrave regimen is materially aligned with the patent’s core limitations. Each extended-release tablet contains 8 mg naltrexone hydrochloride and 90 mg bupropion hydrochloride. The prescribing information directs the following titration:

Week	Morning dose	Evening dose	Daily total
Week 1	1 tablet	None	8 mg/90 mg
Week 2	1 tablet	1 tablet	16 mg/180 mg
Week 3	2 tablets	1 tablet	24 mg/270 mg
Week 4 onward	2 tablets	2 tablets	32 mg/360 mg

The FDA label also identifies Contrave as an extended-release product and directs use for chronic weight management in adults meeting specified BMI criteria. That label structure corresponds closely to claims 2, 9, 10, 14, 15 and 17. [2]

The patent does not require the exact morning/evening split used by the FDA label. Its claims are framed around the total daily amount and the weekly escalation. This increases the range of dosing schedules that could potentially satisfy the claims.

When does U.S. Patent 9,125,868 expire?

The patent issued on September 8, 2015. Public patent records identify a May 26, 2026 expiration date based on the patent family’s earliest effective nonprovisional filing date, subject to any applicable patent-term adjustment. [1]

The relevant commercial timeline is:

Event	Date
Earliest relevant family priority	May 26, 2006
Patent issued	September 8, 2015
Nominal expiration	May 26, 2026
Product associated with the claims	Contrave
Primary protection type	Method of treatment and dosage regimen

Patent expiration is separate from FDA exclusivity. A patent may remain enforceable after FDA marketing exclusivity ends, and an ANDA applicant can challenge the patent before expiration through a Paragraph IV certification.

What is the Orange Book status of Patent 9,125,868?

Patent 9,125,868 has been associated with the U.S. regulatory protection for Contrave, an FDA-approved naltrexone hydrochloride/bupropion hydrochloride extended-release product marketed by Currax Pharmaceuticals after the product’s acquisition from Orexigen Therapeutics.

The Orange Book is the controlling FDA source for listed patents and certifications tied to an approved drug application. Patent listings can change through delisting, correction, expiration or changes in the approved application. The relevant Orange Book inquiry is therefore product-specific and must be evaluated against the current listing for NDA 200063. [3]

The patent’s subject matter is well suited to Orange Book listing because the claims cover an approved method of use and a commercially relevant dosage regimen. A listing does not establish validity or infringement. It requires an ANDA applicant to address the listed patent through a Paragraph I, II, III or IV certification, or through a section viii statement where permitted.

What Paragraph IV challenges could target this patent?

An ANDA applicant seeking approval for generic naltrexone/bupropion extended-release tablets could challenge Patent 9,125,868 through a Paragraph IV certification. The principal theories would likely include:

Noninfringement

A generic applicant could argue that its proposed product or labeling does not meet one or more limitations, such as:

No four-week titration schedule;
No first-week dose of approximately 90 mg bupropion;
No first-week dose of approximately 4 mg or 8 mg naltrexone;
No sustained-release form for one or both ingredients;
No single oral dosage form;
No obesity indication in the proposed label; or
No instruction to administer the claimed escalating amounts.

A label that instructs the exact Contrave regimen would weaken these defenses.

Invalidity for obviousness

An applicant could argue that the claimed escalation was obvious from:

Existing bupropion sustained-release products;
Existing naltrexone obesity or addiction-treatment regimens;
Clinical trial protocols;
Dose-escalation practices intended to improve tolerability; and
Prior art combinations of bupropion and naltrexone.

The patent holder would respond that the specific four-week sequence, dosage ratios, sustained-release combination and obesity-treatment context produced a clinically useful regimen not disclosed or suggested by the prior art.

Lack of written description or enablement

The use of “about,” the alternative 4 mg and 8 mg naltrexone amounts, and the broad formulation language could create written-description or enablement arguments. These challenges would depend heavily on the specification’s examples, formulation disclosures and clinical data.

Indefiniteness

The terms “about,” “twice as much,” “three times as much” and “four times as much” could be challenged as indefinite. Courts generally evaluate such terms in the context of the specification, prosecution history and the precision reasonably required in the relevant pharmaceutical field.

How strong is the patent estate for Contrave?

The estate has meaningful commercial strength because the core patent claims correspond to the approved product’s labeled dosing schedule. Its principal weaknesses are structural:

The patent protects a method, not the chemical identity of bupropion or naltrexone.
A generic applicant may be able to design around individual formulation claims.
A skinny-label strategy may remove obesity treatment language or omit the patented titration instructions, depending on the scope of the remaining approved uses.
Method claims require proof that the patented regimen is practiced, induced or otherwise infringed.

The strongest claims against a conventional Contrave-equivalent product are likely claims 2, 9, 10, 14, 15 and 17. Claim 11 is narrower because it requires a specified multilayer tablet. Claims 12 and 13 are more relevant to separate-tablet products than to the standard combination-tablet configuration.

What other patent categories affect the Contrave landscape?

Active-ingredient patents

Bupropion and naltrexone are established active ingredients with no meaningful composition-of-matter exclusivity tied to the commercial product. The principal protection is therefore formulation, combination and method-of-use protection.

Combination-product patents

Combination patents may cover:

Specific bupropion/naltrexone ratios;
Sustained-release delivery;
Separate or combined dosage forms;
Multilayer tablet structures; and
Pharmacokinetic or release profiles.

These patents are distinct from the titration claims in Patent 9,125,868 and must be analyzed claim by claim.

Method-of-use patents

Method patents may cover treatment of obesity, weight management, appetite control or related metabolic conditions. Their enforceability against an ANDA applicant depends heavily on the proposed label and the applicant’s conduct.

Manufacturing and formulation barriers

A generic developer may face technical barriers even after avoiding the claims. These include:

Matching the dissolution profile of an extended-release product;
Preventing chemical or physical interaction between the two active ingredients;
Maintaining dose uniformity;
Controlling bupropion and naltrexone release independently; and
Demonstrating bioequivalence under FDA requirements.

These barriers are commercial and regulatory issues, not automatic patent barriers.

What litigation and settlement issues matter?

A Paragraph IV notice alleging invalidity or noninfringement can trigger a Hatch-Waxman action under 35 U.S.C. § 271(e)(2). The filing of an infringement action generally creates a 30-month stay of FDA approval, subject to statutory exceptions and court action. [4]

For Patent 9,125,868, the key litigation questions are:

Whether the generic label reproduces the four-week titration;
Whether the patent is listed for the relevant NDA at the time of certification;
Whether the patent holder sues within the statutory period;
Whether other Orange Book patents are asserted in the same case;
Whether the parties enter a launch settlement; and
Whether the generic applicant pursues a section viii carveout.

A settlement may establish a licensed launch date before patent expiration. Without a publicly filed agreement or court order, a commercial launch date should not be inferred from the existence of a Paragraph IV certification.

What generic launch scenarios exist?

Scenario	Commercial effect
Generic copies the full titration label	High infringement exposure under claims 2, 9, 10 and 17
Generic uses a section viii carveout	Potentially earlier approval, but limited labeling and marketability
Generic challenges validity under Paragraph IV	Litigation and possible 30-month stay
Generic uses a materially different dose schedule	Reduces method-claim exposure but may impair therapeutic substitution
Generic uses separate bupropion and naltrexone products	Potential exposure under claims 12 and 13
Generic launches after May 2026 expiration	Patent 9,125,868 no longer blocks entry, absent other enforceable patents

The practical launch date depends on the full Orange Book estate, not Patent 9,125,868 alone. A competitor that defeats or avoids this patent may still face other listed patents, regulatory exclusivity or formulation-related claims.

Key Takeaways

U.S. Patent 9,125,868 protects a four-week escalation regimen for sustained-release bupropion and naltrexone.
The commercial target is the Contrave regimen: one 8 mg/90 mg tablet daily in week one, increasing to four tablets daily by week four.
Claims 2, 9, 10 and 17 are the most commercially significant claims for a Contrave-equivalent product.
Claim 11 is narrower and requires a multilayer tablet with a rapidly dissolving intermediate layer.
The patent’s nominal expiration date is May 26, 2026.
The patent does not provide composition-of-matter protection for bupropion or naltrexone.
Paragraph IV risk is driven primarily by the generic label and whether it instructs the patented titration.
A section viii carveout or materially different dosing label could reduce infringement exposure, but may limit the generic product’s commercial scope.
The full generic-entry analysis requires review of every currently listed Contrave patent, not Patent 9,125,868 in isolation.

FAQs About U.S. Patent 9,125,868

Does Patent 9,125,868 cover Contrave itself?

It covers methods of administering a Contrave-type bupropion/naltrexone regimen. It does not broadly claim every composition containing bupropion and naltrexone.

Does the patent require the patient to be obese?

The broad independent claim does not. Claims 14 through 17 add obesity identification or obesity treatment as an express limitation.

Could a generic use a different naltrexone dose?

A product using a dose outside the claimed approximately 4 mg or 8 mg first-week amount may have a noninfringement argument, but the full claim language, prosecution history and other patents must be evaluated.

Does a multilayer tablet automatically infringe claim 11?

No. Claim 11 requires the claimed bupropion layer, naltrexone layer and rapidly dissolving intermediate layer. A multilayer tablet lacking one of those elements would not satisfy claim 11.

Can a generic launch before May 26, 2026?

It may launch earlier through a successful Paragraph IV challenge, a settlement or license, a valid section viii carveout, or another legally permissible pathway. Patent 9,125,868 remains a potential barrier until expiration or a court determination eliminating enforceability.

References

United States Patent and Trademark Office. (2015). U.S. Patent No. 9,125,868, methods of administering a pharmaceutical formulation.
U.S. Food and Drug Administration. (2024). Contrave (naltrexone hydrochloride and bupropion hydrochloride) extended-release tablets: Prescribing information.
U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book.
United States Code. (2024). 35 U.S.C. § 271(e): Infringement of patents relating to drugs and biological products.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Azurity	CONTRAVE	bupropion hydrochloride; naltrexone hydrochloride	TABLET, EXTENDED RELEASE;ORAL	200063-001	Sep 10, 2014		RX	Yes	Yes	9,125,868	⤷ Start Trial				USE OF NALTREXONE AND BUPROPION BASED ON AN ESCALATING DOSE SCHEDULE	⤷ Start Trial
>Applicant	>Tradename	>Generic Name	>Dosage	>NDA	>Approval Date	>TE	>Type	>RLD	>RS	>Patent No.	>Patent Expiration	>Product	>Substance	>Delist Req.	>Patented / Exclusive Use	>Submissiondate

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	063958	⤷ Start Trial
Australia	2007319472	⤷ Start Trial
Canada	2668885	⤷ Start Trial
Chile	2007003246	⤷ Start Trial
China	101573103	⤷ Start Trial
European Patent Office	2088998	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 9,125,868

Which drugs does patent 9,125,868 protect, and when does it expire?

Summary for Patent: 9,125,868