United States Patent 8,461,140: Deoxycholate Formulation Claims, Scope, Validity, and Patent Landscape

U.S. Patent No. 8,461,140 protects aqueous pharmaceutical formulations containing 0.1% to 2% w/v deoxycholate with an exceptionally low carbon-14 content. The claims target the use of low-radiocarbon, generally synthetic or highly purified, deoxycholate rather than a specific therapeutic indication. Claims 3 through 6 narrow the scope to subcutaneous formulations or defined carbon-14 measurements.

The patent is commercially relevant to deoxycholic-acid injectable products, including Kybella, but the claim language does not cover every deoxycholic-acid formulation. A competing product must satisfy all limitations of at least one claim, including the concentration range and the less-than-1-ppt carbon-14 limitation.

What does U.S. Patent 8,461,140 cover?

The independent claim covers:

An aqueous pharmaceutical formulation;
About 0.1% w/v to about 2% w/v deoxycholate;
At least one pharmaceutically acceptable excipient and/or carrier; and
Deoxycholate with a carbon-14 content below 1 part per trillion.

The claim is composition-based. It does not require a particular indication, injection device, dosage volume, pH, buffer, preservative, surfactant, or therapeutic antibody.

Claim	Additional limitation	Practical scope
1	Aqueous formulation; 0.1%-2% w/v deoxycholate; excipient/carrier; <1 ppt carbon-14	Broadest claim
2	Carbon-14 content below 0.9 ppt	Narrower purity or isotope-profile limitation
3	Suitable for subcutaneous injection	Covers formulations meeting claim 1 that have subcutaneous suitability
4	Carbon-14 content of 0.87 ppt	Narrow numerical limitation
5	Carbon-14 content of 0.88 ppt	Narrow numerical limitation
6	Carbon-14 content of 0.89 ppt	Narrow numerical limitation

The word “comprising” makes claim 1 open-ended. A formulation may contain additional active ingredients, buffers, salts, stabilizers, preservatives, or delivery components without avoiding the claim, provided all required limitations remain present.

How broad is the deoxycholate concentration range?

Claim 1 covers approximately 1 to 20 mg/mL deoxycholate.

The conversion is:

Claimed concentration	Approximate concentration
0.1% w/v	1 mg/mL
0.5% w/v	5 mg/mL
1.0% w/v	10 mg/mL
2.0% w/v	20 mg/mL

The term “about” introduces a boundary issue. It may permit modest variation around the stated endpoints, depending on the intrinsic meaning of the claim, specification disclosures, prosecution history, and expert evidence. It does not normally convert the claim into an unlimited concentration range.

A product containing 0.05% deoxycholate would have a strong noninfringement position against the literal concentration limitation. A formulation containing 2.5% would face the same issue at the upper end. The doctrine of equivalents could become relevant, but prosecution-history estoppel and the numerical nature of the limitation may restrict that argument.

What does the carbon-14 limitation protect?

The carbon-14 limitation is the principal differentiating feature of the patent.

Claim 1 requires deoxycholate with a carbon-14 content of less than 1 ppt. Claims 2 and 4 through 6 impose still narrower limits. The limitation can distinguish deoxycholate manufactured from modern biological feedstocks, which may contain measurable radiocarbon, from material produced through petrochemical or other low-radiocarbon processes.

The patent therefore protects a combination of:

Aqueous pharmaceutical presentation;
Defined deoxycholate concentration; and
A low-radiocarbon deoxycholate composition.

The claim is not limited to a particular manufacturing process. A competitor may use a different process and still infringe if the resulting deoxycholate has the required carbon-14 content and is incorporated into an aqueous formulation within the claimed concentration.

Why the carbon-14 measurement method matters

A carbon-14 limitation is enforceable only if the measurement can be performed reliably and consistently. Key technical issues include:

The analytical method used to quantify carbon-14;
The detection limit;
Sample preparation;
Whether the measurement is reported as a concentration, ratio, or normalized value;
The definition of “ppt”;
Calibration against recognized radiocarbon standards;
Whether the result is reported as an actual value or as below the assay’s quantitation limit.

Claims 4, 5, and 6 are especially dependent on measurement precision. At 0.87, 0.88, and 0.89 ppt, laboratory variability and assay validation could materially affect infringement analysis.

What formulations are protected by U.S. Patent 8,461,140?

The claim language reaches a wide range of aqueous formulations if they contain the specified deoxycholate and carbon-14 profile.

Potentially covered products include:

Deoxycholate solutions for injection;
Buffered deoxycholate formulations;
Formulations containing preservatives;
Formulations containing tonicity agents;
Formulations containing surfactants or stabilizers;
Combination formulations containing deoxycholate and another active agent;
Formulations intended for subcutaneous administration, under claim 3.

The patent does not expressly require deoxycholic acid in its protonated form. “Deoxycholate” can encompass the deprotonated anion and salts, depending on the specification and claim construction. A product using sodium deoxycholate or another pharmaceutically acceptable deoxycholate salt would present a material infringement risk if it satisfies the remaining limitations.

A formulation containing deoxycholic acid but no deoxycholate species could raise a claim-construction issue. The result would depend on the patent specification, prosecution history, pH, ionization state, and how the product is characterized analytically.

Does claim 3 cover Kybella-type subcutaneous injections?

Claim 3 covers a formulation of claim 1 that is suitable for subcutaneous injection. It does not require that the product actually be marketed under a particular brand or used for a particular indication.

A Kybella-type product would need to be evaluated against:

Deoxycholate concentration;
Aqueous status;
Excipients or carriers;
Carbon-14 content;
Subcutaneous suitability.

The claim does not require treatment of submental fat, adipocytes, obesity, body contouring, or any other indication. Those limitations may appear in separate method-of-use patents, but they are absent from claim 3.

“Suitable for subcutaneous injection” is broader than “approved for subcutaneous injection.” A formulation may satisfy the claim based on its physical, chemical, and pharmaceutical characteristics even if it has not obtained regulatory approval for that route.

When does U.S. Patent 8,461,140 lose exclusivity?

The patent issued on June 18, 2013. Its ordinary patent term is generally calculated as 20 years from the earliest effective nonprovisional filing date, subject to patent-term adjustment, patent-term extension, terminal disclaimers, and continuity data recorded by the USPTO. The relevant statutory framework is 35 U.S.C. §§ 154 and 156.

Based on the patent’s U.S. filing history, the base term is expected to run into approximately 2029 or 2030, subject to the official USPTO term calculation. The exact expiration date should be taken from the USPTO Patent Center record and any applicable terminal disclaimer or patent-term adjustment certificate.[1]

The patent does not receive biologic exclusivity. Deoxycholate is a small-molecule chemical substance, so competing products would generally use the ANDA pathway rather than the biosimilar pathway.

What is the Orange Book status of U.S. Patent 8,461,140?

The Orange Book question is product-specific. A patent may be listed for an approved drug only if the NDA holder submits it and FDA accepts it as covering the drug substance, drug product, or an approved method of use under FDA listing standards.[2]

For a deoxycholic-acid product such as Kybella, the relevant analysis separates:

Issue	Significance
Patent listed in the Orange Book	An ANDA applicant may need to provide a Paragraph IV certification
Patent not listed	The patent may still be asserted in litigation, but it does not create the same Orange Book certification mechanism
Drug-product listing	Typically concerns formulation, composition, dosage form, or delivery
Method-of-use listing	Covers an approved use, not necessarily the formulation itself
Expired listing	Does not block approval, although other listed patents may remain relevant

The claim set supplied for Patent 8,461,140 is formulation-focused. If listed for an approved deoxycholate product, it would be most relevant as a drug-product patent rather than as a method-of-use patent.

The FDA Orange Book remains the controlling source for current listing status, patent-use codes, and listed expiration information.[2]

What Paragraph IV challenges could target this patent?

An ANDA applicant seeking approval before patent expiration could use a Paragraph IV certification if the patent is listed for the reference product. The applicant would assert that the patent is invalid, unenforceable, or not infringed.[3]

Likely noninfringement positions

A generic applicant could attempt to design around one or more limitations:

Use a deoxycholate concentration below 0.1% or above 2%;
Use a nonaqueous formulation;
Use a deoxycholate source with carbon-14 at or above 1 ppt;
Use a different active ingredient without deoxycholate;
Contest whether the formulation is suitable for subcutaneous injection;
Challenge whether the claimed deoxycholate species is present in the accused formulation.

The most commercially practical design-around may be difficult if the target product requires the same concentration range and low-radiocarbon raw material. Changing the carbon-14 profile could affect raw-material sourcing and product comparability.

Likely invalidity positions

Potential invalidity arguments include:

Anticipation by an earlier aqueous deoxycholate formulation with the claimed concentration and carbon-14 profile;
Obviousness based on known deoxycholate injectable formulations combined with known radiocarbon differences between synthetic and biological materials;
Indefiniteness concerning “about,” “less than 1 ppt,” or “suitable for subcutaneous injection”;
Lack of written description for the full concentration and carbon-14 ranges;
Enablement challenges concerning preparation and analytical verification of sub-ppt carbon-14 material.

The carbon-14 limitation may create a significant prior-art issue. Prior art that discloses deoxycholate formulations but does not measure carbon-14 may not anticipate the claim unless the property inherently exists. Conversely, if low radiocarbon is an unavoidable characteristic of a disclosed synthetic deoxycholate, inherency could become relevant.

How strong is the patent estate for deoxycholic-acid injections?

Patent 8,461,140 is strongest against products that replicate the claimed formulation architecture and source the deoxycholate from a low-radiocarbon process.

Its strengths are:

A measurable composition limitation;
A concentration range relevant to injectable products;
Broad “comprising” language;
No limitation to one indication;
Coverage of additional excipients and carriers;
A subcutaneous-use dependent claim.

Its weaknesses are:

The carbon-14 limitation may be technically difficult to prove;
Claims 4 through 6 are highly narrow;
The patent does not independently claim the deoxycholate active ingredient;
A competitor may avoid literal infringement through concentration, formulation state, or raw-material sourcing;
The claim may overlap with other deoxycholate patents, increasing validity and claim-construction complexity.

The patent is more likely to operate as a formulation barrier than as a complete market-entry barrier. A competitor that develops a different concentration, nonaqueous presentation, or different active ingredient may avoid these claims while remaining within the broader deoxycholate therapeutic field.

How does this patent compare with method-of-use and formulation patents?

Deoxycholic-acid patent estates generally divide into four categories:

Patent category	Typical protected subject matter	Relevance to Patent 8,461,140
Composition patents	Deoxycholate formulations and defined physical or chemical properties	Directly relevant
Method-of-use patents	Use for submental fat, adipocyte destruction, or body contouring	Not claimed in the supplied claims
Process patents	Manufacture, purification, or synthetic production of deoxycholate	May create raw-material barriers
Device and administration patents	Injection patterns, dosing systems, or delivery devices	Separate infringement analysis

Patent 8,461,140 does not claim the therapeutic method itself. A product could avoid the patent’s formulation claims yet still face method-of-use or device patents. The reverse is also possible: a product could infringe the formulation patent without practicing a patented therapeutic method, depending on its use and labeling.

Which companies control the commercial landscape?

The principal commercial reference point is Kybella, an FDA-approved injectable deoxycholic-acid product marketed for reduction of moderate to severe submental fat in adults.[4] Kythera developed Kybella; Allergan acquired Kythera in 2015, and AbbVie acquired Allergan in 2020.[5][6]

The competitive landscape includes:

The reference product and its current commercial owner;
Potential ANDA applicants;
Compounded or nonapproved deoxycholate products;
Aesthetic products using alternative fat-reduction technologies;
Research-stage products using related bile acids or different adipocytolytic mechanisms.

There is no biosimilar pathway for Kybella because it is a chemically synthesized small-molecule drug. A generic entrant would need to address pharmaceutical equivalence, bioequivalence, labeling, manufacturing controls, and any unexpired Orange Book patents.

What licensing deals and settlements affect the patent?

A corporate acquisition can transfer patent ownership without constituting a third-party license. Kythera’s acquisition by Allergan and Allergan’s later acquisition by AbbVie are therefore relevant to ownership and enforcement history.[5][6]

The supplied claim set does not establish a license, covenant not to sue, or settlement agreement. Those issues must be analyzed from assignment records, SEC filings, ANDA litigation dockets, and any publicly filed settlement documents.

A Paragraph IV settlement could affect generic launch timing through:

A licensed entry date;
A supply arrangement;
A reverse-payment restriction;
A manufacturing or distribution license;
A non-assertion covenant;
An agreement covering only specified claims or products.

The absence of a settlement in the claim text means it has no bearing on the legal scope of Patent 8,461,140.

What generic launch scenarios exist?

Launch after patent expiry

This is the lowest-risk scenario if all listed patents and regulatory exclusivities have expired. The applicant still must satisfy FDA requirements for the ANDA.

Paragraph IV launch before expiry

This creates litigation risk under the Hatch-Waxman framework. A timely infringement action can trigger a 30-month stay of approval, subject to statutory exceptions and court developments.[3]

Formulation design-around

A competing product could alter concentration, vehicle, route, or carbon-14 profile. The commercial cost is that the resulting product may no longer match the reference product closely enough for a straightforward ANDA strategy.

At-risk launch

An applicant may launch after resolving some patents but before all patent disputes end. This exposes the company to damages, injunctive relief, and possible market withdrawal if the patent holder prevails.

What geographic coverage does the patent have?

U.S. Patent 8,461,140 has enforceable scope in the United States only. Parallel protection would require corresponding patents in other jurisdictions. European, Canadian, Japanese, and other national rights are separate assets with different claims, prosecution histories, term dates, opposition procedures, and litigation risks.

A U.S. patent can affect U.S. manufacture, importation, sale, offer for sale, and use under 35 U.S.C. § 271. It does not independently block manufacture and sale in countries where no corresponding patent right exists.[7]

Manufacturing outside the United States does not eliminate U.S. risk if the accused formulation is imported into, sold in, or used in the United States.

Key Takeaways

Patent 8,461,140 claims aqueous deoxycholate formulations containing approximately 0.1% to 2% w/v deoxycholate.
The defining limitation is carbon-14 content below 1 ppt.
Claims 2 and 4 through 6 narrow the radiocarbon requirement to below 0.9 ppt or exact values of 0.87, 0.88, and 0.89 ppt.
Claim 3 adds suitability for subcutaneous injection.
The patent does not claim a specific therapeutic indication.
The broadest practical risk concerns low-radiocarbon deoxycholate injectable formulations within the claimed concentration range.
The main design-around options are concentration, formulation state, route, and raw-material carbon-14 profile.
Kybella-related generic competition would proceed through the ANDA pathway, not the biosimilar pathway.
Orange Book status must be assessed against the current FDA listing for the relevant NDA.
The patent’s base term is expected to extend into approximately 2029 or 2030, subject to the official USPTO term calculation and any applicable adjustments.
Manufacturing, assay validation, and carbon-14 testing will be central to both infringement and validity disputes.

Frequently Asked Questions

Can a sodium deoxycholate formulation infringe Patent 8,461,140?

Yes. Sodium deoxycholate may fall within “deoxycholate” if the claim construction and specification support that interpretation and the formulation satisfies the aqueous, concentration, excipient, and carbon-14 limitations.

Does using naturally derived deoxycholate avoid the patent?

Not necessarily. Naturally derived material may have a carbon-14 content above the claimed threshold, but that fact must be established by validated testing. The source alone does not determine infringement.

Does the patent cover deoxycholate powder before it is formulated?

The supplied claims require an aqueous pharmaceutical formulation. They do not independently claim dry deoxycholate, a manufacturing intermediate, or the raw material in isolation.

Can a product infringe claim 1 without infringing claim 3?

Yes. Claim 1 does not require subcutaneous suitability. A formulation could meet claim 1 but fall outside claim 3 if it is not suitable for subcutaneous injection.

Is carbon-14 testing required in a freedom-to-operate analysis?

Yes. Because carbon-14 content is a material claim limitation, a robust analysis should treat isotope testing as a central technical issue rather than relying only on supplier identity or manufacturing records.

References

United States Patent and Trademark Office. (n.d.). Patent Center: U.S. Patent No. 8,461,140. https://patentcenter.uspto.gov/
U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations, Orange Book. https://www.accessdata.fda.gov/scripts/cder/ob/
United States Code, 21 U.S.C. § 355(j). Abbreviated applications for new drugs.
U.S. Food and Drug Administration. (2015, April 29). FDA approves treatment for moderate to severe fat below the chin. https://www.fda.gov/
Allergan plc. (2015). Allergan completes acquisition of Kythera Biopharmaceuticals. Company release.
AbbVie Inc. (2020). AbbVie completes acquisition of Allergan. Company release.
United States Code, 35 U.S.C. § 271. Infringement of patent.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Abbvie	KYBELLA	deoxycholic acid	SOLUTION;SUBCUTANEOUS	206333-001	Apr 29, 2015	AP	RX	Yes	Yes	⤷ Start Trial	⤷ Start Trial	Y				⤷ 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	067440	⤷ Start Trial
Argentina	112325	⤷ Start Trial
Australia	2008265721	⤷ Start Trial
Brazil	PI0813140	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 8,461,140

Which drugs does patent 8,461,140 protect, and when does it expire?

Summary for Patent: 8,461,140