Details for Patent: 9,867,815

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Which drugs does patent 9,867,815 protect, and when does it expire?

Patent 9,867,815 protects GOPRELTO and NUMBRINO and is included in two NDAs.

Summary for Patent: 9,867,815

Title:	Pharmaceutical compositions and methods of using the same
Abstract:	Novel pharmaceutical compositions including cocaine hydrochloride and methods of treating patients using those pharmaceutical compositions are described.
Inventor(s):	Jeffrey M. Moshal, Michael Libman
Assignee:	Noden Pharma DAC
Application Number:	US15/470,133
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,867,815
Patent Claim Types: see list of patent claims	Use; Composition;

US Patent 9,867,815: Scope, Claims, Expiration, and Patent Landscape for Goprelto

US Patent 9,867,815 protects administration protocols for a ready-to-use 4% cocaine hydrochloride nasal anesthetic in patients with hepatic impairment, renal impairment, or advanced age. The patent does not primarily claim cocaine hydrochloride as a molecule or the composition in isolation. Its principal value is in method-of-use coverage tied to dosing conditions, pledget application, procedure duration, patient risk factors, and pharmacokinetic outcomes.

The patent was granted January 9, 2018, and has an expiration date of June 12, 2035, subject to any applicable patent-term adjustment or other statutory adjustment reflected in the USPTO or FDA records. The patent is associated with the FDA-approved product Goprelto, a 4% cocaine hydrochloride nasal solution marketed by NEXUS Pharmaceuticals. [1-4]

What drug and product does US Patent 9,867,815 protect?

The patent covers clinical use of a ready-to-use topical cocaine hydrochloride solution for anesthesia of nasal and related mucous membranes.

Attribute	Patent-linked product information
Active ingredient	Cocaine hydrochloride
Product	Goprelto
Strength	4% cocaine hydrochloride nasal solution
Commercial dosage form	Ready-to-use topical nasal solution
Typical administration vehicle	Pledgets soaked with approximately 4 mL
Contact time	Approximately 20 minutes
FDA indication	Induction of local anesthesia of the mucous membranes of the nasal cavities for diagnostic and surgical procedures
FDA approval	December 14, 2017
NDA	209963
Patent	US 9,867,815
Patent grant date	January 9, 2018
Listed patent expiration	June 12, 2035
NCE exclusivity	Five years from approval, subject to statutory exceptions

Goprelto is not a conventional systemic anesthetic product. Its commercial use depends on topical application to nasal mucosa before a diagnostic or surgical procedure. The patented claims add patient-selection and administration limitations that are particularly relevant to subjects whose cocaine exposure may be increased because of impaired hepatic or renal clearance. [2,3]

What does claim 1 of US 9,867,815 cover?

Claim 1 covers a complete clinical administration method requiring all of the following elements:

1. A hepatically impaired subject.
2. A procedure requiring local anesthesia.
3. One or more pledgets.
4. Approximately 4 mL of a ready-to-use composition.
5. Cocaine hydrochloride at approximately 3.6% to 4.4%.
6. Sodium benzoate at approximately 0.07% to 0.20%.
7. Approximately 0.125% citric acid.
8. Water.
9. An optional coloring additive.
10. Contact of each pledget with a mucous membrane for approximately 20 minutes.
11. Removal of each pledget.
12. No topical cocaine hydrochloride administration within the preceding 24 hours.

The claim is narrower than a claim directed simply to "administering 4% cocaine hydrochloride." A potentially infringing protocol would need to satisfy the composition, volume, pledget, timing, patient, and recent-use limitations.

The 24-hour limitation is commercially important. A method that uses the same product in a hepatically impaired patient but does not establish whether the patient avoided topical cocaine during the prior 24 hours may create an evidentiary issue in an infringement case. The limitation does not necessarily eliminate infringement if the absence of prior use is established through medical records, patient history, or clinical protocol.

How do claims 2 through 9 expand the procedure coverage?

Claims 2 through 9 depend from claim 1 and identify specific procedures. They cover use during:

Claim	Procedure
2	Nasal endoscopy, endoscopy with debridement, or endoscopy with polypectomy
3	Nasal endoscopy
4	Nasal laryngoscopy
5	Nasopharyngeal laryngoscopy
6	Nasal debridement
7	Intraturbinate methylprednisolone acetate injection
8	Turbinate reduction
9	Transnasal esophagoscopy

These dependent claims improve enforcement precision because they connect the patented administration method to identifiable otolaryngology procedures. A protocol used for nasal endoscopy is more directly mapped to claim 3 than to the broader procedure language of claim 1.

The claims also extend beyond purely diagnostic endoscopy. Turbinate reduction, intraturbinate steroid injection, debridement, and transnasal esophagoscopy create coverage across both office-based and procedural ENT settings.

What does claim 10 cover compared with claim 1?

Claim 10 is a separate independent claim. It covers administration before nasal endoscopy to a subject with hepatic or renal impairment.

Limitation	Claim 1	Claim 10
Hepatic impairment	Required	Hepatic or renal impairment
Renal impairment	Not in the independent claim	Required as an alternative
Nasal endoscopy	Not required	Required
Ready-to-use composition	Required	Required
Approximately 4 mL	Required	Required
Cocaine hydrochloride range	3.6%-4.4%	3.6%-4.4%
Sodium benzoate range	0.07%-0.20%	0.07%-0.20%
Citric acid	Approximately 0.125%	Approximately 0.125%
Pledgets	Required	Required
Contact time	Approximately 20 minutes	Approximately 20 minutes
Prior topical cocaine exclusion	Required by claim 1	Not expressly included
Age limitation	None	None

Claim 10 is potentially broader than claim 1 in two respects. It covers renal impairment and does not expressly include the 24-hour no-prior-use requirement. It is narrower in requiring nasal endoscopy.

From a freedom-to-operate perspective, a nasal endoscopy protocol in a renally impaired patient may implicate claim 10 even if the patient has no hepatic impairment. A protocol in a hepatically impaired patient may implicate both claim 1 and claim 10.

What are the pharmacokinetic limitations in claims 11 through 25?

Claims 11 through 18 address hepatic impairment and require specified cocaine exposure results for Child-Pugh Grade B or Grade C subjects. Claims 19 through 25 address renal impairment and include pharmacokinetic and clearance measurements.

Hepatic impairment claims

Claims 11 and 12 establish the hepatic-impaired patient category. Claims 13 and 14 narrow the population to:

• Child-Pugh Grade B subjects; or
• Child-Pugh Grade C subjects.

Claims 15 through 18 require cocaine exposure parameters to fall within 90% confidence intervals recited in Table 20:

• Cmax for Grade B subjects;
• AUClast for Grade B subjects;
• Cmax for Grade C subjects;
• AUClast for Grade C subjects.

These limitations create a technical infringement issue. A claimant would likely need clinical data, patient-specific pharmacokinetic evidence, or an established product label and study protocol to demonstrate that the claimed confidence-interval limitation is met.

Renal impairment claims

Claim 19 identifies increased systemic exposure resulting from renal impairment. Claim 20 identifies the renally impaired subject. Claim 21 narrows the subject to an estimated glomerular filtration rate of approximately 15 to 29 mL/min/1.73 m², generally corresponding to severe chronic kidney disease.

Claims 22 through 25 add Table 7 pharmacokinetic limitations:

• Cmax;
• AUClast;
• CL/F, or apparent oral clearance;
• CLr, or renal clearance.

The renal claims are technically narrower than a general renal-impairment claim. They focus on a defined eGFR range and specific pharmacokinetic outcomes. Their commercial relevance is strongest where a provider or sponsor has a renal-impairment dosing protocol that expressly follows the clinical-study population or Table 7 parameters.

What do claims 26 through 28 protect for elderly patients?

Claims 26 through 28 cover administration to subjects over 65 years old undergoing a diagnostic or surgical procedure.

Claim	Age threshold
26	Over 65
27	Over 70
28	Over 80

The elderly claims do not require hepatic or renal impairment. They also do not require nasal endoscopy. The claim set therefore reaches an older patient population undergoing a broader set of diagnostic or surgical procedures, provided the same solution, pledget, approximate 4 mL volume, 20-minute contact period, and mucous-membrane administration are used.

Claims 26 through 28 may be important for age-based clinical protocols because age alone can create a separate infringement theory even when the patient has normal renal and hepatic function.

What formulation is protected by US 9,867,815?

The claimed formulation has the following composition:

Component	Claimed amount
Cocaine hydrochloride	Approximately 3.6%-4.4%
Sodium benzoate	Approximately 0.07%-0.20%
Citric acid	Approximately 0.125%
Water	Required
Coloring additive	Optional
Volume used	Approximately 4 mL

The patent claims a method using the formulation rather than an unrestricted composition claim. That distinction matters. A manufacturer may avoid literal infringement of these claims if its formulation falls outside the claimed concentration ranges, but changing the formulation does not necessarily eliminate risk under other patents, regulatory requirements, or the doctrine of equivalents.

The term "ready-to-use" also has practical significance. A product requiring dilution, reconstitution, or compounding before administration could present a claim-construction issue. The strongest literal infringement case involves a commercially packaged solution used directly after opening.

What is the FDA and Orange Book status of US 9,867,815?

Goprelto received FDA approval in December 2017 under NDA 209963 for induction of local anesthesia of nasal mucous membranes during diagnostic and surgical procedures. [2]

The patent is associated with the approved product in FDA patent-listing records. The five-year new chemical entity exclusivity period ran from the 2017 approval date and expired in December 2022, subject to the statutory framework governing abbreviated new drug applications. After NCE exclusivity expired, an ANDA applicant could submit a Paragraph IV certification against a listed patent, assuming the applicant had an otherwise approvable generic application. [3,4]

Regulatory event	Date
FDA approval of Goprelto	December 14, 2017
NCE exclusivity expiration	December 14, 2022
US Patent 9,867,815 grant	January 9, 2018
Listed patent expiration	June 12, 2035

Patent expiry, rather than NCE exclusivity, is the principal remaining barrier associated with this patent. The patent does not create biologic exclusivity because Goprelto is a small-molecule drug, not a biologic subject to the BPCIA biosimilar pathway.

When does Goprelto lose exclusivity?

The principal patent term ends June 12, 2035. Regulatory exclusivity ended earlier, in December 2022. A generic applicant could therefore pursue an ANDA and challenge the patent before 2035, subject to the filing strategy and applicable FDA rules.

A Paragraph IV certification would require the applicant to assert that the patent is invalid, unenforceable, or not infringed. If the patent owner brought suit within the statutory period, FDA approval could be subject to a 30-month stay, unless the litigation ended earlier or the stay was otherwise modified. [4]

No biosimilar pathway applies. The relevant competitive entry route is an ANDA for a therapeutically equivalent small-molecule product or, depending on formulation and labeling, a 505(b)(2) application.

Which companies are most likely to challenge the patent?

The commercial challengers would be generic manufacturers with capabilities in:

• Sterile nasal solutions;
• Controlled cocaine hydrochloride handling;
• DEA-regulated manufacturing;
• Single-use packaging;
• FDA ANDA or 505(b)(2) development;
• Controlled-substance distribution.

The strongest generic challenge would likely target one or more of the following issues:

1. Whether the claims are obvious over prior topical cocaine anesthesia protocols and pharmacokinetic studies.
2. Whether "about" makes the concentration and volume limitations indefinite.
3. Whether the pharmacokinetic limitations are adequately supported and enabled.
4. Whether the prior-use limitation in claim 1 is enforceable and reliably proven.
5. Whether a generic product or clinical label necessarily causes performance of all method steps.
6. Whether the claims are anticipated by earlier clinical use of comparable cocaine hydrochloride pledget protocols.

The patent's method-of-use character may reduce automatic infringement risk from product sales. A generic seller could argue that the product itself does not practice a patented method. That position would be weaker if the proposed labeling instructs providers to use the product in elderly, hepatically impaired, or renally impaired subjects in the claimed manner.

How strong is the patent estate for Goprelto?

The patent is strongest in its combined protection of:

• A defined 4% cocaine hydrochloride composition;
• Pledget-based nasal administration;
• Approximately 20-minute mucosal contact;
• Specific ENT procedures;
• Hepatic and renal impairment;
• Child-Pugh classifications;
• Severe renal impairment;
• Patients over 65, 70, or 80.

Its principal weaknesses are claim specificity and proof requirements. The claims depend on several approximate parameters and, in some cases, pharmacokinetic results that may not be apparent from routine treatment records. The elderly claims are commercially broader but may face stronger obviousness arguments because age-based dosing and topical-anesthetic precautions are familiar clinical concepts.

The patent is more valuable as a blocking patent for a labeled clinical-use protocol than as a barrier to all cocaine hydrochloride products. A competitor with a different concentration, different vehicle, different administration method, or materially different instructions may have a stronger noninfringement position.

What patent litigation and settlement risks affect generic entry?

The key litigation trigger would be an ANDA containing a Paragraph IV certification to US 9,867,815. Potential remedies include an injunction, damages for induced or contributory infringement, and negotiated launch restrictions.

Settlement terms could include:

• A licensed early-entry date;
• A date-certain launch before patent expiration;
• A commitment not to market for specified impaired populations;
• Authorized generic arrangements;
• Restrictions on labeling or promotional materials;
• A covenant not to sue for selected uses.

A settlement analysis requires the identity of any ANDA filer and the terms of any filed agreement. The patent record and FDA Orange Book establish the statutory framework, but do not by themselves determine whether a private settlement exists or whether a specific company has filed a Paragraph IV challenge.

What generic launch scenarios exist before 2035?

Scenario	Commercial result
No Paragraph IV challenge	Entry generally deferred until patent expiry or a negotiated license
Paragraph IV challenge defeated	Patent remains a major barrier through June 2035
Patent invalidated	Earlier generic approval and launch become possible
Noninfringing formulation or label	Entry may proceed with reduced method-of-use risk
505(b)(2) route	Possible alternative, but patent certifications and clinical requirements remain relevant
Settlement	Launch date and restrictions depend on agreement terms
Product-only launch without claimed instructions	Potentially lower direct infringement exposure, but induced-infringement risk remains

Key Takeaways

• US Patent 9,867,815 is a method-of-use patent linked to Goprelto, not a broad cocaine molecule patent.
• The core claims require a ready-to-use approximately 4% cocaine hydrochloride solution, pledget administration, approximately 4 mL, and approximately 20 minutes of mucosal contact.
• Claims 1 through 25 focus on hepatic and renal impairment, including Child-Pugh Grade B and C subjects and eGFR of approximately 15-29 mL/min/1.73 m².
• Claims 26 through 28 protect administration to patients over 65, 70, and 80 years old.
• FDA regulatory exclusivity expired in December 2022.
• The listed patent expiration is June 12, 2035.
• The patent is most valuable against clinical protocols and labeling that expressly target impaired or elderly populations.
• Generic entry would likely involve a Paragraph IV certification, a noninfringement or invalidity strategy, a 505(b)(2) pathway, or a negotiated settlement.
• Because the claims are method claims, sale of a cocaine hydrochloride product alone does not automatically establish infringement. Labeling, instructions, provider conduct, and induced-infringement evidence are central.

FAQs About US Patent 9,867,815

Is US 9,867,815 a composition patent?

No. The claims provided are method claims. They require administration of a specified ready-to-use composition under defined clinical conditions.

Does the patent cover all topical cocaine nasal anesthesia?

No. The claims are limited by formulation ranges, pledget use, contact time, volume, patient characteristics, procedure type, and, in certain claims, pharmacokinetic parameters.

Does the patent cover Goprelto use in a patient younger than 65?

Yes, if the patient has the claimed hepatic or renal impairment and the other limitations are satisfied. The age claims do not control the entire patent.

Can a generic launch before June 12, 2035?

Potentially. Earlier entry could follow patent invalidation, a successful noninfringement position, a license, a settlement, or approval of a product and label that do not practice the claimed methods.

Is a biosimilar challenge available against Goprelto?

No. Goprelto is a small-molecule cocaine hydrochloride product. The relevant pathways are an ANDA or potentially a 505(b)(2) application, not a biosimilar application.

References

1. United States Patent and Trademark Office. (2018). U.S. Patent No. 9,867,815, methods of administering a local anesthetic.
2. U.S. Food and Drug Administration. (2017). Goprelto approval letter, NDA 209963.
3. U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations, Orange Book.
4. U.S. Food and Drug Administration. (2024). Approved drug product patent and exclusivity information.

Drugs Protected by US Patent 9,867,815

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Lxo Ireland	GOPRELTO	cocaine hydrochloride	SOLUTION;NASAL	209963-001	Dec 14, 2017		RX	Yes	Yes	9,867,815					METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN PATIENTS WITH HEPATIC IMPAIRMENT
Lxo Ireland	GOPRELTO	cocaine hydrochloride	SOLUTION;NASAL	209963-001	Dec 14, 2017		RX	Yes	Yes	9,867,815					METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN PATIENTS WITH RENAL IMPAIRMENT
Lxo Ireland	GOPRELTO	cocaine hydrochloride	SOLUTION;NASAL	209963-001	Dec 14, 2017		RX	Yes	Yes	9,867,815					METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN GERIATRIC PATIENTS
Omnivium Pharms	NUMBRINO	cocaine hydrochloride	SOLUTION;NASAL	209575-001	Jan 10, 2020		RX	Yes	Yes	9,867,815					METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN PATIENTS WITH HEPATIC IMPAIRMENT
Omnivium Pharms	NUMBRINO	cocaine hydrochloride	SOLUTION;NASAL	209575-001	Jan 10, 2020		RX	Yes	Yes	9,867,815					METHOD OF ADMINISTERING A LOCAL ANESTHETIC PRIOR TO PERFORMING A DIAGNOSTIC OR SURGICAL PROCEDURE ON A SUBJECT WITH HEPATIC OR RENAL IMPAIRMENT
Omnivium Pharms	NUMBRINO	cocaine hydrochloride	SOLUTION;NASAL	209575-001	Jan 10, 2020		RX	Yes	Yes	9,867,815					METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN GERIATRIC PATIENTS
Omnivium Pharms	NUMBRINO	cocaine hydrochloride	SOLUTION;NASAL	209575-001	Jan 10, 2020		RX	Yes	Yes	9,867,815					METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN PATIENTS WITH RENAL IMPAIRMENT