List of Excipients in Branded Drug GRASTEK

Last updated: August 7, 2026

GRASTEK's commercial opportunity is concentrated in excipient-enabled product improvements rather than simple substitution of the existing tablet. The product is a standardized Timothy grass pollen allergen extract tablet containing mannitol, gelatin, croscarmellose sodium, microcrystalline cellulose, and magnesium stearate. Its strongest formulation priorities are rapid sublingual disintegration, allergen potency retention, moisture protection, taste control, and patient-friendly administration. The most credible follow-on opportunities are gelatin-free tablets, improved stability packaging, pediatric-friendly presentations, and differentiated sublingual delivery systems.

GRASTEK Excipient Strategy, Patent Position, and Commercial Opportunities

What is GRASTEK and how is it administered?

GRASTEK is a sublingual immunotherapy tablet containing standardized Timothy grass pollen allergen extract. It is indicated for grass pollen-induced allergic rhinitis, with or without conjunctivitis, in patients aged 5 through 65 years who have a positive skin test or in vitro testing for Timothy grass or cross-reactive grass pollen allergens [1].

The tablet contains 2,800 bioequivalent allergy units, or BAU, of standardized Timothy grass pollen allergen extract. Treatment is initiated under medical supervision because the product can cause systemic allergic reactions, including anaphylaxis. Patients are prescribed epinephrine for emergency treatment [1].

Attribute	GRASTEK profile
Active ingredient	Standardized Timothy grass pollen allergen extract
Dose strength	2,800 BAU per tablet
Dosage form	Sublingual tablet
Route	Under the tongue
U.S. approval	April 2014
U.S. application	NDA 141112
Indication	Grass pollen-induced allergic rhinitis, with or without conjunctivitis
Approved age range	5 to 65 years
Treatment approach	Daily administration, generally initiated before and continued through the relevant pollen season
Manufacturer	ALK-Abelló, A/S; U.S. commercial operations associated with ALK-Abelló
Key clinical restrictions	Not appropriate for patients with severe, unstable, or uncontrolled asthma; contraindicated in patients with eosinophilic esophagitis or certain hypersensitivity conditions

GRASTEK is part of the broader sublingual immunotherapy tablet market, which includes ORALAIR for multiple grass pollens, RAGWITEK for short ragweed, and ODACTRA for house dust mite allergy.

What excipients are used in GRASTEK tablets?

The U.S. prescribing information identifies the following inactive ingredients:

Excipient	Likely formulation role	Commercial significance
Mannitol	Diluent, bulking agent, mouthfeel modifier	Supports low-dose tablet manufacture and can improve oral sensation
Gelatin	Binder and structural excipient	Supports tablet integrity but creates animal-origin, religious, dietary, and supply-chain considerations
Croscarmellose sodium	Superdisintegrant	Promotes rapid tablet breakup after sublingual placement
Microcrystalline cellulose	Diluent and compression aid	Supports tablet hardness, content uniformity, and manufacturability
Magnesium stearate	Lubricant	Reduces tooling friction and supports tablet ejection

The formulation must balance competing requirements. A tablet that is too hard can delay sublingual disintegration. A tablet that disintegrates too quickly can create manufacturing, packaging, or handling problems. Excessive lubricant can impair wetting and dissolution. Changes in excipient grade, particle size, moisture, or supplier can affect allergen distribution and delivered potency.

Because GRASTEK contains a biological allergen extract rather than a conventional small-molecule active ingredient, excipients are part of a broader potency-control system. The finished product must preserve the relevant allergenic proteins and maintain dose consistency throughout shelf life.

How does the GRASTEK excipient system support sublingual delivery?

GRASTEK's excipient strategy is designed for a rapidly disintegrating tablet administered directly under the tongue.

Mannitol

Mannitol is well suited to orally disintegrating and sublingual dosage forms because it provides a relatively clean mouthfeel and low hygroscopicity compared with some alternative polyols. It also contributes to tablet bulk where the active allergen extract is present at a low mass relative to the total tablet.

Commercial formulation opportunities include:

• Direct-compression mannitol grades optimized for rapid disintegration.
• Co-processed mannitol systems that improve flow and compactability.
• Lower-moisture grades that reduce protein degradation risk.
• Taste and mouthfeel systems that do not interfere with allergen exposure.

Gelatin

Gelatin provides binding and mechanical strength. Its use creates a clear reformulation opportunity because some patients avoid animal-derived ingredients for religious, dietary, ethical, or allergy-related reasons.

Potential replacements include modified starches, povidone, hydroxypropyl cellulose, hydroxypropyl methylcellulose, and plant-derived protein or polysaccharide binders. A replacement must maintain tablet strength without slowing sublingual disintegration or altering allergen stability.

A gelatin-free version could be positioned as a formulation differentiation strategy. It would require comparative testing of potency, dissolution or disintegration, moisture sensitivity, microbial control, and clinical performance.

Croscarmellose sodium

Croscarmellose sodium is the principal rapid-disintegration component identified in the label. Its performance depends on particle morphology, swelling capacity, grade, inclusion level, and compression force.

Supplier opportunities include premium grades with:

• More consistent swelling performance.
• Lower microbial and elemental impurity profiles.
• Better compatibility with direct compression.
• Reduced variability after changes in manufacturing scale.

A different disintegrant, such as crospovidone or sodium starch glycolate, could create a new formulation, but replacing croscarmellose sodium would require evidence that the change does not affect in-mouth disintegration or allergen release.

Microcrystalline cellulose

Microcrystalline cellulose supports compressibility and tablet robustness. It also affects porosity and liquid ingress. Excessive compaction can reduce the speed at which saliva penetrates the tablet.

Opportunities exist for co-processed cellulose-mannitol excipients that reduce the number of raw materials and improve powder flow. Such systems may simplify manufacturing but could create new regulatory and intellectual-property considerations if they materially change product performance.

Magnesium stearate

Magnesium stearate is necessary for efficient tablet manufacture, but over-lubrication can create hydrophobic surfaces that slow wetting and disintegration. The critical controls are mixing time, lubricant concentration, particle size, and shear exposure.

A reformulated product could evaluate sodium stearyl fumarate or other alternative lubricants. The commercial value would come from improved wetting, lower lubricant sensitivity, or more robust scale-up rather than from the ingredient substitution alone.

What formulations are protected by GRASTEK-related intellectual property?

Public regulatory materials establish GRASTEK's composition, dosage form, strength, manufacturing controls, and approved use. They do not, by themselves, establish a complete patent inventory.

The principal intellectual-property categories likely relevant to GRASTEK include:

1. Standardized allergen extract composition and potency.
2. Sublingual tablet formulations containing grass pollen allergens.
3. Methods for treating grass pollen-induced allergic rhinitis.
4. Manufacturing processes for extracting, standardizing, blending, and compressing allergen material.
5. Stability systems and packaging for moisture-sensitive allergen tablets.
6. Dosing schedules and pre-season or co-seasonal treatment protocols.
7. Pediatric administration and patient-management methods.

Excipient changes may avoid a narrow formulation claim but still encounter broader claims covering the allergen extract, tablet architecture, treatment method, or manufacturing process. A freedom-to-operate analysis therefore must review claims, prosecution history, continuation applications, foreign family members, and regulatory exclusivity separately.

What is the Orange Book status of GRASTEK?

GRASTEK is approved under NDA 141112. FDA's Orange Book is the relevant source for approved drug-product patent and exclusivity listings, but Orange Book records do not provide a complete view of all intellectual property that may affect commercial entry.

For GRASTEK, the practical review should distinguish:

Protection category	Relevance to GRASTEK
Orange Book-listed patents	May affect an ANDA applicant if listed against the approved product
Method-of-use patents	Could affect labeling, treatment duration, or patient population
Formulation patents	Could cover the sublingual tablet and excipient architecture
Manufacturing patents	May restrict use of particular extraction, standardization, or compression methods
Regulatory exclusivity	Can delay approval independently of patent expiry
Trade secrets	May cover allergen standardization, batch release, and manufacturing controls

A Paragraph IV challenge would be more complex than a conventional small-molecule tablet challenge because the applicant would need to address active-ingredient characterization, potency assays, biological comparability, extract standardization, and the appropriate FDA approval pathway.

When does GRASTEK lose exclusivity?

A single public expiration date should not be treated as the end of GRASTEK's commercial protection. Market entry timing depends on several dates:

• Expiration of any listed formulation or method-of-use patents.
• Expiration of unlisted manufacturing or platform patents.
• Loss of applicable regulatory exclusivity.
• FDA acceptance of the competing product's regulatory pathway.
• Resolution of Paragraph IV litigation or settlement terms.
• Ability of the entrant to reproduce allergen potency and clinical performance.

GRASTEK was approved in 2014. Any five-year new-chemical-entity exclusivity associated with the approval would have expired in 2019, subject to the legal classification of the active allergen product. Pediatric exclusivity, if granted for a particular product, would add six months to applicable exclusivity periods. The FDA Orange Book and Drugs@FDA remain the controlling public sources for the product-specific regulatory record [2,3].

Which companies compete with GRASTEK?

The closest commercial competitors are other sublingual allergen immunotherapy tablets.

Product	Allergen target	Company	Dosage form	Competitive overlap
GRASTEK	Timothy grass pollen	ALK-Abelló	Sublingual tablet	Direct grass-pollen immunotherapy competitor
ORALAIR	Five grass pollens	Stallergenes Greer	Sublingual tablet	Broader grass-pollen coverage
RAGWITEK	Short ragweed pollen	ALK-Abelló	Sublingual tablet	Same platform, different allergen
ODACTRA	House dust mite allergens	ALK-Abelló	Sublingual tablet	Same route and immunotherapy model, different disease target
Allergy shots	Patient-specific allergens	Allergy clinics and extract suppliers	Injectable	Lower convenience, greater clinic involvement

GRASTEK's commercial position depends on allergen specificity, physician familiarity, treatment adherence, payer coverage, seasonal timing, and the availability of competing grass-pollen products.

What excipient commercial opportunities exist around GRASTEK?

Gelatin-free reformulation

The most visible opportunity is a gelatin-free tablet. A successful replacement could support:

• Vegetarian or religious-compliant positioning.
• Reduced dependence on animal-derived raw materials.
• Simplified global procurement.
• Improved acceptance in pediatric and family markets.

The principal risk is that a new binder may alter tablet strength, moisture uptake, disintegration, or allergen stability.

Moisture-control packaging

Allergen proteins are vulnerable to environmental stress. High-barrier blister materials, desiccant-integrated systems, improved seal integrity, and low-moisture manufacturing can create value without changing the tablet composition.

Packaging may be commercially more attractive than a full reformulation because it can improve shelf life or reduce distribution losses while preserving the established clinical product.

Pediatric presentations

GRASTEK is approved for children aged 5 years and older. Pediatric opportunities include easier-to-open blister packaging, clearer dose instructions, low-force peel systems, and administration aids that do not obstruct sublingual exposure.

A lower-strength or modified tablet would create a larger regulatory burden. Packaging and usability improvements are more practical first-line opportunities.

Taste and mouthfeel optimization

Sublingual treatment requires repeated daily administration. Mild taste, low grittiness, rapid disappearance, and limited residual material can affect adherence.

Potential technologies include:

• Mannitol-based mouthfeel systems.
• Low-dose flavor modifiers compatible with allergen proteins.
• Co-processed excipients that reduce chalkiness.
• Microstructured tablets that improve saliva penetration.

Flavoring agents require careful evaluation because they may create new allergens, change local exposure, or affect the safety profile.

Manufacturing robustness

The active allergen extract may have greater batch-to-batch variability than a synthetic active ingredient. Excipients that improve powder flow, content uniformity, and low-force compression can reduce process variability.

High-value supplier claims may focus on:

• Allergen-compatible excipient grades.
• Low-bioburden materials.
• Consistent particle-size distributions.
• Reduced electrostatic segregation.
• Improved tablet hardness at lower compression force.

What generic entry risks exist for GRASTEK?

Generic or follow-on entry faces several barriers:

1. The active ingredient is a standardized biological allergen extract.
2. Potency is expressed in biological allergy units rather than only mass.
3. The extract contains multiple allergenic proteins.
4. The clinical effect depends on standardized allergen exposure.
5. The dosage form must disintegrate rapidly under the tongue.
6. Manufacturing changes can affect extract stability and delivered potency.
7. A substitute product may require specialized clinical or immunological comparability evidence.

An ANDA may be unavailable or difficult if FDA determines that the product cannot be demonstrated equivalent through conventional generic methods. A 505(b)(2) strategy may be more plausible for certain reformulations, but the regulatory pathway depends on the degree of active-ingredient and formulation change. Allergen products also involve specialized FDA oversight and product-specific analytical expectations [4].

What patent litigation and Paragraph IV activity affect GRASTEK?

No broadly reported, high-profile Paragraph IV litigation is established in the core FDA materials cited for GRASTEK. That does not eliminate patent risk. A future challenger could target:

• Formulation patents.
• Sublingual administration claims.
• Treatment-duration claims.
• Manufacturing claims.
• Packaging or stability claims.

Settlement agreements could delay entry through a licensed launch date, authorized-generic arrangement, supply agreement, or geographic limitation. The commercial impact would depend on whether the settlement permits a single entrant or multiple competitors and whether it covers only the United States or broader markets.

How strong is the GRASTEK patent estate?

The commercial strength of the estate is likely greater when patent rights are combined with manufacturing know-how and regulatory complexity. A formulation patent covering only common excipients may be easier to design around than a patent covering a specific standardized extract, potency range, particle profile, or manufacturing process.

Estate component	Relative strategic value
Standardized extract claims	High, if difficult to reproduce and adequately supported
Sublingual tablet claims	Moderate to high, depending on claim breadth
Specific excipient combinations	Moderate; design-around risk is material
Manufacturing process claims	High where process know-how is difficult to replicate
Method-of-use claims	Variable; enforcement depends on labeling and induced-use evidence
Packaging claims	Moderate; useful for lifecycle management
Trade secrets	Potentially high, particularly for potency standardization and release testing

For lifecycle management, the strongest strategy is usually a layered portfolio combining extract standardization, formulation, manufacturing, packaging, and patient-use claims.

What are the main GRASTEK revenue and licensing opportunities?

GRASTEK's public product-level revenue is not separately disclosed in the FDA label or standard regulatory records. Commercial exposure is linked to the broader allergy immunotherapy business and to seasonal prescription demand.

Revenue opportunities include:

• Licensing gelatin-free or vegan-compatible excipient systems.
• Supplying direct-compression mannitol or co-processed excipients.
• Providing high-barrier blister packaging.
• Developing pediatric adherence and packaging systems.
• Licensing analytical methods for allergen potency and stability.
• Extending the platform to additional grass or tree pollen allergens.
• Creating combination or sequential immunotherapy products.

Potential licensees include specialty excipient manufacturers, packaging companies, contract development and manufacturing organizations, allergen extract specialists, and companies developing sublingual immunotherapy platforms.

How does GRASTEK compare with ORALAIR?

GRASTEK uses a Timothy grass pollen extract, while ORALAIR contains a mixture of five grass pollen extracts. GRASTEK may offer a more focused allergen profile and a simpler active composition. ORALAIR may have broader grass-pollen coverage but presents additional extract-standardization and analytical complexity.

From an excipient perspective, both products require:

• Rapid sublingual disintegration.
• Preservation of protein allergen potency.
• Moisture-controlled packaging.
• Reliable low-dose blend uniformity.
• Patient-friendly daily administration.

The key differentiation is therefore less likely to come from conventional tablet excipients alone and more likely to arise from extract standardization, adherence, packaging, and evidence supporting the treatment population.

Key Takeaways

• GRASTEK is a 2,800-BAU Timothy grass pollen sublingual tablet approved by FDA in 2014.
• Its labeled excipients are mannitol, gelatin, croscarmellose sodium, microcrystalline cellulose, and magnesium stearate.
• The strongest formulation opportunity is a gelatin-free tablet that preserves rapid disintegration and allergen potency.
• High-barrier packaging and moisture control may offer a lower-risk commercial route than full reformulation.
• Generic entry is complicated by standardized biological allergen extracts, biological potency assays, and product-specific manufacturing controls.
• Patent risk may extend beyond Orange Book listings to manufacturing, standardization, packaging, and trade-secret protection.
• ORALAIR is the closest direct commercial comparator because it targets grass-pollen allergy through the same sublingual tablet route.
• The most attractive licensing targets are allergen-compatible excipients, low-moisture tablet systems, pediatric packaging, and potency-control technologies.

FAQs About GRASTEK Excipient and Commercial Strategy

Is GRASTEK gelatin-free?

No. The U.S. label identifies gelatin as an inactive ingredient. Gelatin-free reformulation is a clear product-differentiation opportunity.

Does GRASTEK contain lactose?

Lactose is not identified among the inactive ingredients in the cited U.S. prescribing information. The listed excipients include mannitol, gelatin, croscarmellose sodium, microcrystalline cellulose, and magnesium stearate [1].

Can mannitol be replaced in GRASTEK?

Yes, in principle, but replacement would require comparative assessment of compression, disintegration, mouthfeel, allergen potency, stability, and regulatory impact. Mannitol is likely to be retained in many reformulation strategies because it supports both tablet bulk and sublingual mouthfeel.

Is GRASTEK a biologic or a conventional generic drug?

GRASTEK is approved under an NDA, but allergen extract products have biological and standardization characteristics that make conventional generic substitution more difficult than for an ordinary synthetic tablet. The applicable FDA pathway must be assessed product by product.

What is the most valuable GRASTEK lifecycle-management opportunity?

A gelatin-free, moisture-robust, rapidly disintegrating tablet with improved pediatric packaging has the strongest combined commercial rationale. It addresses excipient acceptability, supply-chain resilience, adherence, and product differentiation without requiring a new allergen target.

Sources

1. U.S. Food and Drug Administration. (2023). GRASTEK (Timothy grass pollen allergen extract) sublingual tablet: Prescribing information.
2. U.S. Food and Drug Administration. (2024). Drugs@FDA: GRASTEK, NDA 141112.
3. U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book.
4. U.S. Food and Drug Administration. (2022). Regulatory framework and guidance for allergenic products and allergen immunotherapy products.