List of Excipients in Branded Drug DAPAGLIFLOZIN

Company	Tradename	Ingredient	NDC	Excipient	Potential Generic Entry
A-S Medication Solutions	DAPAGLIFLOZIN	dapagliflozin	50090-7056	ANHYDROUS LACTOSE
A-S Medication Solutions	DAPAGLIFLOZIN	dapagliflozin	50090-7056	CELLULOSE, MICROCRYSTALLINE
A-S Medication Solutions	DAPAGLIFLOZIN	dapagliflozin	50090-7056	CROSPOVIDONE
A-S Medication Solutions	DAPAGLIFLOZIN	dapagliflozin	50090-7056	MAGNESIUM STEARATE
A-S Medication Solutions	DAPAGLIFLOZIN	dapagliflozin	50090-7056	SILICON DIOXIDE

Generic Drugs Containing DAPAGLIFLOZIN

Company	Ingredient	NDC	Excipient
Teva Pharmaceuticals Inc	dapagliflozin	0480-3527	ANHYDROUS LACTOSE
Teva Pharmaceuticals Inc	dapagliflozin	0480-3527	CELLULOSE, MICROCRYSTALLINE
Teva Pharmaceuticals Inc	dapagliflozin	0480-3527	CROSPOVIDONE
Teva Pharmaceuticals Inc	dapagliflozin	0480-3527	FERRIC OXIDE YELLOW
Teva Pharmaceuticals Inc	dapagliflozin	0480-3527	POLYETHYLENE GLYCOL 3350

What are the Most Frequently-Used Excipients in DAPAGLIFLOZIN?

# Of NDCs	Excipient
10	ANHYDROUS LACTOSE
17	CELLULOSE, MICROCRYSTALLINE
2	CI 77492
1	COPOVIDONE
4	CROSCARMELLOSE SODIUM

Dapagliflozin Excipient Strategy, Formulation Patents, Generic Risk, and Commercial Opportunities

Last updated: September 6, 2026

Dapagliflozin is a small-molecule SGLT2 inhibitor with a mature immediate-release tablet platform and a broad fixed-dose combination franchise. The core formulation is technically simple: dapagliflozin propanediol monohydrate is blended with conventional direct-compression excipients and film-coated. Commercial opportunity has shifted from basic branded tablets to generic supply, differentiated formulations, fixed-dose combinations, pediatric and geriatric dosage forms, and manufacturing platforms that improve dissolution, stability, and cost.

The strongest opportunities are in low-cost, bioequivalent tablets; combination products with metformin, saxagliptin, or other cardiometabolic agents; and formulation approaches that address swallowing difficulty, dose flexibility, moisture control, and regional manufacturing requirements.

What is dapagliflozin and how is it formulated?

Dapagliflozin is a selective sodium-glucose cotransporter 2 inhibitor marketed principally by AstraZeneca under the Farxiga brand in the United States and Forxiga in many international markets. The active pharmaceutical ingredient is commonly supplied as dapagliflozin propanediol monohydrate.

The FDA-approved Farxiga tablet is available in 5 mg and 10 mg strengths. The product is an immediate-release, film-coated tablet intended for once-daily oral administration. The label identifies the following inactive ingredients:

Formulation component	Function
Microcrystalline cellulose	Diluent and compression aid
Anhydrous lactose	Filler and bulk-forming excipient
Crospovidone	Superdisintegrant
Silicon dioxide	Glidant and flow modifier
Magnesium stearate	Lubricant
Polyvinyl alcohol	Film-forming polymer
Titanium dioxide	Opacifier and whitening agent
Polyethylene glycol 3350	Plasticizer
Talc	Anti-tacking and coating aid
Iron oxide colorants	Tablet identification

The commercial formulation relies on a conventional direct-compression architecture. That design reduces process complexity and supports high-volume generic manufacture, but it leaves limited room for differentiation unless a developer changes the dosage form, release profile, excipient platform, or combination strategy. (U.S. Food and Drug Administration [FDA], 2024a)

What excipient strategy is best for generic dapagliflozin tablets?

A standard generic strategy is to reproduce the performance profile of the reference product without duplicating every excipient. The development target is rapid and consistent disintegration, adequate dissolution across physiological pH conditions, acceptable tablet strength, low friability, and stability under commercial packaging conditions.

Core excipient strategy

A practical platform uses:

1. A high-functionality diluent such as microcrystalline cellulose, lactose, mannitol, or dibasic calcium phosphate.
2. Crospovidone or croscarmellose sodium for rapid disintegration.
3. Colloidal silicon dioxide to improve powder flow.
4. Magnesium stearate or sodium stearyl fumarate for lubrication.
5. A conventional polyvinyl alcohol or hypromellose film coat.
6. Moisture-protective blister or bottle packaging where stability data justify the cost.

Dapagliflozin is administered at a low dose relative to the tablet mass. Content uniformity therefore becomes more important than API loading efficiency. The formulation must control segregation between the low-dose API and the larger-volume excipient fraction. Ordered mixing, geometric dilution, co-milling, or dry granulation can reduce blend variability.

When should lactose-free excipients be considered?

Lactose-free formulations can target patients with lactose intolerance, procurement systems that avoid animal-derived or dairy-derived materials, and markets where lactose supply or regulatory documentation is inconvenient. Mannitol, microcrystalline cellulose, dibasic calcium phosphate, and pregelatinized starch are potential replacements.

The commercial benefit is clearest when the lactose-free design supports a broader product line, including fixed-dose combinations or chewable and orally disintegrating formats. Replacing lactose alone generally creates limited patent value. The formulation must show a meaningful manufacturing, stability, palatability, or bioequivalence advantage.

Are co-processed excipients commercially attractive?

Co-processed excipients can improve flow, compactability, and content uniformity in direct compression. Examples include combinations of microcrystalline cellulose with colloidal silicon dioxide, mannitol-based direct-compression systems, and multifunctional filler-binder platforms.

The business case depends on scale. For a high-volume generic, a co-processed excipient can reduce granulation, shorten manufacturing time, and improve yield. For a smaller regional product, the higher excipient price may outweigh the process savings.

What formulation patents protect dapagliflozin products?

Dapagliflozin patent protection has included compound, pharmaceutical composition, crystalline-form, manufacturing, and method-of-use claims. The original compound patent estate is distinct from later patents covering dapagliflozin propanediol, specific solid forms, combinations, and therapeutic uses.

Patent category	Typical protected subject matter	Commercial relevance
Compound patents	C-aryl glucoside SGLT2 inhibitors and related structures	Established the original molecule and broad chemical scope
Solid-form patents	Dapagliflozin propanediol and crystalline forms	Can constrain API sourcing and solid-state processes
Composition patents	Tablets, dosage forms, and pharmaceutical compositions	May affect alternative excipient systems
Combination patents	Dapagliflozin with metformin, saxagliptin, or other agents	Important for fixed-dose combination launches
Method-of-use patents	Diabetes, heart failure, chronic kidney disease, and cardiovascular risk reduction	Can affect labeling and ANDA carve-outs
Manufacturing patents	Crystallization, purification, and process controls	Can raise API substitution and freedom-to-operate issues

The foundational U.S. dapagliflozin compound patent, U.S. Patent No. 6,515,117, expired after the original period of protection and patent-term adjustment. Later patents may have extended protection for particular forms, combinations, or uses. The current Orange Book listing, patent-term adjustment, pediatric extensions, litigation settlements, and jurisdiction-specific supplementary protection certificates must be assessed patent by patent. (FDA, 2024b; U.S. Patent and Trademark Office [USPTO], 2024)

For excipient developers, composition claims are the main potential barrier. A generic manufacturer can often use a non-identical excipient system if it matches the reference product’s quality and bioequivalence requirements and does not practice an enforceable claim.

When does dapagliflozin lose exclusivity?

Dapagliflozin’s U.S. new chemical entity exclusivity expired in 2019, five years after FDA approval. Patent protection continued beyond regulatory exclusivity through later patents and listed combination or formulation rights.

U.S. milestone	Date or status
FDA approval of Farxiga	January 2014
New chemical entity exclusivity	Expired in 2019
Original compound patent family	Expired after the original patent term, subject to adjustment
Later formulation and combination rights	Patent-specific; some extended into the 2020s
ANDA pathway	Available after regulatory exclusivity, subject to listed patents and litigation
Biosimilar pathway	Not applicable because dapagliflozin is a small molecule

International timing differs. European supplementary protection certificates, national patent validations, pediatric extensions, and settlement agreements can change the earliest lawful generic entry date by country. A global launch plan should therefore separate the United States, European Union, United Kingdom, Japan, China, India, and emerging markets rather than use one worldwide expiry date.

What is the Orange Book status of dapagliflozin?

Farxiga is an FDA-approved small-molecule product listed in the Orange Book. Its relevant approved dosage forms are oral tablets, including 5 mg and 10 mg strengths. The Orange Book identifies patents submitted by the reference sponsor and provides the patent information used in ANDA certification and patent litigation.

A generic applicant must address listed patents through one of four certifications:

• Paragraph I: no patent information is listed.
• Paragraph II: the patent has expired.
• Paragraph III: the applicant will wait until patent expiration.
• Paragraph IV: the patent is invalid, unenforceable, or will not be infringed.

A Paragraph IV filing can trigger a patent suit within 45 days. The litigation may impose a 30-month stay on final ANDA approval, subject to statutory exceptions and court developments. (FDA, 2024b)

Which companies are challenging dapagliflozin exclusivity?

Generic competition is expected from companies with established cardiometabolic portfolios, API sourcing capability, and experience with Paragraph IV litigation. Potential participants include large Indian, U.S., and European generic manufacturers, although a company’s ANDA filing, litigation position, and settlement terms must be confirmed from current FDA and court records.

The commercial competitive set can include:

• Large-volume generic manufacturers seeking low-cost tablets.
• Regional companies using licensed or locally manufactured API.
• Contract development and manufacturing organizations offering dossier-ready products.
• Combination-product specialists targeting dapagliflozin-metformin and other co-formulations.
• API suppliers with controlled crystallization and solid-form capability.

The relevant competitive question is not only whether a company can manufacture dapagliflozin. It is whether it can obtain a reliable API, demonstrate bioequivalence, manage patent risk, and secure regulatory approval in the target market.

What generic entry risks exist for dapagliflozin?

Generic entry risk is high for the basic immediate-release tablet because the formulation is conventional and the dose strengths are simple. The principal risks are legal and commercial rather than technical.

Technical risks

Key development risks include:

• Low-dose content uniformity.
• API segregation during blending.
• Dissolution differences caused by particle-size distribution or solid form.
• Lubrication sensitivity, especially with excessive magnesium stearate.
• Moisture-related changes in tablet hardness or disintegration.
• Film-coat defects and color matching.
• Stability differences caused by packaging permeability.

Legal risks

Key legal risks include:

• Solid-form patents covering dapagliflozin propanediol or a specific crystalline form.
• Method-of-use patents for heart failure or chronic kidney disease.
• Combination patents covering dapagliflozin with metformin or another active ingredient.
• Manufacturing patents affecting API production.
• Settlement agreements that restrict launch timing or product scope.

Commercial risks

Generic price erosion can be substantial when multiple suppliers launch simultaneously. The first approved or first-to-market company may obtain a temporary advantage, but the advantage declines as additional manufacturers enter. Wholesaler contracting, pharmacy substitution, payer formulary position, and API cost determine the realized margin.

What formulations are protected by dapagliflozin patents?

The strongest formulation opportunities are those that add a defensible technical feature rather than merely changing an excipient.

Immediate-release tablets

The reference tablet is difficult to protect with a broad excipient claim because it uses common materials. A narrower claim might focus on:

• A specified particle-size range.
• A defined dissolution profile.
• A low-dose blend uniformity process.
• A particular solid form.
• A moisture-controlled packaging configuration.
• A defined combination of disintegrant, binder, and lubricant concentrations.

Orally disintegrating tablets

An orally disintegrating dapagliflozin product could target elderly patients, patients with dysphagia, and adherence-sensitive populations. Mannitol, crospovidone, low-substituted hydroxypropyl cellulose, and taste-masking polymers are relevant excipient classes.

The principal challenges are taste, tablet robustness, moisture sensitivity, and achieving rapid disintegration without compromising dose uniformity.

Pediatric and flexible-dose products

Granules, sprinkle formulations, oral powders, and liquid suspensions could expand use in populations unable to swallow tablets. Dapagliflozin has approved pediatric use in selected indications and age groups under current labeling, but dosage-form development must follow the applicable FDA or regional pediatric requirements. (FDA, 2024a)

Liquid products create additional risks involving chemical stability, microbial control, preservative compatibility, sedimentation, and dosing-device accuracy.

Extended-release and combination products

Dapagliflozin is also commercialized in fixed-dose combinations, including products with metformin, saxagliptin, and linagliptin. These products create formulation complexity because the actives may require different release mechanisms, dose ratios, and stability controls.

Modified-release combinations can provide stronger intellectual-property positions than a basic dapagliflozin tablet. They also require more expensive development, more complex dissolution testing, and greater regulatory risk.

How does dapagliflozin compare with competing SGLT2 inhibitors?

Attribute	Dapagliflozin	Empagliflozin	Canagliflozin	Ertugliflozin
Primary class	SGLT2 inhibitor	SGLT2 inhibitor	SGLT2 inhibitor	SGLT2 inhibitor
Key branded product	Farxiga/Forxiga	Jardiance	Invokana	Steglatro
Common dosage form	Immediate-release tablet	Immediate-release tablet	Immediate-release tablet	Immediate-release tablet
Combination opportunity	Metformin, saxagliptin, linagliptin	Metformin, linagliptin	Metformin	Metformin, sitagliptin
Formulation complexity	Low for monotherapy; higher for combinations	Low for monotherapy; higher for combinations	Low for monotherapy	Low for monotherapy
Biosimilar pathway	Not applicable	Not applicable	Not applicable	Not applicable
Main generic opportunity	High-volume tablet and combination products	High-volume tablet and combination products	Generic and combination products	Regional generic products

Dapagliflozin’s commercial differentiation is linked to indications beyond glycemic control, including heart failure and chronic kidney disease. Those indications expand the addressable market but also increase method-of-use patent and labeling considerations. (Heerspink et al., 2020; McMurray et al., 2019)

What licensing deals and commercial partnerships matter?

Dapagliflozin has been commercialized through originator-led development and regional partnerships, including co-promotion and licensing arrangements associated with combination products and geographic markets. Commercial diligence should examine:

• Territory rights for dapagliflozin monotherapy and combinations.
• Ownership of regulatory dossiers.
• API sourcing obligations.
• Royalty rates and minimum purchase commitments.
• Rights to future indications.
• Patent enforcement and settlement responsibilities.
• Manufacturing change-control procedures.
• Exclusivity restrictions on competing SGLT2 products.

For an excipient supplier, the highest-value route is often indirect: qualify a multifunctional excipient with a major generic manufacturer or CDMO, then use the same platform across dapagliflozin, empagliflozin, and metformin products.

What are the main commercial opportunities in dapagliflozin excipients?

Low-cost generic supply

This is the largest near-term opportunity. Suppliers can compete through:

• Direct-compression excipients with consistent flow.
• Low-metal or low-peroxide excipient grades.
• Reliable global supply.
• Regulatory documentation, including DMF support where relevant.
• Reduced lubricant sensitivity.
• Compatibility with high-speed tablet presses.

Excipient substitution

Lactose-free, vegan-positioned, low-moisture, and allergen-controlled products can support regional preferences and procurement specifications. The substitution must preserve dissolution and bioequivalence performance.

Fixed-dose combinations

Combination products require excipients that work across different APIs and release requirements. A supplier with a validated platform for dapagliflozin-metformin or dapagliflozin-DPP-4 inhibitor products can gain repeat business across multiple strengths.

Pediatric and geriatric dosage forms

Taste-masked granules, orally disintegrating tablets, and sprinkle products offer higher differentiation than standard tablets. These formats can support line extensions and lifecycle management.

Manufacturing and packaging

Moisture-barrier films, high-performance coatings, and continuous direct-compression processes can lower defect rates and extend shelf life. Packaging suppliers also have opportunities through alu-alu blister systems, high-barrier bottles, and unit-dose formats.

What is the revenue exposure to dapagliflozin patent expiry?

Farxiga is one of AstraZeneca’s major growth products, supported by diabetes, heart failure, and chronic kidney disease indications. The exact revenue exposure depends on the reporting period and whether Farxiga is reported separately or within the company’s cardiovascular, renal, and metabolic portfolio.

Patent expiry creates two offsetting effects:

1. Branded revenue faces price and volume erosion from generic substitution.
2. The active ingredient becomes a high-volume opportunity for API suppliers, generic manufacturers, CDMOs, excipient suppliers, and combination-product developers.

The greatest revenue risk is in U.S. tablets and reimbursed markets with automatic pharmacy substitution. The greatest opportunity is in markets where generic approval is available but local manufacturing, price, or supply reliability remains limited.

How strong is the dapagliflozin patent estate?

The estate is strongest where claims cover a specific solid form, combination, therapeutic use, or manufacturing process. It is weaker for a conventional immediate-release tablet made with standard excipients because alternative formulations can often be designed around narrow composition claims.

Estate element	Relative strength
Original chemical compound	Low after expiration
Dapagliflozin solid form	Medium to high, depending on jurisdiction and claim scope
Basic immediate-release tablet	Medium to low
Fixed-dose combinations	Medium to high
Heart failure and kidney disease uses	Medium, subject to claim validity and carve-out options
API manufacturing process	Medium to high if commercially difficult to design around
Orally disintegrating or pediatric products	Potentially high if supported by unexpected performance data

Key Takeaways

• Dapagliflozin is well suited to high-volume generic manufacture because the reference tablet uses conventional excipients and immediate-release technology.
• The core formulation opportunity is not a simple excipient swap. It is a platform that improves content uniformity, dissolution, stability, process yield, or patient usability.
• Lactose-free and co-processed excipient systems can support differentiated products, but the commercial return depends on manufacturing scale.
• Fixed-dose combinations with metformin and DPP-4 inhibitors create more complex and potentially stronger formulation positions.
• Dapagliflozin is a small molecule, so generic ANDA competition applies rather than biosimilar competition.
• Patent risk remains relevant for solid forms, combinations, methods of use, and manufacturing processes even after original chemical exclusivity expired.
• High-value commercial opportunities include generic tablets, pediatric and geriatric dosage forms, taste-masked products, moisture-protective packaging, and excipient platforms usable across the SGLT2 class.

FAQs About Dapagliflozin Excipient and Formulation Opportunities

Can dapagliflozin tablets be made without lactose?

Yes. Microcrystalline cellulose, mannitol, dibasic calcium phosphate, and pregelatinized starch are potential alternatives. The replacement must maintain content uniformity, dissolution, tablet strength, and stability.

Does dapagliflozin require a biosimilar development strategy?

No. Dapagliflozin is a chemically synthesized small molecule. Competition generally proceeds through generic drug applications such as ANDAs in the United States, not biosimilar applications.

Is an orally disintegrating dapagliflozin tablet commercially attractive?

Potentially. The format can target dysphagia, elderly patients, and adherence-sensitive populations. Taste masking, moisture control, mechanical strength, and bioequivalence are the main development challenges.

Which excipients are most important for dapagliflozin content uniformity?

The diluent system, glidant, mixing process, API particle-size distribution, and lubricant level are the primary variables. Crospovidone affects disintegration but is less central to blend uniformity than the powder-flow system.

Can a generic manufacturer avoid dapagliflozin formulation patents by changing excipients?

Sometimes. A non-infringing formulation may be possible if the alternative does not practice the relevant composition, solid-form, manufacturing, or method-of-use claims. The analysis requires claim-by-claim freedom-to-operate review in each target jurisdiction.

References

1. AstraZeneca. (2024). Farxiga: Prescribing information. U.S. Food and Drug Administration.

2. Heerspink, H. J. L., Stefánsson, B. V., Correa-Rotter, R., Chertow, G. M., Greene, T., Hou, F. F., Mann, J. F. E., McMurray, J. J. V., Lindberg, M., Rossing, P., Sjöström, C. D., Toto, R. D., Langkilde, A. M., & Wheeler, D. C. (2020). Dapagliflozin in patients with chronic kidney disease. New England Journal of Medicine, 383(15), 1436-1446.

3. McMurray, J. J. V., Solomon, S. D., Inzucchi, S. E., Køber, L., Kosiborod, M. N., Martinez, F. A., Ponikowski, P., Sabatine, M. S., Anand, I. S., Bělohlávek, J., Böhm, M., Chiang, C. E., Chawla, L. S., Desai, A. S., Diez, M., Drozdz, J., Dukát, A., Ge, J., Howlett, J., ... DAPA-HF Trial Committees and Investigators. (2019). Dapagliflozin in patients with heart failure and reduced ejection fraction. New England Journal of Medicine, 381(21), 1995-2008.

4. U.S. Food and Drug Administration. (2024a). Farxiga (dapagliflozin) drug label. Drugs@FDA.

5. U.S. Food and Drug Administration. (2024b). Approved drug products with therapeutic equivalence evaluations: Orange Book. FDA.

6. U.S. Patent and Trademark Office. (2024). Patent Center and Patent Term Adjustment records. USPTO.

7. U.S. Patent No. 6,515,117. (2003). C-aryl glucoside SGLT2 inhibitors. U.S. Patent and Trademark Office.