Details for Patent: 9,561,229

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Which drugs does patent 9,561,229 protect, and when does it expire?

Patent 9,561,229 protects APONVIE and CINVANTI and is included in two NDAs.

This patent has nine patent family members in five countries.

Summary for Patent: 9,561,229

Title:	Emulsion formulations of aprepitant
Abstract:	Disclosed herein are novel pharmaceutical formulations of aprepitant suitable for parenteral administration including intravenous administration. Also included are formulations including both aprepitant and dexamethasone sodium phosphate. The pharmaceutical formulations are stable oil-in-water emulsions for non-oral treatment of emesis and are particularly useful for treatment of subjects undergoing highly emetogenic cancer chemotherapy.
Inventor(s):	Thomas B. Ottoboni, Han Han
Assignee:	Heron Therapeutics LLC
Application Number:	US15/083,071
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,561,229
Patent Claim Types: see list of patent claims	Use;

US Patent 9,561,229: Aprepitant Injectable Emulsion Claims, Exclusivity and Patent Landscape

US Patent 9,561,229 protects a narrowly defined injectable aprepitant emulsion containing egg yolk lecithin, soybean oil and sodium oleate within specified concentration and pH ranges. The patent also covers intravenous treatment of nausea and vomiting, including chemotherapy-induced nausea and vomiting. It is associated with Heron Therapeutics' CINVANTI, an FDA-approved intravenous aprepitant emulsion. The listed patent expiration date is June 3, 2032.[1][2]

What does US Patent 9,561,229 protect?

The patent has two independent composition claims and two independent method claims.

Claim group	Protected subject matter	Commercial significance
Claim 1	Injectable aprepitant emulsion with defined concentration ranges and sodium oleate at pH 7.5-9.0	Broadest composition claim
Claims 2-7	Specific aprepitant, lecithin, sucrose and ethanol concentrations	Narrower formulation fallbacks
Claim 8	Emulsion with 0.7% aprepitant and 14% egg yolk lecithin	Product-specific composition claim
Claims 9-11	Sucrose and ethanol limitations for claim 8	Narrower product formulations
Claim 12	Treatment of nausea and vomiting using the claim 1 emulsion	Independent method-of-use claim
Claims 13-16	Chemotherapy-induced nausea and vomiting, chemotherapy intensity and intravenous administration	Indication-specific method claims
Claim 17	Treatment using the claim 8 emulsion	Independent method claim linked to the narrower composition
Claims 18-21	Chemotherapy-induced nausea and vomiting and intravenous administration	Narrower method-of-use claims

The patent is directed to an emulsion formulation, not to aprepitant as a chemical compound. A product that contains aprepitant but uses a different dosage form, excipient system or pH may avoid literal infringement, subject to the full patent specification and any doctrine-of-equivalents analysis.

How do the independent composition claims operate?

What is required by claim 1?

Claim 1 requires every listed element:

1. An injectable pharmaceutical emulsion.
2. Aprepitant at 0.4 wt/wt% to 1.0 wt/wt%.
3. Egg yolk lecithin at 13 wt/wt% to 15 wt/wt%.
4. Soybean oil at 9 wt/wt% to 10 wt/wt%.
5. Sodium oleate as the pH modifier.
6. A final emulsion pH of 7.5 to 9.0.

The numerical limitations are cumulative. A formulation containing 0.7% aprepitant, 14% lecithin and 9.5% soybean oil falls within those concentration ranges if it also contains sodium oleate and has a pH between 7.5 and 9.0.

The claim does not require sucrose or ethanol. Those components appear only in dependent claims 4-7 and are not necessary for infringement of claim 1.

What is required by claim 8?

Claim 8 is narrower in its active pharmaceutical and lecithin limitations. It requires:

• 0.7 wt/wt% aprepitant;
• 14 wt/wt% egg yolk lecithin;
• 9 wt/wt% to 10 wt/wt% soybean oil;
• sodium oleate as the pH modifier; and
• pH of 7.5 to 9.0.

Claim 8 does not require sucrose or ethanol. Claims 9-11 add those limitations.

Claim 8 creates a concentrated literal-infringement risk for a competitor that copies the principal CINVANTI formulation profile. Its narrower scope may make it easier to design around than claim 1, but it can provide a stronger product-specific position where the commercial formulation uses the claimed 0.7% aprepitant and 14% lecithin concentrations.

What formulation ranges are protected?

The principal formulation ranges are as follows:

Component or parameter	Claim 1 range	Claim 8 range	Legal relevance
Aprepitant	0.4%-1.0%	Exactly 0.7%	Claim 1 has broader numerical coverage
Egg yolk lecithin	13%-15%	Exactly 14%	Claim 1 reaches more formulations
Soybean oil	9%-10%	9%-10%	Common limitation
Sodium oleate	Required	Required	Must be the pH modifier
pH	7.5-9.0	7.5-9.0	Required in both claims
Sucrose	Not required	Not required	Added by claims 4, 5 and 9
Ethanol	Not required	Not required	Added by claims 6, 7, 10 and 11

How do the dependent formulation claims narrow the estate?

Claims 2 and 3 narrow claim 1 to 0.7% aprepitant and 14% lecithin, respectively. Claim 5 narrows the sucrose content to 5%, while claim 4 covers 3%-8% sucrose.

Claims 6 and 7 address ethanol. Claim 6 covers 2%-6% ethanol. Claim 7 covers less than 6% ethanol. Because the ranges overlap, a formulation with 3% ethanol can fall within both claims 6 and 7, assuming it meets the other limitations.

For the claim 8 branch, claim 9 requires 5% sucrose. Claim 10 covers 2%-6% ethanol, and claim 11 covers less than 4% ethanol. The claim 11 limitation is narrower than claim 7 and excludes formulations containing 4% or more ethanol.

A formulation containing neither sucrose nor ethanol can still infringe claims 1 or 8 if all independent-claim elements are present.

What method-of-use patents does US 9,561,229 provide?

Claims 12 and 17 independently cover treating nausea and vomiting by administering the claimed emulsion. Claims 13-15 and 18-20 narrow the indication to chemotherapy-induced nausea and vomiting associated with:

• highly emetic chemotherapy; or
• moderately emetic chemotherapy.

Claims 16 and 21 specify intravenous administration.

The method claims are commercially important because they track the clinical use of intravenous aprepitant for prevention of acute and delayed chemotherapy-induced nausea and vomiting. A competitor may face method-claim exposure even if it disputes the scope of the formulation claims, particularly where the product labeling directs intravenous use for chemotherapy-induced nausea and vomiting.

The claims are treatment claims under US patent law. They generally require administration of an emulsion meeting the incorporated composition limitations. A product that is administered for a different indication could present a different method-of-use analysis, but it would not automatically avoid the composition claims.

When does US Patent 9,561,229 lose exclusivity?

Event	Date or status
Patent number	US 9,561,229 B2
Patent title	Injectable emulsion formulations of aprepitant
Patent holder associated with commercial product	Heron Therapeutics, Inc.
Grant date	January 24, 2017
FDA product linked to the formulation	CINVANTI, NDA 210821
Listed patent expiration	June 3, 2032
Patent term extension	No extension is reflected in the cited Orange Book record
Patent status	Unexpired through the listed expiration date, subject to terminal disclaimer, maintenance, validity and litigation events

The effective commercial exclusivity date may differ from the statutory expiration date if a generic applicant obtains approval through a Paragraph IV pathway, settles with the patent holder, wins an invalidity or noninfringement decision, or launches at risk.

What is the Orange Book status of CINVANTI?

CINVANTI is an FDA-approved injectable emulsion containing aprepitant. FDA approved the product on November 20, 2017, under NDA 210821.[2] It is administered intravenously for prevention of acute and delayed nausea and vomiting associated with highly emetogenic chemotherapy and prevention of nausea and vomiting associated with moderately emetogenic chemotherapy.[2]

The Orange Book identifies US 9,561,229 in connection with CINVANTI and lists a June 3, 2032 expiration date.[1] The listing connects the commercial product to the formulation and method-of-use claims described above.

Unlike a biologic, CINVANTI does not generate a biosimilar pathway. A competing aprepitant product would generally be evaluated as a small-molecule drug under the applicable abbreviated new drug application or 505(b)(2) framework. The relevant challenge is therefore generic or follow-on drug competition, not biosimilar substitution.

How strong is the patent estate for CINVANTI?

The strength of US 9,561,229 is concentrated rather than broad.

Strengths

• The patent combines active ingredient concentration, lipid excipients, pH modifier and pH range in a single formulation claim.
• Claim 1 covers a meaningful formulation window rather than one exact composition.
• Claims 8-11 provide narrower fallbacks directed to the likely commercial concentration.
• Method claims track the principal FDA-approved chemotherapy indications.
• Sodium oleate is expressly required, which can make a copied formulation easier to identify analytically.
• The patent covers the emulsion itself, reducing dependence on method-of-use enforcement.

Potential limitations

• The claims do not cover all aprepitant formulations.
• A formulation using a different pH modifier may avoid literal infringement.
• A competitor could examine alternative lipid systems, different lecithin sources, non-emulsion dosage forms or materially different concentration ranges.
• The claims do not, on their face, cover oral aprepitant, fosaprepitant or every injectable aprepitant dosage form.
• The numerical boundaries create possible design-around opportunities, although a formulation outside a claimed range may still raise equivalents or validity issues depending on the prosecution record and technical differences.

The strongest risk zone is an injectable emulsion using sodium oleate, egg yolk lecithin near 14%, soybean oil at 9%-10%, aprepitant near 0.7% and pH within 7.5-9.0.

How does CINVANTI compare with EMEND and fosaprepitant?

Product	Active ingredient	Dosage form	Primary patent issue
CINVANTI	Aprepitant	Injectable emulsion	US 9,561,229 formulation and method claims
EMEND oral	Aprepitant	Oral capsule or oral suspension	Separate compound, formulation and use patents
EMEND for Injection	Fosaprepitant dimeglumine	Lyophilized injectable product	Fosaprepitant prodrug and formulation estate
Generic aprepitant injection	Aprepitant	Follow-on injectable product	Potential formulation and method-of-use challenges

Fosaprepitant is a prodrug of aprepitant and is chemically distinct from the emulsion formulation claimed in US 9,561,229. A fosaprepitant product would not automatically infringe the aprepitant emulsion claims because it does not necessarily contain the claimed active ingredient or emulsion system.

The competitive overlap is clinical, not necessarily claim-based. CINVANTI and fosaprepitant products compete for intravenous antiemetic use in oncology, while oral aprepitant products compete through a different delivery route.

Which companies are challenging US 9,561,229?

The cited FDA and patent records do not identify a confirmed Paragraph IV challenger, court judgment or settlement specifically directed to US 9,561,229. The absence of an identified challenge does not eliminate future risk. A generic applicant could challenge the patent through an ANDA certification, while a 505(b)(2) applicant could pursue a different regulatory and patent strategy.

The principal competitive pathways are:

1. A direct injectable aprepitant emulsion with a Paragraph IV certification.
2. A 505(b)(2) product using a modified emulsion or excipient system.
3. An intravenous fosaprepitant product competing clinically but outside the literal scope of the claims.
4. A formulation designed around sodium oleate, lecithin concentration, soybean oil concentration or pH.

What generic launch scenarios exist?

Scenario 1: Launch after patent expiration

A generic or follow-on product could launch after June 3, 2032, assuming FDA approval and no other blocking patents or regulatory exclusivities.

Scenario 2: Paragraph IV challenge

An ANDA applicant could allege that US 9,561,229 is invalid, unenforceable or not infringed. A patent-holder suit under the Hatch-Waxman framework could trigger a 30-month stay of approval, subject to statutory exceptions and litigation outcomes.[3]

Scenario 3: Design-around launch

A competitor could pursue a product that changes one or more claim elements, such as:

• replacing sodium oleate;
• using a different lipid or lecithin source;
• moving outside the claimed soybean oil range;
• using a different aprepitant concentration;
• changing the pH outside 7.5-9.0; or
• using a non-emulsion injectable formulation.

A design-around would need to account for other patents, FDA comparability requirements, stability, particle size, safety and manufacturing performance.

Scenario 4: Risk-adjusted launch before expiration

An applicant could launch before patent expiry after an invalidity or noninfringement decision, a settlement permitting an earlier entry date, or an at-risk decision. The commercial exposure would include damages, injunction risk and potential supply disruption.

What manufacturing and geographic barriers matter?

The patent claims a finished injectable emulsion, but manufacturing know-how may create a separate barrier. Relevant technical controls include emulsion particle-size distribution, sterilization, aseptic processing, lecithin quality, sodium oleate control, pH adjustment, ethanol handling and container compatibility.

US 9,561,229 is a US patent. It does not by itself establish protection in Europe, Japan, China, Canada or other jurisdictions. International protection must be assessed family member by family member. A competitor could face separate formulation patents, process patents, regulatory exclusivities or trade-secret barriers outside the United States.

The patent’s geographic value is highest in the US market because the Orange Book listing can affect ANDA approval timing. Foreign market exposure depends on corresponding national patents and local regulatory rules.

What is the revenue exposure from US 9,561,229?

The patent protects the formulation underlying CINVANTI, so its economic exposure is tied to CINVANTI sales in the US intravenous antiemetic market. Public company reporting generally does not isolate revenue attributable solely to one patent claim. Patent value therefore depends on:

• CINVANTI’s US net sales;
• the share of patients receiving intravenous aprepitant rather than fosaprepitant;
• hospital and oncology-clinic contracting;
• generic or follow-on entry timing;
• the availability of non-infringing injectable alternatives; and
• the number and strength of unexpired companion patents.

The highest-value period is the period before June 3, 2032, particularly if the patent remains the principal listed barrier to an ANDA-based injectable aprepitant competitor.

Key Takeaways

• US 9,561,229 is a formulation and method-of-use patent for injectable aprepitant emulsions.
• Claim 1 is the principal broad composition claim, covering 0.4%-1.0% aprepitant, 13%-15% egg yolk lecithin, 9%-10% soybean oil, sodium oleate and pH 7.5-9.0.
• Claim 8 is narrower and targets 0.7% aprepitant and 14% egg yolk lecithin.
• Sucrose and ethanol are optional at the independent-claim level but appear in dependent claims.
• Claims 12-21 cover treatment of nausea and vomiting, especially chemotherapy-induced nausea and vomiting, by intravenous administration.
• The patent is listed for CINVANTI and has a reported expiration date of June 3, 2032.
• Fosaprepitant products compete clinically but are not automatically within the aprepitant emulsion claims.
• The main generic risk is a Paragraph IV challenge or a formulation design-around using a different pH modifier, lipid system or concentration profile.

FAQs About US Patent 9,561,229

Does US 9,561,229 cover oral aprepitant?

No. The asserted claims require an injectable pharmaceutical emulsion. Oral capsules, tablets and oral suspensions are outside the literal scope of these claims.

Does a product without sodium oleate infringe claim 1?

A product lacking sodium oleate would not meet the express sodium oleate limitation of claim 1. Infringement would still require analysis of equivalents and the patent’s prosecution history.

Is fosaprepitant covered by this patent?

Not automatically. Fosaprepitant is a prodrug and may not satisfy the claims requiring aprepitant in the specified injectable emulsion.

Can a generic use 0.7% aprepitant with a different pH?

A product outside the 7.5-9.0 pH range would not literally satisfy the pH limitation in claims 1 and 8. Other patents, regulatory requirements and equivalents analysis could remain relevant.

What is the principal infringement risk for a CINVANTI competitor?

The highest risk arises from an intravenous aprepitant emulsion containing sodium oleate, approximately 0.7% aprepitant, approximately 14% egg yolk lecithin, 9%-10% soybean oil and a pH of 7.5-9.0.

References

1. U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book.
2. U.S. Food and Drug Administration. (2017, November 20). CINVANTI approval package, NDA 210821.
3. U.S. Congress. (1984). Drug Price Competition and Patent Term Restoration Act of 1984, 21 U.S.C. § 355(j).
4. United States Patent and Trademark Office. (2017). U.S. Patent No. 9,561,229, Injectable emulsion formulations of aprepitant.

Drugs Protected by US Patent 9,561,229

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Heron Theraps Inc	APONVIE	aprepitant	EMULSION;INTRAVENOUS	216457-001	Sep 16, 2022		RX	Yes	Yes			Y			A METHOD OF ADMINISTERING APREPITANT FOR PREVENTION OF POST-OPERATIVE NAUSEA AND VOMITING
Heron Theraps Inc	CINVANTI	aprepitant	EMULSION;INTRAVENOUS	209296-001	Nov 9, 2017		RX	Yes	Yes			Y			TREATMENT OF NAUSEA AND VOMITING, INCLUDING THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY OR MODERATELY EMETOGENIC CANCER CHEMOTHERAPY

International Family Members for US Patent 9,561,229

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
China	106852118
European Patent Office	3193830
Japan	2017533183
Japan	2019196398