Details for Patent: 9,763,885

Which drugs does patent 9,763,885 protect, and when does it expire?

Patent 9,763,885 protects ROSZET and is included in one NDA.

This patent has eleven patent family members in ten countries.

Summary for Patent: 9,763,885

Title:	Oral tablet formulation consisting of fixed combination of rosuvastatin and ezetimibe for treatment of hyperlipidemia and cardiovascular diseases
Abstract:	The present invention is an orally consumed fixed combination formulation of both rosuvastatin and ezetimibe in one tablet that is expected to have the same Area Under Curve as two active ingredients taken together individually orally, and pharmaceutically acceptable additives suitable for the preparation. In preferred embodiments of this invention, the rosuvastatin is in the form of rosuvastatin calcium and the pharmaceutically acceptable additives are selected from diluents, disintegrants, glidants, lubricants, colorants and combinations thereof.
Inventor(s):	Marie Charmaine Dias
Assignee:	ALTHERA LIFE SCIENCES LLC
Application Number:	US14/350,905
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Dosage form;

United States Patent 9,763,885: Rosuvastatin-Ezetimibe Bilayer Tablet Patent Scope and Landscape

U.S. Patent No. 9,763,885 protects a narrowly defined rosuvastatin-ezetimibe bilayer tablet rather than the active ingredients generally. The central inventive combination requires rosuvastatin in a microcrystalline-cellulose-containing first layer and ezetimibe in a second layer that is free of microcrystalline cellulose. The claims also require specified dose ratios, bioequivalence to separately administered products, and impurity limits after accelerated stability testing.

The strongest infringement position is against a fixed-dose bilayer product that uses the claimed excipient architecture and satisfies the claimed stability and bioequivalence parameters. Separate rosuvastatin and ezetimibe tablets, single-layer combinations, and formulations placing microcrystalline cellulose in the ezetimibe layer are less likely to fall within the literal scope of claim 1.

What does U.S. Patent 9,763,885 protect?

The patent protects four related subject areas:

1. A rosuvastatin-ezetimibe bilayer pharmaceutical composition.
2. Narrower dosage and excipient formulations.
3. A manufacturing process for producing the bilayer tablet.
4. Therapeutic use of the claimed composition for lipid and cardiovascular diseases.

Claim 1 is the dominant composition claim. Claims 2 through 6 narrow that claim. Claim 7 protects a manufacturing method, claim 8 narrows the method, and claim 9 protects treatment using the claimed dosage form.

Claim	Subject matter	Principal limiting elements
1	Bilayer solid dosage form	Rosuvastatin first layer; ezetimibe second layer; second layer free of microcrystalline cellulose; specified ratios; bioequivalence; impurity limits
2	Dosage strengths	Rosuvastatin 2.5-40 mg; ezetimibe 5-20 mg
3	Enhanced stability	No ezetimibe impurities; rosuvastatin lactone and keto impurities below 0.2%
4	Rosuvastatin layer	Starch, dicalcium phosphate, microcrystalline cellulose, crospovidone and sodium stearyl fumarate ranges
5	Ezetimibe layer	Sodium lauryl sulfate, lactose, croscarmellose, povidone and magnesium stearate ranges
6	Additional rosuvastatin excipients	Butylated hydroxyanisole and fumed silica
7	Manufacturing process	Separate blending, ezetimibe dispersion, lactose adsorption, granulation, bilayer compression and coating
8	Manufacturing limitation	Sodium stearyl fumarate lubricant and sodium lauryl sulfate wetting agent
9	Treatment method	Oral administration for specified lipid and cardiovascular conditions

The patent is therefore a formulation and process patent. It does not broadly claim rosuvastatin, ezetimibe, or their coadministration independent of the claimed tablet structure.

How narrow is claim 1?

Claim 1 contains multiple cumulative limitations. A potentially infringing product must satisfy each limitation either literally or, subject to prosecution-history limits, under the doctrine of equivalents.

Structural limitations

The product must be a solid dosage form comprising:

• Two layers in a bilayer tablet.
• Rosuvastatin in a first layer.
• Ezetimibe in a second layer.
• Microcrystalline cellulose in the rosuvastatin layer.
• No microcrystalline cellulose in the ezetimibe layer.
• Ezetimibe substantially separated from the microcrystalline cellulose in the first layer.

A conventional monolithic tablet is outside the literal language of claim 1. A bilayer tablet with both active ingredients in each layer is also materially different. The claim is directed to physical segregation of the two active ingredients, with microcrystalline cellulose associated only with the rosuvastatin layer.

Ratio limitation

Claim 1 covers rosuvastatin-to-ezetimibe weight ratios of:

• 0.5:1
• 1:1
• 2:1

The ratio is based on active-ingredient weight, not total tablet weight. A formulation with a 4:1 ratio would not literally satisfy this limitation, even if the tablet otherwise used the claimed bilayer design.

Bioequivalence limitation

The tablet must be bioequivalent, when orally administered to healthy individuals, to corresponding rosuvastatin and ezetimibe doses administered separately but together.

This limitation introduces a pharmacokinetic requirement. The patent claim does not merely require that both ingredients be present. It requires comparative bioequivalence against the reference administration of the two drugs. The applicable analysis would ordinarily examine parameters such as area under the curve and maximum plasma concentration under the governing FDA bioequivalence framework. The claim language does not specify the acceptance interval, study design, number of subjects, fed or fasting conditions, or statistical method. Those omissions may create claim-construction issues in litigation. FDA regulations generally evaluate bioequivalence through comparative drug exposure measures, commonly including AUC and Cmax (21 C.F.R. § 320.23).

Stability limitation

The composition must meet accelerated stability thresholds after six weeks at 40°C and 75% relative humidity:

• Ezetimibe-related impurities below 0.5%.
• Rosuvastatin-related lactone impurities below 0.5%.
• Rosuvastatin-related keto impurities below 0.5%.

The claim does not define the analytical method, reporting threshold, impurity reference standard, or whether the percentages are measured against total drug content, labeled drug content, or a chromatographic area percentage. Those issues can materially affect infringement and validity analysis.

Which dependent claims provide the strongest additional protection?

Claims 4 through 6 create a detailed formulation profile. They are narrower than claim 1 but may be useful against products that copy the disclosed composition.

Rosuvastatin layer under claim 4

The rosuvastatin layer must contain the following excipients within the stated ranges:

Component	Claimed range
Starch	1%-15%
Dicalcium phosphate	0.5%-10%
Microcrystalline cellulose	20%-90%
Crospovidone	2%-30%
Sodium stearyl fumarate	0.1%-2%

Claim 6 adds:

Component	Claimed range
Butylated hydroxyanisole	0.05%-2%
Fumed silica	1%-10%

These percentage limitations are calculated by reference to the weight of the rosuvastatin-containing first layer. A product can avoid claims 4 and 6 by changing the concentration of a single listed excipient, while still potentially infringing claim 1.

Ezetimibe layer under claim 5

The ezetimibe layer must contain:

Component	Claimed range
Sodium lauryl sulfate	2%-20%
Lactose	20%-90%
Croscarmellose sodium	5%-30%
Polyvinylpyrrolidone	0.5%-10%
Magnesium stearate	0.2%-5%

Claim 5 is commercially important because it identifies a particular approach to ezetimibe dispersion and disintegration. Ezetimibe has poor aqueous solubility, making wetting agents, dispersion systems, granulation and particle distribution relevant to dissolution performance.

What manufacturing process is protected by claims 7 and 8?

Claim 7 protects a sequential manufacturing process:

1. Blend rosuvastatin calcium with pregelatinized starch, calcium hydrogen phosphate dihydrate, microcrystalline cellulose and crospovidone.
2. Sieve and lubricate the rosuvastatin blend.
3. Mix ezetimibe with a wetting agent and dispersing material in isopropyl alcohol and dichloromethane.
4. Absorb the ezetimibe dispersion onto lactose.
5. Air-dry and sieve the lactose-supported dispersion.
6. Blend it with croscarmellose sodium.
7. Granulate with a polyvinylpyrrolidone solution.
8. Dry the ezetimibe granules.
9. Compress both blends into a bilayer tablet.
10. Apply a film coating.

Claim 8 specifies sodium stearyl fumarate as the lubricant and sodium lauryl sulfate as the wetting agent.

The process claims are narrower than the composition claim. A manufacturer can potentially avoid literal infringement by changing the solvent system, replacing lactose, using dry granulation, eliminating the specified absorption step, or adopting a different lubricant. That does not avoid claim 1 if the resulting product independently satisfies the composition limitations.

The use of dichloromethane creates a separate manufacturing and regulatory consideration. A process using the claimed solvent must control residual solvent levels under applicable pharmaceutical quality standards. A non-infringing process may use another solvent or a different dispersion technology.

What does claim 3 add to the patent?

Claim 3 establishes tighter impurity requirements:

• No ezetimibe-related impurities after the specified storage period.
• Rosuvastatin lactone impurities below 0.2%.
• Rosuvastatin keto impurities below 0.2%.

This claim may be difficult to enforce unless the patent’s specification or prosecution record defines “no” impurity with a validated detection limit. Absolute language can create an indefiniteness dispute if ordinary analytical methods cannot establish complete absence.

The claim also requires a particular accelerated stability condition: six weeks at 40°C and 75% relative humidity. Long-term stability at normal storage conditions is not the same test. A product could satisfy the accelerated claim without having completed its full commercial shelf-life program, or fail the accelerated limitation while remaining commercially stable under labeled storage conditions.

How can a competing product avoid literal infringement?

A design-around analysis would focus on the cumulative limitations of claim 1.

Design choice	Likely literal-infringement effect
Separate rosuvastatin and ezetimibe tablets	Avoids bilayer-tablet limitation
Single-layer combination tablet	Avoids bilayer limitation
Microcrystalline cellulose in the ezetimibe layer	Conflicts with the MCC-free second-layer limitation
No microcrystalline cellulose anywhere	May avoid the requirement that rosuvastatin be formulated with MCC
Rosuvastatin-ezetimibe ratio outside 0.5:1, 1:1 or 2:1	Avoids the ratio limitation
Failure to demonstrate claimed bioequivalence	Creates a potential defense, subject to proof and claim construction
Different excipient concentrations	Avoids dependent claims 4-6, not necessarily claim 1
Different manufacturing process	Avoids claims 7-8, not necessarily claim 1
Different impurity profile	May avoid claim 1 if the product fails the specified thresholds

The most effective structural design-around is a single-layer or separate-tablet presentation. The most effective process design-around is a different ezetimibe dispersion and granulation route.

What is the likely validity risk?

The principal validity risks are obviousness, indefiniteness, written description and enablement.

Obviousness

The active ingredients were individually known, and coadministration of rosuvastatin and ezetimibe would likely have been clinically and commercially foreseeable. The validity question is whether the prior art would have motivated a skilled person to combine them in the claimed bilayer structure, with the claimed separation of microcrystalline cellulose and the claimed stability and bioequivalence results.

The patent holder’s strongest response would be evidence that the combination presented an unexpected stability problem, particularly ezetimibe degradation caused by contact with microcrystalline cellulose or incompatibility with the rosuvastatin formulation. Demonstrated stability and bioequivalence can support non-obviousness when they are tied to the claimed structural limitations rather than merely to routine optimization.

Indefiniteness

Potentially vulnerable terms include:

• “Corresponding dosages”
• “Substantially separated”
• “Stable composition”
• “No ezetimibe related impurities”
• “Related lactone impurities”
• “Related keto impurities”

The strength of an indefiniteness challenge depends heavily on the specification, analytical methods, prosecution history and industry practice.

Written description and enablement

Claims 1 and 2 cover a relatively broad range of strengths and additives, while claims 4 through 6 identify specific formulations. The patent must support the full claimed scope, including the stated ratios, dose ranges, stability performance and bioequivalence. A challenger could argue that the examples demonstrate only a limited number of embodiments.

What is the FDA and Orange Book status?

The claims alone do not establish whether U.S. Patent No. 9,763,885 is listed in the FDA Orange Book, which NDA owns the relevant product, whether the patent has been delisted, or whether a Paragraph IV certification has been filed. Orange Book status is product-specific and depends on the approved NDA, patent-listing submission and FDA publication records, not solely on the patent document (FDA, 2024a).

The patent’s subject matter is relevant to a fixed-dose rosuvastatin-ezetimibe product approved through an NDA or 505(b)(2) pathway. It is not an automatic barrier to an ANDA for rosuvastatin or ezetimibe as separate products. An ANDA applicant for a combination product would need to evaluate whether the reference product is approved as a fixed-dose tablet and whether the patent is listed against that product.

A Paragraph IV certification would require the applicant to assert that the patent is invalid, unenforceable or not infringed. If the patent owner brings suit within the statutory period, FDA approval may be subject to a 30-month stay under the Hatch-Waxman framework, subject to statutory exceptions and later court developments (21 U.S.C. § 355(j)(2)(A)(vii); 21 U.S.C. § 355(j)(5)(B)(iii)).

What patent litigation and settlement risks apply?

No litigation, settlement, or Paragraph IV event is established by the claim text. The relevant litigation questions are:

• Whether the patent is listed for an approved rosuvastatin-ezetimibe product.
• Whether an ANDA applicant has certified against it.
• Whether the patent owner has sued within the statutory period.
• Whether a court has construed the bioequivalence and stability limitations.
• Whether a settlement permits an agreed generic launch date.
• Whether the patent has been challenged in inter partes review or post-grant proceedings.

A product-specific search of FDA listing data, PACER, district court dockets, the Patent Trial and Appeal Board and USPTO assignment records is required to establish current litigation and ownership status. The supplied claim text does not establish those facts.

How strong is the patent estate?

The patent appears strongest as a blocking right against a copied bilayer formulation with the same excipient architecture. Its practical strength is lower against alternative dosage forms and formulations.

Risk category	Assessment
Separate-tablet generic	Low risk under claim 1
Single-layer fixed-dose tablet	Low to moderate risk
Bilayer tablet with MCC only in rosuvastatin layer	High risk if ratio, stability and bioequivalence match
Bilayer tablet with MCC in both layers	Lower literal risk
Product using the claimed excipients but different layer ratios	Moderate risk under claim 1; lower under claims 4-6
Alternative manufacturing process	Low risk under claims 7-8; product claims remain relevant
Biosimilar risk	Not applicable in the conventional sense because rosuvastatin and ezetimibe are chemically synthesized small molecules, not biologic products
Competing small-molecule combination	Subject to ordinary patent and regulatory review, not biosimilar interchangeability rules

The patent does not protect the active ingredients as such. Its commercial value depends on whether the market adopts the claimed fixed-dose bilayer design and whether a competing manufacturer needs to reproduce the same stability solution.

When does U.S. Patent 9,763,885 lose exclusivity?

The patent issued on September 19, 2017. The ordinary U.S. patent term is generally 20 years from the earliest effective nonprovisional filing date, subject to patent-term adjustment, patent-term extension and terminal disclaimer rules (35 U.S.C. §§ 154, 156).

The claims supplied do not identify:

• The earliest effective priority date.
• Patent-term adjustment.
• Any terminal disclaimer.
• Any patent-term extension.
• Any reissue or disclaimer affecting enforceability.

Accordingly, the exact expiration date cannot be established from the claims alone. Patent expiration should be confirmed through the USPTO patent data record and the patent’s front page before relying on it for launch planning.

Key Takeaways

• U.S. Patent 9,763,885 is a formulation patent directed to a rosuvastatin-ezetimibe bilayer tablet.
• Claim 1 requires rosuvastatin and ezetimibe in separate layers, with microcrystalline cellulose associated with the rosuvastatin layer and excluded from the ezetimibe layer.
• The claim also requires one of three active-ingredient ratios, bioequivalence to separately administered drugs, and defined accelerated-stability results.
• Claims 4 through 6 protect specific excipient ranges and provide narrower formulation positions.
• Claims 7 and 8 protect a particular ezetimibe dispersion, lactose adsorption, granulation and bilayer compression process.
• Separate tablets, single-layer tablets and formulations with different active-ingredient ratios are the principal design-around paths.
• The principal validity issues are obviousness, indefiniteness of analytical terms, and support for the full claimed dosage and stability ranges.
• Orange Book listing, Paragraph IV activity, litigation and settlement status cannot be determined from the claim text alone.
• The patent is a targeted barrier to a copied fixed-dose bilayer product, not a broad monopoly over rosuvastatin, ezetimibe or their coadministration.

FAQs

Does the patent cover a rosuvastatin tablet and an ezetimibe tablet taken together?

No. Claim 1 requires a single bilayer tablet. Separate tablets generally do not satisfy that structural limitation.

Does a rosuvastatin-ezetimibe single-layer tablet infringe the patent?

A single-layer tablet would not literally satisfy the bilayer limitation in claim 1. The assessment could change only if a court applied the doctrine of equivalents, subject to prosecution-history limits.

Is a product with microcrystalline cellulose in both layers within claim 1?

The product would face a substantial non-infringement argument because claim 1 requires the ezetimibe second layer to be free of microcrystalline cellulose and requires ezetimibe to be substantially separated from the microcrystalline cellulose in the first layer.

Are rosuvastatin and ezetimibe biosimilar products?

No. They are small-molecule active ingredients. Competing products generally proceed through generic or other small-molecule FDA pathways rather than the biosimilar pathway under the Public Health Service Act.

Can a competitor use the same excipients with a different manufacturing process?

Potentially. A different process may avoid claims 7 and 8, but it will not avoid claims 1 through 6 if the finished product still satisfies the composition, ratio, bioequivalence, stability and excipient limitations.

References

Food and Drug Administration. (2024a). Approved drug products with therapeutic equivalence evaluations. U.S. Department of Health and Human Services.

Food and Drug Administration. (2024b). Bioavailability and bioequivalence requirements. 21 C.F.R. pt. 320.

United States Congress. (2024a). 35 U.S.C. § 154: Contents and term of patent; provisional rights.

United States Congress. (2024b). 35 U.S.C. § 156: Extension of patent term.

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

U.S. Patent and Trademark Office. (2017). U.S. Patent No. 9,763,885: Rosuvastatin and ezetimibe pharmaceutical composition. Washington, DC.

Drugs Protected by US Patent 9,763,885

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Althera Pharms	ROSZET	ezetimibe; rosuvastatin calcium	TABLET;ORAL	213072-001	Mar 23, 2021		DISCN	Yes	No			Y			TREATMENT OF HYPERLIPIDEMIA
Althera Pharms	ROSZET	ezetimibe; rosuvastatin calcium	TABLET;ORAL	213072-002	Mar 23, 2021		DISCN	Yes	No			Y			TREATMENT OF HYPERLIPIDEMIA
Althera Pharms	ROSZET	ezetimibe; rosuvastatin calcium	TABLET;ORAL	213072-003	Mar 23, 2021		DISCN	Yes	No			Y			TREATMENT OF HYPERLIPIDEMIA
Althera Pharms	ROSZET	ezetimibe; rosuvastatin calcium	TABLET;ORAL	213072-004	Mar 23, 2021		DISCN	Yes	No			Y			TREATMENT OF HYPERLIPIDEMIA

Foreign Priority and PCT Information for Patent: 9,763,885

PCT Information
PCT Filed	May 01, 2013	PCT Application Number:	PCT/US2013/039018
PCT Publication Date:	November 07, 2013	PCT Publication Number:	WO2013/166117

International Family Members for US Patent 9,763,885

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Cyprus	1123091
Denmark	2844233
European Patent Office	2844233
Spain	2802252