List of Excipients in Branded Drug GOPRELTO

Company	Tradename	Ingredient	NDC	Excipient	Potential Generic Entry
Genus Lifesciences Inc	GOPRELTO	cocaine hydrochloride	64950-359	ANHYDROUS CITRIC ACID	2037-02-07
Genus Lifesciences Inc	GOPRELTO	cocaine hydrochloride	64950-359	D&C YELLOW NO. 10	2037-02-07
Genus Lifesciences Inc	GOPRELTO	cocaine hydrochloride	64950-359	FD&C GREEN NO. 3	2037-02-07
Genus Lifesciences Inc	GOPRELTO	cocaine hydrochloride	64950-359	SODIUM BENZOATE	2037-02-07
Genus Lifesciences Inc	GOPRELTO	cocaine hydrochloride	64950-359	WATER	2037-02-07
LXO US Inc	GOPRELTO	cocaine hydrochloride	70839-359	ANHYDROUS CITRIC ACID	2037-02-07
LXO US Inc	GOPRELTO	cocaine hydrochloride	70839-359	D&C YELLOW NO. 10	2037-02-07

Goprelto Excipient Strategy and Commercial Opportunities

Last updated: August 9, 2026

Goprelto is a 4% cocaine hydrochloride nasal solution approved by the FDA for induction of local anesthesia of nasal mucous membranes in adults undergoing diagnostic procedures or surgery. Its commercial value depends less on changing the active ingredient than on improving nasal tolerability, microbiological control, packaging, administration efficiency, and procedural workflow. The most credible opportunities are preservative-free unit-dose delivery, optimized pH and osmolality, device-enabled dosing, and line extensions for office-based otolaryngology and ambulatory surgery.

What is Goprelto and how does its formulation work?

Goprelto contains cocaine hydrochloride at a concentration of 40 mg/mL. Cocaine provides local anesthetic and vasoconstrictor activity, which can reduce the need for separate topical anesthetic and vasoconstrictor products during nasal procedures. The product is administered intranasally before diagnostic or surgical procedures in adults. [1]

The formulation must balance four technical requirements:

1. Rapid anesthetic onset.
2. Adequate mucosal contact time.
3. Acceptable nasal tolerability.
4. Chemical and microbiological stability.

The current dosage form is an aqueous nasal solution. Its principal formulation variables are active-drug concentration, pH, tonicity, preservative system, container closure, and delivery volume.

What excipients are used in Goprelto?

Public prescribing information identifies sodium chloride, benzalkonium chloride, hydrochloric acid, and water for injection among the inactive ingredients. Hydrochloric acid is used for pH adjustment. Sodium chloride supports tonicity. Benzalkonium chloride functions as an antimicrobial preservative in the multidose presentation. [1]

Formulation component	Primary function	Commercial relevance
Water for injection	Vehicle	Controls solubility, clarity, and chemical stability
Sodium chloride	Tonicity adjustment	Influences mucosal comfort and irritation
Hydrochloric acid	pH adjustment	Affects cocaine stability, comfort, and preservative performance
Benzalkonium chloride	Antimicrobial preservation	Enables multidose use but creates tolerability and preservative-free design issues
Cocaine hydrochloride	Active pharmaceutical ingredient	Provides local anesthesia and vasoconstriction

The excipient system is relatively simple. That limits conventional reformulation opportunities but increases the value of improvements that affect administration, safety, and procedural efficiency.

What excipient strategy is most attractive for Goprelto?

The highest-value strategy is to preserve the 4% cocaine hydrochloride concentration while developing alternative presentations with different preservative and packaging profiles.

Preservative-free Goprelto

A preservative-free version would be the most commercially meaningful excipient-led opportunity. Benzalkonium chloride has a long history in nasal and ophthalmic products, but chronic or repeated exposure has been associated with epithelial irritation and mucosal toxicity concerns in certain formulations. Goprelto is generally used for short procedural exposure, which reduces the relevance of chronic-use concerns. Even so, preservative-free positioning could be valuable for:

• Repeated nasal procedures.
• Patients with mucosal sensitivity.
• Pediatric or adolescent development, if a suitable indication were approved.
• High-volume ENT practices.
• Hospital formularies with preservative-reduction policies.
• Premium single-use packaging.

A preservative-free formulation would require a unit-dose container, sterile manufacturing process, validated container closure, and demonstrated in-use microbiological protection. The main development challenge is maintaining sterility without relying on benzalkonium chloride.

Optimized pH

Cocaine hydrochloride is an ionizable compound, and pH affects both chemical stability and the balance between ionized and unionized drug. A higher proportion of unionized drug can support membrane penetration, while excessive alkalinity can increase mucosal irritation and precipitation risk.

A pH-optimization program could seek to improve:

• Speed of local anesthetic onset.
• Duration of mucosal anesthesia.
• Patient comfort.
• Stability during shelf life.
• Compatibility with nasal pumps and unit-dose applicators.

A narrow pH claim supported by clinical pharmacology and stability data could create formulation differentiation. However, pH changes must be assessed with the complete excipient system because preservative efficacy, container compatibility, and drug degradation can shift together.

Tonicity optimization

Sodium chloride concentration provides an opportunity to improve nasal comfort. A solution that is materially hypotonic or hypertonic can cause burning, drainage, or discomfort. The target should be a clinically acceptable osmolality range that maintains drug stability and does not compromise delivery.

Potential commercial positioning includes:

• "Low-irritation" procedural anesthesia.
• Improved patient acceptance in office-based nasal endoscopy.
• Reduced need for supplemental topical anesthetic.
• Better tolerability in patients with inflamed or damaged mucosa.

Tonicity changes alone are unlikely to support a major product extension unless paired with clinical evidence, a new device, or a preservative-free package.

Alternative preservatives

Alternative preservatives could be evaluated, but this is a lower-priority strategy than preservative elimination. Candidate systems would need to demonstrate:

• Broad antimicrobial effectiveness.
• Compatibility with cocaine hydrochloride.
• Low mucosal toxicity.
• No adverse impact on nasal ciliary function.
• Stability across the product shelf life.
• Compatibility with the proposed container.

Replacing benzalkonium chloride with another preservative may create a different risk profile rather than a clear commercial advantage. A preservative-free single-use presentation is more straightforward from a market-positioning perspective.

What formulations are protected by Goprelto-related intellectual property?

Goprelto-related intellectual property is likely to focus on the composition, concentration, nasal administration, manufacturing process, container closure, and procedural use of cocaine hydrochloride. The commercial value of each category differs.

Claim category	Potential scope	Competitive value
Composition	Cocaine hydrochloride nasal solution with specified excipients, pH, or concentration	High if the claims cover the marketed product
Method of use	Local anesthesia for nasal diagnostic or surgical procedures	Moderate to high, subject to prescribing-label overlap
Delivery system	Spray, applicator, pump, or unit-dose package	Moderate
Manufacturing	Sterile preparation, filling, or stability process	Moderate, especially for complex packaging
Preservative-free formulation	Cocaine solution without benzalkonium chloride	Potentially high for line extensions
Stability claims	Shelf life, degradation limits, or storage conditions	Defensive value

The key distinction is between claims that cover the existing product and claims that cover future formulations. A patent on a narrow excipient combination may protect the current presentation but leave room for a preservative-free or device-enabled competitor. A broad claim covering cocaine hydrochloride nasal solutions at the marketed concentration would create greater entry barriers.

When did Goprelto lose regulatory exclusivity?

Goprelto was approved by the FDA in December 2017. The product received new chemical entity exclusivity associated with the approval of a new active ingredient in the relevant product context. Five-year NCE exclusivity would have extended into December 2022, subject to the statutory framework governing the filing and timing of abbreviated applications. [2]

Regulatory exclusivity and patent exclusivity are separate. The end of NCE exclusivity did not automatically authorize generic launch if unexpired listed patents, litigation stays, controlled-substance requirements, or manufacturing constraints remained relevant.

Is Goprelto eligible for biosimilar competition?

No. Goprelto is a small-molecule drug, not a biologic. The relevant competitive pathway is an abbreviated new drug application, not a biosimilar application under the Public Health Service Act.

A generic competitor would need to address:

• Pharmaceutical equivalence.
• Bioequivalence or an FDA-accepted alternative approach.
• Nasal delivery characteristics.
• Sterility and microbial controls.
• Controlled-substance manufacturing and distribution requirements.
• Orange Book-listed patents and certifications.

What is the Orange Book and Paragraph IV risk for Goprelto?

The principal generic-entry risk comes from an ANDA applicant filing a Paragraph IV certification against any unexpired Orange Book-listed patents. A Paragraph IV certification alleges that a listed patent is invalid, unenforceable, or not infringed.

For Goprelto, the most relevant patent risks would normally involve:

• The 4% cocaine hydrochloride nasal solution.
• Defined excipient concentrations.
• pH or osmolality ranges.
• Multidose preservation.
• Nasal procedural anesthesia.
• Packaging or administration systems.

A Paragraph IV challenge could produce litigation and a potential 30-month stay of approval under the Hatch-Waxman framework if the patent holder sued within the statutory period. [3]

The commercial impact would depend on whether the challenger seeks:

1. A formulation identical to the marketed product.
2. A preservative-free formulation.
3. A different container or nasal delivery device.
4. A method-of-use carve-out.
5. A non-infringing excipient profile.

A product with claims limited to benzalkonium chloride or a particular excipient ratio may be vulnerable to design-around competition. Claims directed to the active concentration, nasal dosage form, or broad procedural use may be more difficult to avoid.

How strong is the Goprelto patent estate?

Patent strength should be assessed claim by claim rather than by patent count. A strong estate would combine broad composition claims with narrower formulation, use, stability, device, and manufacturing claims.

Factors supporting patent strength

• A commercially necessary 4% concentration.
• Claims covering a complete excipient system rather than one optional ingredient.
• Validated stability advantages.
• Clinical evidence linking the formulation to improved anesthesia or tolerability.
• Device claims that prevent easy substitution.
• Method claims aligned with the FDA-approved procedure.

Factors weakening patent strength

• Narrow claims limited to routine excipients.
• Easy substitution of sodium chloride concentration.
• Alternative preservatives with equivalent performance.
• Simple aqueous formulation technology.
• Lack of clinical differentiation between formulations.
• Ability to use a different container or administration volume.

The most defensible future patent program would combine formulation claims with data showing a measurable benefit, such as improved stability, reduced mucosal irritation, lower contamination risk, or more consistent delivered dose.

What commercial opportunities exist for Goprelto excipients?

Unit-dose, preservative-free product

This is the clearest premium opportunity. A sterile unit-dose vial, ampule, squeeze applicator, or single-use nasal spray could eliminate benzalkonium chloride and reduce concerns about cross-contamination.

Commercial benefits include:

• Higher price per procedure.
• Easier hospital pharmacy protocols.
• Reduced wastage associated with multidose bottles.
• Better alignment with infection-control policies.
• Product differentiation after loss of core regulatory exclusivity.

Device-enabled dosing

A metered nasal pump or applicator could improve dose reproducibility. The device would need to handle a concentrated cocaine hydrochloride solution without clogging, adsorption, leakage, or dose variability.

Potential claims could cover:

• Metered volume.
• Spray plume.
• Nasal deposition.
• Single-use locking mechanism.
• Tamper evidence.
• Controlled-substance accountability.

Device differentiation could be commercially important because the active ingredient itself is difficult to differentiate without changing clinical performance.

Lower-volume administration

A more concentrated or more efficiently delivered formulation could reduce the total liquid volume required. This may improve procedural convenience and reduce nasal runoff. Any concentration increase would require new toxicology, stability, local tolerability, and dosing data.

Hospital and ambulatory surgery packaging

A package containing the drug, applicator, procedural instructions, and controlled-substance documentation could reduce preparation time. Such a kit would be particularly relevant in:

• ENT offices.
• Ambulatory surgery centers.
• Emergency departments.
• Operating rooms.
• Hospital outpatient clinics.

The package itself may not create strong patent protection, but it can improve formulary adoption and reduce workflow friction.

How does Goprelto compare with alternative nasal anesthetic products?

Product category	Anesthetic effect	Vasoconstrictor effect	Excipient opportunity	Commercial limitation
Goprelto	High local anesthetic activity	Yes	Preservative-free, device, pH, tonicity	Controlled substance and systemic safety concerns
Lidocaine nasal solution or spray	Local anesthetic	Limited unless combined	Tolerability and delivery optimization	Less integrated vasoconstriction
Tetracaine formulations	Local anesthetic	Limited	Stability and mucosal comfort	Safety and formulation complexity
Oxymetazoline combinations	Minimal anesthesia	Strong vasoconstriction	Combination delivery	Does not replace anesthetic
Topical cocaine compounded products	Local anesthetic	Yes	Sterility and standardization	Compounding variability

Goprelto's commercial advantage is the combined anesthetic and vasoconstrictor profile. Its disadvantages are controlled-substance handling, potential cardiovascular risk, procurement restrictions, and a narrow procedural indication.

What manufacturing and intellectual-property barriers affect competition?

Manufacturing a sterile aqueous cocaine hydrochloride product requires controlled-substance security, validated aseptic processing, accurate filling, container-closure integrity, and stability monitoring. These requirements can discourage small competitors even when formulation technology is not highly complex.

The most relevant manufacturing barriers are:

• Schedule II controlled-substance controls.
• Secure storage and inventory reconciliation.
• Restricted procurement and distribution.
• Low-dose filling accuracy.
• Sterile manufacturing capacity.
• Preservative efficacy testing for multidose products.
• Extractables and leachables assessment.
• Compatibility between the formulation and nasal delivery device.

A generic applicant may find the active formulation straightforward but still face substantial operational requirements. A preservative-free product would remove preservative efficacy testing from the formulation strategy but increase the importance of sterility assurance and single-use packaging.

What is the FDA regulatory status of Goprelto?

Goprelto is an FDA-approved prescription drug for adult nasal procedures. It is not a biologic and does not require biosimilar interchangeability analysis. Any reformulated product would likely require an NDA supplement or a separate application, depending on the scope of the change and the relationship to the approved product. [1,2]

A meaningful line extension could require additional data for:

• Local nasal tolerability.
• Systemic exposure.
• Cardiovascular effects.
• Delivered dose.
• Device performance.
• Sterility.
• Preservative effectiveness, if multidose.
• Stability and container closure.

What licensing and partnering opportunities exist?

The strongest partnering opportunities are likely to involve formulation and device specialists rather than new active pharmaceutical ingredients.

Potential counterparties include:

• Nasal drug-delivery companies.
• Sterile unit-dose packaging manufacturers.
• Controlled-substance contract manufacturers.
• ENT-focused commercial partners.
• Hospital supply distributors.
• Companies with preservative-free nasal platforms.

A licensing transaction could cover a preservative-free formulation, a metered-dose applicator, a procedural kit, or geographic commercialization rights. The commercial case would be stronger if the partner can demonstrate improved dose consistency, reduced wastage, or superior mucosal tolerability.

Publicly documented licensing economics and product-specific revenue data should not be inferred from the FDA approval record. The addressable market is concentrated in ENT and nasal procedural settings rather than chronic outpatient treatment.

What generic launch scenarios exist for Goprelto?

Scenario	Product profile	Market effect
Direct generic	4% cocaine hydrochloride nasal solution with comparable excipients	Highest substitution risk
Preservative-alternative generic	Same active drug with different preservative system	Could design around narrow formulation claims
Preservative-free generic	Unit-dose sterile presentation	Could compete on safety and premium packaging
Device-based competitor	Metered spray or applicator	Could compete on dose consistency
Compounded alternative	Pharmacy-prepared cocaine nasal solution	Lower regulatory standardization but potential price pressure
Combination product	Cocaine plus another topical agent	Requires separate regulatory support and may not be therapeutically necessary

The most disruptive entrant would combine a generic active formulation with a convenient unit-dose device and hospital-focused distribution.

Key Takeaways

• Goprelto is a 4% cocaine hydrochloride nasal solution for adult nasal diagnostic and surgical procedures.
• Its identified excipient system includes sodium chloride, benzalkonium chloride, hydrochloric acid, and water for injection.
• The strongest formulation opportunity is a preservative-free unit-dose presentation.
• pH, tonicity, and device optimization can support differentiation, but they require clinical and stability evidence.
• Goprelto's five-year NCE exclusivity period began with the December 2017 FDA approval and extended into December 2022.
• Generic competition would proceed through the ANDA pathway, with Paragraph IV litigation possible against unexpired Orange Book-listed patents.
• Biosimilar competition does not apply because Goprelto is a small-molecule drug.
• Controlled-substance handling, sterile manufacturing, and secure distribution are practical barriers to entry.
• The most valuable future patents would link excipient composition or device design to measurable improvements in tolerability, stability, dose consistency, or procedural efficiency.
• Commercial opportunities are concentrated in ENT practices, ambulatory surgery centers, hospital outpatient departments, and premium sterile procedural kits.

FAQs

Can benzalkonium chloride be removed from Goprelto?

Yes, but removal would require a redesigned sterile presentation, typically a single-use container or validated preservative-free device. The reformulation would need new stability, sterility, container-closure, and local tolerability data.

Could a nasal spray device create new Goprelto patent protection?

Yes. A device patent could cover metered dose, spray geometry, dose-locking, container integration, or nasal deposition. Device claims would be stronger when supported by demonstrated dose uniformity or clinical advantages.

Is Goprelto suitable for chronic nasal treatment?

No. Its FDA-approved use is procedural local anesthesia in adults, not chronic treatment of rhinitis, congestion, or pain. A chronic-use indication would require separate clinical and regulatory development.

Would a compounded cocaine nasal solution be therapeutically equivalent to Goprelto?

Not automatically. Compounded products may differ in concentration, sterility assurance, excipients, stability, packaging, and delivered dose. Those differences can affect safety and procedural performance.

What is the most attractive commercial line extension for Goprelto?

A preservative-free, single-use, metered-dose nasal applicator is the strongest line-extension concept. It addresses contamination control, dose consistency, workflow, and excipient-related tolerability in one product design.

References

1. U.S. Food and Drug Administration. (2017). Goprelto (cocaine hydrochloride) nasal solution, prescribing information. FDA.

2. U.S. Food and Drug Administration. (n.d.). Drugs@FDA: Goprelto. FDA.

3. U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations. FDA.