List of Excipients in Branded Drug PRASUGREL

Generic Drugs Containing PRASUGREL

Company	Ingredient	NDC	Excipient
Mylan Pharmaceuticals Inc	prasugrel	0378-5185	CROSPOVIDONE
Mylan Pharmaceuticals Inc	prasugrel	0378-5185	FD&C YELLOW NO. 6
Mylan Pharmaceuticals Inc	prasugrel	0378-5185	FERRIC OXIDE YELLOW
Mylan Pharmaceuticals Inc	prasugrel	0378-5185	GLYCERYL DIBEHENATE
Mylan Pharmaceuticals Inc	prasugrel	0378-5185	HYPROMELLOSE
Mylan Pharmaceuticals Inc	prasugrel	0378-5185	LACTOSE MONOHYDRATE
Mylan Pharmaceuticals Inc	prasugrel	0378-5185	MANNITOL

What are the Most Frequently-Used Excipients in PRASUGREL?

# Of NDCs	Excipient
16	CELLULOSE, MICROCRYSTALLINE
2	CROSPOVIDONE
2	DIETHYL PHTHALATE
1	ETHYLCELLULOSE
1	ETHYLCELLULOSES
2	FD&C YELLOW NO. 6
9	FERRIC OXIDE RED

Prasugrel Excipient Strategy and Commercial Opportunities

Last updated: September 1, 2026

Prasugrel is a mature, genericized oral P2Y12 antiplatelet drug. The main commercial opportunity is not a new chemical entity or biosimilar pathway. It is differentiated oral dosage-form development using excipients to improve manufacturability, dose flexibility, swallowing, stability, adherence, and access in acute coronary syndrome populations.

The reference product, Effient, is an immediate-release prasugrel hydrochloride tablet in 5 mg and 10 mg strengths. Its formulation uses conventional direct-compression or granulation excipients, including mannitol, microcrystalline cellulose, low-substituted hydroxypropyl cellulose, croscarmellose sodium, magnesium stearate, hypromellose, lactose, titanium dioxide, triacetin, and iron oxides.[1]

What is prasugrel and where does excipient strategy matter?

Prasugrel hydrochloride is an oral thienopyridine prodrug that irreversibly inhibits platelet P2Y12 receptors after conversion to an active metabolite. FDA approved Effient in 2009 for reducing thrombotic cardiovascular events in patients with acute coronary syndrome managed with percutaneous coronary intervention.[1]

Prasugrel is commercially relevant in settings where rapid platelet inhibition and predictable antiplatelet activity are required. The principal formulation constraints are:

Formulation issue	Commercial implication
Low-dose tablet strengths of 5 mg and 10 mg	Requires content uniformity and reliable low-dose blending
Rapid conversion to active metabolite	Immediate-release performance is commercially important
Antiplatelet use in acute-care settings	Packaging, stability, and rapid administration affect product selection
Elderly and post-procedure patients	Swallowability and dose flexibility can support differentiation
Irreversible platelet inhibition	Labeling and medication-error controls are important
Generic price erosion	Differentiation must come from dosage form, supply reliability, or channel access

The excipient strategy should prioritize rapid disintegration, uniform distribution of the active ingredient, low moisture exposure, mechanical robustness, and compatibility with high-volume generic manufacturing.

What excipients are used in Effient prasugrel tablets?

The Effient label identifies a conventional immediate-release tablet platform.[1]

Core tablet excipients

The reference formulation uses:

• Mannitol as a diluent and mouthfeel-supporting filler
• Microcrystalline cellulose as a compressibility aid
• Low-substituted hydroxypropyl cellulose as a disintegrant and binder-supporting excipient
• Croscarmellose sodium as a superdisintegrant
• Magnesium stearate as a lubricant

Film-coating excipients

The coating system includes:

• Hypromellose
• Lactose monohydrate
• Titanium dioxide
• Triacetin
• Iron oxide colorants

This composition supports a standard film-coated immediate-release tablet with differentiated tablet color by strength. The color coding has practical value because prasugrel dosing errors can create clinically significant bleeding risk.

A generic applicant does not need to duplicate the reference product's excipient identity. It must demonstrate pharmaceutical equivalence, bioequivalence, appropriate quality, and compliance with FDA inactive-ingredient requirements. A materially different excipient system can be commercially useful if it improves manufacturability or patient administration without creating new safety or bioequivalence risks.

What excipient platforms are suitable for generic prasugrel?

Direct-compression tablets

Direct compression is the lowest-complexity commercial platform when the active pharmaceutical ingredient has suitable flow and compressibility. A formulation may combine microcrystalline cellulose, mannitol, lactose, or dibasic calcium phosphate with croscarmellose sodium or sodium starch glycolate.

Advantages include:

• Fewer processing steps
• Lower manufacturing cost
• Shorter cycle time
• Lower solvent and drying burden
• Easier scale-up

The principal risks are segregation, low-dose content uniformity, tablet weight variation, and sensitivity to lubricant overmixing.

Wet-granulated tablets

Wet granulation can improve blend uniformity and tablet strength when prasugrel hydrochloride has poor flow or poor compactability. Povidone, copovidone, hydroxypropyl cellulose, or starch-based binders can be considered.

The main limitation is moisture and thermal exposure. The process requires stability studies to establish that prasugrel and its degradation products remain within specification. Wet granulation also raises operating cost and may reduce the advantage of a low-price generic.

Dry granulation and roller compaction

Dry granulation is relevant when a manufacturer needs improved flow and compressibility without introducing water. It can support high-speed tableting and continuous manufacturing.

Potential disadvantages include:

• Ribbon-density variability
• Fines generation
• Tabletability loss after compaction
• Greater risk of segregation during downstream blending

Orally disintegrating tablets

An orally disintegrating tablet could target patients with dysphagia, elderly patients, and post-procedure populations. Mannitol, crospovidone, croscarmellose sodium, and low-substituted hydroxypropyl cellulose are common excipient choices for this platform.

The commercial challenge is clinical and regulatory rather than purely technical. A rapidly disintegrating tablet must deliver equivalent systemic exposure and maintain acceptable taste, friability, dose uniformity, and moisture stability. The product also needs careful packaging because high-surface-area tablets can be more hygroscopic.

Orodispersible or dispersible tablets

A dispersible tablet may offer a more practical hospital or caregiver-administered dosage form than a conventional tablet. It could be designed for dispersion in water before administration.

This strategy requires control of:

• Dispersion time
• Sedimentation
• Dose recovery from the administration vessel
• Palatability
• Stability after reconstitution
• Compatibility with nasogastric or enteral administration, if claimed

A manufacturer should not assume that a dispersible dosage form automatically creates a regulatory advantage. The product may require a new clinical or bioequivalence strategy depending on the dosage form, labeling, and intended use.

What formulation patents protect prasugrel products?

Prasugrel's original U.S. exclusivity was based on compound and product-related intellectual property associated with prasugrel hydrochloride. The commercial market has since transitioned to generic products. The key remaining opportunity is formulation differentiation rather than basic compound exclusivity.

Potentially protectable formulation concepts include:

• Novel polymorphs or crystalline forms
• Particle-size-controlled prasugrel hydrochloride
• Moisture-stabilized formulations
• Taste-masked orally disintegrating tablets
• Modified-release formulations
• Fixed-dose combinations with aspirin
• Specific excipient ratios that improve dissolution or content uniformity
• Packaging systems that reduce degradation
• Manufacturing processes that improve yield or impurity control

A formulation patent must contain more than a routine substitution of one standard filler or disintegrant for another. Commercially stronger claims would link the excipient system to a measurable technical effect, such as improved stability, reduced impurity formation, faster disintegration, improved dissolution under discriminatory conditions, or successful low-dose content uniformity.

What patent barriers affect generic prasugrel?

The principal U.S. barriers to early generic entry were the original product patent, regulatory exclusivity, and product-related patent listings associated with Effient. Those barriers no longer provide a meaningful protection period for a new conventional prasugrel tablet.

A new entrant is more likely to face:

• Formulation patent risk from a differentiated product
• Process patent risk involving solid-state control or impurity management
• Trademark and trade-dress restrictions
• Labeling constraints for pediatric or reduced-dose claims
• Patent disputes over a fixed-dose combination or novel delivery system

The Orange Book should be reviewed for the live patent and exclusivity status of the specific reference-listed drug before filing or licensing decisions. FDA's Orange Book identifies approved drug products, therapeutic equivalence evaluations, and listed patent or exclusivity information.[2]

When did prasugrel lose exclusivity?

Effient received FDA approval on July 10, 2009.[1] Its regulatory exclusivity and patent protection periods have expired for purposes of conventional generic prasugrel development. FDA approved generic prasugrel products beginning in 2017, confirming that the market is open to ANDA-based competition.

Milestone	Date or status
Effient FDA approval	July 10, 2009
Reference product	Prasugrel hydrochloride tablets, 5 mg and 10 mg
Regulatory pathway for standard generics	ANDA
Generic U.S. entry	Began in 2017
Conventional tablet patent opportunity	Largely exhausted
Biosimilar pathway	Not applicable
Current commercial focus	Cost, supply, formulation differentiation, and channel access

A new conventional tablet would generally compete as a commodity generic. A differentiated formulation may require a separate 505(b)(2) strategy, depending on the changes to dosage form, route, dosing, or clinical use.

What is the FDA regulatory status of prasugrel?

FDA-approved prasugrel products are immediate-release oral tablets in 5 mg and 10 mg strengths. The reference product is approved for acute coronary syndrome patients managed with PCI, including unstable angina, non-ST-elevation myocardial infarction, and ST-elevation myocardial infarction in the labeled setting.[1]

Important label restrictions include:

• Contraindication in patients with a history of transient ischemic attack or stroke
• Generally no recommended use in patients age 75 years or older because of increased risk of fatal and intracranial bleeding, except in specific high-risk circumstances
• Weight below 60 kg requires consideration of the 5 mg dose
• Discontinuation before surgery may be required when clinically appropriate
• Concomitant anticoagulant and antiplatelet therapy increases bleeding risk

These restrictions limit the commercial value of broad promotional positioning. A formulation company should focus on administration and adherence improvements rather than unsupported safety claims.

What commercial opportunities exist for prasugrel excipients?

Low-cost generic tablet platform

The largest opportunity is a robust, low-cost tablet using widely accepted excipients. A formulation that avoids specialized excipients can reduce supply-chain risk and simplify regulatory review.

The target profile is:

• Immediate release
• 5 mg and 10 mg strengths
• High blend uniformity
• Low tablet friability
• Rapid disintegration
• Stable dissolution after accelerated storage
• Standard HDPE bottle or blister packaging
• Manufacturability on existing high-speed equipment

Patient-friendly dosage form

An orally disintegrating or dispersible prasugrel product could address swallowing difficulty and acute-care administration. The commercial opportunity is strongest if the product demonstrates a clear operational advantage, such as administration without a full glass of water or improved use in patients unable to swallow conventional tablets.

Fixed-dose prasugrel and aspirin combination

A fixed-dose combination could reduce pill burden in selected cardiovascular patients. It would also create substantial regulatory and commercial complexity.

Key issues include:

• Different dose titration requirements
• Aspirin contraindications and gastrointestinal risk
• Need to preserve prasugrel stability alongside aspirin
• Dose flexibility when aspirin or prasugrel must be changed
• Potential need for a 505(b)(2) application
• Clinical justification for the combination
• Competition from inexpensive separate generic tablets

The combination has commercial logic but is less attractive than a conventional generic unless it produces a measurable adherence or hospital-workflow benefit.

Pediatric and low-dose opportunities

Prasugrel has limited pediatric commercial potential because its principal market is adult acute coronary care and the label contains major bleeding restrictions. A lower-dose formulation may have utility for patients below 60 kg, but a 2.5 mg or liquid product would require clinical, labeling, and market-size analysis.

A liquid formulation would face additional issues:

• Chemical stability in aqueous media
• Dose measurement accuracy
• Taste masking
• Preservative selection
• Container-closure compatibility
• Microbiological control

Contract manufacturing and regional licensing

Prasugrel can support regional licensing in markets where branded Effient has limited presence but generic antiplatelet demand remains high. The strongest partners are manufacturers with:

• Existing prasugrel API supply
• Tablet compression capacity
• Established cardiovascular sales channels
• Regulatory registrations in multiple jurisdictions
• Proven pharmacovigilance systems
• Reliable blister and bottle packaging

Licensing value is likely to depend more on registration status, supply reliability, and pricing than on expired compound patents.

How strong is the prasugrel patent estate?

The estate is weak for a conventional generic tablet and potentially stronger for a genuinely differentiated delivery system.

Asset type	Current commercial strength
Original prasugrel compound patent	Low for new market entry
Reference immediate-release tablet	Low to moderate, depending on jurisdiction and listed rights
New polymorph or solid form	Moderate if technically distinct and commercially necessary
Orally disintegrating formulation	Moderate if supported by unexpected performance data
Fixed-dose combination	Moderate, but regulatory complexity is high
Manufacturing process	Moderate where impurity or yield advantages are demonstrated
Packaging and stability system	Limited unless linked to a patentable technical effect
Method-of-use patent	Limited for established labeled indications

Patent strength should be evaluated claim by claim. Excipient patents that cover routine use of mannitol, microcrystalline cellulose, croscarmellose sodium, or hypromellose generally provide limited blocking value unless the claims require a specific composition and demonstrated performance.

Which companies challenge prasugrel exclusivity?

Generic prasugrel competition has come from multiple ANDA applicants and established generic manufacturers after the expiration of the relevant reference-product barriers. The market includes manufacturers such as Teva, Lupin, and other approved generic suppliers across different jurisdictions.

Prasugrel does not have a biosimilar market because it is a small-molecule drug. Competition occurs through ANDAs, national generic procedures, and, for modified products, potentially 505(b)(2) applications in the United States.

What Paragraph IV risks exist?

Paragraph IV risk is now primarily historical for the original Effient product. A new formulation applicant could create fresh Paragraph IV exposure if it patents a formulation, polymorph, combination, or method of use and lists the patent against an approved reference product.

For a standard ANDA:

• The applicant must address listed patents for the reference product
• A Paragraph IV certification may trigger litigation
• A first-filer position can have commercial value where exclusivity remains available
• The value of early filing is limited for a mature, heavily genericized product

A reformulated product with meaningful clinical or administration benefits may have greater litigation value than a standard 5 mg or 10 mg tablet.

What litigation and settlement issues affect prasugrel?

The important litigation period involved patent challenges to the reference product before generic entry. Because conventional prasugrel generics are already marketed, current commercial decisions should focus on formulation-specific litigation rather than historical Effient patent disputes.

Potential disputes include:

• Patent infringement over crystalline forms
• Infringement over particle-size specifications
• ANDA litigation involving an orally disintegrating tablet
• Trade-dress claims involving tablet color or shape
• Regulatory exclusivity disputes for a new formulation
• License agreements covering regional distribution or API supply

Settlement value is limited when multiple generic manufacturers already supply standard prasugrel tablets. It becomes more meaningful when a company controls a differentiated formulation, a scarce API source, or an approved combination product.

How does prasugrel compare with competing P2Y12 drugs?

Drug	Dosage form	Generic status	Excipient opportunity	Commercial position
Prasugrel	Immediate-release tablet	Generic	ODT, dispersible, low-dose, combination	Price-sensitive PCI market
Clopidogrel	Immediate-release tablet	Generic	Very limited conventional-tablet differentiation	Broadest generic use
Ticagrelor	Immediate-release tablet	Generic or patent-transition market depending on jurisdiction	Taste, swallowing, packaging, combination strategies	Direct branded and generic competition
Cangrelor	Intravenous product	Branded hospital product in relevant markets	Parenteral formulation and reconstitution	Procedural and inpatient use

Prasugrel's strongest clinical differentiation is in selected PCI patients, but its contraindications and bleeding warnings constrain broad substitution. Clopidogrel has greater market breadth and lower cost. Ticagrelor competes on pharmacology and dosing rather than excipient innovation. A prasugrel product must therefore win through price, supply, administration, or a targeted clinical workflow.

What generic launch scenarios exist for prasugrel?

Scenario 1: Standard low-cost tablet

This is the most realistic strategy. Success depends on bioequivalence, manufacturing cost, API security, and payer access. Patent barriers are limited, but price competition is intense.

Scenario 2: Orally disintegrating tablet

This offers greater differentiation but requires formulation optimization, taste management, moisture protection, and a stronger regulatory rationale. The product may support higher pricing if hospitals or patients value administration advantages.

Scenario 3: Fixed-dose aspirin combination

This could reduce pill burden but faces dose-flexibility and clinical adoption barriers. It is commercially more complex than a generic tablet and likely requires a 505(b)(2) or equivalent pathway.

Scenario 4: Regional branded generic

A manufacturer could differentiate through hospital contracting, blister packaging, dependable supply, and cardiovascular sales coverage. This strategy is more defensible than relying on formulation patents alone.

Key Takeaways

• Prasugrel is a mature genericized small-molecule antiplatelet drug, not a biosimilar opportunity.
• Effient uses a conventional immediate-release tablet with mannitol, microcrystalline cellulose, low-substituted hydroxypropyl cellulose, croscarmellose sodium, magnesium stearate, and a hypromellose-based film coat.
• The strongest near-term opportunity is a low-cost, stable, high-throughput generic tablet in 5 mg and 10 mg strengths.
• Orally disintegrating and dispersible formulations offer the clearest excipient-led differentiation.
• Fixed-dose prasugrel-aspirin combinations have commercial logic but face substantial regulatory and dose-flexibility constraints.
• Original compound and reference-product exclusivity no longer provide a strong barrier to conventional generic entry.
• New patent value would depend on a technically meaningful formulation, solid form, manufacturing process, or delivery system.
• Revenue exposure for a new entrant is constrained by broad generic competition and the lower price of clopidogrel.
• The product must account for major bleeding restrictions, the history of stroke or TIA contraindication, age-related risk, and low-body-weight dosing.
• Supply reliability, hospital access, and regulatory execution are likely to matter more than legacy prasugrel patents.

FAQs

Can excipients create a new patent position for prasugrel?

Yes, but routine substitution of common fillers or disintegrants is unlikely to create strong protection. A patent position is more credible when the formulation produces unexpected stability, dissolution, dose-uniformity, taste, or administration results.

Is a liquid prasugrel formulation commercially attractive?

It is technically possible but commercially narrow. Chemical stability, taste, dose accuracy, microbial control, and limited pediatric demand would make a liquid product more complex than a tablet or orally disintegrating dosage form.

Can prasugrel be administered through an enteral tube?

The approved product labeling and institutional protocols control this question. A manufacturer should not make an enteral-administration claim without data on dispersion, recovery, adsorption, stability, and delivered dose.

Are prasugrel excipient changes automatically eligible for an ANDA?

No. The regulatory pathway depends on whether the changed formulation remains pharmaceutically equivalent and can meet bioequivalence and quality requirements. A significant dosage-form or labeling change may require a 505(b)(2) application.

Which excipient is most important for prasugrel tablet performance?

No single excipient determines performance. Croscarmellose sodium and low-substituted hydroxypropyl cellulose are central to disintegration, while microcrystalline cellulose and mannitol affect compression, flow, tablet size, and mouthfeel. The commercial result depends on the complete formulation and process.

References

1. U.S. Food and Drug Administration. (2009). Effient (prasugrel hydrochloride) tablets prescribing information. https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022307lbl.pdf

2. U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book. https://www.fda.gov/drugs/drug-approvals-and-databases/approved-drug-products-therapeutic-equivalence-evaluations-orange-book

3. U.S. Food and Drug Administration. (2024). Drugs@FDA: FDA-approved drugs. https://www.accessdata.fda.gov/scripts/cder/daf/

4. Wiviott, S. D., Braunwald, E., McCabe, C. H., Montalescot, G., Ruzyllo, W., Gottlieb, S., Neumann, F. J., Ardissino, D., De Servi, S., Murphy, S. A., Riesmeyer, J., Weerakkody, G., Gibson, C. M., Antman, E. M., & TRITON-TIMI 38 Investigators. (2007). Prasugrel versus clopidogrel in patients with acute coronary syndromes. New England Journal of Medicine, 357(20), 2001-2015. https://doi.org/10.1056/NEJMoa0706482

5. U.S. Food and Drug Administration. (2024). Abbreviated new drug application process for generic drugs. https://www.fda.gov/drugs/abbreviated-new-drug-application-anda/abbreviated-new-drug-application-anda-process-generic-drugs