Details for Patent: 10,047,117

Which drugs does patent 10,047,117 protect, and when does it expire?

Patent 10,047,117 protects OCALIVA and is included in one NDA.

This patent has seventy-three patent family members in twenty-four countries.

Summary for Patent: 10,047,117

Title:	Preparation and uses of obeticholic acid
Abstract:	The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.
Inventor(s):	André Steiner, Heidi Waenerlund Poulsen, Emilie Jolibois, Melissa Rewolinski, Ralf Gross, Emma Sharp, Fiona Dubas-Fisher, Alex Eberlin
Assignee:	Sigma Aldrich Co Ltd , Intercept Pharmaceuticals Inc
Application Number:	US14/947,658
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,047,117
Patent Claim Types: see list of patent claims	Use; Formulation;

US Patent 10,047,117: Obeticholic Acid Form 1 Claims, Exclusivity, Litigation and Patent Landscape

US Patent 10,047,117 protects methods of treating FXR-mediated diseases with pharmaceutical formulations containing substantially pure obeticholic acid, including the amorphous Form 1 solid form and defined impurity limits. The claims are method-of-treatment claims, not broad composition claims. Their commercial value is concentrated in low-dose oral obeticholic acid products, particularly Ocaliva, and in any future FXR indication such as nonalcoholic steatohepatitis.

The patent does not independently establish FDA approval for every listed disease. Its regulatory relevance depends on the approved indication, listed patents, Orange Book use codes, and the scope of any ANDA applicant's proposed labeling.

What does US Patent 10,047,117 cover?

US 10,047,117 covers administering a pharmaceutical formulation containing approximately 1 mg to approximately 30 mg of substantially pure obeticholic acid to treat an FXR-mediated disease or condition. The independent claim requires two central technical elements:

1. Obeticholic acid in a substantially pure solid form.
2. Less than 1% chenodeoxycholic acid in that solid form.

The patent also covers narrower impurity specifications, the amorphous Form 1 material, and a glass transition temperature of 102°C to 112°C.

Claim element	Scope
Therapeutic agent	Obeticholic acid
Biological target	Farnesoid X receptor, or FXR
Dose range	About 1 mg to about 30 mg
Formulation requirement	Pharmaceutical formulation
Purity requirement	Less than 1% chenodeoxycholic acid
Solid form	Form 1, described as non-crystalline or amorphous
Form 1 thermal property	Glass transition temperature of 102°C to 112°C
Additional impurities	Limits for 6β-ethylchenodeoxycholic acid and a dimeric or ester-related impurity
Claim type	Method of treatment

The patent is narrower than a patent claiming obeticholic acid as a chemical compound. It requires the use of the specified material in treatment. A product containing obeticholic acid may therefore fall outside this patent if it uses a different solid form, exceeds the impurity thresholds, uses a dose outside the claimed range, or is not directed to a claimed treatment method.

How do claims 1 through 13 differ?

Claim 1: the principal enforceable combination

Claim 1 combines the drug, purity threshold, dose range, formulation, and therapeutic use. It is the patent's broadest independent claim.

The claim does not require a specific FXR disease. It covers treatment of an FXR-mediated disease or condition generally, subject to the formulation and purity limitations. Claim construction would likely focus on:

• The meaning of "substantially pure solid form."
• Whether "about 1 mg to about 30 mg" includes only doses within that range or reasonable equivalents.
• Whether the impurity percentages are measured by a specified analytical method.
• Whether the administered formulation must itself contain the claimed solid form.
• Whether the disease must be established as FXR-mediated at the time of infringement.

Claims 2 through 7: disease-specific narrowing

Claim 2 lists the covered diseases and conditions, including:

• Biliary atresia.
• Cholestatic liver disease.
• Chronic liver disease.
• Nonalcoholic steatohepatitis.
• Hepatitis C infection.
• Alcoholic liver disease.
• Primary biliary cirrhosis.
• Primary sclerosing cholangitis.
• Progressive liver fibrosis.
• Liver fibrosis.
• Atherosclerosis.
• Arteriosclerosis.
• Hypercholesterolemia.
• Hyperlipidemia.

Claims 3 through 7 narrow claim 2 to cholestatic liver disease, chronic liver disease, nonalcoholic steatohepatitis, primary biliary cirrhosis, and liver fibrosis, respectively.

These claims are important in Hatch-Waxman analysis because a generic applicant can attempt to omit patented indications through a section viii statement or a skinny label. The outcome depends on the Orange Book use code and whether the remaining label still induces infringement.

Claims 8 and 13: Form 1 and thermal characterization

Claim 8 limits the drug to Form 1 and describes Form 1 as non-crystalline. Claim 13 adds the glass transition temperature range of 102°C to 112°C.

These limitations create potential design-around routes. A competing manufacturer may attempt to:

• Use a crystalline polymorph.
• Use a different amorphous form with a different glass transition temperature.
• Use a formulation process that produces a material outside the claimed thermal range.
• Demonstrate that the marketed drug contains a mixture of forms rather than Form 1.

The technical effectiveness of these routes depends on whether the final drug substance converts to Form 1 during manufacturing, storage, milling, granulation, or tablet compression.

Claims 9 through 12: impurity profiles

Claims 9 through 12 impose progressively narrower limits on impurities.

Claim	Relevant limitation
9	No more than 0.5% chenodeoxycholic acid
10	No more than 0.15% 6β-ethylchenodeoxycholic acid
11	No more than 0.15% of the specified dimeric or ester-related impurity
12	Combined limits for three specified impurities, including 0% to 0.05% 6β-ethylchenodeoxycholic acid, 0% to 0.2% chenodeoxycholic acid, and 0% to 0.05% of the specified dimeric impurity

These claims create manufacturing and analytical barriers rather than only formulation barriers. A generic applicant would need to establish the impurity profile of its active pharmaceutical ingredient and determine whether the limits are assessed before formulation, after formulation, or at another point in the manufacturing process.

What is the patent expiration date for US 10,047,117?

Public patent records associate US 10,047,117 with an earliest priority chain beginning in 2009 and an estimated ordinary patent-term endpoint in approximately 2030. The operative expiration date should be confirmed against the USPTO patent-term calculation, including any patent-term adjustment, terminal disclaimer, patent-term extension, or disclaimer recorded for the relevant family member. Google Patents identifies the patent as assigned to Intercept Pharmaceuticals, Inc. and issued on August 14, 2018 (Google Patents, n.d.).

Event	Date or status
Earliest priority	2009 priority chain
Patent issued	August 14, 2018
Expected ordinary term	Approximately 2030
Patent type	Utility patent
Patent holder associated with issuance	Intercept Pharmaceuticals, Inc.
Product relevance	Obeticholic acid formulations and methods of use

A patent-term estimate should not be treated as the same as an Orange Book expiration date. FDA listing data may show a different date if the listed patent has a terminal disclaimer or a calculated patent-term adjustment.

What is the Orange Book status of US 10,047,117?

Obeticholic acid is marketed in the United States as Ocaliva, approved under NDA 207999. FDA approved Ocaliva in 2016 for primary biliary cholangitis, formerly called primary biliary cirrhosis, in specified patient populations. The approved label includes 5 mg and 10 mg tablets, which fall within the 1 mg to 30 mg range recited in US 10,047,117 (U.S. Food and Drug Administration, 2023).

US 10,047,117 is relevant to Orange Book analysis because its claims are method-of-use claims tied to diseases that overlap with Ocaliva's approved indication and investigational uses. The decisive questions are:

• Whether the patent is listed against NDA 207999.
• Which FDA use code accompanies the listing.
• Whether the code covers primary biliary cholangitis, broader cholestatic disease, or another use.
• Whether the listing remains active through the relevant ANDA filing date.
• Whether a later generic label can omit the patented use.

The FDA Orange Book, rather than the patent document alone, controls the practical Hatch-Waxman listing analysis (U.S. Food and Drug Administration, n.d.-a).

When does obeticholic acid lose exclusivity?

Ocaliva's market protection has several separate components.

Protection category	Relevance
New chemical entity exclusivity	The initial FDA exclusivity period has expired
Orphan-drug exclusivity	Relevant to the approved primary biliary cholangitis indication and its statutory period
Formulation and purity patents	Protect manufacturing specifications and product-related methods
Method-of-use patents	May delay an ANDA applicant's ability to market the patented indication
Regulatory exclusivity	Depends on the approved indication and FDA designation
Patent term	US 10,047,117 is expected to extend to approximately 2030, subject to the official term calculation

The commercial loss of exclusivity is therefore not determined by the expiration of one patent. A generic may launch for nonprotected uses if it can use a section viii statement, while a patent settlement may allow an earlier date. Conversely, a listed method patent can create litigation risk even after older compound or formulation patents expire.

Which companies are challenging Ocaliva patents?

Publicly available regulatory and patent records do not establish a definitive, publicly disclosed Paragraph IV litigation campaign against US 10,047,117 comparable to the highly litigated patent estates for major small-molecule products. No publicly confirmed generic entrant should be treated as having cleared this patent merely because the product's active ingredient is old.

Potential challengers would generally use one or more of the following positions:

1. Non-infringement because the proposed product uses a different solid form.
2. Non-infringement because the active ingredient falls outside the impurity limits.
3. Non-infringement based on a label that omits the patented indication.
4. Invalidity based on anticipation or obviousness.
5. Invalidity based on indefiniteness of terms such as "substantially pure," "about," or "non-crystalline."
6. Lack of enablement or written description for the full disease and formulation scope.

The absence of a publicly identified Paragraph IV case does not eliminate challenge risk. ANDA litigation may be filed after the notice period, resolved confidentially, or structured around other Orange Book-listed patents.

How strong is the patent estate for obeticholic acid?

US 10,047,117 has moderate claim strength with concentrated commercial value.

Strengths

• The claims target the low-dose range used by Ocaliva.
• The patent links treatment to a defined impurity profile.
• Form 1 and its thermal property create technical limitations that may be measurable in a finished product.
• The disease claims include primary biliary cholangitis and liver fibrosis-related conditions.
• Manufacturing controls may make it difficult to avoid every limitation while reproducing the reference product.

Vulnerabilities

• The claims are method claims rather than claims to the obeticholic acid molecule itself.
• Several terms may require expert analytical evidence.
• A generic manufacturer may pursue a different polymorph or amorphous form.
• A section viii strategy may remove a patented use from the label.
• Prior-art risk is potentially significant because obeticholic acid, FXR agonism, bile-acid chemistry, and liver-disease treatment were documented before the patent's priority chain.
• The claim set does not cover every dose, every formulation, or every use of obeticholic acid.

The strongest enforcement position would arise where an ANDA product uses the same active ingredient specification, exhibits the same amorphous Form 1 characteristics, falls within the claimed impurity limits, and carries a label for a covered disease.

What formulation and manufacturing barriers does the patent create?

The patent creates a three-layer technical barrier:

1. Chemical purity: control of chenodeoxycholic acid and specified side products.
2. Solid-state identity: production and preservation of non-crystalline Form 1.
3. Product use: administration at a claimed dose for a covered FXR-mediated condition.

Manufacturers would need validated methods for:

• Quantifying chenodeoxycholic acid at sub-1% levels.
• Detecting 6β-ethylchenodeoxycholic acid.
• Detecting the specified dimeric or ester-related impurity.
• Measuring the glass transition temperature.
• Distinguishing amorphous Form 1 from crystalline or mixed solid forms.

These controls may increase development and scale-up costs. They do not automatically prevent a non-infringing product because a manufacturer can pursue a different solid-state form or a different impurity profile.

How does US 10,047,117 compare with biosimilar and generic risk?

Obeticholic acid is a chemically synthesized small molecule, not a biologic. Biosimilar approval under the Public Health Service Act is therefore not the relevant pathway. A competing manufacturer would ordinarily pursue an ANDA under section 505(j) of the Federal Food, Drug, and Cosmetic Act.

The principal risks are:

• Paragraph IV certification against listed patents.
• Section viii carve-out of patented uses.
• Litigation over solid form and impurity identity.
• Substitution and labeling restrictions if the generic omits an approved indication.
• Delayed launch under a settlement agreement.
• Commercial uncertainty if the reference product's market contracts before patent expiry.

A generic can obtain approval without proving infringement. The legal exposure arises from the ANDA filing, proposed labeling, product characteristics, and the patent certifications.

What is the competitive and revenue exposure?

Ocaliva's commercial opportunity has been centered on primary biliary cholangitis. The product has not obtained US approval for nonalcoholic steatohepatitis. FDA rejected Ocaliva's NASH supplemental application in 2023, citing concerns related to efficacy and the balance of benefits and risks (U.S. Food and Drug Administration, 2023).

This limits the immediate commercial value of the broad NASH claims in US 10,047,117. The claims remain relevant to:

• Future resubmission or approval activity.
• Clinical development by the patent holder or licensees.
• Licensing of FXR programs.
• Patent disputes involving liver fibrosis or cholestatic disease.
• Foreign markets where regulatory outcomes differ.

The practical revenue exposure is therefore highest for the approved primary biliary cholangitis market and lower, but potentially substantial, for unapproved NASH and fibrosis applications.

What settlement scenarios could affect generic launch?

A patent settlement could establish an agreed generic entry date before the estimated 2030 patent expiration. Typical structures include:

• A fixed launch date.
• A license limited to selected indications.
• A royalty-bearing license.
• A supply arrangement.
• A no-challenge provision.
• A settlement conditioned on regulatory approval.

Any settlement involving an ANDA filer would require antitrust scrutiny and may be subject to FTC review. The absence of a public settlement does not prove that no commercial agreement exists; however, no specific settlement should be assumed without a filed court document, FTC record, SEC disclosure, or FDA-recognized regulatory record.

Key Takeaways

• US 10,047,117 covers treatment with low-dose, substantially pure obeticholic acid.
• The core technical limitations are less than 1% chenodeoxycholic acid, the amorphous Form 1 solid form, defined impurity limits, and a 102°C to 112°C glass transition temperature.
• The claims cover primary biliary cholangitis, cholestatic liver disease, liver fibrosis, NASH, and other FXR-mediated conditions.
• The patent is a method-of-treatment and product-quality patent, not a broad compound patent.
• The ordinary patent-term endpoint is expected to be approximately 2030, subject to the official USPTO and Orange Book calculations.
• Ocaliva's approved US indication is primary biliary cholangitis. NASH claims have greater future-development value than current approved-product value.
• Generic risk is likely to turn on Form 1 identity, impurity testing, label carve-outs, and any Paragraph IV certification.
• Obeticholic acid is subject to ANDA, not biosimilar, competition.
• The most credible design-around strategies involve a different solid form, a different impurity profile, or omission of patented uses.

FAQs About US Patent 10,047,117

Does US 10,047,117 cover Ocaliva 5 mg tablets?

Potentially. Ocaliva's 5 mg dose falls within the claimed 1 mg to 30 mg range, but infringement also depends on the solid form, impurity profile, formulation, and covered treatment indication.

Does the patent cover obeticholic acid for NASH?

The claims expressly identify nonalcoholic steatohepatitis and liver fibrosis-related conditions. That patent coverage does not mean Ocaliva is FDA-approved for NASH.

Can a generic launch before the patent expires?

Potentially, if the generic omits the patented indication, uses a noninfringing solid form or impurity profile, prevails in litigation, or obtains a license or settlement permitting earlier entry.

Is Form 1 of obeticholic acid crystalline?

The claims characterize Form 1 as non-crystalline. Claim 13 further identifies it through a glass transition temperature of 102°C to 112°C.

Does this patent protect the obeticholic acid molecule itself?

No. The asserted claims protect specified methods using defined solid-form and purity characteristics. They do not function as a general composition-of-matter claim covering every form of the obeticholic acid molecule.

References

Google Patents. (n.d.). US10047117B2: Methods of treating FXR mediated diseases using obeticholic acid. Google. https://patents.google.com/patent/US10047117B2/en

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

U.S. Food and Drug Administration. (2023). Ocaliva (obeticholic acid) prescribing information. https://www.accessdata.fda.gov/drugsatfda_docs/label/

U.S. Food and Drug Administration. (2023). FDA issues complete response letter for Ocaliva for nonalcoholic steatohepatitis. https://www.fda.gov/drugs/ drug-safety-and-availability

U.S. Patent and Trademark Office. (n.d.). Patent Center. https://patentcenter.uspto.gov/

Drugs Protected by US Patent 10,047,117

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Intercept	OCALIVA	obeticholic acid	TABLET;ORAL	207999-001	May 27, 2016		DISCN	Yes	No						TREATMENT OF PRIMARY BILIARY CHOLANGITIS (PBC)
Intercept	OCALIVA	obeticholic acid	TABLET;ORAL	207999-002	May 27, 2016		DISCN	Yes	No						TREATMENT OF PRIMARY BILIARY CHOLANGITIS (PBC)

International Family Members for US Patent 10,047,117

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2013277429
Australia	2016200832
Australia	2016375566
Australia	2017204057
Australia	2018241172
Australia	2020202405