Details for Patent: 9,233,959

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Which drugs does patent 9,233,959 protect, and when does it expire?

Patent 9,233,959 protects AUSTEDO and is included in one NDA.

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

This patent has twenty-one patent family members in ten countries.

Summary for Patent: 9,233,959

Title:	Formulations and pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
Abstract:	The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.
Inventor(s):	Andreas Sommer, Chengzhi Zhang, John Carter, John Arthur, Margaret Bradbury, Thomas Gant, Manouchehr Shahbaz
Assignee:	Auspex Pharmaceuticals Inc
Application Number:	US14/479,823
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,233,959
Patent Claim Types: see list of patent claims	Composition; Delivery; Dosage form;

United States Patent 9,233,959: Deutetrabenazine Formulation Scope, Expiration, and Generic-Entry Risk

US Patent No. 9,233,959 protects specific oral solid formulations containing d6-tetrabenazine, commonly known as deutetrabenazine. Its commercial value lies in the excipient system and dosage-form architecture rather than in a broad claim to deutetrabenazine itself. The central formulation combines mannitol, microcrystalline cellulose, povidone, polysorbate, PEG-45M, and magnesium stearate, with optional antioxidants and an aqueous film coating.

The patent presents meaningful formulation barriers for tablets that copy the disclosed composition, but it does not prevent all deutetrabenazine products. A competitor may reduce risk through a different excipient system, a different dosage form, a different coating, or a non-infringing manufacturing formulation. The claims also contain numerical inconsistencies that could affect scope, validity, and enforcement.

What does US Patent 9,233,959 protect?

US 9,233,959 is directed to pharmaceutical compositions containing d6-tetrabenazine in an oral solid dosage form. The claims focus on:

• The percentage of active ingredient and excipients;
• The total dosage-form weight;
• Specific grades or chemical identities of excipients;
• Antioxidant inclusion;
• Aqueous film coating composition; and
• Specific 6 mg, 12 mg, 15 mg, and 18 mg dosage embodiments.

Claim 1 is the principal independent composition claim. It requires all of the following:

Component	Claimed amount or identity
d6-tetrabenazine	About 2% to about 18%
Mannitol	About 60% to about 70%
Microcrystalline cellulose	About 15% to about 25%
Polyvinylpyrrolidone	About 1% to about 10%
Polysorbate	About 0.5% to about 2%
Poly(ethylene oxide) polymer	About 5% to about 20%
Magnesium stearate	About 0.5% to about 2%
Total dosage form	About 100 mg to about 1 g
Administration	Oral, solid dosage form

An accused product would generally need to satisfy every limitation of claim 1 for literal infringement. A formulation outside one required quantitative range may avoid literal infringement, although the doctrine of equivalents could remain relevant depending on the facts and the prosecution history.

How broad is the independent claim?

Claim 1 is chemically specific but numerically broad. It does not require the exact excipient grades specified in later dependent claims. For example:

• The polyvinylpyrrolidone need not expressly be the molecular-weight grade identified in claim 2.
• The polysorbate need not expressly be polysorbate 80.
• The poly(ethylene oxide) polymer need not expressly be PEG-45M.
• The claim does not require an antioxidant.
• The claim does not require a film coating.
• The claim covers dosage-form weights from approximately 100 mg to 1 g.

The claim is therefore broader than the commercial embodiments in claims 15, 19, 22, and 25. A formulation using a different grade of povidone, a different polysorbate, or another poly(ethylene oxide) polymer could still fall within claim 1 if the generic component categories and quantitative ranges are met.

The claim is not a broad claim to all deutetrabenazine tablets. A product lacking one of the required excipient classes, such as PEG-45M or polysorbate, would have a substantial non-infringement argument under the literal claim language.

What formulations are protected by the dependent claims?

The dependent claims progressively narrow the formulation and create fallback positions.

Excipient-specific claims

Claim	Limitation
2	Povidone with average molecular weight of about 58,000 and K-value of 29 to 32
3	Polysorbate is polyoxyethylene (20) sorbitan monooleate, commonly polysorbate 80
4	Poly(ethylene oxide) is PEG-45M
5	Addition of an antioxidant
6	Antioxidant is BHA or BHT
7	Addition of an aqueous film coating
8	Coating contains polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, and FD&C color additive

Claims 2 through 4 identify the excipient grades associated with the disclosed commercial formulation. These limitations may be important in an infringement case because a generic manufacturer could attempt to use the same functional excipient classes while selecting a different molecular-weight grade or different surfactant.

Dosage-strength claims

Claim 10 narrows the active ingredient to approximately 5 mg to 30 mg. Claims 11 through 14 identify approximately:

• 6 mg;
• 12 mg;
• 15 mg; and
• 18 mg.

Claims 15 through 18 cover an approximately 350 mg tablet containing 15 mg of d6-tetrabenazine. Claims 19 through 21 cover the approximately 6 mg embodiment. Claims 22 through 24 cover the approximately 12 mg embodiment. Claims 25 through 27 cover the approximately 18 mg embodiment.

These claims are directed to composition structure, not treatment method. They do not require use for Huntington's disease, tardive dyskinesia, chorea, or any other indication.

How do the disclosed formulations compare with commercial deutetrabenazine tablets?

The claims closely track the type of formulation used for oral deutetrabenazine tablets marketed as AUSTEDO. AUSTEDO contains deutetrabenazine and is approved for chorea associated with Huntington's disease and tardive dyskinesia. The FDA-approved product is a small-molecule drug, so future competition proceeds through the generic drug pathway rather than the biosimilar pathway (FDA, 2024a).

The patent's commercial relevance is strongest where a competitor seeks to duplicate:

• The 6 mg, 12 mg, or 18 mg strength;
• The approximately 350 mg tablet weight;
• The mannitol and microcrystalline-cellulose filler system;
• Povidone K29-K32;
• Polysorbate 80;
• PEG-45M;
• Magnesium stearate;
• BHA and BHT; and
• The specified aqueous film coating.

A generic manufacturer does not necessarily need to reproduce the reference product's exact qualitative formula if it can demonstrate pharmaceutical equivalence and bioequivalence using a different, non-infringing formulation.

What numerical issues affect claim scope?

The claims contain apparent internal inconsistencies.

Claim 19 and the 2% minimum

Claim 1 requires d6-tetrabenazine at approximately 2% to 18% of total dosage-form weight. Claim 19 depends from claim 1 but specifies 6 mg in a 350 mg dosage form.

Six milligrams divided by 350 mg equals approximately 1.71%, below the 2% minimum in claim 1. This creates a dependency and claim-construction issue. The patent owner could argue that the percentages are approximate, that the stated 350 mg is approximate, or that the formulation percentages are calculated on a different basis. A challenger could argue that claim 19 is technically inconsistent with claim 1 and therefore vulnerable to indefiniteness or lack of written-description support.

The issue is more pronounced because claim 19 identifies 6 mg as an express embodiment rather than merely describing a broad range.

Percentage totals

The listed ingredients in claim 15 total approximately 95.8% before accounting for the 15 mg active ingredient as a percentage of a 350 mg tablet. Adding the active ingredient at approximately 4.29% produces approximately 100.09%, which is consistent with rounding.

The claim 19 formulation totals approximately 95.2% for the listed percentages. Six milligrams in a 350 mg tablet is approximately 1.71%, producing approximately 96.91%. The same issue appears in the 12 mg and 18 mg embodiments, although rounding and unlisted material may explain part of the difference.

These discrepancies do not automatically invalidate the claims. Courts generally interpret "about" in context, and formulation percentages commonly include rounding. The discrepancies could nevertheless become relevant to claim construction, enablement, written description, or an indefiniteness challenge.

When does US 9,233,959 lose patent protection?

The patent issued on January 12, 2016. Its ordinary 20-year term is calculated from the relevant nonprovisional filing date, subject to patent-term adjustment and any applicable terminal disclaimer. Public patent records identify the patent as originating from an August 15, 2014 filing, with an August 15, 2013 priority date for the underlying disclosure (USPTO, 2016).

On that basis, the expected base expiration is in August 2034, subject to the official USPTO term calculation. The priority date does not ordinarily shorten the term to 20 years from the provisional or priority filing date. Patent-term adjustment can move the expiration date later, while a terminal disclaimer can move it earlier.

Event	Date or status
Earliest stated priority	August 15, 2013
Nonprovisional filing	August 15, 2014
Patent issued	January 12, 2016
Expected base expiration	August 2034, subject to PTA and terminal-disclaimer review
Patent type	Small-molecule formulation patent
Patent-term extension	No extension is established from the claim text alone

The patent's effective commercial life can be shorter than its statutory expiration if FDA exclusivity, Orange Book listing, litigation settlements, or a successful invalidity challenge alters generic-entry timing.

What is the Orange Book status of US 9,233,959?

US 9,233,959 is associated with the AUSTEDO deutetrabenazine product and has been treated as a formulation patent in the FDA patent-listing framework. Orange Book relevance depends on the specific approved product, dosage form, and patent use code recorded by FDA (FDA, 2024b).

An Orange Book listing does not itself establish validity or infringement. It enables an ANDA applicant to address the patent through a certification:

• Paragraph I: no patent information has been submitted;
• Paragraph II: the patent has expired;
• Paragraph III: the applicant will wait until patent expiration; or
• Paragraph IV: the patent is invalid, unenforceable, or will not be infringed.

For this patent, a Paragraph IV certification would likely focus on formulation differences, claim construction, written-description support, indefiniteness, obviousness, and the scope of the listed product claims.

Which companies are likely to challenge the patent?

Potential challengers would be manufacturers seeking an ANDA for generic deutetrabenazine. The applicable route is an ANDA, not a biosimilar application. The strongest commercial candidates are generic companies with experience in CNS drugs, complex oral formulations, and Paragraph IV litigation.

A company seeking early approval could use one of two broad strategies:

1. Challenge the patent directly through Paragraph IV certification; or
2. Design around the formulation and certify that the listed claims are not infringed.

The second strategy may be commercially attractive because claim 1 requires a relatively distinctive combination of excipient classes. A formulation omitting PEG-45M, changing the surfactant, using a different binder system, or adopting a different dosage form may avoid literal infringement.

No conclusion about a particular company's current Paragraph IV filing or litigation position follows from the claim text alone. Such status is controlled by FDA submissions, ANDA litigation complaints, docket activity, and settlement terms.

What patent litigation affects generic entry?

A Paragraph IV certification can trigger litigation under Hatch-Waxman if the patent owner files suit within the statutory period after receiving notice. Filing suit can create a 30-month stay of FDA approval, subject to statutory exceptions and court action (21 U.S.C. § 355).

The principal litigation issues for this patent would be:

• Whether the accused formulation contains every element of claim 1;
• Whether "about" permits the accused percentage ranges;
• Whether the 6 mg embodiment is consistent with the 2% lower limit;
• Whether the claimed excipient combination was obvious;
• Whether the disclosure adequately supports all claimed ranges;
• Whether the patent is enforceable; and
• Whether a formulation change avoids the claim while remaining bioequivalent.

A settlement could establish a licensed or authorized-generic entry date before the patent's nominal expiration. Settlement terms are often confidential, and a market-entry date cannot be inferred from the patent claims.

How strong is the patent estate?

The patent is strongest against a close copy of the disclosed tablet. Its strength is lower against materially different formulations.

Risk factor	Assessment
Coverage of exact commercial formulation	High
Coverage of all deutetrabenazine tablets	Low
Formulation-specific technical detail	High
Design-around difficulty	Moderate
Vulnerability from numerical inconsistencies	Moderate
Core API coverage	Not established by these claims
Method-of-use coverage	None in the supplied claims
Manufacturing-process coverage	None in the supplied claims
Biosimilar relevance	None; deutetrabenazine is a small molecule
ANDA relevance	High

The strongest claim is claim 1 because it covers a range of excipient identities and concentrations. The strongest practical fallback claims are claims 2 through 4 and claims 15 through 27, assuming the commercial product conforms to those narrower formulations. Narrow claims can be easier to prove against an exact copy but easier to design around.

Does the patent cover manufacturing methods or method of use?

No. The supplied claims do not claim:

• Synthesis of d6-tetrabenazine;
• Deuterium incorporation;
• Granulation;
• Compression;
• Coating manufacture;
• Dissolution performance;
• Treatment of Huntington's disease;
• Treatment of tardive dyskinesia; or
• A dosing regimen.

The patent may coexist with separate patents covering the active pharmaceutical ingredient, methods of treatment, polymorphs, salts, dosage regimens, extended-release formulations, or manufacturing processes. Those rights must be analyzed separately from US 9,233,959.

What generic launch scenarios exist?

Launch after patent expiration

This is the lowest litigation-risk scenario if no other blocking patent remains listed or enforceable. Market entry would be subject to ANDA approval and any applicable regulatory exclusivity.

Paragraph IV challenge and litigation

A challenger may seek approval before August 2034 by asserting non-infringement or invalidity. The commercial value of this strategy depends on the strength of the formulation design-around and the remaining market size.

Formulation design-around

A competitor may alter one or more required elements, such as:

• Replacing PEG-45M;
• Omitting polysorbate;
• Using a different binder;
• Changing the filler ratio;
• Using a capsule or alternate solid dosage form;
• Selecting a different tablet weight; or
• Eliminating the claimed antioxidant or coating system.

The formulation must still meet FDA requirements for pharmaceutical equivalence, bioequivalence, stability, dissolution, and manufacturability.

Authorized or licensed entry

A license or settlement could permit earlier entry under agreed conditions. Such an arrangement would reduce litigation uncertainty but could transfer value to the patent owner through royalties, supply terms, or delayed-entry provisions.

Key Takeaways

• US 9,233,959 is a deutetrabenazine formulation patent, not a broad patent on the active molecule.
• Claim 1 requires a specific combination of mannitol, microcrystalline cellulose, povidone, polysorbate, poly(ethylene oxide), and magnesium stearate.
• Claims 15 through 27 target approximately 350 mg tablets containing 6 mg, 12 mg, 15 mg, or 18 mg of d6-tetrabenazine.
• The patent does not claim a method of treatment, manufacturing process, or biosimilar product.
• The expected base patent expiration is August 2034, subject to official patent-term adjustment and any terminal disclaimer.
• Claim 19 appears inconsistent with claim 1 because 6 mg in a 350 mg tablet equals approximately 1.71%, below claim 1's 2% minimum.
• The patent presents a material barrier to an exact formulation copy but leaves meaningful design-around options.
• Generic competition would proceed through the ANDA and Paragraph IV framework.
• Biosimilar analysis is not applicable because deutetrabenazine is a small-molecule drug.
• Separate API, method-of-use, extended-release, polymorph, and manufacturing patents may materially change the overall entry analysis.

FAQs

Is US 9,233,959 a patent on AUSTEDO itself?

It is a patent on specified oral solid compositions containing d6-tetrabenazine. It is not, based on the supplied claims, a broad patent covering every form or use of AUSTEDO.

Does changing the tablet coating avoid infringement?

Not necessarily. The coating is optional in claim 1. Removing the coating may avoid claims 7, 8, and 17 through 27, but it would not avoid claim 1 if the uncoated core still satisfies all claim 1 limitations.

Can a generic use a different amount of PEG-45M?

A different amount may avoid literal infringement only if it falls outside the applicable range and does not remain within the scope of another claim. A product using no PEG-45M may have a stronger design-around position, although the broader generic poly(ethylene oxide) language in claim 1 must be assessed.

Does the patent block a liquid deutetrabenazine product?

The supplied claims require a solid dosage form for oral delivery. A liquid product would have a strong argument that it does not literally infringe these claims, subject to other patents and the doctrine of equivalents.

Is a 6 mg tablet necessarily covered by the patent?

Not necessarily. The 6 mg claims require the surrounding excipient system and approximately 350 mg solid dosage form. Claim 19 also presents a numerical inconsistency with claim 1's 2% active-ingredient minimum, which could affect enforceability and construction.

References

1. Food and Drug Administration. (2024a). AUSTEDO (deutetrabenazine) prescribing information. U.S. Department of Health and Human Services.

2. Food and Drug Administration. (2024b). Approved drug products with therapeutic equivalence evaluations: Orange Book. U.S. Department of Health and Human Services.

3. United States Congress. (2024). 21 U.S.C. § 355: New drugs. United States Code.

4. United States Patent and Trademark Office. (2016). United States Patent No. 9,233,959: Pharmaceutical compositions comprising d6-tetrabenazine. U.S. Department of Commerce.

Drugs Protected by US Patent 9,233,959

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Teva Branded Pharm	AUSTEDO	deutetrabenazine	TABLET;ORAL	208082-001	Apr 3, 2017		RX	Yes	No	9,233,959*PED				Y
Teva Branded Pharm	AUSTEDO	deutetrabenazine	TABLET;ORAL	208082-002	Apr 3, 2017		RX	Yes	No	9,233,959*PED				Y
Teva Branded Pharm	AUSTEDO	deutetrabenazine	TABLET;ORAL	208082-003	Apr 3, 2017		RX	Yes	Yes	9,233,959*PED				Y

International Family Members for US Patent 9,233,959

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2013318182
Australia	2018222896
Australia	2020205297
Brazil	112015005894
Canada	2883641
Canada	3124804
China	104684555